SMILES
stringlengths
71
300
POI_Name
stringclasses
164 values
POI_Sequence
stringclasses
133 values
Ligase_Name
stringclasses
9 values
Cell_Line
stringclasses
155 values
Value_Type
stringclasses
2 values
Value_Unit
stringclasses
2 values
Value
float64
-53.5
100k
Value_Error
float64
1
81.3
Value_Range_Min
float64
0.1
1.49k
Value_Range_Max
float64
0.76
1.99k
Value_Concentration
float64
0.1
100
Assay_Time
float64
2
96
Value_Operator
stringclasses
5 values
Value_Category
stringclasses
2 values
Value_Concentration_Unit
stringclasses
2 values
Modality
stringclasses
1 value
POI_UniProt
stringclasses
131 values
Ligase_UniProt
stringclasses
11 values
Ligase_Sequence
stringclasses
11 values
Cell_Line_ID
stringclasses
154 values
Cell_Line_Species
stringclasses
4 values
Reference
stringclasses
367 values
Description
stringclasses
501 values
Database
stringclasses
6 values
Assay
stringclasses
21 values
TPD_ID
stringlengths
10
10
Cell_Line_Description
stringclasses
151 values
POI_Cluster
int64
-1
37
SMILES_Held_Out
bool
2 classes
SMILES_Scaffold_Cluster
int64
-1
2.35k
SMILES_Butina_Cluster
int64
-1
278
COc1cc(/C=C2\SC(=O)N(Cc3cn(CCCNC(=O)[C@@H](N)Cc4c[nH]cn4)nn3)C2=O)ccc1Oc1ccc(C#N)cc1C(F)(F)F
ESRRA
MSSQVVGIEPLYIKAEPASPDSPKGSSETETEPPVALAPGPAPTRCLPGHKEEEDGEGAGPGEQGGGKLVLSSLPKRLCLVCGDVASGYHYGVASCEACKAFFKRTIQGSIEYSCPASNECEITKRRRKACQACRFTKCLRVGMLKEGVRLDRVRGGRQKYKRRPEVDPLPFPGPFPAGPLAVAGGPRKTAAPVNALVSHLLVVEPEKLYAMPDPAGPDGHLPAVATLCDLFDREIVVTISWAKSIPGFSSLSLSDQMSVLQSVWMEVLVLGVAQRSLPLQDELAFAEDLVLDEEGARAAGLGELGAALLQLVRRLQALR...
UBR1
MCF-7
Dmax
%
90
null
null
null
null
48
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P11474
Q8IWV7
MADEEAGGTERMEISAELPQTPQRLASWWDQQVDFYTAFLHHLAQLVPEIYFAEMDPDLEKQEESVQMSIFTPLEWYLFGEDPDICLEKLKHSGAFQLCGRVFKSGETTYSCRDCAIDPTCVLCMDCFQDSVHKNHRYKMHTSTGGGFCDCGDTEAWKTGPFCVNHEPGRAGTIKENSRCPLNEEVIVQARKIFPSVIKYVVEMTIWEEEKELPPELQIREKNERYYCVLFNDEHHSYDHVIYSLQRALDCELAEAQLHTTAIDKEGRRAVKAGAYAACQEAKEDIKSHSENVSQHPLHVEVLHSEIMAHQKFALRLGSW...
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31511327/
null
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
true
-1
-1
COc1cc(C(=O)N2CCN(c3c(C)cc(-c4cc5c(-c6cnn(C7CCN(C)CC7)c6)c[nH]c5nn4)cc3C)CC2)cc(N2CCC(=O)NC2=O)c1
MAP4K1
MDVVDPDIFNRDPRDHYDLLQRLGGGTYGEVFKARDKVSGDLVALKMVKMEPDDDVSTLQKEILILKTCRHANIVAYHGSYLWLQKLWICMEFCGAGSLQDIYQVTGSLSELQISYVCREVLQGLAYLHSQKKIHRDIKGANILINDAGEVRLADFGISAQIGATLARRLSFIGTPYWMAPEVAAVALKGGYNELCDIWSLGITAIELAELQPPLFDVHPLRVLFLMTKSGYQPPRLKEKGKWSAAFHNFIKVTLTKSPKKRPSATKMLSHQLVSQPGLNRGLILDLLDKLKNPGKGPSIGDIEDEEPELPPAIPRRIRS...
CRBN
Ramos
Dmax
%
50
null
40
60
null
null
null
range
null
PROteolysis-TArgeting Chimera (PROTAC)
Q92918
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0597
Homo sapiens
PROTAC CHIMERIC COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF (patent)
HPK1 protein degradation detection WB method was used to test HPK1 protein degradation and DC50/Dmax to evaluate the in vitro degradation ability of the compound. RAMOS cell line was selected as the degradation cell line, and the culture conditions were RMPI 1640 medium with 10% FBS, 37°C, 5% CO2. Experimental steps: (...
TPDdb
Western Blot
TPD-8YH8IC
EBV-negative. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*03 A*03 A*03 A*03 Stable (MSS). In situ; Ascites; Caucasian. B-cell; CL=CL_0000236. Cancer cell line
-1
true
-1
-1
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
A-549
DC50
nM
243
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in A549/Hep3B2.1-7/SNU-387 cells after 18 h treatment
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
A-549
Dmax
%
80
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in A549/Hep3B2.1-7/SNU-387 cells after 18 h treatment
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
HLE
DC50
nM
25
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1281
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLE/HuH-7/SNU-423 cells after 18 h treatment
PROTAC-DB
null
null
African=1.86%; Native American=0%; East Asian, North=85.81%; East Asian, South=8.43%; South Asian=0%; European, North=0%; European, South=3.89%. TP53 mutation indicated incorrectly as being at c.747G>T in PubMed=8389256. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Stable (MSS) (Sanger). In situ; Liver; Japanese. Epithel...
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
HLE
Dmax
%
85
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1281
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLE/HuH-7/SNU-423 cells after 18 h treatment
PROTAC-DB
null
null
African=1.86%; Native American=0%; East Asian, North=85.81%; East Asian, South=8.43%; South Asian=0%; European, North=0%; European, South=3.89%. TP53 mutation indicated incorrectly as being at c.747G>T in PubMed=8389256. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Stable (MSS) (Sanger). In situ; Liver; Japanese. Epithel...
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
HLF
DC50
nM
40
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_2947
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLF/SNU-398/HUCCT1 cells after 18 h treatment
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=85.67%; East Asian, South=14.33%; South Asian=0%; European, North=0%; European, South=0%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 In situ; Liver; Japanese. Fibroblast; CL=CL_0000057. Cancer cell line
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
HLF
Dmax
%
66
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_2947
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLF/SNU-398/HUCCT1 cells after 18 h treatment
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=85.67%; East Asian, South=14.33%; South Asian=0%; European, North=0%; European, South=0%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 In situ; Liver; Japanese. Fibroblast; CL=CL_0000057. Cancer cell line
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
Hep 3B2.1-7
DC50
nM
631
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0326
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in A549/Hep3B2.1-7/SNU-387 cells after 18 h treatment
PROTAC-DB
null
null
African=71.82%; Native American=0.52%; East Asian, North=3.16%; East Asian, South=0%; South Asian=0%; European, North=8.8%; European, South=15.69%. Has lost chromosome Y. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Stable (MSS) (Sanger). In situ; Liver; African American. Patented cell line. NCBI_TaxID; 10407; Hepatitis ...
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
Hep 3B2.1-7
Dmax
%
59
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0326
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in A549/Hep3B2.1-7/SNU-387 cells after 18 h treatment
PROTAC-DB
null
null
African=71.82%; Native American=0.52%; East Asian, North=3.16%; East Asian, South=0%; South Asian=0%; European, North=8.8%; European, South=15.69%. Has lost chromosome Y. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Stable (MSS) (Sanger). In situ; Liver; African American. Patented cell line. NCBI_TaxID; 10407; Hepatitis ...
