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
C=C(F)C(=O)N1CCN(c2nc(OC[C@@H]3CCCN3CCCOCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)nc3c2CCN(c2cccc4cccc(Cl)c24)C3)C[C@@H]1CC#N
KRAS G12C
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
NCI-H23
Dmax
%
90
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1547
Homo sapiens
10.1021/acscentsci.0c00411
Degradation of KRAS G12C in NCI-H23/NCI-H358 cells after 24 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
40
0
C=C(F)C(=O)N1CCN(c2nc(OC[C@@H]3CCCN3CCCOCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)nc3c2CCN(c2cccc4cccc(Cl)c24)C3)C[C@@H]1CC#N
KRAS G12C
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
NCI-H358
DC50
nM
520
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1559
Homo sapiens
10.1021/acscentsci.0c00411
Degradation of KRAS G12C in NCI-H23/NCI-H358 cells after 24 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
40
0
C=C(F)C(=O)N1CCN(c2nc(OC[C@@H]3CCCN3CCCOCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)nc3c2CCN(c2cccc4cccc(Cl)c24)C3)C[C@@H]1CC#N
KRAS G12C
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
NCI-H358
Dmax
%
40
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1559
Homo sapiens
10.1021/acscentsci.0c00411
Degradation of KRAS G12C in NCI-H23/NCI-H358 cells after 24 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
40
0
C=C(F)C(=O)N1CCN(c2nc(OC[C@@H]3CCCN3CCCOCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)nc3c2CCN(c2cccc4cccc(Cl)c24)C3)C[C@@H]1CC#N
KRAS G12C
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
SW1573
DC50
nM
760
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
10.1021/acscentsci.0c00411
Degradation of KRAS G12C in NCI-H2030/MIA PaCa-2/SW1573 cells after 24 h treatment
PROTAC-DB
null
null
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
-1
false
40
0
C=C(F)C(=O)N1CCN(c2nc(OC[C@@H]3CCCN3CCCOCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)nc3c2CCN(c2cccc4cccc(Cl)c24)C3)C[C@@H]1CC#N
KRAS G12C
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
SW1573
Dmax
%
90
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
10.1021/acscentsci.0c00411
Degradation of KRAS G12C in NCI-H2030/MIA PaCa-2/SW1573 cells after 24 h treatment
PROTAC-DB
null
null
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
-1
false
40
0
C=C(F)C(=O)N1CCN(c2nc(OC[C@@H]3CCCN3CCOCCOCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)nc3c2CCN(c2cccc4cccc(Cl)c24)C3)C[C@@H]1CC#N
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
SW1573
DC50
nM
10,000
null
null
null
null
24
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/32875077/
null
PROTACpedia
null
null
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
-1
false
41
0
C=C(F)C(=O)N1CCN(c2nc(OC[C@@H]3CCCN3CCOCCOCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)nc3c2CCN(c2cccc4cccc(Cl)c24)C3)C[C@@H]1CC#N
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
SW1573
Dmax
%
50
null
null
null
null
72
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/32875077/
null
PROTACpedia
null
null
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
-1
false
41
0
C=C(F)C(=O)N1CCN(c2nc(OC[C@@H]3CCCN3CCOCCOCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)nc3c2CCN(c2cccc4cccc(Cl)c24)C3)C[C@@H]1CC#N
KRAS G12C
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
SW1573
DC50
nM
10,000
null
null
null
null
24
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
10.1021/acscentsci.0c00411
Degradation of KRAS G12C in SW1573 cells after 24 h treatment
PROTAC-DB
null
null
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
-1
false
41
0
C=C(F)C(=O)N1CCN(c2nc(OC[C@@H]3CCCN3CCOCCOCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)nc3c2CCN(c2cccc4cccc(Cl)c24)C3)C[C@@H]1CC#N
KRAS G12C
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
SW1573
Dmax
%
50
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
10.1021/acscentsci.0c00411
Degradation of KRAS G12C in SW1573 cells after 24 h treatment
PROTAC-DB
null
null
African=0.36%; Native American=0.18%; East Asian, North=0.45%; East Asian, South=0%; South Asian=0%; European, North=66.92%; European, South=32.09%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Stable (MSS) (Sanger). In situ...
-1
false
41
0
C=C/C=C(\C=C)Oc1ccc(-c2nn3c(c2C(N)=O)NCC[C@H]3C2CCN(C(=O)/C=C/CN(C)CCCN3C(=O)CCC(N4Cc5c(N)cccc5C4=O)C3=O)CC2)cc1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
Ramos
DC50
nM
428
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0597
Homo sapiens
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INIDBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE (patent)
Cells in 96 well plate are harvested by centrifugation (1200rpm) , and wash once with ice-cold PBS. Then, 100ul 1×cell extraction buffer is added in each well. The cells are placed on a shaker for 20min at 4°C; 5ul lysate is transferred to 45ul of 1×cell extraction buffer in ELISA plate, and 50ul of the antibody cockta...
TPDdb
ELISA
TPD-31LHRD
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
31
false
42
188
C=C1CCC(N2C(=O)c3ccc(N4CCC(CNc5ccc6c(c5)CCn5nc(-c7ccc(Oc8ccccc8)cc7)c(C(N)=O)c5N6)CC4)cc3C2=O)C(=O)N1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
20.6
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-U606A8
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
true
-1
-1
C=C1CN(C2CCC(=O)NC2=O)C(=O)c2ccc(N3CCN(CC4CCN(c5ccc(C(=O)N[C@H]6C(C)(C)[C@H](Oc7ccc(C#N)c(Cl)c7)C6(C)C)cc5)CC4)CC3)cc21
AR
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL...
CRBN
VCaP
DC50
nM
1
null
null
null
null
null
<
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P10275
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_2235
Homo sapiens
Cereblon ligands and bifunctional compounds comprising the same (patent)
5. AR ELISA Assay Protocol Compounds were evaluated in this assay in LNCaP and/or VCaP cells utilizing similar protocols. The protocols used with VCaP cells are described below. The androgen receptor ELISA assay was performed using PathScan AR Sandwich ELISA (Cell Signaling Catalog 12850) according to the following ass...
TPDdb
AR ELISA
TPD-GMPK2P
African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%. Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Established from a xenograft produced by...
16
false
43
81
C=C1CN(C2CCC(=O)NC2=O)C(=O)c2ccc(N3CCN(CC4CCN(c5ccc(C(=O)N[C@H]6C(C)(C)[C@H](Oc7ccc(C#N)c(Cl)c7)C6(C)C)cc5)CC4)CC3)cc21
AR
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL...
