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| ChEMBL ligand: CHEMBL3392741 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ubiquitin specific peptidase 2/Ubiquitin carboxyl-terminal hydrolase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293227] [GtoPdb: 2430] [UniProtKB: O75604] | ||||||||
| GtoPdb | Binding affinity for hUSP2 | - | 5.28 | pKd | 5200 | nM | Kd | Sci Transl Med (2023) 15: eadh7668 [PMID:38055802] |
| ChEMBL | Inhibition of USP2 (267 to 599 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells using ubiquitin-rhodamine-110 as substrate preincubated with compound for 30 mins followed by substrate addition measured after 30 mins by fluorometric assay | B | 5.44 | pIC50 | 3600 | nM | IC50 | Eur J Med Chem (2024) 268: 116275-116275 [PMID:38452725] |
| ChEMBL | Inhibition of human USP2 using Di-Ub IQF as substrate incubated for 15 mins by K63-2 assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | Eur J Med Chem (2020) 191: 112107-112107 [PMID:32092586] |
| ChEMBL | Inhibition of USP2 (unknown origin) using Di-Ub IQF K48-4 as substrate preincubated for 10 mins followed by substrate addition by high-throughput assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | Eur J Med Chem (2024) 268: 116275-116275 [PMID:38452725] |
| GtoPdb | Inhibition of USP2 de-ubiquitinating activity in vitro | - | 5.96 | pIC50 | 1100 | nM | IC50 | Sci Transl Med (2023) 15: eadh7668 [PMID:38055802] |
| ubiquitin specific peptidase 8/Ubiquitin carboxyl-terminal hydrolase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2157854] [GtoPdb: 3209] [UniProtKB: P40818] | ||||||||
| ChEMBL | Inhibition of N-terminal His6 tagged USP8 (734 to 1110 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells using ubiquitin-rhodamine-110 as substrate preincubated with compound for 30 mins followed by substrate addition measured after 30 mins by fluorometric assay | B | 5.33 | pIC50 | 4700 | nM | IC50 | Eur J Med Chem (2024) 268: 116275-116275 [PMID:38452725] |
| ChEMBL | Inhibition of human USP8 using Di-Ub IQF as substrate incubated for 15 mins by K63-2 assay | B | 6.02 | pIC50 | 950 | nM | IC50 | Eur J Med Chem (2020) 191: 112107-112107 [PMID:32092586] |
| ChEMBL | Inhibition of USP8 (unknown origin) using Di-Ub IQF K48-02 as substrate preincubated for 30 mins followed by substrate addition by high-throughput assay | B | 6.02 | pIC50 | 950 | nM | IC50 | Eur J Med Chem (2024) 268: 116275-116275 [PMID:38452725] |
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]