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
Hep-G2
DC50
nM
631
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0027
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HUH-1/HepG2/SK-Hep-1 cells after 18 h treatment
PROTAC-DB
null
null
African=2.83%; Native American=20.88%; East Asian, North=4.48%; East Asian, South=0%; South Asian=0%; European, North=22.82%; European, South=48.99%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 A*02 A*02 In situ; Liver; Caucasian. Patented cell line. Cancer cell line
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
Hep-G2
Dmax
%
65
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0027
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HUH-1/HepG2/SK-Hep-1 cells after 18 h treatment
PROTAC-DB
null
null
African=2.83%; Native American=20.88%; East Asian, North=4.48%; East Asian, South=0%; South Asian=0%; European, North=22.82%; European, South=48.99%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 A*02 A*02 In situ; Liver; Caucasian. Patented cell line. Cancer cell line
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
HuCC-T1
DC50
nM
126
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0324
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLF/SNU-398/HUCCT1 cells after 18 h treatment
PROTAC-DB
null
null
African=7.42%; Native American=0%; East Asian, North=82%; East Asian, South=0%; South Asian=0%; European, North=0%; European, South=10.57%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Stable (MSS) (Sanger). Metastatic; Ascites; Japanese. Cancer cell line
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
HuCC-T1
Dmax
%
86
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0324
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLF/SNU-398/HUCCT1 cells after 18 h treatment
PROTAC-DB
null
null
African=7.42%; Native American=0%; East Asian, North=82%; East Asian, South=0%; South Asian=0%; European, North=0%; European, South=10.57%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Stable (MSS) (Sanger). Metastatic; Ascites; Japanese. Cancer cell line
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
HuH-1
DC50
nM
79
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_2956
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HUH-1/HepG2/SK-Hep-1 cells after 18 h treatment
PROTAC-DB
null
null
African=0.02%; Native American=0.87%; East Asian, North=80.09%; East Asian, South=18.1%; South Asian=0%; European, North=0%; European, South=0.92%. Contains multiple copies of integrated hepatitis B virus (HBV) genomes. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ; Liver; Japanese. NCB...
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
HuH-1
Dmax
%
79
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_2956
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HUH-1/HepG2/SK-Hep-1 cells after 18 h treatment
PROTAC-DB
null
null
African=0.02%; Native American=0.87%; East Asian, North=80.09%; East Asian, South=18.1%; South Asian=0%; European, North=0%; European, South=0.92%. Contains multiple copies of integrated hepatitis B virus (HBV) genomes. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ; Liver; Japanese. NCB...
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
Huh-7
DC50
nM
100
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0336
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLE/HuH-7/SNU-423 cells after 18 h treatment
PROTAC-DB
null
null
African=1.56%; Native American=0%; East Asian, North=79.68%; East Asian, South=13.08%; South Asian=0%; European, North=0%; European, South=5.69%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11 Stable (MSS) (Sanger). In situ; Liver; Japanese. Cancer cell line
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
Huh-7
Dmax
%
79
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0336
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLE/HuH-7/SNU-423 cells after 18 h treatment
PROTAC-DB
null
null
African=1.56%; Native American=0%; East Asian, North=79.68%; East Asian, South=13.08%; South Asian=0%; European, North=0%; European, South=5.69%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11 Stable (MSS) (Sanger). In situ; Liver; Japanese. Cancer cell line
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
SK-HEP-1
DC50
nM
126
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0525
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HUH-1/HepG2/SK-Hep-1 cells after 18 h treatment
PROTAC-DB
null
null
African=0.65%; Native American=1.18%; East Asian, North=0%; East Asian, South=2.22%; South Asian=8.09%; European, North=23.66%; European, South=64.2%. Has lost chromosome Y. Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC A*02 A*02 Stable (MSS) (Sanger). Metastatic; Ascites; Caucasian. Endothelial cell; CL=CL_0000115. ...
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
SK-HEP-1
Dmax
%
87
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0525
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HUH-1/HepG2/SK-Hep-1 cells after 18 h treatment
PROTAC-DB
null
null
African=0.65%; Native American=1.18%; East Asian, North=0%; East Asian, South=2.22%; South Asian=8.09%; European, North=23.66%; European, South=64.2%. Has lost chromosome Y. Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC A*02 A*02 Stable (MSS) (Sanger). Metastatic; Ascites; Caucasian. Endothelial cell; CL=CL_0000115. ...
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
SNU-387
DC50
nM
32
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0250
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in A549/Hep3B2.1-7/SNU-387 cells after 18 h treatment
PROTAC-DB
null
null
African=0.32%; Native American=0.32%; East Asian, North=64.77%; East Asian, South=33.73%; South Asian=0%; European, North=0%; European, South=0.87%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ; Liver; Korean. NCBI_TaxID; 10407; Hepatitis B virus (HBV). Cancer cell...
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
SNU-387
Dmax
%
98
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0250
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in A549/Hep3B2.1-7/SNU-387 cells after 18 h treatment
PROTAC-DB
null
null
African=0.32%; Native American=0.32%; East Asian, North=64.77%; East Asian, South=33.73%; South Asian=0%; European, North=0%; European, South=0.87%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ; Liver; Korean. NCBI_TaxID; 10407; Hepatitis B virus (HBV). Cancer cell...
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
SNU-398
DC50
nM
10
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0077
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLF/SNU-398/HUCCT1 cells after 18 h treatment
PROTAC-DB
null
null
African=1.33%; Native American=0.85%; East Asian, North=66.35%; East Asian, South=28.86%; South Asian=0%; European, North=0%; European, South=2.61%. Has lost chromosome Y. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ; Liver; Korean. NCBI_TaxID; 10407; Hepatitis B virus (HBV). Cancer ce...
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
SNU-398
Dmax
%
99
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0077
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLF/SNU-398/HUCCT1 cells after 18 h treatment
PROTAC-DB
null
null
African=1.33%; Native American=0.85%; East Asian, North=66.35%; East Asian, South=28.86%; South Asian=0%; European, North=0%; European, South=2.61%. Has lost chromosome Y. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ; Liver; Korean. NCBI_TaxID; 10407; Hepatitis B virus (HBV). Cancer ce...
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
SNU-423
DC50
nM
79
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0366
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLE/HuH-7/SNU-423 cells after 18 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.82%; East Asian, North=62.68%; East Asian, South=36.24%; South Asian=0%; European, North=0%; European, South=0.26%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 Stable (MSS) (Sanger). In situ; Liver; Korean. NCBI_TaxID; 10407; Hepatitis B virus (HBV). Cancer cell line
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
VHL
SNU-423
Dmax
%
87
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0366
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLE/HuH-7/SNU-423 cells after 18 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.82%; East Asian, North=62.68%; East Asian, South=36.24%; South Asian=0%; European, North=0%; European, South=0.26%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 Stable (MSS) (Sanger). In situ; Liver; Korean. NCBI_TaxID; 10407; Hepatitis B virus (HBV). Cancer cell line
24
false
811
0
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
A-549
DC50
nM
27
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0023
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in A549/Hep3B2.1-7/SNU-387 cells after 18 h treatment
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
A-549
Dmax
%
95
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0023
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in A549/Hep3B2.1-7/SNU-387 cells after 18 h treatment
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
HLE
DC50
nM
158
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1281
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLE/HuH-7/SNU-423 cells after 18 h treatment
PROTAC-DB
null
null
African=1.86%; Native American=0%; East Asian, North=85.81%; East Asian, South=8.43%; South Asian=0%; European, North=0%; European, South=3.89%. TP53 mutation indicated incorrectly as being at c.747G>T in PubMed=8389256. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Stable (MSS) (Sanger). In situ; Liver; Japanese. Epithel...
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
HLE
Dmax
%
79
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1281
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLE/HuH-7/SNU-423 cells after 18 h treatment
PROTAC-DB
null
null
African=1.86%; Native American=0%; East Asian, North=85.81%; East Asian, South=8.43%; South Asian=0%; European, North=0%; European, South=3.89%. TP53 mutation indicated incorrectly as being at c.747G>T in PubMed=8389256. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Stable (MSS) (Sanger). In situ; Liver; Japanese. Epithel...