CRBN
VCaP
Dmax
%
75
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P10275
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_2235
Homo sapiens
Cereblon ligands and bifunctional compounds comprising the same (patent)
5. AR ELISA Assay Protocol Compounds were evaluated in this assay in LNCaP and/or VCaP cells utilizing similar protocols. The protocols used with VCaP cells are described below. The androgen receptor ELISA assay was performed using PathScan AR Sandwich ELISA (Cell Signaling Catalog 12850) according to the following ass...
TPDdb
AR ELISA
TPD-GMPK2P
African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%. Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Established from a xenograft produced by...
16
false
43
81
C=C1CN2[C@H](CN3CCC(c4cn([C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)N[C@@H](C)c5ccc(-c6scnc6C)cc5)C(C)C)nn4)CC3)CC[C@@]2(COc2nc(N3CCC[C@@](C)(O)C3)c3cnc(-c4cc(O)cc5ccc(F)c(CC)c45)cc3n2)C1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
AGS
DC50
nM
122
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0139
Homo sapiens
COMPOUND TARGETING PAN-KRAS PROTEIN DEGRADATION AGENT AND USE THEREOF (patent)
1) Observation under a microscope showed that the cells were in good condition, in the logarithmic growth phase, and the cell density was 80-90%. 2) Digest the cells with trypsin for 1-2 minutes, terminate the digestion with 5 mL of fresh culture medium, gently blow the cells to make a single cell suspension, and centr...
TPDdb
Western Blot
TPD-ZMU5K7
African=3.44%; Native American=32.25%; East Asian, North=5.38%; East Asian, South=0%; South Asian=0.23%; European, North=27.58%; European, South=31.12%. Persistently infected with parainfluenza virus type 5 (PIV5) strain PIV5-AGS. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutat...
-1
false
44
0
C=C1CN2[C@H](COC(=O)N3CCC4(CC3)CC(CNC(=O)C[C@H](NC(=O)[C@@H]3C[C@@H](O)CN3C(=O)C(c3cc(C)no3)C(C)C)c3ccc(-c5scnc5C)cc3)C4)CC[C@@]2(COc2nc(N3CCC[C@@](C)(O)C3)c3cnc(-c4cc(O)cc5ccc(F)c(CC)c45)c(F)c3n2)C1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
AGS
DC50
nM
31
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0139
Homo sapiens
COMPOUND TARGETING PAN-KRAS PROTEIN DEGRADATION AGENT AND USE THEREOF (patent)
1) Observation under a microscope showed that the cells were in good condition, in the logarithmic growth phase, and the cell density was 80-90%. 2) Digest the cells with trypsin for 1-2 minutes, terminate the digestion with 5 mL of fresh culture medium, gently blow the cells to make a single cell suspension, and centr...
TPDdb
Western Blot
TPD-DII5OI
African=3.44%; Native American=32.25%; East Asian, North=5.38%; East Asian, South=0%; South Asian=0.23%; European, North=27.58%; European, South=31.12%. Persistently infected with parainfluenza virus type 5 (PIV5) strain PIV5-AGS. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutat...
-1
false
45
0
C=C1CN2[C@H](COC(=O)N3CCC4(CC3)CC(CNC(=O)C[C@H](NC(=O)[C@@H]3C[C@@H](O)CN3C(=O)C(c3cc(C)no3)C(C)C)c3ccc(-c5scnc5C)cc3)C4)CC[C@@]2(COc2nc(N3CCC[C@@](C)(O)C3)c3cnc(-c4cc(O)cc5ccc(F)c(CC)c45)c(F)c3n2)C1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
AGS
Dmax
%
95
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0139
Homo sapiens
COMPOUND TARGETING PAN-KRAS PROTEIN DEGRADATION AGENT AND USE THEREOF (patent)
1) Observation under a microscope showed that the cells were in good condition, in the logarithmic growth phase, and the cell density was 80-90%. 2) Digest the cells with trypsin for 1-2 minutes, terminate the digestion with 5 mL of fresh culture medium, gently blow the cells to make a single cell suspension, and centr...
TPDdb
Western Blot
TPD-DII5OI
African=3.44%; Native American=32.25%; East Asian, North=5.38%; East Asian, South=0%; South Asian=0.23%; European, North=27.58%; European, South=31.12%. Persistently infected with parainfluenza virus type 5 (PIV5) strain PIV5-AGS. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutat...
-1
false
45
0
C=C1CN2[C@H](COC(=O)NCC34CC(c5cn([C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)N[C@@H](C)c6ccc(-c7scnc7C)cc6)C(C)C)nn5)(C3)C4)CC[C@@]2(COc2nc(N3CCC[C@@](C)(O)C3)c3cnc(-c4cc(O)cc5ccc(F)c(CC)c45)cc3n2)C1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
AGS
DC50
nM
23
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0139
Homo sapiens
COMPOUND TARGETING PAN-KRAS PROTEIN DEGRADATION AGENT AND USE THEREOF (patent)
1) Observation under a microscope showed that the cells were in good condition, in the logarithmic growth phase, and the cell density was 80-90%. 2) Digest the cells with trypsin for 1-2 minutes, terminate the digestion with 5 mL of fresh culture medium, gently blow the cells to make a single cell suspension, and centr...
TPDdb
Western Blot
TPD-QHWSEE
African=3.44%; Native American=32.25%; East Asian, North=5.38%; East Asian, South=0%; South Asian=0.23%; European, North=27.58%; European, South=31.12%. Persistently infected with parainfluenza virus type 5 (PIV5) strain PIV5-AGS. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutat...
-1
false
46
0
C=C1CN2[C@H](COC(=O)NCC34CC(c5cn([C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)N[C@@H](C)c6ccc(-c7scnc7C)cc6)C(C)C)nn5)(C3)C4)CC[C@@]2(COc2nc(N3CCC[C@@](C)(O)C3)c3cnc(-c4cc(O)cc5ccc(F)c(CC)c45)cc3n2)C1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
AGS
Dmax
%
95
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0139
Homo sapiens
COMPOUND TARGETING PAN-KRAS PROTEIN DEGRADATION AGENT AND USE THEREOF (patent)
1) Observation under a microscope showed that the cells were in good condition, in the logarithmic growth phase, and the cell density was 80-90%. 2) Digest the cells with trypsin for 1-2 minutes, terminate the digestion with 5 mL of fresh culture medium, gently blow the cells to make a single cell suspension, and centr...
TPDdb
Western Blot
TPD-QHWSEE
African=3.44%; Native American=32.25%; East Asian, North=5.38%; East Asian, South=0%; South Asian=0.23%; European, North=27.58%; European, South=31.12%. Persistently infected with parainfluenza virus type 5 (PIV5) strain PIV5-AGS. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutat...
