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
CCCS(=O)(=O)Nc1ccc(F)c(C(=O)c2c[nH]c3ncc(-c4ccc(N5CCN(CC(=O)N[C@H](C(=O)N6C[C@H](O)C[C@H]6C(=O)NCc6ccc(-c7scnc7C)cc6)C(C)(C)C)CC5)cc4)cc23)c1F
BRAF V600E
MAALSGGGGGGAEPGQALFNGDMEPEAGAGAGAAASSAADPAIPEEVWNIKQMIKLTQEHIEALLDKFGGEHNPPSIYLEAYEEYTSKLDALQQREQQLLESLGNGTDFSVSSSASMDTVTSSSSSSLSVLPSSLSVFQNPTDVARSNPKSPQKPIVRVFLPNKQRTVVPARCGVTVRDSLKKALMMRGLIPECCAVYRIQDGEKKPIGWDTDISWLTGEELHVEVLENVPLTTHNFVRKTFFTLAFCDFCRKLLFQGFRCQTCGYKFHQRCSTEVPLMCVNYDQLDLLFVSKFFEHHPIPQEEASLAETALTSGSSPSA...
VHL
SK-MEL-28
Dmax
%
95
null
null
null
null
null
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P15056
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0526
Homo sapiens
10.1038/s41467-021-21159-7
Degradation of BRAF V600E in SK-MEL-28 cells
PROTAC-DB
null
null
African=1.75%; Native American=0.56%; East Asian, North=3%; East Asian, South=1.38%; South Asian=8.29%; European, North=20.11%; European, South=64.91%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Lightly pigmented. A*11 A*11 A*11 Stable (...
-1
false
446
0
CCC[C@H](NC(=O)COCCCOCCCCOCCCOc1ccc(Nc2ncc(Br)c(NCCCN(C)C(=O)C3CCC3)n2)cc1)C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1
TBK1
MQSTSNHLWLLSDILGQGATANVFRGRHKKTGDLFAIKVFNNISFLRPVDVQMREFEVLKKLNHKNIVKLFAIEEETTTRHKVLIMEFCPCGSLYTVLEEPSNAYGLPESEFLIVLRDVVGGMNHLRENGIVHRDIKPGNIMRVIGEDGQSVYKLTDFGAARELEDDEQFVSLYGTEEYLHPDMYERAVLRKDHQKKYGATVDLWSIGVTFYHAATGSLPFRPFEGPRRNKEVMYKIITGKPSGAISGVQKAENGPIDWSGDMPVSCSLSRGLQVLLTPVLANILEADQEKCWGFDQFFAETSDILHRMVIHVFSLQQMT...
VHL
Panc 02.13
DC50
nM
288
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q9UHD2
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1634
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/28692295/
null
PROTACpedia
null
null
African=2.03%; Native American=0.98%; East Asian, North=0.28%; East Asian, South=0%; South Asian=0.04%; European, North=63.98%; European, South=32.69%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC In situ; Pancreas; Caucasian. Cancer cell line
-1
false
95
0
CCC[C@H](NC(=O)COCCCOCCCCOCCCOc1ccc(Nc2ncc(Br)c(NCCCN(C)C(=O)C3CCC3)n2)cc1)C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1
TBK1
MQSTSNHLWLLSDILGQGATANVFRGRHKKTGDLFAIKVFNNISFLRPVDVQMREFEVLKKLNHKNIVKLFAIEEETTTRHKVLIMEFCPCGSLYTVLEEPSNAYGLPESEFLIVLRDVVGGMNHLRENGIVHRDIKPGNIMRVIGEDGQSVYKLTDFGAARELEDDEQFVSLYGTEEYLHPDMYERAVLRKDHQKKYGATVDLWSIGVTFYHAATGSLPFRPFEGPRRNKEVMYKIITGKPSGAISGVQKAENGPIDWSGDMPVSCSLSRGLQVLLTPVLANILEADQEKCWGFDQFFAETSDILHRMVIHVFSLQQMT...
VHL
Panc 02.13
Dmax
%
75
null
null
null
null
16
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q9UHD2
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1634
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/28692295/
null
PROTACpedia
null
null
African=2.03%; Native American=0.98%; East Asian, North=0.28%; East Asian, South=0%; South Asian=0.04%; European, North=63.98%; European, South=32.69%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC In situ; Pancreas; Caucasian. Cancer cell line
-1
false
95
0
CCC[C@H](NC(=O)[C@@H]1[C@H]2CCC[C@H]2CN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)c1cnc(C(=O)NCCCCCCNc2cccc3c2CN(C2CCC(=O)NC2=O)C3=O)cn1)C1CCCCC1)C(C)(C)C)C(=O)C(=O)NC1CC1
NS3
PNIEEVALPTTGEIPFYGKAIPLELIKGGRHLIFCHSKKKCDELARQLTSLGLNAVAYYRGLDVSVIPTSGDVVVCATDALMTGFTGDYDSVIDY
CRBN
Huh-7.5
DC50
nM
669
null
null
null
null
4
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O39228
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_7927
Homo sapiens
10.1038/s41467-019-11429-w
Degradation of NS3 in Huh7.5 cells after 4 h treatment
PROTAC-DB
null
null
Highly permissive for hepatitis C virus (HCV) replication. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC CVCL_0336 ! Huh-7 In situ; Liver; Japanese. Cancer cell line
1
false
447
229
CCC[C@H](NC(=O)[C@@H]1[C@H]2CCC[C@H]2CN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)c1cnc(C(=O)NCCOCCOCCNc2cccc3c2C(=O)N(C2CCC(=O)NC2=O)C3=O)cn1)C1CCCCC1)C(C)(C)C)C(=O)C(=O)NC1CC1
NS3
PNIEEVALPTTGEIPFYGKAIPLELIKGGRHLIFCHSKKKCDELARQLTSLGLNAVAYYRGLDVSVIPTSGDVVVCATDALMTGFTGDYDSVIDY
CRBN
Huh-7.5
DC50
nM
489
null
null
null
null
4
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O39228
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_7927
Homo sapiens
10.1038/s41467-019-11429-w
Degradation of NS3 in Huh7.5 cells after 4 h treatment
PROTAC-DB
null
null
Highly permissive for hepatitis C virus (HCV) replication. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC CVCL_0336 ! Huh-7 In situ; Liver; Japanese. Cancer cell line
1
false
448
0
CCC[C@H](NC(=O)[C@@H]1[C@H]2CCC[C@H]2CN1C(=O)[C@@H](NC(=O)[C@@H](NC(=O)c1cnc(C(=O)NCCOCCOCCOc2cc3c4c(cccc4c2)C(=O)N(C2CCC(=O)NC2=O)C3=O)cn1)C1CCCCC1)C(C)(C)C)C(=O)C(=O)NC1CC1
NS3
PNIEEVALPTTGEIPFYGKAIPLELIKGGRHLIFCHSKKKCDELARQLTSLGLNAVAYYRGLDVSVIPTSGDVVVCATDALMTGFTGDYDSVIDY
CRBN
Huh-7.5
DC50
nM
50
null
null
null
null
4
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O39228
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_7927
Homo sapiens
10.1038/s41467-019-11429-w
Degradation of NS3 in Huh7.5 cells after 4 h treatment
PROTAC-DB
null
null
Highly permissive for hepatitis C virus (HCV) replication. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC CVCL_0336 ! Huh-7 In situ; Liver; Japanese. Cancer cell line
1
false
449
0
CCCn1c(C)c(C(=O)NCCN2CCN(C)CC2)c(-c2cc(F)cc(N3CCN(c4ccc(NS(=O)(=O)c5ccc(NC(CCN6CCN(C(=O)CCCCCC(=O)N[C@H](C(=O)N7C[C@H](O)C[C@H]7C(=O)N[C@@H](C)c7ccc(-c8scnc8C)cc7)C(C)(C)C)CC6)CSc6ccccc6)c([N+](=O)[O-])c5)cc4)CC3)c2)c1-c1ccc(F)cc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MDA-MB-231
DC50
nM
54
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0062
Homo sapiens
BCL-2/BCL-XL PROTEIN DEGRADER AND USE THEREOF (patent)
Cells were collected and lysed in a lysis buffer (Cat. No. BP-115DG, Boston Bio Products, Ashland, MA, USA) containing protease and phosphatase inhibitor cocktails (Cat. No. PPC1010, Sigma-Aldrich, St. Louis, MO, USA) . An equal amount of protein lysates was separated on precasted 4-20%Tris-glycine gels (Mini-PROTEAN T...
TPDdb
Western Blot
TPD-F0VT42
African=1.95%; Native American=0%; East Asian, North=2.44%; East Asian, South=0%; South Asian=7.42%; European, North=28.16%; European, South=60.03%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02/28; B*07,08; C*w02,w06. A*02 A...
5
false
450
0
CCN(C(=O)c1ccc(N2CCN(CCCCCOc3ccc([C@@H]4c5ccc(O)cc5CC[C@@H]4c4ccccc4)cc3)CC2)cc1OC)C1CCC(=O)NC1=O
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
CRBN
MCF-7
DC50
nM
100
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0031
Homo sapiens
Cereblon ligands and bifunctional compounds comprising the same (patent)
2. Estrogen Receptor-alpha (ERa) degradation assay in MCF-7 cells using western blot method for Table 5. The exemplary novel ERa degraders were assessed for their activity in degrading ERa in MCF-7 cells via western blot. The assay was carried out in the presence of 10 percent FBS or high percentage of human or mouse ...
TPDdb
In-Cell Western/Western Blot
TPD-9DD1TR
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
451
275
CCN(C(=O)c1ccc(N2CCN(CCCCCOc3ccc([C@@H]4c5ccc(O)cc5CC[C@@H]4c4ccccc4)cc3)CC2)cc1OC)C1CCC(=O)NC1=O
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
CRBN
MCF-7
Dmax
%
50
null
null
null
null
null
<
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0031
Homo sapiens
Cereblon ligands and bifunctional compounds comprising the same (patent)
2. Estrogen Receptor-alpha (ERa) degradation assay in MCF-7 cells using western blot method for Table 5. The exemplary novel ERa degraders were assessed for their activity in degrading ERa in MCF-7 cells via western blot. The assay was carried out in the presence of 10 percent FBS or high percentage of human or mouse ...