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
HLF
DC50
nM
398
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_2947
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLF/SNU-398/HUCCT1 cells after 18 h treatment
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=85.67%; East Asian, South=14.33%; South Asian=0%; European, North=0%; European, South=0%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 In situ; Liver; Japanese. Fibroblast; CL=CL_0000057. Cancer cell line
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
HLF
Dmax
%
30
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_2947
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLF/SNU-398/HUCCT1 cells after 18 h treatment
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=85.67%; East Asian, South=14.33%; South Asian=0%; European, North=0%; European, South=0%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 In situ; Liver; Japanese. Fibroblast; CL=CL_0000057. Cancer cell line
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
Hep 3B2.1-7
DC50
nM
13
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0326
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in A549/Hep3B2.1-7/SNU-387 cells after 18 h treatment
PROTAC-DB
null
null
African=71.82%; Native American=0.52%; East Asian, North=3.16%; East Asian, South=0%; South Asian=0%; European, North=8.8%; European, South=15.69%. Has lost chromosome Y. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Stable (MSS) (Sanger). In situ; Liver; African American. Patented cell line. NCBI_TaxID; 10407; Hepatitis ...
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
Hep 3B2.1-7
Dmax
%
96
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0326
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in A549/Hep3B2.1-7/SNU-387 cells after 18 h treatment
PROTAC-DB
null
null
African=71.82%; Native American=0.52%; East Asian, North=3.16%; East Asian, South=0%; South Asian=0%; European, North=8.8%; European, South=15.69%. Has lost chromosome Y. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Stable (MSS) (Sanger). In situ; Liver; African American. Patented cell line. NCBI_TaxID; 10407; Hepatitis ...
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
Hep-G2
DC50
nM
32
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0027
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HUH-1/HepG2/SK-Hep-1 cells after 18 h treatment
PROTAC-DB
null
null
African=2.83%; Native American=20.88%; East Asian, North=4.48%; East Asian, South=0%; South Asian=0%; European, North=22.82%; European, South=48.99%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 A*02 A*02 In situ; Liver; Caucasian. Patented cell line. Cancer cell line
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
Hep-G2
Dmax
%
89
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0027
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HUH-1/HepG2/SK-Hep-1 cells after 18 h treatment
PROTAC-DB
null
null
African=2.83%; Native American=20.88%; East Asian, North=4.48%; East Asian, South=0%; South Asian=0%; European, North=22.82%; European, South=48.99%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 A*02 A*02 In situ; Liver; Caucasian. Patented cell line. Cancer cell line
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
HuCC-T1
DC50
nM
13
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0324
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLF/SNU-398/HUCCT1 cells after 18 h treatment
PROTAC-DB
null
null
African=7.42%; Native American=0%; East Asian, North=82%; East Asian, South=0%; South Asian=0%; European, North=0%; European, South=10.57%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Stable (MSS) (Sanger). Metastatic; Ascites; Japanese. Cancer cell line
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
HuCC-T1
Dmax
%
90
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0324
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLF/SNU-398/HUCCT1 cells after 18 h treatment
PROTAC-DB
null
null
African=7.42%; Native American=0%; East Asian, North=82%; East Asian, South=0%; South Asian=0%; European, North=0%; European, South=10.57%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Stable (MSS) (Sanger). Metastatic; Ascites; Japanese. Cancer cell line
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
HuH-1
DC50
nM
251
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_2956
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HUH-1/HepG2/SK-Hep-1 cells after 18 h treatment
PROTAC-DB
null
null
African=0.02%; Native American=0.87%; East Asian, North=80.09%; East Asian, South=18.1%; South Asian=0%; European, North=0%; European, South=0.92%. Contains multiple copies of integrated hepatitis B virus (HBV) genomes. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ; Liver; Japanese. NCB...
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
HuH-1
Dmax
%
50
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_2956
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HUH-1/HepG2/SK-Hep-1 cells after 18 h treatment
PROTAC-DB
null
null
African=0.02%; Native American=0.87%; East Asian, North=80.09%; East Asian, South=18.1%; South Asian=0%; European, North=0%; European, South=0.92%. Contains multiple copies of integrated hepatitis B virus (HBV) genomes. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ; Liver; Japanese. NCB...
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
Huh-7
DC50
nM
50
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0336
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLE/HuH-7/SNU-423 cells after 18 h treatment
PROTAC-DB
null
null
African=1.56%; Native American=0%; East Asian, North=79.68%; East Asian, South=13.08%; South Asian=0%; European, North=0%; European, South=5.69%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11 Stable (MSS) (Sanger). In situ; Liver; Japanese. Cancer cell line
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
Huh-7
Dmax
%
93
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0336
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLE/HuH-7/SNU-423 cells after 18 h treatment
PROTAC-DB
null
null
African=1.56%; Native American=0%; East Asian, North=79.68%; East Asian, South=13.08%; South Asian=0%; European, North=0%; European, South=5.69%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11 Stable (MSS) (Sanger). In situ; Liver; Japanese. Cancer cell line
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
SK-HEP-1
DC50
nM
32
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0525
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HUH-1/HepG2/SK-Hep-1 cells after 18 h treatment
PROTAC-DB
null
null
African=0.65%; Native American=1.18%; East Asian, North=0%; East Asian, South=2.22%; South Asian=8.09%; European, North=23.66%; European, South=64.2%. Has lost chromosome Y. Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC A*02 A*02 Stable (MSS) (Sanger). Metastatic; Ascites; Caucasian. Endothelial cell; CL=CL_0000115. ...
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
SK-HEP-1
Dmax
%
89
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0525
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HUH-1/HepG2/SK-Hep-1 cells after 18 h treatment
PROTAC-DB
null
null
African=0.65%; Native American=1.18%; East Asian, North=0%; East Asian, South=2.22%; South Asian=8.09%; European, North=23.66%; European, South=64.2%. Has lost chromosome Y. Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC A*02 A*02 Stable (MSS) (Sanger). Metastatic; Ascites; Caucasian. Endothelial cell; CL=CL_0000115. ...
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
SNU-387
DC50
nM
25
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0250
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in A549/Hep3B2.1-7/SNU-387 cells after 18 h treatment
PROTAC-DB
null
null
African=0.32%; Native American=0.32%; East Asian, North=64.77%; East Asian, South=33.73%; South Asian=0%; European, North=0%; European, South=0.87%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ; Liver; Korean. NCBI_TaxID; 10407; Hepatitis B virus (HBV). Cancer cell...
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
SNU-387
Dmax
%
90
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0250
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in A549/Hep3B2.1-7/SNU-387 cells after 18 h treatment
PROTAC-DB
null
null
African=0.32%; Native American=0.32%; East Asian, North=64.77%; East Asian, South=33.73%; South Asian=0%; European, North=0%; European, South=0.87%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ; Liver; Korean. NCBI_TaxID; 10407; Hepatitis B virus (HBV). Cancer cell...
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
SNU-398
DC50
nM
3
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0077
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLF/SNU-398/HUCCT1 cells after 18 h treatment
PROTAC-DB
null
null
African=1.33%; Native American=0.85%; East Asian, North=66.35%; East Asian, South=28.86%; South Asian=0%; European, North=0%; European, South=2.61%. Has lost chromosome Y. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ; Liver; Korean. NCBI_TaxID; 10407; Hepatitis B virus (HBV). Cancer ce...
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
SNU-398
Dmax
%
95
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0077
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLF/SNU-398/HUCCT1 cells after 18 h treatment
PROTAC-DB
null
null
African=1.33%; Native American=0.85%; East Asian, North=66.35%; East Asian, South=28.86%; South Asian=0%; European, North=0%; European, South=2.61%. Has lost chromosome Y. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ; Liver; Korean. NCBI_TaxID; 10407; Hepatitis B virus (HBV). Cancer ce...
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
SNU-423
DC50
nM
13
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0366
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLE/HuH-7/SNU-423 cells after 18 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.82%; East Asian, North=62.68%; East Asian, South=36.24%; South Asian=0%; European, North=0%; European, South=0.26%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 Stable (MSS) (Sanger). In situ; Liver; Korean. NCBI_TaxID; 10407; Hepatitis B virus (HBV). Cancer cell line
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCC(=O)Nc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
SNU-423
Dmax
%
93
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0366
Homo sapiens
10.1021/acs.jmedchem.8b01826
Degradation of Fak in HLE/HuH-7/SNU-423 cells after 18 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.82%; East Asian, North=62.68%; East Asian, South=36.24%; South Asian=0%; European, North=0%; European, South=0.26%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 Stable (MSS) (Sanger). In situ; Liver; Korean. NCBI_TaxID; 10407; Hepatitis B virus (HBV). Cancer cell line
24
false
812
243
COc1cc(C(=O)NCCOCCOCCOCCNC(=O)C[C@@H]2N=C(c3ccc(Cl)cc3)c3c(sc(C)c3C)-n3c(C)nnc32)ccc1NC(=O)[C@@H]1N[C@@H](CC(C)(C)C)[C@](C#N)(c2ccc(Cl)cc2F)[C@H]1c1cccc(Cl)c1F
BRD4
MSAESGPGTRLRNLPVMGDGLETSQMSTTQAQAQPQPANAASTNPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEETEIMIVQAKGRGRGRKETGTAKPGVSTVPNTTQASTPPQTQTPQPNPPPVQATPHPFPAVTPDLIVQTPVMTVVPPQPLQTPPPVPPQPQPPPAPAPQPVQSHPPIIAATPQPVKTKKGVKRKADTTTPTTIDPIHEPPSLPPEPKTTKLGQ...