-1
false
46
0
C=C1CN2[C@H](COCc3ccc(-c4cn([C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)N[C@@H](C)c5ccc(-c6scnc6C)cc5)C(C)C)nn4)cc3)CC[C@@]2(COc2nc(N3CCC[C@@](C)(O)C3)c3cnc(-c4cc(O)cc5ccc(F)c(CC)c45)cc3n2)C1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
AGS
DC50
nM
22
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0139
Homo sapiens
COMPOUND TARGETING PAN-KRAS PROTEIN DEGRADATION AGENT AND USE THEREOF (patent)
1) Observation under a microscope showed that the cells were in good condition, in the logarithmic growth phase, and the cell density was 80-90%. 2) Digest the cells with trypsin for 1-2 minutes, terminate the digestion with 5 mL of fresh culture medium, gently blow the cells to make a single cell suspension, and centr...
TPDdb
Western Blot
TPD-6XC8G1
African=3.44%; Native American=32.25%; East Asian, North=5.38%; East Asian, South=0%; South Asian=0.23%; European, North=27.58%; European, South=31.12%. Persistently infected with parainfluenza virus type 5 (PIV5) strain PIV5-AGS. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutat...
-1
false
47
0
C=C1CN2[C@H](COCc3ccc(-c4cn([C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)N[C@@H](C)c5ccc(-c6scnc6C)cc5)C(C)C)nn4)cc3)CC[C@@]2(COc2nc(N3CCC[C@@](C)(O)C3)c3cnc(-c4cc(O)cc5ccc(F)c(CC)c45)cc3n2)C1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
AGS
Dmax
%
95
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0139
Homo sapiens
COMPOUND TARGETING PAN-KRAS PROTEIN DEGRADATION AGENT AND USE THEREOF (patent)
1) Observation under a microscope showed that the cells were in good condition, in the logarithmic growth phase, and the cell density was 80-90%. 2) Digest the cells with trypsin for 1-2 minutes, terminate the digestion with 5 mL of fresh culture medium, gently blow the cells to make a single cell suspension, and centr...
TPDdb
Western Blot
TPD-6XC8G1
African=3.44%; Native American=32.25%; East Asian, North=5.38%; East Asian, South=0%; South Asian=0.23%; European, North=27.58%; European, South=31.12%. Persistently infected with parainfluenza virus type 5 (PIV5) strain PIV5-AGS. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutat...
-1
false
47
0
C=C1CN2[C@H](COCc3cnnn3[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)N[C@@H](C)c3ccc(-c4scnc4C)cc3)C(C)C)CC[C@@]2(COc2nc(N3CCC[C@@](C)(O)C3)c3cnc(-c4cc(O)cc5ccc(F)c(CC)c45)c(F)c3n2)C1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
AGS
DC50
nM
11
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0139
Homo sapiens
COMPOUND TARGETING PAN-KRAS PROTEIN DEGRADATION AGENT AND USE THEREOF (patent)
1) Observation under a microscope showed that the cells were in good condition, in the logarithmic growth phase, and the cell density was 80-90%. 2) Digest the cells with trypsin for 1-2 minutes, terminate the digestion with 5 mL of fresh culture medium, gently blow the cells to make a single cell suspension, and centr...
TPDdb
Western Blot
TPD-1S65YG
African=3.44%; Native American=32.25%; East Asian, North=5.38%; East Asian, South=0%; South Asian=0.23%; European, North=27.58%; European, South=31.12%. Persistently infected with parainfluenza virus type 5 (PIV5) strain PIV5-AGS. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutat...
-1
false
48
0
C=C1CN2[C@H](COCc3cnnn3[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)N[C@@H](C)c3ccc(-c4scnc4C)cc3)C(C)C)CC[C@@]2(COc2nc(N3CCC[C@@](C)(O)C3)c3cnc(-c4cc(O)cc5ccc(F)c(CC)c45)c(F)c3n2)C1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
AGS
Dmax
%
95
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0139
Homo sapiens
COMPOUND TARGETING PAN-KRAS PROTEIN DEGRADATION AGENT AND USE THEREOF (patent)
1) Observation under a microscope showed that the cells were in good condition, in the logarithmic growth phase, and the cell density was 80-90%. 2) Digest the cells with trypsin for 1-2 minutes, terminate the digestion with 5 mL of fresh culture medium, gently blow the cells to make a single cell suspension, and centr...
TPDdb
Western Blot
TPD-1S65YG
African=3.44%; Native American=32.25%; East Asian, North=5.38%; East Asian, South=0%; South Asian=0.23%; European, North=27.58%; European, South=31.12%. Persistently infected with parainfluenza virus type 5 (PIV5) strain PIV5-AGS. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutat...
-1
false
48
0
C=C1CN2[C@H](COc3cc(-c4cn([C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)N[C@@H](C)c5ccc(-c6scnc6C)cc5)C(C)C)nn4)ccn3)CC[C@@]2(COc2nc(N3CCC[C@@](C)(O)C3)c3cnc(-c4cc(O)cc5ccc(F)c(CC)c45)c(F)c3n2)C1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
AGS
DC50
nM
30
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0139
Homo sapiens
COMPOUND TARGETING PAN-KRAS PROTEIN DEGRADATION AGENT AND USE THEREOF (patent)
1) Observation under a microscope showed that the cells were in good condition, in the logarithmic growth phase, and the cell density was 80-90%. 2) Digest the cells with trypsin for 1-2 minutes, terminate the digestion with 5 mL of fresh culture medium, gently blow the cells to make a single cell suspension, and centr...
TPDdb
Western Blot
TPD-NWZU4K
African=3.44%; Native American=32.25%; East Asian, North=5.38%; East Asian, South=0%; South Asian=0.23%; European, North=27.58%; European, South=31.12%. Persistently infected with parainfluenza virus type 5 (PIV5) strain PIV5-AGS. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutat...
-1
false
49
0
C=C1CN2[C@H](COc3cc(-c4cn([C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)N[C@@H](C)c5ccc(-c6scnc6C)cc5)C(C)C)nn4)ccn3)CC[C@@]2(COc2nc(N3CCC[C@@](C)(O)C3)c3cnc(-c4cc(O)cc5ccc(F)c(CC)c45)c(F)c3n2)C1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
AGS
Dmax
%
95
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0139
Homo sapiens
COMPOUND TARGETING PAN-KRAS PROTEIN DEGRADATION AGENT AND USE THEREOF (patent)
1) Observation under a microscope showed that the cells were in good condition, in the logarithmic growth phase, and the cell density was 80-90%. 2) Digest the cells with trypsin for 1-2 minutes, terminate the digestion with 5 mL of fresh culture medium, gently blow the cells to make a single cell suspension, and centr...
TPDdb
Western Blot
TPD-NWZU4K
African=3.44%; Native American=32.25%; East Asian, North=5.38%; East Asian, South=0%; South Asian=0.23%; European, North=27.58%; European, South=31.12%. Persistently infected with parainfluenza virus type 5 (PIV5) strain PIV5-AGS. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutat...