TPDdb
In-Cell Western/Western Blot
TPD-9DD1TR
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
451
275
CCN(C(=O)c1ccc(OCCCCCN2CCN(c3ccc(C(=O)N[C@H]4C(C)(C)[C@H](Oc5ccc(C#N)c(Cl)c5)C4(C)C)cn3)CC2)cc1)C1CCC(=O)NC1=O
AR
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL...
CRBN
VCaP
DC50
nM
100
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-FTADPY
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
452
122
CCN(C(=O)c1ccc(OCCCCCN2CCN(c3ccc(C(=O)N[C@H]4C(C)(C)[C@H](Oc5ccc(C#N)c(Cl)c5)C4(C)C)cn3)CC2)cc1)C1CCC(=O)NC1=O
AR
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL...
CRBN
VCaP
Dmax
%
50
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-FTADPY
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
452
122
CCN(C)S(=O)(=O)Nc1ccc(F)c(C(=O)c2c[nH]c3ncc(-c4ccc(N5CCN(C(=O)CCCNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)nc4)cc23)c1F
BRAF V600E
MAALSGGGGGGAEPGQALFNGDMEPEAGAGAGAAASSAADPAIPEEVWNIKQMIKLTQEHIEALLDKFGGEHNPPSIYLEAYEEYTSKLDALQQREQQLLESLGNGTDFSVSSSASMDTVTSSSSSSLSVLPSSLSVFQNPTDVARSNPKSPQKPIVRVFLPNKQRTVVPARCGVTVRDSLKKALMMRGLIPECCAVYRIQDGEKKPIGWDTDISWLTGEELHVEVLENVPLTTHNFVRKTFFTLAFCDFCRKLLFQGFRCQTCGYKFHQRCSTEVPLMCVNYDQLDLLFVSKFFEHHPIPQEEASLAETALTSGSSPSA...
CRBN
A-375
DC50
nM
26
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P15056
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0132
Homo sapiens
10.1021/acsmedchemlett.2c00039
Degradation of BRAF V600E in A375 cells after 24 h treatment
PROTAC-DB
null
null
African=0.84%; Native American=0.49%; East Asian, North=1.69%; East Asian, South=0%; South Asian=0%; European, North=67.22%; European, South=29.75%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01,02; B*12,13. A*01 A*01 Stable (MSS) (Sanger). In situ; Leg, skin; Caucasian. Canc...
-1
false
453
0
CCN(C)S(=O)(=O)Nc1ccc(F)c(C(=O)c2c[nH]c3ncc(-c4ccc(N5CCN(C(=O)CCCOc6cccc7c6CN(C6CCC(=O)NC6=O)C7=O)CC5)cc4)cc23)c1F
BRAF V600E
MAALSGGGGGGAEPGQALFNGDMEPEAGAGAGAAASSAADPAIPEEVWNIKQMIKLTQEHIEALLDKFGGEHNPPSIYLEAYEEYTSKLDALQQREQQLLESLGNGTDFSVSSSASMDTVTSSSSSSLSVLPSSLSVFQNPTDVARSNPKSPQKPIVRVFLPNKQRTVVPARCGVTVRDSLKKALMMRGLIPECCAVYRIQDGEKKPIGWDTDISWLTGEELHVEVLENVPLTTHNFVRKTFFTLAFCDFCRKLLFQGFRCQTCGYKFHQRCSTEVPLMCVNYDQLDLLFVSKFFEHHPIPQEEASLAETALTSGSSPSA...
CRBN
A-375
DC50
nM
16
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P15056
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0132
Homo sapiens
10.1021/acsmedchemlett.2c00039
Degradation of BRAF V600E in A375 cells after 24 h treatment
PROTAC-DB
null
null
African=0.84%; Native American=0.49%; East Asian, North=1.69%; East Asian, South=0%; South Asian=0%; European, North=67.22%; European, South=29.75%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01,02; B*12,13. A*01 A*01 Stable (MSS) (Sanger). In situ; Leg, skin; Caucasian. Canc...
-1
false
454
0
CCN(C)S(=O)(=O)Nc1ccc(F)c(C(=O)c2c[nH]c3ncc(-c4ccc(N5CCN(C(=O)CCCOc6cccc7c6CN(C6CCC(=O)NC6=O)C7=O)CC5)nc4)cc23)c1F
BRAF V600E
MAALSGGGGGGAEPGQALFNGDMEPEAGAGAGAAASSAADPAIPEEVWNIKQMIKLTQEHIEALLDKFGGEHNPPSIYLEAYEEYTSKLDALQQREQQLLESLGNGTDFSVSSSASMDTVTSSSSSSLSVLPSSLSVFQNPTDVARSNPKSPQKPIVRVFLPNKQRTVVPARCGVTVRDSLKKALMMRGLIPECCAVYRIQDGEKKPIGWDTDISWLTGEELHVEVLENVPLTTHNFVRKTFFTLAFCDFCRKLLFQGFRCQTCGYKFHQRCSTEVPLMCVNYDQLDLLFVSKFFEHHPIPQEEASLAETALTSGSSPSA...
CRBN
A-375
DC50
nM
10
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P15056
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0132
Homo sapiens
10.1021/acsmedchemlett.2c00039
Degradation of BRAF V600E in A375 cells after 24 h treatment
PROTAC-DB
null
null
African=0.84%; Native American=0.49%; East Asian, North=1.69%; East Asian, South=0%; South Asian=0%; European, North=67.22%; European, South=29.75%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01,02; B*12,13. A*01 A*01 Stable (MSS) (Sanger). In situ; Leg, skin; Caucasian. Canc...
-1
false
455
0
CCN(C)S(=O)(=O)Nc1ccc(F)c(C(=O)c2c[nH]c3ncc(-c4ccc(N5CCN(C(=O)[C@H]6C[C@H](Nc7cccc8c7C(=O)N(C7CCC(=O)NC7=O)C8=O)C6)CC5)cc4)cc23)c1F
BRAF V600E
MAALSGGGGGGAEPGQALFNGDMEPEAGAGAGAAASSAADPAIPEEVWNIKQMIKLTQEHIEALLDKFGGEHNPPSIYLEAYEEYTSKLDALQQREQQLLESLGNGTDFSVSSSASMDTVTSSSSSSLSVLPSSLSVFQNPTDVARSNPKSPQKPIVRVFLPNKQRTVVPARCGVTVRDSLKKALMMRGLIPECCAVYRIQDGEKKPIGWDTDISWLTGEELHVEVLENVPLTTHNFVRKTFFTLAFCDFCRKLLFQGFRCQTCGYKFHQRCSTEVPLMCVNYDQLDLLFVSKFFEHHPIPQEEASLAETALTSGSSPSA...
CRBN
A-375
DC50
nM
23
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P15056
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0132
Homo sapiens
10.1021/acsmedchemlett.2c00039
Degradation of BRAF V600E in A375 cells after 24 h treatment
PROTAC-DB
null
null
African=0.84%; Native American=0.49%; East Asian, North=1.69%; East Asian, South=0%; South Asian=0%; European, North=67.22%; European, South=29.75%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01,02; B*12,13. A*01 A*01 Stable (MSS) (Sanger). In situ; Leg, skin; Caucasian. Canc...
-1
false
456
0
CCN(C)S(=O)(=O)Nc1ccc(F)c(C(=O)c2c[nH]c3ncc(-c4ccc(N5CCN(C(=O)[C@H]6C[C@H](Nc7cccc8c7C(=O)N(C7CCC(=O)NC7=O)C8=O)C6)CC5)nc4)cc23)c1F
BRAF V600E
MAALSGGGGGGAEPGQALFNGDMEPEAGAGAGAAASSAADPAIPEEVWNIKQMIKLTQEHIEALLDKFGGEHNPPSIYLEAYEEYTSKLDALQQREQQLLESLGNGTDFSVSSSASMDTVTSSSSSSLSVLPSSLSVFQNPTDVARSNPKSPQKPIVRVFLPNKQRTVVPARCGVTVRDSLKKALMMRGLIPECCAVYRIQDGEKKPIGWDTDISWLTGEELHVEVLENVPLTTHNFVRKTFFTLAFCDFCRKLLFQGFRCQTCGYKFHQRCSTEVPLMCVNYDQLDLLFVSKFFEHHPIPQEEASLAETALTSGSSPSA...
CRBN
A-375
DC50
nM
10
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P15056
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0132
Homo sapiens
10.1021/acsmedchemlett.2c00039
Degradation of BRAF V600E in A375 cells after 24 h treatment
PROTAC-DB
null
null
African=0.84%; Native American=0.49%; East Asian, North=1.69%; East Asian, South=0%; South Asian=0%; European, North=67.22%; European, South=29.75%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01,02; B*12,13. A*01 A*01 Stable (MSS) (Sanger). In situ; Leg, skin; Caucasian. Canc...
-1
false
457
0
CCN(C)S(=O)(=O)Nc1ccc(F)c(C(=O)c2c[nH]c3ncc(-c4cnc(N5CCN(C(=O)CCCOc6cccc7c6CN(C6CCC(=O)NC6=O)C7=O)CC5)nc4)cc23)c1F
BRAF V600E
MAALSGGGGGGAEPGQALFNGDMEPEAGAGAGAAASSAADPAIPEEVWNIKQMIKLTQEHIEALLDKFGGEHNPPSIYLEAYEEYTSKLDALQQREQQLLESLGNGTDFSVSSSASMDTVTSSSSSSLSVLPSSLSVFQNPTDVARSNPKSPQKPIVRVFLPNKQRTVVPARCGVTVRDSLKKALMMRGLIPECCAVYRIQDGEKKPIGWDTDISWLTGEELHVEVLENVPLTTHNFVRKTFFTLAFCDFCRKLLFQGFRCQTCGYKFHQRCSTEVPLMCVNYDQLDLLFVSKFFEHHPIPQEEASLAETALTSGSSPSA...