MDM2
HCT 116
DC50
nM
32
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
O60885
Q00987
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
CVCL_0291
Homo sapiens
10.1158/0008-5472.CAN-18-2918; https://pubmed.ncbi.nlm.nih.gov/30385614/
Degradation of BRD4 in HCT116 cells after 24 h treatment
PROTAC-DB; PROTACpedia
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
20
false
813
0
COc1cc(C(=O)NCCOCCOCCOCCNC(=O)C[C@@H]2N=C(c3ccc(Cl)cc3)c3c(sc(C)c3C)-n3c(C)nnc32)ccc1NC(=O)[C@@H]1N[C@@H](CC(C)(C)C)[C@](C#N)(c2ccc(Cl)cc2F)[C@H]1c1cccc(Cl)c1F
BRD4
MSAESGPGTRLRNLPVMGDGLETSQMSTTQAQAQPQPANAASTNPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEETEIMIVQAKGRGRGRKETGTAKPGVSTVPNTTQASTPPQTQTPQPNPPPVQATPHPFPAVTPDLIVQTPVMTVVPPQPLQTPPPVPPQPQPPPAPAPQPVQSHPPIIAATPQPVKTKKGVKRKADTTTPTTIDPIHEPPSLPPEPKTTKLGQ...
MDM2
HCT 116
Dmax
%
98
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
O60885
Q00987
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
CVCL_0291
Homo sapiens
10.1158/0008-5472.CAN-18-2918; https://pubmed.ncbi.nlm.nih.gov/30385614/
Degradation of BRD4 in HCT116 cells after 24 h treatment
PROTAC-DB; PROTACpedia
null
null
African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut...
20
false
813
0
COc1cc(C(=O)Nc2cc(C(F)(F)F)ccn2)ccc1-c1nn2c(c1C(N)=O)Nc1ccc(N3CCN(CC4CCN(c5ccc(N6CCC(=O)NC6=O)cc5)CC4)CC3)cc1CC2
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
0.849
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-0PM9UB
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
481
15
COc1cc(C(=O)Nc2cccc(C)n2)ccc1-c1nn2c(c1C(N)=O)Nc1ccc(N3CCN(CC4CCN(c5ccc(N6CCC(=O)NC6=O)cc5)CC4)CC3)cc1CC2
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
0.338
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-U2XQRY
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
481
15
COc1cc(C)ccc1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1C
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
3.1
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-YIAJVM
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
783
15
COc1cc(C2Nc3ncnc(-c4ccc([C@@H](C)NC(=O)c5nc(C(C)(C)C)no5)c(C)c4)c3N2)ccc1N1CCN(CC2CCN(c3ccc(N4CCC(=O)NC4=O)c(C)c3)CC2)CC1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
null
DC50
nM
0.97
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
null
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE (patent)
HTFR assay After 6h treatment, add 10μl 4xlysis buffer to each well; seal the plate and incubate 30min at room temperature on a plate shaker; Once the cells are lysed, 16 μL of cell lysate are transferred to a PE 384-well HTRF detection plate; 4 μL of pre-mixed HTRF antibodies are added to each well; Cover the plate wi...
TPDdb
HTRF
TPD-AKN2PV
null
31
false
814
167
COc1cc(C=C2SC(=O)N(CCOCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)C2=O)ccc1Oc1ccc(C#N)cc1C(F)(F)F
ESRRA
MSSQVVGIEPLYIKAEPASPDSPKGSSETETEPPVALAPGPAPTRCLPGHKEEEDGEGAGPGEQGGGKLVLSSLPKRLCLVCGDVASGYHYGVASCEACKAFFKRTIQGSIEYSCPASNECEITKRRRKACQACRFTKCLRVGMLKEGVRLDRVRGGRQKYKRRPEVDPLPFPGPFPAGPLAVAGGPRKTAAPVNALVSHLLVVEPEKLYAMPDPAGPDGHLPAVATLCDLFDREIVVTISWAKSIPGFSSLSLSDQMSVLQSVWMEVLVLGVAQRSLPLQDELAFAEDLVLDEEGARAAGLGELGAALLQLVRRLQALR...
VHL
MCF-7
DC50
nM
100
null
null
null
null
8
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P11474
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/26075522/
protein reduction by nearly 50% was observed as early as 1 h post‐treatment, and almost complete degradation was achieved after 4 h of treatment
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
810
0
COc1cc(C=C2SC(=O)N(CCOCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)C2=O)ccc1Oc1ccc(C#N)cc1C(F)(F)F
ESRRA
MSSQVVGIEPLYIKAEPASPDSPKGSSETETEPPVALAPGPAPTRCLPGHKEEEDGEGAGPGEQGGGKLVLSSLPKRLCLVCGDVASGYHYGVASCEACKAFFKRTIQGSIEYSCPASNECEITKRRRKACQACRFTKCLRVGMLKEGVRLDRVRGGRQKYKRRPEVDPLPFPGPFPAGPLAVAGGPRKTAAPVNALVSHLLVVEPEKLYAMPDPAGPDGHLPAVATLCDLFDREIVVTISWAKSIPGFSSLSLSDQMSVLQSVWMEVLVLGVAQRSLPLQDELAFAEDLVLDEEGARAAGLGELGAALLQLVRRLQALR...
VHL
MCF-7
Dmax
%
86
null
null
null
null
4
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P11474
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/26075522/
protein reduction by nearly 50% was observed as early as 1 h post‐treatment, and almost complete degradation was achieved after 4 h of treatment
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
810
0
COc1cc(CCN2CCN(C3CCN(c4ccc(Nc5nc(Nc6cccc7c6N(S(C)(=O)=O)CC7)c6cc[nH]c6n5)cc4F)CC3)CC2)ccc1C1CCC(=O)NC1=O
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
HCC827
DC50
nM
33.4
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_2063
Homo sapiens
BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent)
Cell treatment On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100...
TPDdb
HTRF
TPD-7V0U13
African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%. Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566). Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11 Stable (MSS) (Sanger). In situ; Lung; Caucasia...
23
true
-1
-1
COc1cc(CCN2CCN(C3CCN(c4ccc(Nc5nc(Nc6cccc7c6N(S(C)(=O)=O)CC7)c6cc[nH]c6n5)cc4F)CC3)CC2)ccc1C1CCC(=O)NC1=O
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
NCI-H1975
DC50
nM
36.9
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1511
Homo sapiens
BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent)
Cell treatment On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ...
TPDdb
HTRF
TPD-7V0U13
African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01 Stable (MSS) (Sanger). In situ; Lung; Caucasian. Cancer cell line
23
true
-1
-1
COc1cc(Cl)c(-c2cc(Cl)ccc2Cl)cc1C(=O)N1CCN(C(=O)/C=C/C(=O)NCCCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1
KRAS G12C
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
CRBN
NCI-H23
DC50
nM
2,500
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1547
Homo sapiens
10.1016/j.bioorg.2021.105447
Degradation of KRAS G12C in NCI-H358/NCI-H23 cells after 48 h treatment
PROTAC-DB
null
null
African=67.86%; Native American=2.12%; East Asian, North=2.83%; East Asian, South=0%; South Asian=0%; European, North=10.88%; European, South=16.3%. Has lost chromosome Y. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*80 A*80 Stable (MSS) (Sanger). In situ; Lung; African America...