-1
false
49
0
C=C1CN2[C@H](COc3ccc(-c4cn([C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)N[C@@H](C)c5ccc(-c6scnc6C)cc5)C(C)C)nn4)cn3)CC[C@@]2(COc2nc(N3CCC[C@@](C)(O)C3)c3cnc(-c4cc(O)cc5ccc(F)c(CC)c45)c(F)c3n2)C1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
AGS
DC50
nM
21
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0139
Homo sapiens
COMPOUND TARGETING PAN-KRAS PROTEIN DEGRADATION AGENT AND USE THEREOF (patent)
1) Observation under a microscope showed that the cells were in good condition, in the logarithmic growth phase, and the cell density was 80-90%. 2) Digest the cells with trypsin for 1-2 minutes, terminate the digestion with 5 mL of fresh culture medium, gently blow the cells to make a single cell suspension, and centr...
TPDdb
Western Blot
TPD-N9RWAM
African=3.44%; Native American=32.25%; East Asian, North=5.38%; East Asian, South=0%; South Asian=0.23%; European, North=27.58%; European, South=31.12%. Persistently infected with parainfluenza virus type 5 (PIV5) strain PIV5-AGS. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutat...
-1
false
50
0
C=C1CN2[C@H](COc3ccc(-c4cn([C@H](C(=O)N5C[C@H](O)C[C@H]5C(=O)N[C@@H](C)c5ccc(-c6scnc6C)cc5)C(C)C)nn4)cn3)CC[C@@]2(COc2nc(N3CCC[C@@](C)(O)C3)c3cnc(-c4cc(O)cc5ccc(F)c(CC)c45)c(F)c3n2)C1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
VHL
AGS
Dmax
%
95
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0139
Homo sapiens
COMPOUND TARGETING PAN-KRAS PROTEIN DEGRADATION AGENT AND USE THEREOF (patent)
1) Observation under a microscope showed that the cells were in good condition, in the logarithmic growth phase, and the cell density was 80-90%. 2) Digest the cells with trypsin for 1-2 minutes, terminate the digestion with 5 mL of fresh culture medium, gently blow the cells to make a single cell suspension, and centr...
TPDdb
Western Blot
TPD-N9RWAM
African=3.44%; Native American=32.25%; East Asian, North=5.38%; East Asian, South=0%; South Asian=0.23%; European, North=27.58%; European, South=31.12%. Persistently infected with parainfluenza virus type 5 (PIV5) strain PIV5-AGS. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutat...
-1
false
50
0
C=C1c2cc3c(n2CCN1c1nccc(-c2cc(Nc4ccc(N5CCC6(CC5)CCN(c5ccc7c(c5)C(=O)N(C5CCC(=O)NC5=O)C7=O)CC6)cn4)c(=O)n(C)c2)c1CO)CC(C)(C)C3
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
Ramos
DC50
nM
1.292
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0597
Homo sapiens
NITROGEN-CONTAINING TRICYCLIC BIFUNCTIONAL COMPOUND, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF (patent)
Evaluation of Compounds' BTK Protein Degradation Activity in Ramos Cells Experimental Methods: 1. RAMOS cells were seeded in 96-well U-bottom cell culture plates, with 80 μL of cell suspension per well (50,000 RAMOS cells per well). The plates were placed in a CO2 incubator and incubated overnight at 37°C. 2. The test ...
TPDdb
HTRF
TPD-BN4TJS
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
31
false
51
50
C=CC(=O)N1CCC[C@H](n2c(Nc3ccccc3)nc3cnc(Nc4ccc(N5CCN(CCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)N[C@@H](C)c6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4)nc32)C1
EGFR E19D
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
HCC827
DC50
nM
0.49
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_2063
Homo sapiens
10.1021/acs.jmedchem.1c01827
Degradation of EGFR e19d in HCC827 cells after 24 h treatment
PROTAC-DB
null
null
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
52
0
C=CC(=O)N1CCC[C@H](n2c(Nc3ccccc3)nc3cnc(Nc4ccc(N5CCN(CCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)N[C@@H](C)c6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4)nc32)C1
EGFR E19D
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
HCC827
Dmax
%
82
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_2063
Homo sapiens
10.1021/acs.jmedchem.1c01827
Degradation of EGFR e19d in HCC827 cells after 24 h treatment
PROTAC-DB
null
null
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
52
0
C=CC(=O)N1CCC[C@H](n2c(Nc3ccccc3)nc3cnc(Nc4ccc(N5CCN(CCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)N[C@@H](C)c6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4)nc32)C1
EGFR L858R/T790M
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
NCI-H1975
DC50
nM
1.56
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1511
Homo sapiens
10.1021/acs.jmedchem.1c01827
Degradation of EGFR L858R/T790M in H1975 cells after 48 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
52
0
C=CC(=O)N1CCC[C@H](n2c(Nc3ccccc3)nc3cnc(Nc4ccc(N5CCN(CCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)N[C@@H](C)c6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4)nc32)C1
EGFR L858R/T790M
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
NCI-H1975
Dmax
%
86
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1511
Homo sapiens
10.1021/acs.jmedchem.1c01827
Degradation of EGFR L858R/T790M in H1975 cells after 48 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
52
0
C=CC(=O)N1CCN(c2nc(NCCCCCCCCCCCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
CRBN
Flp-In-293
Dmax
%
1
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_U421
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31883964/
null
PROTACpedia
null
null
CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. Transformed cell line
-1
false
53
47
C=CC(=O)N1CCN(c2nc(NCCCCN3CCN(CCCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
CRBN
Flp-In-293
Dmax
%
17
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_U421
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31883964/
null
PROTACpedia
null
null
CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. Transformed cell line
-1
false
54
47
C=CC(=O)N1CCN(c2nc(NCCCN(C)CCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
CRBN
Flp-In-293
Dmax
%
25
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_U421
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31883964/
Engagment was tested in-vitro
PROTACpedia
null
null
CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. Transformed cell line
-1
false
55
47
C=CC(=O)N1CCN(c2nc(NCCCN3CCN(CCCNc4ccc5c(c4)C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
CRBN
Flp-In-293
Dmax
%
35
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_U421
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31883964/
null
PROTACpedia
null
null
CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. Transformed cell line
-1
false
56
47
C=CC(=O)N1CCN(c2nc(NCCCN3CCN(CCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
CRBN
Flp-In-293
Dmax
%
32
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_U421
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31883964/
Engagment was tested in-vitro
PROTACpedia
null
null
CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. Transformed cell line
-1
false
57
47
C=CC(=O)N1CCN(c2nc(NCCN3CCN(CCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
CRBN
Flp-In-293
Dmax
%
24
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_U421
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31883964/
null
PROTACpedia
null
null
CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. Transformed cell line
-1
false
58
47
C=CC(=O)N1CCN(c2nc(NCCOCCCN3CCN(CCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
CRBN
Flp-In-293
Dmax
%
10
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_U421
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31883964/
null
PROTACpedia
null
null
CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. Transformed cell line
-1
false
59
0
C=CC(=O)N1CCN(c2nc(NCCOCCOCCNc3ccc4c(c3)C(=O)N(C3CCC(=O)NC3=O)C4=O)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
CRBN
Flp-In-293
Dmax
%
4
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_U421
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31883964/
null
PROTACpedia
null
null
CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. Transformed cell line
-1
false
60
47
C=CC(=O)N1CCN(c2nc(NCCOCCOCCOCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
CRBN
Flp-In-293
Dmax
%
19
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_U421
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31883964/
Engagment was tested in-vitro
PROTACpedia
null
null
CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. Transformed cell line
-1
false
61
47