CRBN
A-375
DC50
nM
20
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P15056
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0132
Homo sapiens
10.1021/acsmedchemlett.2c00039
Degradation of BRAF V600E in A375 cells after 24 h treatment
PROTAC-DB
null
null
African=0.84%; Native American=0.49%; East Asian, North=1.69%; East Asian, South=0%; South Asian=0%; European, North=67.22%; European, South=29.75%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01,02; B*12,13. A*01 A*01 Stable (MSS) (Sanger). In situ; Leg, skin; Caucasian. Canc...
-1
false
458
118
CCN(CCCC#Cc1cnn(CCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](C)c2ccc(-c3scnc3C)cc2)C(C)(C)C)c1)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
30
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM 99.5 %).
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
459
0
CCN(CCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
37
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
460
9
CCN(CCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
10
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
461
0
CCN(CCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
74
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
462
4
CCN(CCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
68
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
463
4
CCN(CCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
21
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM 29 %).
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
464
0
CCN(CCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
79
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM 99.6 %).
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
464
0
CCN(CCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(Cn2c(-c3ccc(O)cc3)c(C)c3cc(O)ccc32)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
26
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
DCmax was measured in 1 nM (at 90 nM 3 %).
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
465
0
CCN(CCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc([C@@H]2c3ccc(O)cc3CC[C@@H]2c2ccccc2)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
26
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
DCmax was measured in 1 nM (at 10 nM 95 %).
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
466
0
CCN(CCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(Cl)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
1
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
22
13
CCN(CCCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
77
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
467
0
CCN(CCCCCCCCCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
75
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM.
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
468
0
CCN(CCCCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1
ER
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
DC50
nM
0.17
null
null
null
null
4
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
10.1021/acs.jmedchem.8b01572
Degradation of ER in MCF-7/T47D cells after 4 h treatment
PROTAC-DB
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
469
0
CCN(CCCCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1
ER
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
95
null
null
null
null
4
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
10.1021/acs.jmedchem.8b01572
Degradation of ER in MCF-7/T47D cells after 4 h treatment
PROTAC-DB
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
469
0
CCN(CCCCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1
ER
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
T-47D
DC50
nM
0.43
null
null
null
null
4
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0553
Homo sapiens
10.1021/acs.jmedchem.8b01572
Degradation of ER in MCF-7/T47D cells after 4 h treatment
PROTAC-DB
null
null
African=0.86%; Native American=1.2%; East Asian, North=3.03%; East Asian, South=1.59%; South Asian=8.04%; European, North=22.59%; European, South=62.69%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*33 A*33 A*33 Stable (MSS). CVCL_3945 ! T-47 Metastatic; Pleural effusion; Caucasian. Cancer cell line
15
false
469
0
CCN(CCCCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1
ER
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
T-47D
Dmax
%
95
null
null
null
null
4
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0553
Homo sapiens
10.1021/acs.jmedchem.8b01572
Degradation of ER in MCF-7/T47D cells after 4 h treatment
PROTAC-DB
null
null
African=0.86%; Native American=1.2%; East Asian, North=3.03%; East Asian, South=1.59%; South Asian=8.04%; European, North=22.59%; European, South=62.69%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*33 A*33 A*33 Stable (MSS). CVCL_3945 ! T-47 Metastatic; Pleural effusion; Caucasian. Cancer cell line
15
false
469
0
CCN(CCCCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
DC50
nM
0.43
null
null
null
null
4
<
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of PROTAC was measured in MCF7 cell line. DC50 is 0.17 nM MCF-7, 0.43 T47D. EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 5 nM > 95 %).
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
469
0
CCN(CCCCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
92
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of PROTAC was measured in MCF7 cell line. DC50 is 0.17 nM MCF-7, 0.43 T47D. EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 5 nM > 95 %).
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
469
0
CCN(CCCCc1cnn(CC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](C)c2ccc(-c3scnc3C)cc2)C(C)(C)C)c1)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
1
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM 80 %).
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
470
0
CCN(CCCc1ccc(N2CCC(CN3C[C@H]4C[C@@H]3CN4c3ccc4c(c3)CN(C3CCC(=O)NC3=O)C4=O)CC2)cc1)c1ccc(C#N)c(C(F)(F)F)c1
AR
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL...
CRBN
LNCaP
DC50
nM
88.1
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P10275
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0395
Homo sapiens
COMPOUNDS AND THEIR USE IN TREATING CANCER (patent)
LNCaP Androgen Receptor Imaging Assay This cell-based imaging assay uses immuno-fluorescence to measure both cell number and endogenous nuclear AR staining in the prostate cancer cell line LNCaP (expressing AR-full length). The purpose of the assay is to identify compounds that regulate AR protein level according to th...
TPDdb
Fluorescence Imaging Assay
TPD-Q21RUP
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01 Instable (MSI). Metastatic; Left supraclavicular lymph node; Caucasian. Space-flown cell line (cellonaut). Cancer cell line
16
false
471
274
CCN(CCCc1ccc(N2CCC(CN3C[C@H]4C[C@@H]3CN4c3ccc4c(c3)CN(C3CCC(=O)NC3=O)C4=O)CC2)cc1)c1ccc(C#N)c(C(F)(F)F)c1
AR
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL...
CRBN
LNCaP
Dmax
%
88
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P10275
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0395
Homo sapiens
COMPOUNDS AND THEIR USE IN TREATING CANCER (patent)
LNCaP Androgen Receptor Imaging Assay This cell-based imaging assay uses immuno-fluorescence to measure both cell number and endogenous nuclear AR staining in the prostate cancer cell line LNCaP (expressing AR-full length). The purpose of the assay is to identify compounds that regulate AR protein level according to th...
TPDdb
Fluorescence Imaging Assay
TPD-Q21RUP
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*01 Instable (MSI). Metastatic; Left supraclavicular lymph node; Caucasian. Space-flown cell line (cellonaut). Cancer cell line
16
false
471
274
CCN(CCOCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H](C)c1ccc(-c2scnc2C)cc1)C(C)(C)C)CCOc1ccc(C(=O)c2c(-c3ccc(O)cc3)sc3cc(O)ccc23)cc1
ESR1
MTMTLHTKASGMALLHQIQGNELEPLNRPQLKIPLERPLGEVYLDSSKPAVYNYPEGAAYEFNAAAAANAQVYGQTGLPYGPGSEAAAFGSNGLGGFPPLNSVSPSPLMLLHPPPQLSPFLQPHGQQVPYYLENEPSGYTVREAGPPAFYRPNSDNRRQGGRERLASTNDKGSMAMESAKETRYCAVCNDYASGYHYGVWSCEGCKAFFKRSIQGHNDYMCPATNQCTIDKNRRKSCQACRLRKCYEVGMMKGGIRKDRRGGRMLKHKRQRDDGEGRGEVGSAGDMRAANLWPSPLMIKRSKKNSLALSLTADQMVSALL...
VHL
MCF-7
Dmax
%
6
null
null
null
null
4
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P03372
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0031
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/30990042/
EC50 of ligand was measured in MCF7 cells. DCmax was measured in 1 nM (at 10 nM > 99.6 %).
PROTACpedia
null
null
African=0.74%; Native American=0%; East Asian, North=4.2%; East Asian, South=0%; South Asian=0%; European, North=56.91%; European, South=38.15%. Helen Marion Mallon (sister Catherine Frances), the patient from which this cell line is derived was a nun at the Immaculate Heart of Mary convent in Monroe, Michigan (CelloPu...
15
false
472
0
CCN(c1ccc(C#N)c(Cl)c1)[C@H]1CC[C@H](NC(=O)c2ccc(N3CCC(N4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)cc2)CC1
AR
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL...
CRBN
VCaP
DC50
nM
0.1
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P10275
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_2235
Homo sapiens
10.1021/acs.jmedchem.1c00900
Degradation of AR in VCaP cells after 24 h treatment
PROTAC-DB
null
null
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
431
78
CCN(c1ccc(C#N)c(Cl)c1)[C@H]1CC[C@H](NC(=O)c2ccc(N3CCC(N4CCN(c5ccc6c(c5)C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)CC3)cc2)CC1
AR
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL...
CRBN
VCaP
Dmax
%
99
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P10275
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_2235
Homo sapiens
10.1021/acs.jmedchem.1c00900
Degradation of AR in VCaP cells after 24 h treatment
PROTAC-DB
null
null
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
431
78
CCN1CC2(CN(c3cc(-c4ccccc4O)nnc3N)C2)c2ccc(N3CCC(C(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)N[C@@H](C)c4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)cc21
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
HT-1080
DC50
nM
1.49
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0317
Homo sapiens
SUBSTITUTED TRICYCLIC DERIVATIVE, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent)
1. On the first day, cells were plated, 10,000 HT-1080 (ATCC-CCL-121) cells were added to each well of a 384-well plate (Corning-3764), and cultured overnight at 37°C and 5% CO? (volume fraction, the rest was air). 2. On the second day, the compound was dissolved in DMSO with an initial concentration of 10 mM. The comp...
TPDdb
null
TPD-J65UL3
African=0.86%; Native American=0.35%; East Asian, North=1.36%; East Asian, South=0.29%; South Asian=0%; European, North=68.21%; European, South=28.94%. This cell line is considered by some researchers to represent a dedifferentiated chondrosarcoma due to the presence of an IDH1 mutation. Gene deletion; HGNC; HGNC Mutat...
9
false
473
9
CCN1CC2(CN(c3cc(-c4ccccc4O)nnc3N)C2)c2ccc(N3CCC(C(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)N[C@@H](C)c4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)cc21
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
HT-1080
DC50
nM
9.17
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0317
Homo sapiens
SUBSTITUTED TRICYCLIC DERIVATIVE, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF (patent)
1. On the first day, cells were plated, 10,000 HT-1080 (ATCC-CCL-121) cells were added to each well of a 384-well plate (Corning-3764), and cultured overnight at 37°C and 5% CO? (volume fraction, the rest was air). 2. On the second day, the compound was dissolved in DMSO with an initial concentration of 10 mM. The comp...