-1
false
815
268
COc1cc(Cl)c(-c2cc(Cl)ccc2Cl)cc1C(=O)N1CCN(C(=O)/C=C/C(=O)NCCCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1
KRAS G12C
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
CRBN
NCI-H358
DC50
nM
1,250
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1559
Homo sapiens
10.1016/j.bioorg.2021.105447
Degradation of KRAS G12C in NCI-H358/NCI-H23 cells after 48 h treatment
PROTAC-DB
null
null
African=3.45%; Native American=0%; East Asian, North=4.63%; East Asian, South=0%; South Asian=0%; European, North=56.1%; European, South=35.82%. NCI-H358 and NCI-H358M (Cellosaurus=CVCL_JA53) could be identical. Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*03 Stable (MSS) (Sanger). In situ; Lun...
-1
false
815
268
COc1cc(F)c(F)cc1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
0.611
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-J8XFB0
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
783
15
COc1cc(F)c(F)cc1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1C
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
3.91
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-3YI3C2
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
783
15
COc1cc(F)ccc1C(=O)NCc1ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)cc1C
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
5.36
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_A442
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent)
TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro...
TPDdb
HTRF
TPD-KW4OLL
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
783
15
COc1cc(N2CC(N3CC(N4CC5CC(n6nc(-c7ccc(Oc8ccccc8)cc7)c7c(N)ncnc76)CC5C4)C3)C2)ccc1C(=O)NC1CCC(=O)NC1=O
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
Mino
DC50
nM
10
null
null
null
null
null
<
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1872
Homo sapiens
PROTAC COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING SAME, PREPARATION METHOD THEREFOR, AND USE THEREOF (patent)
Use Mino and HEK293 transfection BTK (C481S) cells to detect the degradation ability of the compound on BTK (WT) and BTK (C481S) protein. Mino human mantle cell lymphoma cell line was purchased from ATCC, cultured in RPMI-1640 medium with 15% FBS and 1% antibiotics. HEK293 OE BTK (C481S) human embryonic kidney cells 29...
TPDdb
Western Blot
TPD-8HOEB1
African=0.85%; Native American=0%; East Asian, North=1.5%; East Asian, South=0%; South Asian=6.1%; European, North=39.56%; European, South=51.98%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11,68; B*35,39; C*04,12. A*11 In situ; Peripheral blood; Caucasian. Cancer cell line
31
false
816
109
COc1cc(N2CC(N3CC(N4CC5CC(n6nc(-c7ccc(Oc8ccccc8)cc7)c7c(N)ncnc76)CC5C4)C3)C2)ccc1C(=O)NC1CCC(=O)NC1=O
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
Mino
Dmax
%
93.16
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1872
Homo sapiens
PROTAC COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING SAME, PREPARATION METHOD THEREFOR, AND USE THEREOF (patent)
Use Mino and HEK293 transfection BTK (C481S) cells to detect the degradation ability of the compound on BTK (WT) and BTK (C481S) protein. Mino human mantle cell lymphoma cell line was purchased from ATCC, cultured in RPMI-1640 medium with 15% FBS and 1% antibiotics. HEK293 OE BTK (C481S) human embryonic kidney cells 29...
TPDdb
Western Blot
TPD-8HOEB1
African=0.85%; Native American=0%; East Asian, North=1.5%; East Asian, South=0%; South Asian=6.1%; European, North=39.56%; European, South=51.98%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11,68; B*35,39; C*04,12. A*11 In situ; Peripheral blood; Caucasian. Cancer cell line
31
false
816
109
COc1cc(N2CC(N3CC(N4CC5CC(n6nc(-c7ccc(Oc8ccccc8)cc7)c7c(N)ncnc76)CC5C4)C3)C2)ccc1C(=O)NC1CCC(=O)NC1=O
IKZF1
MDADEGQDMSQVSGKESPPVSDTPDEGDEPMPIPEDLSTTSGGQQSSKSDRVVASNVKVETQSDEENGRACEMNGEECAEDLRMLDASGEKMNGSHRDQGSSALSGVGGIRLPNGKLKCDICGIICIGPNVLMVHKRSHTGERPFQCNQCGASFTQKGNLLRHIKLHSGEKPFKCHLCNYACRRRDALTGHLRTHSVGKPHKCGYCGRSYKQRSSLEEHKERCHNYLESMGLPGTLYPVIKEETNHSEMAEDLCKIGSERSLVLDRLASNVAKRKSSMPQKFLGDKGLSDTPYDSSASYEKENEMMKSHVMDQAINNAIN...
CRBN
Mino
DC50
nM
1,000
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q13422
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1872
Homo sapiens
PROTAC COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING SAME, PREPARATION METHOD THEREFOR, AND USE THEREOF (patent)
The IKZF1 protein is one of the target protein substrates for the degradation of amine compounds. The IMiD activity of the compound is judged by the IKZF1 protein degradation experiment. The Mino cell samples degraded by the above BTK protein were detected, and the IKZF1 (CST, Cat. 14859S) protein was simultaneously de...
TPDdb
Western Blot
TPD-8HOEB1
African=0.85%; Native American=0%; East Asian, North=1.5%; East Asian, South=0%; South Asian=6.1%; European, North=39.56%; European, South=51.98%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11,68; B*35,39; C*04,12. A*11 In situ; Peripheral blood; Caucasian. Cancer cell line
12
false
816
109
COc1cc(N2CC(N3CC(N4CC5CC(n6nc(-c7ccc(Oc8ccccc8)cc7)c7c(N)ncnc76)CC5C4)C3)C2)ccc1C(=O)NC1CCC(=O)NC1=O
IKZF1
MDADEGQDMSQVSGKESPPVSDTPDEGDEPMPIPEDLSTTSGGQQSSKSDRVVASNVKVETQSDEENGRACEMNGEECAEDLRMLDASGEKMNGSHRDQGSSALSGVGGIRLPNGKLKCDICGIICIGPNVLMVHKRSHTGERPFQCNQCGASFTQKGNLLRHIKLHSGEKPFKCHLCNYACRRRDALTGHLRTHSVGKPHKCGYCGRSYKQRSSLEEHKERCHNYLESMGLPGTLYPVIKEETNHSEMAEDLCKIGSERSLVLDRLASNVAKRKSSMPQKFLGDKGLSDTPYDSSASYEKENEMMKSHVMDQAINNAIN...
CRBN
Mino
Dmax
%
31.97
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q13422
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1872
Homo sapiens
PROTAC COMPOUND, PHARMACEUTICAL COMPOSITION COMPRISING SAME, PREPARATION METHOD THEREFOR, AND USE THEREOF (patent)
The IKZF1 protein is one of the target protein substrates for the degradation of amine compounds. The IMiD activity of the compound is judged by the IKZF1 protein degradation experiment. The Mino cell samples degraded by the above BTK protein were detected, and the IKZF1 (CST, Cat. 14859S) protein was simultaneously de...
TPDdb
Western Blot
TPD-8HOEB1
African=0.85%; Native American=0%; East Asian, North=1.5%; East Asian, South=0%; South Asian=6.1%; European, North=39.56%; European, South=51.98%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11,68; B*35,39; C*04,12. A*11 In situ; Peripheral blood; Caucasian. Cancer cell line
12
false
816
109
COc1cc(N2CCC(CN3CCN(c4ccc(-c5cc6c(-c7ccc([C@@H](C)NC(=O)c8nc(C(C)(C)C)no8)c(C)c7)ncnc6[nH]5)cc4)CC3)CC2)ccc1N1CCC(=O)NC1=O
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
null
DC50
nM
1.8
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
null
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE (patent)
HTFR assay After 6h treatment, add 10μl 4xlysis buffer to each well; seal the plate and incubate 30min at room temperature on a plate shaker; Once the cells are lysed, 16 μL of cell lysate are transferred to a PE 384-well HTRF detection plate; 4 μL of pre-mixed HTRF antibodies are added to each well; Cover the plate wi...
TPDdb
HTRF
TPD-OJI1R7
null
31
false
142
0
COc1cc(N2CCC(N3CCN(C(=O)C4CCN(CC5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
HCC827
DC50
nM
11.1
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_2063
Homo sapiens
BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent)
Cell treatment On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100...
TPDdb
HTRF
TPD-VRICT3
African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%. Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566). Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11 Stable (MSS) (Sanger). In situ; Lung; Caucasia...