C=CC(=O)N1CCN(c2nc(NCCOCCOCCOCCOCCOCCOc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
CRBN
Flp-In-293
Dmax
%
3
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_U421
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31883964/
null
PROTACpedia
null
null
CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. Transformed cell line
-1
false
62
0
C=CC(=O)N1CCN(c2nc(NCCOCCOCCOCCOCCOc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
CRBN
Flp-In-293
Dmax
%
6
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_U421
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31883964/
null
PROTACpedia
null
null
CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. Transformed cell line
-1
false
63
47
C=CC(=O)N1CCN(c2nc(NCCOCCOCCOCCOc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)nc3c(F)c(-c4cc(O)cc5ccccc45)c(Cl)cc23)CC1
KRAS
MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM
CRBN
Flp-In-293
Dmax
%
7
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P01116
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_U421
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31883964/
null
PROTACpedia
null
null
CVCL_0045 ! HEK293 In situ; Fetal kidney; NCBI_TaxID; 28285; Human adenovirus C serotype 5. Transformed cell line
-1
false
64
47
C=CC(=O)N1C[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)OCCOCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C
BLK
MGLVSSKKPDKEKPIKEKDKGQWSPLKVSAQDKDAPPLPPLVVFNHLTPPPPDEHLDEDKHFVVALYDYTAMNDRDLQMLKGEKLQVLKGTGDWWLARSLVTGREGYVPSNFVARVESLEMERWFFRSQGRKEAERQLLAPINKAGSFLIRESETNKGAFSLSVKDVTTQGELIKHYKIRCLDEGGYYISPRITFPSLQALVQHYSKKGDGLCQRLTLPCVRPAPQNPWAQDEWEIPRQSLRLVRKLGSGQFGEVWMGYYKNNMKVAIKTLKEGTMSPEAFLGEANVMKALQHERLVRLYAVVTKEPIYIVTEYMARGCL...
VHL
Ramos
DC50
nM
220
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P51451
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0597
Homo sapiens
10.1039/c9cc08238g
Degradation of BLK in Ramos cells after 18 h treatment
PROTAC-DB
null
null
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
30
false
65
0
C=CC(=O)N1C[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)OCCOCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C
BLK
MGLVSSKKPDKEKPIKEKDKGQWSPLKVSAQDKDAPPLPPLVVFNHLTPPPPDEHLDEDKHFVVALYDYTAMNDRDLQMLKGEKLQVLKGTGDWWLARSLVTGREGYVPSNFVARVESLEMERWFFRSQGRKEAERQLLAPINKAGSFLIRESETNKGAFSLSVKDVTTQGELIKHYKIRCLDEGGYYISPRITFPSLQALVQHYSKKGDGLCQRLTLPCVRPAPQNPWAQDEWEIPRQSLRLVRKLGSGQFGEVWMGYYKNNMKVAIKTLKEGTMSPEAFLGEANVMKALQHERLVRLYAVVTKEPIYIVTEYMARGCL...
VHL
Ramos
Dmax
%
75
null
null
null
null
18
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P51451
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0597
Homo sapiens
10.1039/c9cc08238g
Degradation of BLK in Ramos cells after 18 h treatment
PROTAC-DB
null
null
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
30
false
65
0
C=CC(=O)N1C[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)OCCOCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
VHL
K-562
DC50
nM
136
null
null
null
null
21
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0004
Homo sapiens
10.1039/c9cc08238g; https://pubmed.ncbi.nlm.nih.gov/31922153/
Degradation of BTK in K562 cells after 18 h treatment; Covalent Protac
PROTAC-DB; PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
31
false
65
0
C=CC(=O)N1C[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)OCCOCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
VHL
K-562
Dmax
%
88
null
null
null
null
21
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0004
Homo sapiens
10.1039/c9cc08238g; https://pubmed.ncbi.nlm.nih.gov/31922153/
Degradation of BTK in K562 cells after 18 h treatment; Covalent Protac
PROTAC-DB; PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
31
false
65
0
C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)NCCCCCCCCCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
K-562
Dmax
%
50
null
null
null
null
24
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0004
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31922153/
Covalent Protac
PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
31
false
66
0
C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)NCCCCCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
K-562
Dmax
%
50
null
null
null
null
24
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0004
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31922153/
Covalent Protac
PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
31
false
67
0
C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)NCCCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
K-562
Dmax
%
50
null
null
null
null
24
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0004
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31922153/
Covalent Protac
PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
31
false
68
0
C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)NCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
K-562
Dmax
%
50
null
null
null
null
24
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0004
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31922153/
Covalent Protac
PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
31
false
69
171
C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)OCCOCCOCC(=O)Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
K-562
Dmax
%
50
null
null
null
null
24
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0004
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31922153/
Covalent Protac
PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
31
false
70
0
C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)OCCOCCOCCOCC(=O)Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
K-562
Dmax
%
50
null
null
null
null
24
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0004
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31922153/
Covalent Protac
PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
31
false
71
0
C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)OCCOCCOCCOCCOCC(=O)Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
K-562
Dmax
%
50
null
null
null
null
24
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0004
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31922153/
Covalent Protac
PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
31
false
72
0
C=CC(=O)N1C[C@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C[C@H]1C(=O)OCCOCCOCCOCCOCCOCC(=O)Nc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
K-562
Dmax
%
50
null
null
null
null
24
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0004
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31922153/
Covalent Protac
PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
31
false
73
0
C=CC(=O)N[C@@H](CCC(=O)NCCCCCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)C(=O)Nc1cccc(Nc2ncc(NC(=O)c3cc(NC(=O)c4cccc(C)c4)ccc3C)cn2)c1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
K-562
DC50
nM
300
null
null
null
null
24
<
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0004
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31922153/
Covalent Protac
PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
31
false
74
0
C=CC(=O)N[C@@H](CCC(=O)NCCCCCCCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)C(=O)Nc1cccc(Nc2ncc(NC(=O)c3cc(NC(=O)c4cccc(C)c4)ccc3C)cn2)c1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
K-562
Dmax
%
75
null
null
null
null
24
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q06187
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0004
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31922153/
Covalent Protac
PROTACpedia
null
null
African=5.19%; Native American=0%; East Asian, North=8.4%; East Asian, South=0%; South Asian=0%; European, North=43.44%; European, South=42.97%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11; B*40,35/39; C*03,05. A*31 Stable (MSS). In situ; Pleural effusion; Caucasian. Cancer cell line
31
false
74
0
C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)CCOCCOCCOCCOCC(=O)Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
PC-9
DC50
nM
161
null
null
null
null
15
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_B260
Homo sapiens
10.1016/j.bmcl.2020.127167; https://pubmed.ncbi.nlm.nih.gov/32317208/
Degradation of EGFR in PC9 cells after 6 h treatment; EC50: 0.413±0.087uM, 1.344±0.112uM, 0.657±0.008uM for PC9/HCC827/H1975 cells, respectively.