TPDdb
null
TPD-J65UL3
African=0.86%; Native American=0.35%; East Asian, North=1.36%; East Asian, South=0.29%; South Asian=0%; European, North=68.21%; European, South=28.94%. This cell line is considered by some researchers to represent a dedifferentiated chondrosarcoma due to the presence of an IDH1 mutation. Gene deletion; HGNC; HGNC Mutat...
9
false
473
9
CCN1CCN(Cc2ccc(NC(=O)c3cccc(-c4ccc5nc(NC(=O)COCCOCCOCCNC(=O)[C@@H](NC(=O)[C@@H]6CCCN6C(=O)[C@@H](NC(=O)[C@H](C)NC)C6CCCCC6)C(c6ccccc6)c6ccccc6)sc5n4)c3)cc2C(F)(F)F)CC1
BCR-ABL
MVDPVGFAEAWKAQFPDSEPPRMELRSVGDIEQELERCKASIRRLEQEVNQERFRMIYLQTLLAKEKKSYDRQRWGFRRAAQAPDGASEPRASASRPQPAPADGADPPPAEEPEARPDGEGSPGKARPGTARRPGAAASGERDDRGPPASVAALRSNFERIRKGHGQPGADAEKPFYVNVEFHHERGLVKVNDKEVSDRISSLGSQAMQMERKKSQHGAGSSVGDASRPPYRGRSSESSCGVDGDYEDAELNPRFLKDNLIDANGGSRPPWPPLEYQPYQSIYVGGMMEGEGKGPLLRSQSTSEQEKRLTWPRRSYSPRS...
IAP
K-562
DC50
nM
2,000
null
null
null
null
6
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
A9UF07
P98170
MTFNSFEGSKTCVPADINKEEEFVEEFNRLKTFANFPSGSPVSASTLARAGFLYTGEGDTVRCFSCHAAVDRWQYGDSAVGRHRKVSPNCRFINGFYLENSATQSTNSGIQNGQYKVENYLGSRDHFALDRPSETHADYLLRTGQVVDISDTIYPRNPAMYSEEARLKSFQNWPDYAHLTPRELASAGLYYTGIGDQVQCFCCGGKLKNWEPCDRAWSEHRRHFPNCFFVLGRNLNIRSESDAVSSDRNFPNSTNLPRNPSMADYEARIFTFGTWIYSVNKEQLARAGFYALGEGDKVKCFHCGGGLTDWKPSEDPWEQH...
CVCL_0004
Homo sapiens
10.1111/cas.13284
Degradation of BCR-ABL in K562 cells after 6 h treatment
PROTAC-DB
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
27
false
474
0
CCN1CCN(Cc2ccc(NC(=O)c3cccc(-c4ccc5nc(NC(=O)COCCOCCOCCNC(=O)[C@H](CC(C)C)NC(=O)[C@@H](O)[C@H](N)Cc6ccccc6)sc5n4)c3)cc2C(F)(F)F)CC1
BCR-ABL
MVDPVGFAEAWKAQFPDSEPPRMELRSVGDIEQELERCKASIRRLEQEVNQERFRMIYLQTLLAKEKKSYDRQRWGFRRAAQAPDGASEPRASASRPQPAPADGADPPPAEEPEARPDGEGSPGKARPGTARRPGAAASGERDDRGPPASVAALRSNFERIRKGHGQPGADAEKPFYVNVEFHHERGLVKVNDKEVSDRISSLGSQAMQMERKKSQHGAGSSVGDASRPPYRGRSSESSCGVDGDYEDAELNPRFLKDNLIDANGGSRPPWPPLEYQPYQSIYVGGMMEGEGKGPLLRSQSTSEQEKRLTWPRRSYSPRS...
IAP
K-562
DC50
nM
10,000
null
null
null
null
6
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
A9UF07
P98170
MTFNSFEGSKTCVPADINKEEEFVEEFNRLKTFANFPSGSPVSASTLARAGFLYTGEGDTVRCFSCHAAVDRWQYGDSAVGRHRKVSPNCRFINGFYLENSATQSTNSGIQNGQYKVENYLGSRDHFALDRPSETHADYLLRTGQVVDISDTIYPRNPAMYSEEARLKSFQNWPDYAHLTPRELASAGLYYTGIGDQVQCFCCGGKLKNWEPCDRAWSEHRRHFPNCFFVLGRNLNIRSESDAVSSDRNFPNSTNLPRNPSMADYEARIFTFGTWIYSVNKEQLARAGFYALGEGDKVKCFHCGGGLTDWKPSEDPWEQH...
CVCL_0004
Homo sapiens
10.1111/cas.13284
Degradation of BCR-ABL in K562 cells after 6 h treatment
PROTAC-DB
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
27
false
475
0
CCN1CCN(Cc2ccc(NC(=O)c3cccc(-c4ccc5nc(NC(=O)COCCOCCOCCOc6cccc(C(=O)c7csc([C@@H]8CCCN8C(=O)[C@@H](NC(=O)[C@H](C)NC)C8CCCCC8)n7)c6)sc5n4)c3)cc2C(F)(F)F)CC1
BCR-ABL
MVDPVGFAEAWKAQFPDSEPPRMELRSVGDIEQELERCKASIRRLEQEVNQERFRMIYLQTLLAKEKKSYDRQRWGFRRAAQAPDGASEPRASASRPQPAPADGADPPPAEEPEARPDGEGSPGKARPGTARRPGAAASGERDDRGPPASVAALRSNFERIRKGHGQPGADAEKPFYVNVEFHHERGLVKVNDKEVSDRISSLGSQAMQMERKKSQHGAGSSVGDASRPPYRGRSSESSCGVDGDYEDAELNPRFLKDNLIDANGGSRPPWPPLEYQPYQSIYVGGMMEGEGKGPLLRSQSTSEQEKRLTWPRRSYSPRS...
IAP
K-562
DC50
nM
300
null
null
null
null
6
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
A9UF07
P98170
MTFNSFEGSKTCVPADINKEEEFVEEFNRLKTFANFPSGSPVSASTLARAGFLYTGEGDTVRCFSCHAAVDRWQYGDSAVGRHRKVSPNCRFINGFYLENSATQSTNSGIQNGQYKVENYLGSRDHFALDRPSETHADYLLRTGQVVDISDTIYPRNPAMYSEEARLKSFQNWPDYAHLTPRELASAGLYYTGIGDQVQCFCCGGKLKNWEPCDRAWSEHRRHFPNCFFVLGRNLNIRSESDAVSSDRNFPNSTNLPRNPSMADYEARIFTFGTWIYSVNKEQLARAGFYALGEGDKVKCFHCGGGLTDWKPSEDPWEQH...
CVCL_0004
Homo sapiens
10.1111/cas.13284
Degradation of BCR-ABL in K562 cells after 6 h treatment
PROTAC-DB
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
27
false
476
0
CCNc1nn(C2CCN(CC3CC4(C3)CN(C(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)N[C@@H](C)c3ccc(-c5scnc5C)cc3)C(C)(C)C)C4)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
DC50
nM
2.6
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
Detecting Compounds' BRM and BRG1 Protein Degradation Activity Using HiBiT Detection Technology 1. Cell Line Construction: The effects of compounds on BRM and BRG1 protein degradation were detected using HiBiT detection technology. A HiBiT tag was inserted after the start codon or before the stop codon of the BRM and B...
TPDdb
HiBiT
TPD-LNMTSO
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...
9
false
477
7
CCNc1nn(C2CCN(CC3CC4(C3)CN(C(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)N[C@@H](C)c3ccc(-c5scnc5C)cc3)C(C)(C)C)C4)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
Dmax
%
96
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
Detecting Compounds' BRM and BRG1 Protein Degradation Activity Using HiBiT Detection Technology 1. Cell Line Construction: The effects of compounds on BRM and BRG1 protein degradation were detected using HiBiT detection technology. A HiBiT tag was inserted after the start codon or before the stop codon of the BRM and B...
TPDdb
HiBiT
TPD-LNMTSO
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...
9
false
477
7
CCNc1nn(C2CCN(CC3CC4(C3)CN(C(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)N[C@@H](C)c3ccc(-c5scnc5C)cc3)C(C)(C)C)C4)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
DC50
nM
25
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
Detecting Compounds' BRM and BRG1 Protein Degradation Activity Using HiBiT Detection Technology 1. Cell Line Construction: The effects of compounds on BRM and BRG1 protein degradation were detected using HiBiT detection technology. A HiBiT tag was inserted after the start codon or before the stop codon of the BRM and B...
TPDdb
HiBiT
TPD-LNMTSO
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...
9
false
477
7
CCNc1nn(C2CCN(CC3CC4(C3)CN(C(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)N[C@@H](C)c3ccc(-c5scnc5C)cc3)C(C)(C)C)C4)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
Dmax
%
81
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
Detecting Compounds' BRM and BRG1 Protein Degradation Activity Using HiBiT Detection Technology 1. Cell Line Construction: The effects of compounds on BRM and BRG1 protein degradation were detected using HiBiT detection technology. A HiBiT tag was inserted after the start codon or before the stop codon of the BRM and B...
TPDdb
HiBiT
TPD-LNMTSO
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...
9
false
477
7
CCNc1nn(C2CCN(CC3CCN(CC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)N[C@@H](C)c4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
A-549
DC50
nM
2
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-99ZEJA
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
9
false
434
4
CCNc1nn(C2CCN(CC3CCN(CC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)N[C@@H](C)c4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
A-549
Dmax
%
90
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-99ZEJA
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
9
false
434
4
CCNc1nn(C2CCN(CC3CCN(CC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)N[C@@H](C)c4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
DC50
nM
0.82
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-99ZEJA
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...
9
false
434
4
CCNc1nn(C2CCN(CC3CCN(CC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)N[C@@H](C)c4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
Dmax
%
96
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-99ZEJA
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...
9
false
434
4
CCNc1nn(C2CCN(CC3CCN(CC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)N[C@@H](C)c4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
DC50
nM
65
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-99ZEJA
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...
9
false
434
4
CCNc1nn(C2CCN(CC3CCN(CC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)N[C@@H](C)c4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
Dmax
%
59
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-99ZEJA
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...