23
false
817
0
COc1cc(N2CCC(N3CCN(C(=O)C4CCN(CC5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)CC4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
NCI-H1975
DC50
nM
49.1
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1511
Homo sapiens
BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent)
Cell treatment On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ...
TPDdb
HTRF
TPD-VRICT3
African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01 Stable (MSS) (Sanger). In situ; Lung; Caucasian. Cancer cell line
23
false
817
0
COc1cc(N2CCC(N3CCN(C(=O)C4CCN(c5cc(F)c(C6CCC(=O)NC6=O)c(F)c5)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
Ba/F3
DC50
nM
16.5
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q01279
Q8C7D2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0161
Mus musculus
BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent)
Cell treatment BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS...
TPDdb
HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation)
TPD-YWHUV6
Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse. IL3 dependent. C3H. In situ; Bone marrow; Pro-B cell; CL=CL_0000826. Factor-dependent cell line
23
true
-1
-1
COc1cc(N2CCC(N3CCN(C(=O)C4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)CC2)c(C)cc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
Ba/F3
DC50
nM
15.5
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q01279
Q8C7D2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0161
Mus musculus
BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent)
Cell treatment BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS...
TPDdb
HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation)
TPD-7289UC
Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse. IL3 dependent. C3H. In situ; Bone marrow; Pro-B cell; CL=CL_0000826. Factor-dependent cell line
23
false
818
64
COc1cc(N2CCC(N3CCN(C(=O)C4CN(c5cc(F)c(C6CCC(=O)NC6=O)c(F)c5)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
Ba/F3
DC50
nM
10.5
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q01279
Q8C7D2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0161
Mus musculus
BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent)
Cell treatment BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS...
TPDdb
HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation)
TPD-OU35FY
Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse. IL3 dependent. C3H. In situ; Bone marrow; Pro-B cell; CL=CL_0000826. Factor-dependent cell line
23
true
-1
-1
COc1cc(N2CCC(N3CCN(C(=O)C4CN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
Ba/F3
DC50
nM
6.5
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q01279
Q8C7D2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0161
Mus musculus
BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent)
Cell treatment BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS...
TPDdb
HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation)
TPD-40W2KS
Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse. IL3 dependent. C3H. In situ; Bone marrow; Pro-B cell; CL=CL_0000826. Factor-dependent cell line
23
false
819
64
COc1cc(N2CCC(N3CCN(C(=O)C4CN(c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
Ba/F3
DC50
nM
6.5
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q01279
Q8C7D2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0161
Mus musculus
BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent)
Cell treatment BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS...
TPDdb
HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation)
TPD-4SZN7R
Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse. IL3 dependent. C3H. In situ; Bone marrow; Pro-B cell; CL=CL_0000826. Factor-dependent cell line
23
false
820
98
COc1cc(N2CCC(N3CCN(C(=O)C4CN(c5ccc6c(c5)CN(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
HCC827
DC50
nM
2
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_2063
Homo sapiens
BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent)
Cell treatment On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100...
TPDdb
HTRF
TPD-4SZN7R
African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%. Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566). Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11 Stable (MSS) (Sanger). In situ; Lung; Caucasia...
23
false
820
98
COc1cc(N2CCC(N3CCN(C(=O)CCCCCCC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)NCc4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1
ALK
MGAIGLLWLLPLLLSTAAVGSGMGTGQRAGSPAAGPPLQPREPLSYSRLQRKSLAVDFVVPSLFRVYARDLLLPPSSSELKAGRPEARGSLALDCAPLLRLLGPAPGVSWTAGSPAPAEARTLSRVLKGGSVRKLRRAKQLVLELGEEAILEGCVGPPGEAAVGLLQFNLSELFSWWIRQGEGRLRIRLMPEKKASEVGREGRLSAAIRASQPRLLFQIFGTGHSSLESPTNMPSPSPDYFTWNLTWIMKDSFPFLSHRSRYGLECSFDFPCELEYSPPLHDLRNQSWSWRRIPSEEASQMDLLDGPGAERSKEMPRGSF...
VHL
SR
DC50
nM
11.4
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q9UM73
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1711
Homo sapiens
10.1016/j.ejmech.2020.112190; https://pubmed.ncbi.nlm.nih.gov/32179332/
Degradation of ALK in SR cells after 16 h treatment; EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells).
PROTAC-DB; PROTACpedia
null
null
African=0%; Native American=0%; East Asian, North=3.12%; East Asian, South=0%; South Asian=0%; European, North=62.78%; European, South=34.1%. Gene fusion; HGNC; HGNC A*02,03; B*37 A*02 A*02 Stable (MSS) (Sanger). In situ; Pleural effusion; Caucasian. Cancer cell line
-1
false
821
0
COc1cc(N2CCC(N3CCN(C(=O)CCCCCCCC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)NCc4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1
ALK
MGAIGLLWLLPLLLSTAAVGSGMGTGQRAGSPAAGPPLQPREPLSYSRLQRKSLAVDFVVPSLFRVYARDLLLPPSSSELKAGRPEARGSLALDCAPLLRLLGPAPGVSWTAGSPAPAEARTLSRVLKGGSVRKLRRAKQLVLELGEEAILEGCVGPPGEAAVGLLQFNLSELFSWWIRQGEGRLRIRLMPEKKASEVGREGRLSAAIRASQPRLLFQIFGTGHSSLESPTNMPSPSPDYFTWNLTWIMKDSFPFLSHRSRYGLECSFDFPCELEYSPPLHDLRNQSWSWRRIPSEEASQMDLLDGPGAERSKEMPRGSF...
VHL
SR
DC50
nM
25.1
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q9UM73
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1711
Homo sapiens
10.1016/j.ejmech.2020.112190; https://pubmed.ncbi.nlm.nih.gov/32179332/
Degradation of ALK in SR cells after 16 h treatment; EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells).
PROTAC-DB; PROTACpedia
null
null
African=0%; Native American=0%; East Asian, North=3.12%; East Asian, South=0%; South Asian=0%; European, North=62.78%; European, South=34.1%. Gene fusion; HGNC; HGNC A*02,03; B*37 A*02 A*02 Stable (MSS) (Sanger). In situ; Pleural effusion; Caucasian. Cancer cell line
-1
false
822
0
COc1cc(N2CCC(N3CCN(C(=O)CCCCCCCCC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)NCc4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1
ALK
MGAIGLLWLLPLLLSTAAVGSGMGTGQRAGSPAAGPPLQPREPLSYSRLQRKSLAVDFVVPSLFRVYARDLLLPPSSSELKAGRPEARGSLALDCAPLLRLLGPAPGVSWTAGSPAPAEARTLSRVLKGGSVRKLRRAKQLVLELGEEAILEGCVGPPGEAAVGLLQFNLSELFSWWIRQGEGRLRIRLMPEKKASEVGREGRLSAAIRASQPRLLFQIFGTGHSSLESPTNMPSPSPDYFTWNLTWIMKDSFPFLSHRSRYGLECSFDFPCELEYSPPLHDLRNQSWSWRRIPSEEASQMDLLDGPGAERSKEMPRGSF...
VHL
SR
DC50
nM
7.5
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q9UM73
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1711
Homo sapiens
10.1016/j.ejmech.2020.112190; https://pubmed.ncbi.nlm.nih.gov/32179332/
Degradation of ALK in SR cells after 16 h treatment; EC50 of ligand is 2.7 ± 0.4nM (SF cells), 58.2 ± 20.7 nM (H2228 cells).
PROTAC-DB; PROTACpedia
null
null
African=0%; Native American=0%; East Asian, North=3.12%; East Asian, South=0%; South Asian=0%; European, North=62.78%; European, South=34.1%. Gene fusion; HGNC; HGNC A*02,03; B*37 A*02 A*02 Stable (MSS) (Sanger). In situ; Pleural effusion; Caucasian. Cancer cell line
-1
false
823
0
COc1cc(N2CCC(N3CCN(C(=O)CCN4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
HCC827
DC50
nM
4.9
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_2063
Homo sapiens
BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent)
Cell treatment On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100...
TPDdb
HTRF
TPD-HOUUTK
African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%. Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566). Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11 Stable (MSS) (Sanger). In situ; Lung; Caucasia...
