ChEMBL ligand: CHEMBL3182437
ubiquitin specific peptidase 1/Ubiquitin carboxyl-terminal hydrolase 1 in Human [ChEMBL: CHEMBL1795087] [GtoPdb: 2428] [UniProtKB: O94782] There should be some charts here, you may need to enable JavaScript!
ubiquitin specific peptidase 1/Ubiquitin carboxyl-terminal hydrolase 1/WD repeat-containing protein 48 in Human [ChEMBL: CHEMBL3430885] [GtoPdb: 2428] [UniProtKB: O94782, Q8TAF3] There should be some charts here, you may need to enable JavaScript!
Ubiquitin carboxyl-terminal hydrolase 7 in Human [ChEMBL: CHEMBL2157850] [UniProtKB: Q93009] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
ubiquitin specific peptidase 1/Ubiquitin carboxyl-terminal hydrolase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795087] [GtoPdb: 2428] [UniProtKB: O94782]
ChEMBL	Inhibition of human recombinant USP1 expressed in Escherichia coli BL21 (DE3) cells	B	7.12	pIC50	76	nM	IC50	J Med Chem (2024) 67: 11488-11521 [PMID:38955347]
GtoPdb	-	-	7.12	pIC50	76	nM	IC50	J Med Chem (2014) 57: 8099-110 [PMID:25229643]
ubiquitin specific peptidase 1/Ubiquitin carboxyl-terminal hydrolase 1/WD repeat-containing protein 48 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430885] [GtoPdb: 2428] [UniProtKB: O94782, Q8TAF3]
ChEMBL	Inhibition of USP1/UAF1 complex (unknown origin) by Ub-PCNA substrate assay	B	6.09	pIC50	820	nM	IC50	J Med Chem (2015) 58: 1581-1595 [PMID:25364867]
ChEMBL	Inhibition of USP1/UAF1 complex (unknown origin) assessed as reduction in K63-linked diUb cleavage by gel electrophoresis based orthogonal diUb cleavage assay	B	6.76	pIC50	174	nM	IC50	J Med Chem (2015) 58: 1581-1595 [PMID:25364867]
ChEMBL	Inhibition of human USP1/UAF1 using Ub-AMC substrate by fluorescence assay	B	7.12	pIC50	76	nM	IC50	J Med Chem (2014) 57: 8099-8110 [PMID:25229643]
ChEMBL	Inhibition of USP1/UAF1 complex (unknown origin) by Ub-Rho110 assay	B	7.12	pIC50	76	nM	IC50	J Med Chem (2015) 58: 1581-1595 [PMID:25364867]
ChEMBL	Inhibition Assay: This example demonstrates reversible inhibition of USP1/UAF1 by an embodiment of the invention.The compound (81) at a concentration of ten times its 1050 value was pre-incubated with 10 μM USP1/UAF1 at room temperature for 15 min. This solution was then diluted by 100-fold in assay buffer containing 50 mM HEPES, pH 7.8, 0.1 mg/mL BSA, 0.5 mM EDTA, and 1 mM DTT and incubated at room temperature for an additional 15 min. Next, 20 μM K63-linked diubiquitin was added into the solution and incubated at 37° C. for 10 min. Laemmli sample buffer was added to quench the reaction. The reaction products were then separated on a 20% denaturing SDS-PAGE gel and stained with Coomassie Blue. USP1/UAF1 incubated with DMSO was treated as 100% USP1/UAF1 activity.	B	7.12	pIC50	76	nM	IC50	US-9802904-B2. Inhibitors of the USP1/UAF1 deubiquitinase complex and uses thereof (2017)
GtoPdb	-	-	7.12	pIC50	76	nM	IC50	J Med Chem (2014) 57: 8099-110 [PMID:25229643]
ChEMBL	Inhibition Assay: This example demonstrates reversible inhibition of USP1/UAF1 by an embodiment of the invention.The compound (81) at a concentration of ten times its 1050 value was pre-incubated with 10 μM USP1/UAF1 at room temperature for 15 min. This solution was then diluted by 100-fold in assay buffer containing 50 mM HEPES, pH 7.8, 0.1 mg/mL BSA, 0.5 mM EDTA, and 1 mM DTT and incubated at room temperature for an additional 15 min. Next, 20 μM K63-linked diubiquitin was added into the solution and incubated at 37° C. for 10 min. Laemmli sample buffer was added to quench the reaction. The reaction products were then separated on a 20% denaturing SDS-PAGE gel and stained with Coomassie Blue. USP1/UAF1 incubated with DMSO was treated as 100% USP1/UAF1 activity.	B	7.77	pIC50	17	nM	IC50	US-9802904-B2. Inhibitors of the USP1/UAF1 deubiquitinase complex and uses thereof (2017)
ChEMBL	Inhibition of human USP1/UAF1 in human H1299 cells assessed as reduction in colony formation after 7 days	B	5.52	pEC50	3000	nM	EC50	J Med Chem (2014) 57: 8099-8110 [PMID:25229643]
Ubiquitin carboxyl-terminal hydrolase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2157850] [UniProtKB: Q93009]
ChEMBL	Inhibition of USP7 (unknown origin)	B	7.12	pIC50	76	nM	IC50	Eur J Med Chem (2024) 266: 116161-116161 [PMID:38262120]

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]