9
false
434
4
CCNc1nn(C2CCN(CC3CCN(c4cc(C(C(=O)N5C[C@H](O)C[C@H]5C(=O)N[C@@H](C)c5ccc(-c6scnc6C)cc5)C(C)C)on4)CC3)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
A-549
DC50
nM
0.35
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-DNZCPR
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
9
false
435
0
CCNc1nn(C2CCN(CC3CCN(c4cc(C(C(=O)N5C[C@H](O)C[C@H]5C(=O)N[C@@H](C)c5ccc(-c6scnc6C)cc5)C(C)C)on4)CC3)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
A-549
Dmax
%
78
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0023
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-DNZCPR
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
9
false
435
0
CCNc1nn(C2CCN(CC3CCN(c4cc(C(C(=O)N5C[C@H](O)C[C@H]5C(=O)N[C@@H](C)c5ccc(-c6scnc6C)cc5)C(C)C)on4)CC3)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
DC50
nM
0.16
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-DNZCPR
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...
9
false
435
0
CCNc1nn(C2CCN(CC3CCN(c4cc(C(C(=O)N5C[C@H](O)C[C@H]5C(=O)N[C@@H](C)c5ccc(-c6scnc6C)cc5)C(C)C)on4)CC3)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
Dmax
%
91
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-DNZCPR
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...
9
false
435
0
CCNc1nn(C2CCN(CC3CCN(c4cc(C(C(=O)N5C[C@H](O)C[C@H]5C(=O)N[C@@H](C)c5ccc(-c6scnc6C)cc5)C(C)C)on4)CC3)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
DC50
nM
1.4
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-DNZCPR
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...
9
false
435
0
CCNc1nn(C2CCN(CC3CCN(c4cc(C(C(=O)N5C[C@H](O)C[C@H]5C(=O)N[C@@H](C)c5ccc(-c6scnc6C)cc5)C(C)C)on4)CC3)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
Dmax
%
77
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
In-cell Western blotting was used to examine the effects of compounds on BRM and BRG1 degradation. Methods: Cells were seeded into 384-well plates at varying concentrations (A549: 5000 cells/well, SW1573: 8000 cells/well, both purchased from ATCC) and incubated overnight at 37°C, 5% CO?. Compounds were dissolved in DMS...
TPDdb
In-Cell Western
TPD-DNZCPR
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...
9
false
435
0
CCNc1nn(C2CCN(C[C@H]3CC[C@H](C(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)N[C@@H](C)c4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
DC50
nM
7
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
Detecting Compounds' BRM and BRG1 Protein Degradation Activity Using HiBiT Detection Technology 1. Cell Line Construction: The effects of compounds on BRM and BRG1 protein degradation were detected using HiBiT detection technology. A HiBiT tag was inserted after the start codon or before the stop codon of the BRM and B...
TPDdb
HiBiT
TPD-3AKBJX
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...
9
false
478
7
CCNc1nn(C2CCN(C[C@H]3CC[C@H](C(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)N[C@@H](C)c4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA2
MSTPTDPGAMPHPGPSPGPGPSPGPILGPSPGPGPSPGSVHSMMGPSPGPPSVSHPMPTMGSTDFPQEGMHQMHKPIDGIHDKGIVEDIHCGSMKGTGMRPPHPGMGPPQSPMDQHSQGYMSPHPSPLGAPEHVSSPMSGGGPTPPQMPPSQPGALIPGDPQAMSQPNRGPSPFSPVQLHQLRAQILAYKMLARGQPLPETLQLAVQGKRTLPGLQQQQQQQQQQQQQQQQQQQQQQQPQQQPPQPQTQQQQQPALVNYNRPSGPGPELSGPSTPQKLPVPAPGGRPSPAPPAAAQPPAAAVPGPSVPQPAPGQPSPVLQ...
VHL
SW1573
Dmax
%
90
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51531
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
Detecting Compounds' BRM and BRG1 Protein Degradation Activity Using HiBiT Detection Technology 1. Cell Line Construction: The effects of compounds on BRM and BRG1 protein degradation were detected using HiBiT detection technology. A HiBiT tag was inserted after the start codon or before the stop codon of the BRM and B...
TPDdb
HiBiT
TPD-3AKBJX
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...
9
false
478
7
CCNc1nn(C2CCN(C[C@H]3CC[C@H](C(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)N[C@@H](C)c4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
DC50
nM
1,000
null
null
null
null
null
>
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
Detecting Compounds' BRM and BRG1 Protein Degradation Activity Using HiBiT Detection Technology 1. Cell Line Construction: The effects of compounds on BRM and BRG1 protein degradation were detected using HiBiT detection technology. A HiBiT tag was inserted after the start codon or before the stop codon of the BRM and B...
TPDdb
HiBiT
TPD-3AKBJX
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...
9
false
478
7
CCNc1nn(C2CCN(C[C@H]3CC[C@H](C(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)N[C@@H](C)c4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)CC2)c2cc(-c3ccccc3O)nnc12
SMARCA4
MSTPDPPLGGTPRPGPSPGPGPSPGAMLGPSPGPSPGSAHSMMGPSPGPPSAGHPIPTQGPGGYPQDNMHQMHKPMESMHEKGMSDDPRYNQMKGMGMRSGGHAGMGPPPSPMDQHSQGYPSPLGGSEHASSPVPASGPSSGPQMSSGPGGAPLDGADPQALGQQNRGPTPFNQNQLHQLRAQIMAYKMLARGQPLPDHLQMAVQGKRPMPGMQQQMPTLPPPSVSATGPGPGPGPGPGPGPGPAPPNYSRPHGMGGPNMPPPGPSGVPPGMPGQPPGGPPKPWPEGPMANAAAPTSTPQKLIPPQPTGRPSPAPPAVPP...
VHL
SW1573
Dmax
%
42
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P51532
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_1720
Homo sapiens
BRM SELECTIVE DEGRADATION AGENT COMPOUND AND USE THEREOF (patent)
Detecting Compounds' BRM and BRG1 Protein Degradation Activity Using HiBiT Detection Technology 1. Cell Line Construction: The effects of compounds on BRM and BRG1 protein degradation were detected using HiBiT detection technology. A HiBiT tag was inserted after the start codon or before the stop codon of the BRM and B...
TPDdb
HiBiT
TPD-3AKBJX
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...
9
false
478
7
CCOC(=O)c1[nH]c2cc(Cl)ccc2c1C(C(=O)NC(C)(C)C)N(Cc1cc(F)c(F)c(F)c1)C(=O)CCCCC#Cc1cccc2c1CN(C1CCC(=O)NC1=O)C2=O
MDM2
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
CRBN
RS4;11
DC50
nM
4.1
null
null
null
null
12
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q00987
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0093
Homo sapiens
10.1016/j.ejmech.2021.113425
Degradation of MDM2 in RS4;11 cells after 12 h treatment
PROTAC-DB
null
null
African=0%; Native American=0.02%; East Asian, North=0%; East Asian, South=1.26%; South Asian=1.83%; European, North=65.49%; European, South=31.4%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*03 Instable (MSI-high). In situ; Bone marrow; Caucasian. Cancer cell line
10
true
-1
-1
CCOc1c(C#N)cc2c(c1Cl)CCCC2c1cnc(NCCOCCOc2ccc3c(c2)C(=O)N(C2CCC(=O)NC2=O)C3=O)nc1
AR3
MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL...
CRBN
22Rv1
DC50
nM
13
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P10275
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1045
Homo sapiens
BENZO(HETERO)CYCLOALKYL COMPOUNDS FOR ANDROGEN RECEPTOR-DEPENDENT DISEASES (patent)
In this experiment, CRISPR/Cas9 technology was used to integrate HiBiT tag (PromegaTM) into the C-terminus of the AR-V7 genome of 22RV1 cells (ATCC) to construct 22RV1 cells that stably express AR-V7-HiBiT. The test compound was diluted 3-fold with DMSO starting from 1000nM to 11 points, and the cells were cultured wit...
TPDdb
HiBiT
TPD-CIYW6B
African=0.89%; Native American=0.23%; East Asian, North=0.52%; East Asian, South=0%; South Asian=0.27%; European, North=67.46%; European, South=30.62%. Contains at least 10 integrated copies of xenotropic murine leukemia virus-related virus (XMRV) genome and produces a high titer of the virus. Mutation; HGNC; HGNC Muta...
16
true
-1
-1
CCOc1cc(C(C)(C)C)ccc1C1=NC(c2ccc(Cl)cc2)C(c2ccc(Cl)cc2)N1C(=O)N1CCN(CC#Cc2cccc3c2CN(C2CCC(=O)NC2=O)C3=O)CC1
MDM2
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
CRBN
RS4;11
DC50
nM
100
null
null
null
null
6
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q00987
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0093
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31128449/
null
PROTACpedia
null
null
African=0%; Native American=0.02%; East Asian, North=0%; East Asian, South=1.26%; South Asian=1.83%; European, North=65.49%; European, South=31.4%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*03 Instable (MSI-high). In situ; Bone marrow; Caucasian. Cancer cell line
10
false
479
273
CCOc1cc(C(C)(C)C)ccc1C1=NC(c2ccc(Cl)cc2)C(c2ccc(Cl)cc2)N1C(=O)N1CCN(CC(=O)NCCOCCOCCOCCNC(=O)CN2CCN(C(=O)N3C(c4ccc(C(C)(C)C)cc4OCC)=NC(c4ccc(Cl)cc4)C3c3ccc(Cl)cc3)CC2=O)C(=O)C1
MDM2
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
MDM2
A-549
DC50
nM
1,010
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q00987
Q00987
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
CVCL_0023
Homo sapiens
10.1016/j.apsb.2020.11.022
Degradation of MDM2 in A549 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
10
true
-1
-1
CCOc1cc(C(C)(C)C)ccc1C1=NC(c2ccc(Cl)cc2)C(c2ccc(Cl)cc2)N1C(=O)N1CCN(CC(=O)NCCOCCOCCOCCNC(=O)CN2CCN(C(=O)N3C(c4ccc(C(C)(C)C)cc4OCC)=NC(c4ccc(Cl)cc4)C3c3ccc(Cl)cc3)CC2=O)C(=O)C1
MDM2
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
MDM2
A-549
Dmax
%
95
null
null
null
null
24
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q00987
Q00987
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
CVCL_0023
Homo sapiens
10.1016/j.apsb.2020.11.022
Degradation of MDM2 in A549 cells after 24 h treatment
PROTAC-DB
null
null
African=0%; Native American=0%; East Asian, North=0.72%; East Asian, South=0%; South Asian=0%; European, North=66.12%; European, South=33.16%. Highly susceptible to infection by Zika virus (ZIKV). Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Expresses HPRT1 at the surface of the cell membrane. A*10,w1...