PROTAC-DB; PROTACpedia
null
null
Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Metastatic; Lymph node; Chinese; Han and Japanese. Cancer cell line
23
false
75
0
C=CC(=O)Nc1cc(Nc2nccc(-c3cn(C)c4ccccc34)n2)c(OC)cc1N(C)CCN(C)CCOCCOCCOCCOCC(=O)Nc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
PC-9
Dmax
%
68
null
null
null
null
15
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_B260
Homo sapiens
10.1016/j.bmcl.2020.127167; https://pubmed.ncbi.nlm.nih.gov/32317208/
Degradation of EGFR in PC9 cells after 6 h treatment; EC50: 0.413±0.087uM, 1.344±0.112uM, 0.657±0.008uM for PC9/HCC827/H1975 cells, respectively.
PROTAC-DB; PROTACpedia
null
null
Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Metastatic; Lymph node; Chinese; Han and Japanese. Cancer cell line
23
false
75
0
C=CC(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1OCCCN1CCN(C(=O)CCCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1
EGFR L858R/T790M
MAVDPLSSKALKVKRELSENTPHLSDEALMGLSVRELNRNLRGLSAEEVTRLKQRRRTLKNRGYAASCRVKRVCQKEELQKQKSELEREVDKLARENAAMRLELDALRGKCEALQGFARSVAAARGPAALVAPASVITIVKSAPGPAPAADPAPCS
CRBN
Ba/F3
DC50
nM
100
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O54791
Q8C7D2
MAGEGDQQDAAHNMGNHLPLLPADSEDEDDEIEMEVEDQDSKEARKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPEVLMILIPGQTLPLQLSHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQEFGIEVVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQVFPSKPISWEDQYSCKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPENPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNK...
CVCL_0161
Mus musculus
10.1016/j.ejmech.2021.113328
Degradation of EGFR L858R/T790M in H1975/(Ba/F3) cells after 16 h treatment
PROTAC-DB
null
null
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
-1
false
76
0
C=CC(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1OCCCN1CCN(C(=O)CCCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1
EGFR L858R/T790M
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
NCI-H1975
DC50
nM
30
null
null
null
null
16
<
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1511
Homo sapiens
10.1016/j.ejmech.2021.113328
Degradation of EGFR L858R/T790M in H1975/(Ba/F3) cells after 16 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
76
0
C=CC(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1OCCCN1CCN(C(=O)CCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1
EGFR E19D
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
PC-9
DC50
nM
100
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_B260
Homo sapiens
10.1016/j.ejmech.2021.113328
Degradation of EGFR e19d in PC9 cells after 48 h treatment
PROTAC-DB
null
null
Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Metastatic; Lymph node; Chinese; Han and Japanese. Cancer cell line
23
false
77
0
C=CC(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1OCCCN1CCN(C(=O)CCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1
EGFR E19D
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
PC-9
Dmax
%
40
null
null
null
null
48
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_B260
Homo sapiens
10.1016/j.ejmech.2021.113328
Degradation of EGFR e19d in PC9 cells after 48 h treatment
PROTAC-DB
null
null
Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02 Metastatic; Lymph node; Chinese; Han and Japanese. Cancer cell line
23
false
77
0
C=CC(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1OCCCN1CCN(C(=O)CCCCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1
EGFR L858R/T790M
MAVDPLSSKALKVKRELSENTPHLSDEALMGLSVRELNRNLRGLSAEEVTRLKQRRRTLKNRGYAASCRVKRVCQKEELQKQKSELEREVDKLARENAAMRLELDALRGKCEALQGFARSVAAARGPAALVAPASVITIVKSAPGPAPAADPAPCS
CRBN
Ba/F3
DC50
nM
100
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O54791
Q8C7D2
MAGEGDQQDAAHNMGNHLPLLPADSEDEDDEIEMEVEDQDSKEARKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPEVLMILIPGQTLPLQLSHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQEFGIEVVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQVFPSKPISWEDQYSCKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPENPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNK...
CVCL_0161
Mus musculus
10.1016/j.ejmech.2021.113328
Degradation of EGFR L858R/T790M in H1975/(Ba/F3) cells after 16 h treatment
PROTAC-DB
null
null
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
-1
false
77
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
A-431
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0037
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR in A431 cells after 16 h treatment
PROTAC-DB
null
null
African=3.82%; Native American=0%; East Asian, North=7.84%; East Asian, South=0%; South Asian=6.03%; European, North=17.15%; European, South=65.16%. Hypertriploid karyotype (ATCC=CRL-1555). Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*03 A*03 Stable (MSS) (Sanger). In situ; Skin, epidermis; Caucasian. Cancer cell li...
23
false
78
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR L858R/T790M
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
NCI-H1975
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1511
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR L858R/T790M in H1975 cells after 16h 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
78
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
A-431
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0037
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR in A431 cells after 16 h treatment
PROTAC-DB
null
null
African=3.82%; Native American=0%; East Asian, North=7.84%; East Asian, South=0%; South Asian=6.03%; European, North=17.15%; European, South=65.16%. Hypertriploid karyotype (ATCC=CRL-1555). Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*03 A*03 Stable (MSS) (Sanger). In situ; Skin, epidermis; Caucasian. Cancer cell li...
23
false
79
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
NCI-H1975
DC50
nM
235
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1511
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/32171162/
Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)
PROTACpedia
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
79
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR L858R/T790M
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
NCI-H1975
DC50
nM
235
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1511
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR L858R/T790M in H1975 cells after 16h 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
79
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
A-431
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0037
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR in A431 cells after 16 h treatment
PROTAC-DB
null
null
African=3.82%; Native American=0%; East Asian, North=7.84%; East Asian, South=0%; South Asian=6.03%; European, North=17.15%; European, South=65.16%. Hypertriploid karyotype (ATCC=CRL-1555). Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*03 A*03 Stable (MSS) (Sanger). In situ; Skin, epidermis; Caucasian. Cancer cell li...