23
false
824
0
COc1cc(N2CCC(N3CCN(C(=O)CCN4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)CC2)c(C)cc1Nc1ncc(Br)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
NCI-H1975
DC50
nM
13.5
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1511
Homo sapiens
BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent)
Cell treatment On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ...
TPDdb
HTRF
TPD-HOUUTK
African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01 Stable (MSS) (Sanger). In situ; Lung; Caucasian. Cancer cell line
23
false
824
0
COc1cc(N2CCC(N3CCN(C(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1
ALK
MGAIGLLWLLPLLLSTAAVGSGMGTGQRAGSPAAGPPLQPREPLSYSRLQRKSLAVDFVVPSLFRVYARDLLLPPSSSELKAGRPEARGSLALDCAPLLRLLGPAPGVSWTAGSPAPAEARTLSRVLKGGSVRKLRRAKQLVLELGEEAILEGCVGPPGEAAVGLLQFNLSELFSWWIRQGEGRLRIRLMPEKKASEVGREGRLSAAIRASQPRLLFQIFGTGHSSLESPTNMPSPSPDYFTWNLTWIMKDSFPFLSHRSRYGLECSFDFPCELEYSPPLHDLRNQSWSWRRIPSEEASQMDLLDGPGAERSKEMPRGSF...
CRBN
SR
DC50
nM
10
null
null
null
null
24
<
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q9UM73
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1711
Homo sapiens
10.1021/acs.jmedchem.1c00373
Degradation of ALK in SR cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=3.12%; East Asian, South=0%; South Asian=0%; European, North=62.78%; European, South=34.1%. Gene fusion; HGNC; HGNC A*02,03; B*37 A*02 A*02 Stable (MSS) (Sanger). In situ; Pleural effusion; Caucasian. Cancer cell line
-1
false
825
267
COc1cc(N2CCC(N3CCN(C(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1
ALK G1202R
MGAIGLLWLLPLLLSTAAVGSGMGTGQRAGSPAAGPPLQPREPLSYSRLQRKSLAVDFVVPSLFRVYARDLLLPPSSSELKAGRPEARGSLALDCAPLLRLLGPAPGVSWTAGSPAPAEARTLSRVLKGGSVRKLRRAKQLVLELGEEAILEGCVGPPGEAAVGLLQFNLSELFSWWIRQGEGRLRIRLMPEKKASEVGREGRLSAAIRASQPRLLFQIFGTGHSSLESPTNMPSPSPDYFTWNLTWIMKDSFPFLSHRSRYGLECSFDFPCELEYSPPLHDLRNQSWSWRRIPSEEASQMDLLDGPGAERSKEMPRGSF...
CRBN
HEK293T
DC50
nM
100
null
null
null
null
72
<
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q9UM73
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0063
Homo sapiens
10.1021/acs.jmedchem.1c00373
Degradation of ALK G1202R in 293T cells after 72 h treatment
PROTAC-DB
null
null
Highly susceptible to infection by Zika virus (ZIKV). CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. NCBI_TaxID; 1891767; Simian virus 40 (SV40) (Note=tsA). Transformed cell line
-1
false
825
267
COc1cc(N2CCC(N3CCN(C(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1
EGFR L858R/T790M
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
NCI-H1975
DC50
nM
100
null
null
null
null
72
<
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1511
Homo sapiens
10.1021/acs.jmedchem.1c00373
Degradation of EGFR L858R/T790M in H1975 cells after 72 h treatment
PROTAC-DB
null
null
African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01 Stable (MSS) (Sanger). In situ; Lung; Caucasian. Cancer cell line
23
false
825
267
COc1cc(N2CCC(N3CCN(C(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
A-549
DC50
nM
1
null
null
null
null
16
<
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0023
Homo sapiens
10.1021/acs.jmedchem.1c00373
Degradation of FAK in NCI-H2228/A549/Calu-1 cells after 16 h treatment
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
24
false
825
267
COc1cc(N2CCC(N3CCN(C(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
Calu-1
DC50
nM
1
null
null
null
null
16
<
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0608
Homo sapiens
10.1021/acs.jmedchem.1c00373
Degradation of FAK in NCI-H2228/A549/Calu-1 cells after 16 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.74%; East Asian, North=0.11%; East Asian, South=0%; South Asian=9.94%; European, North=31.4%; European, South=57.8%. Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*10,11; B*15,w35 (CLS=300141). A*26 Metastatic; Pleural effusion; Caucasian. Cancer cell line
24
false
825
267
COc1cc(N2CCC(N3CCN(C(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1
FAK
MAAAYLDPNLNHTPNSSTKTHLGTGMERSPGAMERVLKVFHYFESNSEPTTWASIIRHGDATDVRGIIQKIVDSHKVKHVACYGFRLSHLRSEEVHWLHVDMGVSSVREKYELAHPPEEWKYELRIRYLPKGFLNQFTEDKPTLNFFYQQVKSDYMLEIADQVDQEIALKLGCLEIRRSYWEMRGNALEKKSNYEVLEKDVGLKRFFPKSLLDSVKAKTLRKLIQQTFRQFANLNREESILKFFEILSPVYRFDKECFKCALGSSWIISVELAIGPEEGISYLTDKGCNPTHLADFTQVQTIQYSNSEDKDRKGMLQLKI...
CRBN
NCI-H2228
DC50
nM
1
null
null
null
null
16
<
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q05397
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1543
Homo sapiens
10.1021/acs.jmedchem.1c00373
Degradation of FAK in NCI-H2228/A549/Calu-1 cells after 16 h treatment
PROTAC-DB
null
null
African=0.1%; Native American=0.08%; East Asian, North=0.5%; East Asian, South=0.06%; South Asian=0.85%; European, North=65.31%; European, South=33.09%. Gene fusion; HGNC; HGNC Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ; Lung; Caucasian. Cancer cell line
24
false
825
267
COc1cc(N2CCC(N3CCN(C(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1
FER
MGFGSDLKNSHEAVLKLQDWELRLLETVKKFMALRIKSDKEYASTLQNLCNQVDKESTVQMNYVSNVSKSWLLMIQQTEQLSRIMKTHAEDLNSGPLHRLTMMIKDKQQVKKSYIGVHQQIEAEMIKVTKTELEKLKCSYRQLIKEMNSAKEKYKEALAKGKETEKAKERYDKATMKLHMLHNQYVLALKGAQLHQNQYYDITLPLLLDSLQKMQEEMIKALKGIFDEYSQITSLVTEEIVNVHKEIQMSVEQIDPSTEYNNFIDVHRTTAAKEQEIEFDTSLLEENENLQANEIMWNNLTAESLQVMLKTLAEELMQTQ...
CRBN
SR
DC50
nM
10
null
null
null
null
24
<
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P16591
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1711
Homo sapiens
10.1021/acs.jmedchem.1c00373
Degradation of FER in SR cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=3.12%; East Asian, South=0%; South Asian=0%; European, North=62.78%; European, South=34.1%. Gene fusion; HGNC; HGNC A*02,03; B*37 A*02 A*02 Stable (MSS) (Sanger). In situ; Pleural effusion; Caucasian. Cancer cell line
-1
false
825
267
COc1cc(N2CCC(N3CCN(C(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1
PTK6
MVSRDQAHLGPKYVGLWDFKSRTDEELSFRAGDVFHVARKEEQWWWATLLDEAGGAVAQGYVPHNYLAERETVESEPWFFGCISRSEAVRRLQAEGNATGAFLIRVSEKPSADYVLSVRDTQAVRHYKIWRRAGGRLHLNEAVSFLSLPELVNYHRAQSLSHGLRLAAPCRKHEPEPLPHWDDWERPREEFTLCRKLGSGYFGEVFEGLWKDRVQVAIKVISRDNLLHQQMLQSEIQAMKKLRHKHILALYAVVSVGDPVYIITELMAKGSLLELLRDSDEKVLPVSELLDIAWQVAEGMCYLESQNYIHRDLAARNILV...
CRBN
MDA-MB-231
DC50
nM
1
null
null
null
null
16
<
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q13882
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0062
Homo sapiens
10.1021/acs.jmedchem.1c00373
Degradation of PTK6 in MDA-MB-231 cells after 16 h treatment
PROTAC-DB
null
null
African=1.95%; Native American=0%; East Asian, North=2.44%; East Asian, South=0%; South Asian=7.42%; European, North=28.16%; European, South=60.03%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02/28; B*07,08; C*w02,w06. A*02 A...