10
true
-1
-1
CCOc1cc(C(C)(C)C)ccc1C1=N[C@@H](c2ccc(Cl)cc2)[C@@H](c2ccc(Cl)cc2)N1C(=O)N1CCN(CC#Cc2cccc3c2CN(C2CCC(=O)NC2=O)C3=O)CC1
MDM2
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
CRBN
RS4;11
DC50
nM
23
null
null
null
null
15
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q00987
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0093
Homo sapiens
10.1016/j.ejmech.2019.05.046; https://pubmed.ncbi.nlm.nih.gov/31128449/
Degradation of MDM2 in RS4; 11 cells after 24 h treatment
PROTAC-DB; PROTACpedia
null
null
African=0%; Native American=0.02%; East Asian, North=0%; East Asian, South=1.26%; South Asian=1.83%; European, North=65.49%; European, South=31.4%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*03 Instable (MSI-high). In situ; Bone marrow; Caucasian. Cancer cell line
10
true
-1
-1
CCOc1cc(C(C)(C)C)ccc1C1=N[C@@H](c2ccc(Cl)cc2)[C@@H](c2ccc(Cl)cc2)N1C(=O)N1CCN(CC#Cc2cccc3c2CN(C2CCC(=O)NC2=O)C3=O)CC1
MDM2
MCNTNMSVPTDGAVTTSQIPASEQETLVRPKPLLLKLLKSVGAQKDTYTMKEVLFYLGQYIMTKRLYDEKQQHIVYCSNDLLGDLFGVPSFSVKEHRKIYTMIYRNLVVVNQQESSDSGTSVSENRCHLEGGSDQKDLVQELQEEKPSSSHLVSRPSTSSRRRAISETEENSDELSGERQRKRHKSDSISLSFDESLALCVIREICCERSSSSESTGTPSNPDLDAGVSEHSGDWLDQDSVSDQFSVEFEVESLDSEDYSLSEEGQELSDEDDEVYQVTVYQAGESDTDSFEEDPEISLADYWKCTSCNEMNPPLPSHCN...
CRBN
RS4;11
Dmax
%
90
null
null
null
null
15
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q00987
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0093
Homo sapiens
10.1016/j.ejmech.2019.05.046; https://pubmed.ncbi.nlm.nih.gov/31128449/
Degradation of MDM2 in RS4; 11 cells after 24 h treatment
PROTAC-DB; PROTACpedia
null
null
African=0%; Native American=0.02%; East Asian, North=0%; East Asian, South=1.26%; South Asian=1.83%; European, North=65.49%; European, South=31.4%. Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*03 Instable (MSI-high). In situ; Bone marrow; Caucasian. Cancer cell line
10
true
-1
-1
CCOc1cc(N2CCC(N3CCN(CCc4cc(F)c([C@H]5CCC(=O)NC5=O)c(F)c4)CC3)CC2)c(CC)cc1Nc1ncc(Br)c(Nc2ccc(CC)c3c2N(S(C)(=O)=O)CC3)n1
EGFR
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEE...
CRBN
Ba/F3
DC50
nM
83
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q01279
Q8C7D2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0161
Mus musculus
BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE (patent)
Cell treatment BaF3 cells are seeded at 100000 cells/well at a volume of 30μl/well in cell culture medium [RPMI1640, 10%heat-inactive FBS, 1%PS ] in Corning 96 well plate. BaF3 cells are treated with compounds diluted in 0.2%DMSO, dilution is done according to the following protocol: (1) make 500× stock solution in DMS...
TPDdb
HTRF LTC (L858R / T790M / C797S triple mutation)
TPD-1OF3XJ
Originally thought to originate from a BALB/c mouse but is in fact from a C3H mouse. IL3 dependent. C3H. In situ; Bone marrow; Pro-B cell; CL=CL_0000826. Factor-dependent cell line
23
true
-1
-1
CCOc1cc(S(=O)(=O)Nc2ccc(N3CCN(c4cc(F)cc(-c5c(C(=O)NCCN(C)C)c(C)n(CC)c5-c5ccc(Cl)cc5)c4)CC3)cc2)ccc1N[C@H](CCN1CCN(C(=O)CCCCCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](C)c2ccc(-c3scnc3C)cc2)C(C)(C)C)CC1)CSc1ccccc1
BCL2L1
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
VHL
MDA-MB-231
DC50
nM
18
null
null
null
null
null
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q07817
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0062
Homo sapiens
BCL-2/BCL-XL PROTEIN DEGRADER AND USE THEREOF (patent)
Cells were collected and lysed in a lysis buffer (Cat. No. BP-115DG, Boston Bio Products, Ashland, MA, USA) containing protease and phosphatase inhibitor cocktails (Cat. No. PPC1010, Sigma-Aldrich, St. Louis, MO, USA) . An equal amount of protein lysates was separated on precasted 4-20%Tris-glycine gels (Mini-PROTEAN T...
TPDdb
Western Blot
TPD-7JIS22
African=1.95%; Native American=0%; East Asian, North=2.44%; East Asian, South=0%; South Asian=7.42%; European, North=28.16%; European, South=60.03%. Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*02/28; B*07,08; C*w02,w06. A*02 A...
5
false
480
0
CCOc1ccnc(NC(=O)c2ccc(-c3nn4c(c3C(N)=O)Nc3ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)cc3CC4)c(F)c2C)c1
BTK
MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF...
CRBN
TMD8
DC50
nM
13.5
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-QDXBTT
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Genetically heterogeneous, consists of 3 subclones. A*02 In situ; Bone marrow; Japanese. Cancer cell line
31
false
481
15
CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3nc(Nc4ccc(C(=O)NC5CCN(c6ccc(C7CCC(=O)NC7=O)cc6)CC5)cc4)nc4[nH]ccc34)cn2)C1
JAK2
MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSGEYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYFPRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLGMAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQFSQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSRGKHKESETLTEQDLQLYCDF...
CRBN
MHH-CALL-4
DC50
nM
26
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O60674
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1410
Homo sapiens
10.1021/acsmedchemlett.1c00650
Degradation of JAK2 in MHH-CALL-4 cells after 24 h treatment
PROTAC-DB
null
null
African=0.24%; Native American=0%; East Asian, North=0.15%; East Asian, South=1.34%; South Asian=1.97%; European, North=65.48%; European, South=30.81%. Mutation; HGNC; HGNC A*03 Stable (MSS) (Sanger). In situ; Peripheral blood; Caucasian. Cancer cell line
22
false
482
205
CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3nc(Nc4ccc(C(=O)NC5CCN(c6ccc7c(c6)C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)cc4)nc4[nH]ccc34)cn2)C1
JAK2
MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSGEYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYFPRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLGMAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQFSQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSRGKHKESETLTEQDLQLYCDF...
CRBN
MHH-CALL-4
DC50
nM
21
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O60674
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1410
Homo sapiens
10.1021/acsmedchemlett.1c00650
Degradation of JAK2 in MHH-CALL-4 cells after 24 h treatment
PROTAC-DB
null
null
African=0.24%; Native American=0%; East Asian, North=0.15%; East Asian, South=1.34%; South Asian=1.97%; European, North=65.48%; European, South=30.81%. Mutation; HGNC; HGNC A*03 Stable (MSS) (Sanger). In situ; Peripheral blood; Caucasian. Cancer cell line
22
false
483
205
CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3nc(Nc4ccc(C(=O)NCCCCNc5cccc(C6CCC(=O)NC6=O)c5)cc4)nc4[nH]ccc34)cn2)C1
JAK2
MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSGEYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYFPRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLGMAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQFSQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSRGKHKESETLTEQDLQLYCDF...
CRBN
MHH-CALL-4
DC50
nM
14
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O60674
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1410
Homo sapiens
10.1021/acsmedchemlett.1c00650
Degradation of JAK2 in MHH-CALL-4 cells after 24 h treatment
PROTAC-DB
null
null
African=0.24%; Native American=0%; East Asian, North=0.15%; East Asian, South=1.34%; South Asian=1.97%; European, North=65.48%; European, South=30.81%. Mutation; HGNC; HGNC A*03 Stable (MSS) (Sanger). In situ; Peripheral blood; Caucasian. Cancer cell line
22
true
-1
-1
CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3nc(Nc4ccc(C(=O)NCCCCOc5ccc(C6CCC(=O)NC6=O)cc5)cc4)nc4[nH]ccc34)cn2)C1
JAK2
MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSGEYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYFPRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLGMAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQFSQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSRGKHKESETLTEQDLQLYCDF...
CRBN
MHH-CALL-4
DC50
nM
17
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O60674
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1410
Homo sapiens
10.1021/acsmedchemlett.1c00650
Degradation of JAK2 in MHH-CALL-4 cells after 24 h treatment
PROTAC-DB
null
null
African=0.24%; Native American=0%; East Asian, North=0.15%; East Asian, South=1.34%; South Asian=1.97%; European, North=65.48%; European, South=30.81%. Mutation; HGNC; HGNC A*03 Stable (MSS) (Sanger). In situ; Peripheral blood; Caucasian. Cancer cell line
22
false
484
205
CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3nc(Nc4ccc(C(=O)NCCCN5CCN(c6ccc(C7CCC(=O)NC7=O)cc6)CC5)cc4)nc4[nH]ccc34)cn2)C1
JAK2
MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSGEYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYFPRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLGMAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQFSQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSRGKHKESETLTEQDLQLYCDF...
