inhibitor 1 [Colombo et al., 2012] [Ligand Id: 8624] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2086421 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ST14 transmembrane serine protease matriptase /Matriptase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3018] [GtoPdb: 2418] [UniProtKB: Q9Y5Y6] | ||||||||
| ChEMBL | Tight binding inhibition of human matriptase expressed in Drosophila melanogaster S2 cells using Boc-QAR-AMC as substrate incubated for 15 mins prior to substrate addition measured for 30 mins by fluorimetric analysis | B | 10.96 | pKi | 0.01 | nM | Ki | ACS Med Chem Lett (2012) 3: 530-534 [PMID:24900505] |
| GtoPdb | - | - | 10.96 | pKi | 0.01 | nM | Ki | ACS Med Chem Lett (2012) 3: 530-4 [PMID:24900505] |
| Serine protease hepsin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2079849] [UniProtKB: P05981] | ||||||||
| ChEMBL | Tight binding inhibition of human hepsin expressed in Drosophila melanogaster S2 cells using Boc-QAR-AMC as substrate incubated for 15 mins prior to substrate addition measured for 30 mins by fluorimetric analysis | B | 8.96 | pKi | 1.1 | nM | Ki | ACS Med Chem Lett (2012) 3: 530-534 [PMID:24900505] |
| coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734] | ||||||||
| ChEMBL | Mixed inhibition of human thrombin expressed in Drosophila melanogaster S2 cells using Boc-QAR-AMC as substrate by fluorimetric analysis | B | 6.2 | pKi | 637 | nM | Ki | ACS Med Chem Lett (2012) 3: 530-534 [PMID:24900505] |
| transmembrane serine protease 11D/Transmembrane protease serine 11D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795138] [GtoPdb: 2420] [UniProtKB: O60235] | ||||||||
| ChEMBL | Tight binding inhibition of human TMPRSS11D expressed in Drosophila melanogaster S2 cells using Boc-QAR-AMC as substrate incubated for 15 mins prior to substrate addition measured for 30 mins by fluorimetric analysis | B | 8.08 | pKi | 8.4 | nM | Ki | ACS Med Chem Lett (2012) 3: 530-534 [PMID:24900505] |
| GtoPdb | - | - | 8.08 | pKi | 8.4 | nM | Ki | ACS Med Chem Lett (2012) 3: 530-4 [PMID:24900505] |
| transmembrane serine protease 6/Transmembrane protease serine 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795139] [GtoPdb: 2422] [UniProtKB: Q8IU80] | ||||||||
| GtoPdb | - | - | 8.48 | pKi | 3.3 | nM | Ki | ACS Med Chem Lett (2012) 3: 530-4 [PMID:24900505] |
| ChEMBL | Tight binding inhibition of human matriptase2 expressed in Drosophila melanogaster S2 cells using Boc-QAR-AMC as substrate incubated for 15 mins prior to substrate addition measured for 30 mins by fluorimetric analysis | B | 8.48 | pKi | 3.3 | nM | Ki | ACS Med Chem Lett (2012) 3: 530-534 [PMID:24900505] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