23
false
80
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
NCI-H1975
DC50
nM
69
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1511
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/32171162/
Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)
PROTACpedia
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
80
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR L858R/T790M
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
NCI-H1975
DC50
nM
69
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1511
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR L858R/T790M in H1975 cells after 16h 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
80
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
A-431
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0037
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR in A431 cells after 16 h treatment
PROTAC-DB
null
null
African=3.82%; Native American=0%; East Asian, North=7.84%; East Asian, South=0%; South Asian=6.03%; European, North=17.15%; European, South=65.16%. Hypertriploid karyotype (ATCC=CRL-1555). Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*03 A*03 Stable (MSS) (Sanger). In situ; Skin, epidermis; Caucasian. Cancer cell li...
23
false
81
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
NCI-H1975
DC50
nM
313
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1511
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/32171162/
Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)
PROTACpedia
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
81
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR L858R/T790M
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
NCI-H1975
DC50
nM
312.9
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1511
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR L858R/T790M in H1975 cells after 16h 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
81
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCCCC(=O)Nc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
A-431
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0037
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR in A431 cells after 16 h treatment
PROTAC-DB
null
null
African=3.82%; Native American=0%; East Asian, North=7.84%; East Asian, South=0%; South Asian=6.03%; European, North=17.15%; European, South=65.16%. Hypertriploid karyotype (ATCC=CRL-1555). Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*03 A*03 Stable (MSS) (Sanger). In situ; Skin, epidermis; Caucasian. Cancer cell li...
23
false
82
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCCCC(=O)Nc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)cc4OC)nc32)c1
EGFR L858R/T790M
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
NCI-H1975
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1511
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR L858R/T790M in H1975 cells after 16h 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
82
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCCCCNC(=O)[C@H](CC(C)C)NC(=O)[C@@H](O)[C@H](N)Cc6ccccc6)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
cIAP1
A-431
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q13490
MHKTASQRLFPGPSYQNIKSIMEDSTILSDWTNSNKQKMKYDFSCELYRMSTYSTFPAGVPVSERSLARAGFYYTGVNDKVKCFCCGLMLDNWKLGDSPIQKHKQLYPSCSFIQNLVSASLGSTSKNTSPMRNSFAHSLSPTLEHSSLFSGSYSSLSPNPLNSRAVEDISSSRTNPYSYAMSTEEARFLTYHMWPLTFLSPSELARAGFYYIGPGDRVACFACGGKLSNWEPKDDAMSEHRRHFPNCPFLENSLETLRFSISNLSMQTHAARMRTFMYWPSSVPVQPEQLASAGFYYVGRNDDVKCFCCDGGLRCWESGD...
CVCL_0037
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR in A431 cells after 16 h treatment
PROTAC-DB
null
null
African=3.82%; Native American=0%; East Asian, North=7.84%; East Asian, South=0%; South Asian=6.03%; European, North=17.15%; European, South=65.16%. Hypertriploid karyotype (ATCC=CRL-1555). Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*03 A*03 Stable (MSS) (Sanger). In situ; Skin, epidermis; Caucasian. Cancer cell li...
23
false
83
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCCCCNC(=O)[C@H](CC(C)C)NC(=O)[C@@H](O)[C@H](N)Cc6ccccc6)CC5)cc4OC)nc32)c1
EGFR L858R/T790M
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
cIAP1
NCI-H1975
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q13490
MHKTASQRLFPGPSYQNIKSIMEDSTILSDWTNSNKQKMKYDFSCELYRMSTYSTFPAGVPVSERSLARAGFYYTGVNDKVKCFCCGLMLDNWKLGDSPIQKHKQLYPSCSFIQNLVSASLGSTSKNTSPMRNSFAHSLSPTLEHSSLFSGSYSSLSPNPLNSRAVEDISSSRTNPYSYAMSTEEARFLTYHMWPLTFLSPSELARAGFYYIGPGDRVACFACGGKLSNWEPKDDAMSEHRRHFPNCPFLENSLETLRFSISNLSMQTHAARMRTFMYWPSSVPVQPEQLASAGFYYVGRNDDVKCFCCDGGLRCWESGD...
CVCL_1511
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR L858R/T790M in H1975 cells after 16h 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
83
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCCCCNC(=O)c6ccc(NC(=O)[C@@H]7N[C@@H](CC(C)(C)C)[C@](C#N)(c8ccc(Cl)cc8F)[C@H]7c7cccc(Cl)c7F)c(OC)c6)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
MDM2
A-431
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q00987
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
CVCL_0037
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR in A431 cells after 16 h treatment
PROTAC-DB
null
null
African=3.82%; Native American=0%; East Asian, North=7.84%; East Asian, South=0%; South Asian=6.03%; European, North=17.15%; European, South=65.16%. Hypertriploid karyotype (ATCC=CRL-1555). Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*03 A*03 Stable (MSS) (Sanger). In situ; Skin, epidermis; Caucasian. Cancer cell li...
23
false
84
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCCCCNC(=O)c6ccc(NC(=O)[C@@H]7N[C@@H](CC(C)(C)C)[C@](C#N)(c8ccc(Cl)cc8F)[C@H]7c7cccc(Cl)c7F)c(OC)c6)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
MDM2
NCI-H1975
DC50
nM
264
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q00987
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
CVCL_1511
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/32171162/
Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)
PROTACpedia
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
84
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCCCCNC(=O)c6ccc(NC(=O)[C@@H]7N[C@@H](CC(C)(C)C)[C@](C#N)(c8ccc(Cl)cc8F)[C@H]7c7cccc(Cl)c7F)c(OC)c6)CC5)cc4OC)nc32)c1
EGFR L858R/T790M
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
MDM2
NCI-H1975
DC50
nM
263.8
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q00987
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
CVCL_1511
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR L858R/T790M in H1975 cells after 16h 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
84
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCCNC(=O)c6ccc(NC(=O)[C@@H]7N[C@@H](CC(C)(C)C)[C@](C#N)(c8ccc(Cl)cc8F)[C@H]7c7cccc(Cl)c7F)c(OC)c6)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
MDM2
A-431
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q00987
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
CVCL_0037
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR in A431 cells after 16 h treatment
PROTAC-DB
null
null
African=3.82%; Native American=0%; East Asian, North=7.84%; East Asian, South=0%; South Asian=6.03%; European, North=17.15%; European, South=65.16%. Hypertriploid karyotype (ATCC=CRL-1555). Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*03 A*03 Stable (MSS) (Sanger). In situ; Skin, epidermis; Caucasian. Cancer cell li...