CRBN
ALL-1
DC50
nM
14
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O60674
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_QW61
Homo sapiens
10.1021/acsmedchemlett.1c00650
Degradation of JAK2 in PDX SJBALL020589/MHH-CALL-4 cells after 24 h treatment
PROTAC-DB
null
null
Gene fusion; HGNC; HGNC Can be differentiated into dendritic-like cells in culture with a combination of cytokines (IL1B, IL3, IL7, TNF, KITLG and CD40LG). In situ; Bone marrow; Cancer cell line
22
false
485
0
CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3nc(Nc4ccc(C(=O)NCCCN5CCN(c6ccc(C7CCC(=O)NC7=O)cc6)CC5)cc4)nc4[nH]ccc34)cn2)C1
JAK2
MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSGEYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYFPRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLGMAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQFSQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSRGKHKESETLTEQDLQLYCDF...
CRBN
ALL-1
Dmax
%
90
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O60674
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_QW61
Homo sapiens
10.1021/acsmedchemlett.1c00650
Degradation of JAK2 in PDX SJBALL020589/MHH-CALL-4 cells after 24 h treatment
PROTAC-DB
null
null
Gene fusion; HGNC; HGNC Can be differentiated into dendritic-like cells in culture with a combination of cytokines (IL1B, IL3, IL7, TNF, KITLG and CD40LG). In situ; Bone marrow; Cancer cell line
22
false
485
0
CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3nc(Nc4ccc(C(=O)NCCCN5CCN(c6ccc(C7CCC(=O)NC7=O)cc6)CC5)cc4)nc4[nH]ccc34)cn2)C1
JAK2
MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSGEYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYFPRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLGMAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQFSQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSRGKHKESETLTEQDLQLYCDF...
CRBN
MHH-CALL-4
DC50
nM
24
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O60674
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1410
Homo sapiens
10.1021/acsmedchemlett.1c00650
Degradation of JAK2 in PDX SJBALL020589/MHH-CALL-4 cells after 24 h treatment
PROTAC-DB
null
null
African=0.24%; Native American=0%; East Asian, North=0.15%; East Asian, South=1.34%; South Asian=1.97%; European, North=65.48%; European, South=30.81%. Mutation; HGNC; HGNC A*03 Stable (MSS) (Sanger). In situ; Peripheral blood; Caucasian. Cancer cell line
22
false
485
0
CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3nc(Nc4ccc(C(=O)NCCCN5CCN(c6ccc(C7CCC(=O)NC7=O)cc6)CC5)cc4)nc4[nH]ccc34)cn2)C1
JAK2
MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSGEYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYFPRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLGMAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQFSQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSRGKHKESETLTEQDLQLYCDF...
CRBN
MHH-CALL-4
Dmax
%
82
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O60674
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1410
Homo sapiens
10.1021/acsmedchemlett.1c00650
Degradation of JAK2 in PDX SJBALL020589/MHH-CALL-4 cells after 24 h treatment
PROTAC-DB
null
null
African=0.24%; Native American=0%; East Asian, North=0.15%; East Asian, South=1.34%; South Asian=1.97%; European, North=65.48%; European, South=30.81%. Mutation; HGNC; HGNC A*03 Stable (MSS) (Sanger). In situ; Peripheral blood; Caucasian. Cancer cell line
22
false
485
0
CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3nc(Nc4ccc(C(=O)NCCCN5CCN(c6ccc(C7CCC(=O)NC7=O)cc6)CC5)cc4)nc4[nH]ccc34)cn2)C1
JAK2 R683G
MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSGEYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYFPRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLGMAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQFSQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSRGKHKESETLTEQDLQLYCDF...
CRBN
KOPN-49
DC50
nM
74
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O60674
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_W276
Homo sapiens
10.1021/acsmedchemlett.1c00650
Degradation of JAK2 R683G in KOPN49 cells after 24 h treatment
PROTAC-DB
null
null
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC In situ; Peripheral blood; Japanese. Cancer cell line
22
false
485
0
CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3nc(Nc4ccc(C(=O)NCCCN5CCN(c6ccc(C7CCC(=O)NC7=O)cc6)CC5)cc4)nc4[nH]ccc34)cn2)C1
JAK3
MAPPSEETPLIPQRSCSLLSTEAGALHVLLPARGPGPPQRLSFSFGDHLAEDLCVQAAKASGILPVYHSLFALATEDLSCWFPPSHIFSVEDASTQVLLYRIRFYFPNWFGLEKCHRFGLRKDLASAILDLPVLEHLFAQHRSDLVSGRLPVGLSLKEQGECLSLAVLDLARMAREQAQRPGELLKTVSYKACLPPSLRDLIQGLSFVTRRRIRRTVRRALRRVAACQADRHSLMAKYIMDLERLDPAGAAETFHVGLPGALGGHDGLGLLRVAGDGGIAWTQGEQEVLQPFCDFPEIVDISIKQAPRVGPAGEHRLVTV...
CRBN
ALL-1
DC50
nM
11
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P52333
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_QW61
Homo sapiens
10.1021/acsmedchemlett.1c00650
Degradation of JAK3 in PDX SJBALL020589 cells after 24 h treatment
PROTAC-DB
null
null
Gene fusion; HGNC; HGNC Can be differentiated into dendritic-like cells in culture with a combination of cytokines (IL1B, IL3, IL7, TNF, KITLG and CD40LG). In situ; Bone marrow; Cancer cell line
22
false
485
0
CCS(=O)(=O)N1CC(CC#N)(n2cc(-c3nc(Nc4ccc(C(=O)NCCCN5CCN(c6ccc(C7CCC(=O)NC7=O)cc6)CC5)cc4)nc4[nH]ccc34)cn2)C1
JAK3
MAPPSEETPLIPQRSCSLLSTEAGALHVLLPARGPGPPQRLSFSFGDHLAEDLCVQAAKASGILPVYHSLFALATEDLSCWFPPSHIFSVEDASTQVLLYRIRFYFPNWFGLEKCHRFGLRKDLASAILDLPVLEHLFAQHRSDLVSGRLPVGLSLKEQGECLSLAVLDLARMAREQAQRPGELLKTVSYKACLPPSLRDLIQGLSFVTRRRIRRTVRRALRRVAACQADRHSLMAKYIMDLERLDPAGAAETFHVGLPGALGGHDGLGLLRVAGDGGIAWTQGEQEVLQPFCDFPEIVDISIKQAPRVGPAGEHRLVTV...
CRBN
ALL-1
Dmax
%
92
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
P52333
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_QW61
Homo sapiens
10.1021/acsmedchemlett.1c00650
Degradation of JAK3 in PDX SJBALL020589 cells after 24 h treatment
PROTAC-DB
null
null
Gene fusion; HGNC; HGNC Can be differentiated into dendritic-like cells in culture with a combination of cytokines (IL1B, IL3, IL7, TNF, KITLG and CD40LG). In situ; Bone marrow; Cancer cell line
22
false
485
0
CC[C@@H]1C(=O)N(C)c2cnc(Nc3ccc(C(=O)NCCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)cc3OC)nc2N1C1CCCC1
BRD4
MSAESGPGTRLRNLPVMGDGLETSQMSTTQAQAQPQPANAASTNPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEETEIMIVQAKGRGRGRKETGTAKPGVSTVPNTTQASTPPQTQTPQPNPPPVQATPHPFPAVTPDLIVQTPVMTVVPPQPLQTPPPVPPQPQPPPAPAPQPVQSHPPIIAATPQPVKTKKGVKRKADTTTPTTIDPIHEPPSLPPEPKTTKLGQ...
CRBN
MV4-11
DC50
nM
5
null
null
null
null
24
<
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
O60885
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0064
Homo sapiens
10.1016/j.bbrc.2019.11.007; https://pubmed.ncbi.nlm.nih.gov/31708096/
Degradation of BRD4 in MV4-11 cells after 24 h treatment; They show "dual" degradation but don't do any test that the dual degradation actually made any difference. They make it sound novel but of course we can call our PROTACs "dual" degraders if you can the off-targets "targets". EC50 of ligand is in measured in MV4-...
PROTAC-DB; PROTACpedia
null
null
African=0.59%; Native American=0%; East Asian, North=0.34%; East Asian, South=0%; South Asian=2.57%; European, North=67.58%; European, South=28.91%. 48,XY,t(4;11)(q21;q23),+8,+19 (ATCC=CRL-9591). Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC CSF2 and IL3 dependent. A*03 A*03 Stable (MSS) (Sanger). In situ; Peripheral bl...
20
false
486
36
CC[C@@H]1C(=O)N(C)c2cnc(Nc3ccc(C(=O)NCCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)cc3OC)nc2N1C1CCCC1
BRD4
MSAESGPGTRLRNLPVMGDGLETSQMSTTQAQAQPQPANAASTNPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEETEIMIVQAKGRGRGRKETGTAKPGVSTVPNTTQASTPPQTQTPQPNPPPVQATPHPFPAVTPDLIVQTPVMTVVPPQPLQTPPPVPPQPQPPPAPAPQPVQSHPPIIAATPQPVKTKKGVKRKADTTTPTTIDPIHEPPSLPPEPKTTKLGQ...
CRBN
MV4-11
Dmax
%
100
null
null
null
null
24
~
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
O60885
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_0064
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31708096/
They show "dual" degradation but don't do any test that the dual degradation actually made any difference. They make it sound novel but of course we can call our PROTACs "dual" degraders if you can the off-targets "targets". EC50 of ligand is in measured in MV4-11 cell line. EC50 of PROTAC is between 4.5nM-6.94nM (depe...
PROTACpedia
null
null
African=0.59%; Native American=0%; East Asian, North=0.34%; East Asian, South=0%; South Asian=2.57%; European, North=67.58%; European, South=28.91%. 48,XY,t(4;11)(q21;q23),+8,+19 (ATCC=CRL-9591). Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC CSF2 and IL3 dependent. A*03 A*03 Stable (MSS) (Sanger). In situ; Peripheral bl...