30
false
825
267
COc1cc(N2CCC(N3CCN(C(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1
PYK2
MSGVSEPLSRVKLGTLRRPEGPAEPMVVVPVDVEKEDVRILKVCFYSNSFNPGKNFKLVKCTVQTEIREIITSILLSGRIGPNIRLAECYGLRLKHMKSDEIHWLHPQMTVGEVQDKYECLHVEAEWRYDLQIRYLPEDFMESLKEDRTTLLYFYQQLRNDYMQRYASKVSEGMALQLGCLELRRFFKDMPHNALDKKSNFELLEKEVGLDLFFPKQMQENLKPKQFRKMIQQTFQQYASLREEECVMKFFNTLAGFANIDQETYRCELIQGWNITVDLVIGPKGIRQLTSQDAKPTCLAEFKQIRSIRCLPLEEGQAVL...
CRBN
SR
DC50
nM
1
null
null
null
null
24
<
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q14289
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1711
Homo sapiens
10.1021/acs.jmedchem.1c00373
Degradation of PYK2 in SR cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=3.12%; East Asian, South=0%; South Asian=0%; European, North=62.78%; European, South=34.1%. Gene fusion; HGNC; HGNC A*02,03; B*37 A*02 A*02 Stable (MSS) (Sanger). In situ; Pleural effusion; Caucasian. Cancer cell line
24
false
825
267
COc1cc(N2CCC(N3CCN(C(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1
RSK1
MPLAQLKEPWPLMELVPLDPENGQTSGEEAGLQPSKDEGVLKEISITHHVKAGSEKADPSHFELLKVLGQGSFGKVFLVRKVTRPDSGHLYAMKVLKKATLKVRDRVRTKMERDILADVNHPFVVKLHYAFQTEGKLYLILDFLRGGDLFTRLSKEVMFTEEDVKFYLAELALGLDHLHSLGIIYRDLKPENILLDEEGHIKLTDFGLSKEAIDHEKKAYSFCGTVEYMAPEVVNRQGHSHSADWWSYGVLMFEMLTGSLPFQGKDRKETMTLILKAKLGMPQFLSTEAQSLLRALFKRNPANRLGSGPDGAEEIKRHVF...
CRBN
A-549
DC50
nM
100
null
null
null
null
16
<
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q15418
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0023
Homo sapiens
10.1021/acs.jmedchem.1c00373
Degradation of RSK1 in NCI-H2228/A549/Calu-1 cells after 16 h treatment
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
29
false
825
267
COc1cc(N2CCC(N3CCN(C(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1
RSK1
MPLAQLKEPWPLMELVPLDPENGQTSGEEAGLQPSKDEGVLKEISITHHVKAGSEKADPSHFELLKVLGQGSFGKVFLVRKVTRPDSGHLYAMKVLKKATLKVRDRVRTKMERDILADVNHPFVVKLHYAFQTEGKLYLILDFLRGGDLFTRLSKEVMFTEEDVKFYLAELALGLDHLHSLGIIYRDLKPENILLDEEGHIKLTDFGLSKEAIDHEKKAYSFCGTVEYMAPEVVNRQGHSHSADWWSYGVLMFEMLTGSLPFQGKDRKETMTLILKAKLGMPQFLSTEAQSLLRALFKRNPANRLGSGPDGAEEIKRHVF...
CRBN
Calu-1
DC50
nM
100
null
null
null
null
16
<
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q15418
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0608
Homo sapiens
10.1021/acs.jmedchem.1c00373
Degradation of RSK1 in NCI-H2228/A549/Calu-1 cells after 16 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.74%; East Asian, North=0.11%; East Asian, South=0%; South Asian=9.94%; European, North=31.4%; European, South=57.8%. Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*10,11; B*15,w35 (CLS=300141). A*26 Metastatic; Pleural effusion; Caucasian. Cancer cell line
29
false
825
267
COc1cc(N2CCC(N3CCN(C(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1
RSK1
MPLAQLKEPWPLMELVPLDPENGQTSGEEAGLQPSKDEGVLKEISITHHVKAGSEKADPSHFELLKVLGQGSFGKVFLVRKVTRPDSGHLYAMKVLKKATLKVRDRVRTKMERDILADVNHPFVVKLHYAFQTEGKLYLILDFLRGGDLFTRLSKEVMFTEEDVKFYLAELALGLDHLHSLGIIYRDLKPENILLDEEGHIKLTDFGLSKEAIDHEKKAYSFCGTVEYMAPEVVNRQGHSHSADWWSYGVLMFEMLTGSLPFQGKDRKETMTLILKAKLGMPQFLSTEAQSLLRALFKRNPANRLGSGPDGAEEIKRHVF...
CRBN
NCI-H2228
DC50
nM
100
null
null
null
null
16
<
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q15418
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1543
Homo sapiens
10.1021/acs.jmedchem.1c00373
Degradation of RSK1 in NCI-H2228/A549/Calu-1 cells after 16 h treatment
PROTAC-DB
null
null
African=0.1%; Native American=0.08%; East Asian, North=0.5%; East Asian, South=0.06%; South Asian=0.85%; European, North=65.31%; European, South=33.09%. Gene fusion; HGNC; HGNC Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ; Lung; Caucasian. Cancer cell line
29
false
825
267
COc1cc(N2CCC(N3CCN(C(=O)[C@@H]4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
Ba/F3
DC50
nM
29.45
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q01279
Q8C7D2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0161
Mus musculus
BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent)
Cell treatment BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS...
TPDdb
HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation)
TPD-06P9WK
Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse. IL3 dependent. C3H. In situ; Bone marrow; Pro-B cell; CL=CL_0000826. Factor-dependent cell line
23
false
826
64
COc1cc(N2CCC(N3CCN(C(=O)[C@@H]4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
HCC827
DC50
nM
2.7
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_2063
Homo sapiens
BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent)
Cell treatment On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100...
TPDdb
HTRF
TPD-06P9WK
African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%. Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566). Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11 Stable (MSS) (Sanger). In situ; Lung; Caucasia...
23
false
826
64
COc1cc(N2CCC(N3CCN(C(=O)[C@@H]4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
NCI-H1975
DC50
nM
4.2
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1511
Homo sapiens
BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent)
Cell treatment On day1, H1975 cells are seeded at 30000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, H1975 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 1000× ...
TPDdb
HTRF
TPD-06P9WK
African=0.35%; Native American=0%; East Asian, North=1.32%; East Asian, South=0%; South Asian=7.46%; European, North=30.01%; European, South=60.85%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01 Stable (MSS) (Sanger). In situ; Lung; Caucasian. Cancer cell line
23
false
826
64
COc1cc(N2CCC(N3CCN(C(=O)[C@H]4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
Ba/F3
DC50
nM
9.45
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q01279
Q8C7D2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0161
Mus musculus
BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent)
Cell treatment BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS...
TPDdb
HTRF DTC (Del19 / T790M / C797S triple mutation); HTRF LTC (L858R / T790M / C797S triple mutation)
TPD-H15E5M
Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse. IL3 dependent. C3H. In situ; Bone marrow; Pro-B cell; CL=CL_0000826. Factor-dependent cell line
23
false
826
64
COc1cc(N2CCC(N3CCN(C(=O)[C@H]4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)C4)CC3)CC2)ccc1Nc1ncc(Cl)c(Nc2cccc3c2N(S(C)(=O)=O)CC3)n1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
HCC827
DC50
nM
3.1
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_2063
Homo sapiens
BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent)
Cell treatment On day 1, HCC827 cells are seeded at 20000 cells/well at a volume of 90μl/well in cell culture medium [RPMI1640 , 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate, HCC827 cells are treated with compounds diluted in 0.2%DMSO on day 2, dilution is done according to the following protocol: (1) make 100...
TPDdb
HTRF
TPD-H15E5M
African=1.62%; Native American=0.39%; East Asian, North=3.47%; East Asian, South=0%; South Asian=7.09%; European, North=19.48%; European, South=67.96%. Flat-moded hypotriploid karyotype with 6% polyploidy (DSMZ=ACC-566). Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11 Stable (MSS) (Sanger). In situ; Lung; Caucasia...
23
false
826
64