23
false
85
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCCNC(=O)c6ccc(NC(=O)[C@@H]7N[C@@H](CC(C)(C)C)[C@](C#N)(c8ccc(Cl)cc8F)[C@H]7c7cccc(Cl)c7F)c(OC)c6)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
MDM2
NCI-H1975
DC50
nM
77
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q00987
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
CVCL_1511
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/32171162/
Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)
PROTACpedia
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
85
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCCCNC(=O)c6ccc(NC(=O)[C@@H]7N[C@@H](CC(C)(C)C)[C@](C#N)(c8ccc(Cl)cc8F)[C@H]7c7cccc(Cl)c7F)c(OC)c6)CC5)cc4OC)nc32)c1
EGFR L858R/T790M
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
MDM2
NCI-H1975
DC50
nM
77
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q00987
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
CVCL_1511
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR L858R/T790M in H1975 cells after 16h 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
85
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCNC(=O)c6ccc(NC(=O)[C@@H]7N[C@@H](CC(C)(C)C)[C@](C#N)(c8ccc(Cl)cc8F)[C@H]7c7cccc(Cl)c7F)c(OC)c6)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
MDM2
A-431
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q00987
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
CVCL_0037
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR in A431 cells after 16 h treatment
PROTAC-DB
null
null
African=3.82%; Native American=0%; East Asian, North=7.84%; East Asian, South=0%; South Asian=6.03%; European, North=17.15%; European, South=65.16%. Hypertriploid karyotype (ATCC=CRL-1555). Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*03 A*03 Stable (MSS) (Sanger). In situ; Skin, epidermis; Caucasian. Cancer cell li...
23
false
86
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCCCNC(=O)c6ccc(NC(=O)[C@@H]7N[C@@H](CC(C)(C)C)[C@](C#N)(c8ccc(Cl)cc8F)[C@H]7c7cccc(Cl)c7F)c(OC)c6)CC5)cc4OC)nc32)c1
EGFR L858R/T790M
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
MDM2
NCI-H1975
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q00987
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
CVCL_1511
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR L858R/T790M in H1975 cells after 16h 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
86
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCNC(=O)c6ccc(NC(=O)[C@@H]7N[C@@H](CC(C)(C)C)[C@](C#N)(c8ccc(Cl)cc8F)[C@H]7c7cccc(Cl)c7F)c(OC)c6)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
MDM2
A-431
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q00987
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
CVCL_0037
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR in A431 cells after 16 h treatment
PROTAC-DB
null
null
African=3.82%; Native American=0%; East Asian, North=7.84%; East Asian, South=0%; South Asian=6.03%; European, North=17.15%; European, South=65.16%. Hypertriploid karyotype (ATCC=CRL-1555). Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*03 A*03 Stable (MSS) (Sanger). In situ; Skin, epidermis; Caucasian. Cancer cell li...
23
false
87
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(C(=O)CCCCCNC(=O)c6ccc(NC(=O)[C@@H]7N[C@@H](CC(C)(C)C)[C@](C#N)(c8ccc(Cl)cc8F)[C@H]7c7cccc(Cl)c7F)c(OC)c6)CC5)cc4OC)nc32)c1
EGFR L858R/T790M
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
MDM2
NCI-H1975
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
Q00987
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
CVCL_1511
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR L858R/T790M in H1975 cells after 16h 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
87
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(CCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
A-431
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0037
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR in A431 cells after 16 h treatment
PROTAC-DB
null
null
African=3.82%; Native American=0%; East Asian, North=7.84%; East Asian, South=0%; South Asian=6.03%; European, North=17.15%; European, South=65.16%. Hypertriploid karyotype (ATCC=CRL-1555). Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*03 A*03 Stable (MSS) (Sanger). In situ; Skin, epidermis; Caucasian. Cancer cell li...
23
false
88
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(CCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR L858R/T790M
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
NCI-H1975
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1511
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR L858R/T790M in H1975 cells after 16h 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
88
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(CCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
A-431
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0037
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR in A431 cells after 16 h treatment
PROTAC-DB
null
null
African=3.82%; Native American=0%; East Asian, North=7.84%; East Asian, South=0%; South Asian=6.03%; European, North=17.15%; European, South=65.16%. Hypertriploid karyotype (ATCC=CRL-1555). Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*03 A*03 Stable (MSS) (Sanger). In situ; Skin, epidermis; Caucasian. Cancer cell li...
23
false
89
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(CCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
NCI-H1975
DC50
nM
5.9
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1511
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/32171162/
Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity). EC50 of PROTAC was measured in H1975 cell line
PROTACpedia
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
89
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(CCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
NCI-H1975
Dmax
%
100
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1511
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/32171162/
Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity). EC50 of PROTAC was measured in H1975 cell line
PROTACpedia
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
89
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(CCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR L858R/T790M
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
NCI-H1975
DC50
nM
5.9
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1511
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR L858R/T790M in H1975 cells after 16h 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
89
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(CCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
A-431
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0037
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR in A431 cells after 16 h treatment
PROTAC-DB
null
null
African=3.82%; Native American=0%; East Asian, North=7.84%; East Asian, South=0%; South Asian=6.03%; European, North=17.15%; European, South=65.16%. Hypertriploid karyotype (ATCC=CRL-1555). Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*03 A*03 Stable (MSS) (Sanger). In situ; Skin, epidermis; Caucasian. Cancer cell li...
23
false
90
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(CCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
NCI-H1975
DC50
nM
466
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1511
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/32171162/
Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)
PROTACpedia
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
90
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(CCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR L858R/T790M
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
NCI-H1975
DC50
nM
466
null
null
null
null
16
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1511
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR L858R/T790M in H1975 cells after 16h 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
90
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(CCCCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
A-431
DC50
nM
2,000
null
null
null
null
16
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0037
Homo sapiens
10.1016/j.ejmech.2020.112199
Degradation of EGFR in A431 cells after 16 h treatment
PROTAC-DB
null
null
African=3.82%; Native American=0%; East Asian, North=7.84%; East Asian, South=0%; South Asian=6.03%; European, North=17.15%; European, South=65.16%. Hypertriploid karyotype (ATCC=CRL-1555). Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC A*03 A*03 Stable (MSS) (Sanger). In situ; Skin, epidermis; Caucasian. Cancer cell li...
23
false
91
0
C=CC(=O)Nc1cccc(-n2c(=O)cc(C)c3cnc(Nc4ccc(N5CCN(CCCCCCCCCC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4OC)nc32)c1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
VHL
NCI-H1975
DC50
nM
132
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P00533
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1511
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/32171162/
Ligand IC50 is 0.26 nM (Kd), 4.0 nM (kinase activity)
PROTACpedia
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
91
0