20
false
486
36
CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C/C=C/CCCCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](C)c2ccc(-c3scnc3C)cc2)C(C)(C)C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O
PPIA
MVNPTVFFDIAVDGEPLGRVSFELFADKVPKTAENFRALSTGEKGFGYKGSCFHRIIPGFMCQGGDFTRHNGTGGKSIYGEKFEDENFILKHTGPGILSMANAGPNTNGSQFFICTAKTEWLDGKHVVFGKVKEGMNIVEAMERFGSRNGKTSKKITIADCGQLE
VHL
Huh-7
DC50
nM
30
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P62937
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0336
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/32539931/
Exhibits potent anti-HCV activity. The first demonstration of a PROTAC antiviral effect by degradation of a host protein (cyclophilin A).
PROTACpedia
null
null
African=1.56%; Native American=0%; East Asian, North=79.68%; East Asian, South=13.08%; South Asian=0%; European, North=0%; European, South=5.69%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11 Stable (MSS) (Sanger). In situ; Liver; Japanese. Cancer cell line
2
false
487
0
CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C/C=C/CCCCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H](C)c2ccc(-c3scnc3C)cc2)C(C)(C)C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O
PPIA
MVNPTVFFDIAVDGEPLGRVSFELFADKVPKTAENFRALSTGEKGFGYKGSCFHRIIPGFMCQGGDFTRHNGTGGKSIYGEKFEDENFILKHTGPGILSMANAGPNTNGSQFFICTAKTEWLDGKHVVFGKVKEGMNIVEAMERFGSRNGKTSKKITIADCGQLE
VHL
Huh-7
Dmax
%
90
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
P62937
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_0336
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/32539931/
Exhibits potent anti-HCV activity. The first demonstration of a PROTAC antiviral effect by degradation of a host protein (cyclophilin A).
PROTACpedia
null
null
African=1.56%; Native American=0%; East Asian, North=79.68%; East Asian, South=13.08%; South Asian=0%; European, North=0%; European, South=5.69%. Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC A*11 A*11 Stable (MSS) (Sanger). In situ; Liver; Japanese. Cancer cell line
2
false
487
0
CC[C@@H]1[C@H](F)C(=O)N[C@@H]1COc1ncc(C#CCCCCCCCCCCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)c2cc(C(N)=O)c(OC)cc12
IRAK4
MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD...
VHL
PBMC iPSC #1
DC50
nM
259
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q9NWZ3
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_WR41
Homo sapiens
10.1021/acsmedchemlett.9b00219; https://pubmed.ncbi.nlm.nih.gov/31312412/
Degradation of IRAK4 in PBMC cells after 24 h treatment
PROTAC-DB; PROTACpedia
null
null
In situ; Peripheral blood; Induced pluripotent stem cell
25
false
488
0
CC[C@@H]1[C@H](F)C(=O)N[C@@H]1COc1ncc(C#CCCCCCCCCCCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)c2cc(C(N)=O)c(OC)cc12
IRAK4
MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD...
VHL
PBMC iPSC #1
Dmax
%
90
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q9NWZ3
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_WR41
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31312412/
null
PROTACpedia
null
null
In situ; Peripheral blood; Induced pluripotent stem cell
25
false
488
0
CC[C@@H]1[C@H](F)C(=O)N[C@@H]1COc1ncc(C#CCN2CCC3(CC2)CCN(c2ncc(C(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)NCc4ccc(-c5scnc5C)cc4)C(C)(C)C)cn2)CC3)c2cc(C(N)=O)c(OC)cc12
IRAK4
MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD...
VHL
PBMC iPSC #1
DC50
nM
151
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q9NWZ3
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_WR41
Homo sapiens
10.1021/acsmedchemlett.9b00219; https://pubmed.ncbi.nlm.nih.gov/31312412/
Degradation of IRAK4 in PBMC cells/dermal fibroblast after 24/24 h treatment
PROTAC-DB; PROTACpedia
null
null
In situ; Peripheral blood; Induced pluripotent stem cell
25
false
489
0
CC[C@@H]1[C@H](F)C(=O)N[C@@H]1COc1ncc(C#CCN2CCC3(CC2)CCN(c2ncc(C(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)NCc4ccc(-c5scnc5C)cc4)C(C)(C)C)cn2)CC3)c2cc(C(N)=O)c(OC)cc12
IRAK4
MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD...
VHL
PBMC iPSC #1
Dmax
%
90
null
null
null
null
24
null
numeric
null
PROteolysis-TArgeting Chimera (PROTAC)
Q9NWZ3
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
CVCL_WR41
Homo sapiens
https://pubmed.ncbi.nlm.nih.gov/31312412/
null
PROTACpedia
null
null
In situ; Peripheral blood; Induced pluripotent stem cell
25
false
489
0
CC[C@@H]1[C@H](F)C(=O)N[C@@H]1COc1ncc(C#CCN2CCC3(CC2)CCN(c2ncc(C(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)NCc4ccc(-c5scnc5C)cc4)C(C)(C)C)cn2)CC3)c2cc(C(N)=O)c(OC)cc12
IRAK4
MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD...
VHL
null
DC50
nM
36
null
null
null
null
24
null
null
null
PROteolysis-TArgeting Chimera (PROTAC)
Q9NWZ3
P40337
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
null
null
10.1021/acsmedchemlett.9b00219
Degradation of IRAK4 in PBMC cells/dermal fibroblast after 24/24 h treatment
PROTAC-DB
null
null
null
25
false
489
0
CC[C@@H]1c2nnc(C)n2-c2cnc(Nc3ccc(C(=O)NC4CCN(C(=O)COc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cc3OC)nc2N1CC1CCCCC1
BRD4
MSAESGPGTRLRNLPVMGDGLETSQMSTTQAQAQPQPANAASTNPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEETEIMIVQAKGRGRGRKETGTAKPGVSTVPNTTQASTPPQTQTPQPNPPPVQATPHPFPAVTPDLIVQTPVMTVVPPQPLQTPPPVPPQPQPPPAPAPQPVQSHPPIIAATPQPVKTKKGVKRKADTTTPTTIDPIHEPPSLPPEPKTTKLGQ...
CRBN
22Rv1
DC50
nM
1
null
null
null
null
24
<
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O60885
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1045
Homo sapiens
10.1016/j.ejmech.2021.113922
Degradation of BRD4 in 22Rv1/VCaP cells after 24 h treatment
PROTAC-DB
null
null
African=0.89%; Native American=0.23%; East Asian, North=0.52%; East Asian, South=0%; South Asian=0.27%; European, North=67.46%; European, South=30.62%. Contains at least 10 integrated copies of xenotropic murine leukemia virus-related virus (XMRV) genome and produces a high titer of the virus. Mutation; HGNC; HGNC Muta...
20
false
490
272
CC[C@@H]1c2nnc(C)n2-c2cnc(Nc3ccc(C(=O)NC4CCN(C(=O)COc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cc3OC)nc2N1CC1CCCCC1
BRD4
MSAESGPGTRLRNLPVMGDGLETSQMSTTQAQAQPQPANAASTNPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEETEIMIVQAKGRGRGRKETGTAKPGVSTVPNTTQASTPPQTQTPQPNPPPVQATPHPFPAVTPDLIVQTPVMTVVPPQPLQTPPPVPPQPQPPPAPAPQPVQSHPPIIAATPQPVKTKKGVKRKADTTTPTTIDPIHEPPSLPPEPKTTKLGQ...
CRBN
22Rv1
Dmax
%
99
null
null
null
null
24
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O60885
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_1045
Homo sapiens
10.1016/j.ejmech.2021.113922
Degradation of BRD4 in 22Rv1/VCaP cells after 24 h treatment
PROTAC-DB
null
null
African=0.89%; Native American=0.23%; East Asian, North=0.52%; East Asian, South=0%; South Asian=0.27%; European, North=67.46%; European, South=30.62%. Contains at least 10 integrated copies of xenotropic murine leukemia virus-related virus (XMRV) genome and produces a high titer of the virus. Mutation; HGNC; HGNC Muta...
20
false
490
272
CC[C@@H]1c2nnc(C)n2-c2cnc(Nc3ccc(C(=O)NC4CCN(C(=O)COc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cc3OC)nc2N1CC1CCCCC1
BRD4
MSAESGPGTRLRNLPVMGDGLETSQMSTTQAQAQPQPANAASTNPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEETEIMIVQAKGRGRGRKETGTAKPGVSTVPNTTQASTPPQTQTPQPNPPPVQATPHPFPAVTPDLIVQTPVMTVVPPQPLQTPPPVPPQPQPPPAPAPQPVQSHPPIIAATPQPVKTKKGVKRKADTTTPTTIDPIHEPPSLPPEPKTTKLGQ...
CRBN
VCaP
DC50
nM
1
null
null
null
null
24
<
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O60885
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_2235
Homo sapiens
10.1016/j.ejmech.2021.113922
Degradation of BRD4 in 22Rv1/VCaP cells after 24 h treatment
PROTAC-DB
null
null
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...
20
false
490
272
CC[C@@H]1c2nnc(C)n2-c2cnc(Nc3ccc(C(=O)NC4CCN(C(=O)COc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cc3OC)nc2N1CC1CCCCC1
BRD4
MSAESGPGTRLRNLPVMGDGLETSQMSTTQAQAQPQPANAASTNPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEETEIMIVQAKGRGRGRKETGTAKPGVSTVPNTTQASTPPQTQTPQPNPPPVQATPHPFPAVTPDLIVQTPVMTVVPPQPLQTPPPVPPQPQPPPAPAPQPVQSHPPIIAATPQPVKTKKGVKRKADTTTPTTIDPIHEPPSLPPEPKTTKLGQ...
CRBN
VCaP
Dmax
%
99
null
null
null
null
24
>
null
null
PROteolysis-TArgeting Chimera (PROTAC)
O60885
Q96SW2
MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS...
CVCL_2235
Homo sapiens
10.1016/j.ejmech.2021.113922
Degradation of BRD4 in 22Rv1/VCaP cells after 24 h treatment
PROTAC-DB
null
null
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...
20
false
490
272