compound 37 [PMID: 24418773] [Ligand Id: 8612] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3115901
  • coagulation factor X/Coagulation factor X in Human [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742]
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  • coagulation factor XI/Coagulation factor XI in Human [ChEMBL: CHEMBL2820] [GtoPdb: 2360] [UniProtKB: P03951]
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  • coagulation factor II, thrombin/Thrombin in Human [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
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  • protein C, inactivator of coagulation factors Va and VIIIa/Vitamin K-dependent protein C in Human [ChEMBL: CHEMBL4444] [GtoPdb: 2396] [UniProtKB: P04070]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
coagulation factor X/Coagulation factor X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742]
ChEMBL Competitive inhibition of human coagulation factor 10a using S-2765 as substrate B 4.82 pKi >15000 nM Ki Bioorg Med Chem Lett (2014) 24: 821-827 [PMID:24418773]
ChEMBL Inhibition of human coagulation factor 10a using S-2765 as substrate preincubated for 300 seconds followed by substrate addition measured after 40 mins by spectrophotometric analysis B 4.36 pIC50 >44000 nM IC50 Bioorg Med Chem Lett (2014) 24: 821-827 [PMID:24418773]
coagulation factor XI/Coagulation factor XI in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2820] [GtoPdb: 2360] [UniProtKB: P03951]
ChEMBL Competitive inhibition of human coagulation factor 11a using S-2366 as substrate B 6.52 pKi 300 nM Ki Bioorg Med Chem Lett (2014) 24: 821-827 [PMID:24418773]
ChEMBL Inhibition of human coagulation factor 11a using S-2366 as substrate preincubated for 300 seconds followed by substrate addition measured after 40 mins by spectrophotometric analysis B 6.24 pIC50 580 nM IC50 Bioorg Med Chem Lett (2014) 24: 821-827 [PMID:24418773]
coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
ChEMBL Competitive inhibition of human thrombin using S-2366 as substrate B 6.3 pKi 500 nM Ki Bioorg Med Chem Lett (2014) 24: 821-827 [PMID:24418773]
ChEMBL Inhibition of human thrombin using S-2366 as substrate preincubated for 300 seconds followed by substrate addition measured after 40 mins by spectrophotometric analysis B 6.05 pIC50 900 nM IC50 Bioorg Med Chem Lett (2014) 24: 821-827 [PMID:24418773]
protein C, inactivator of coagulation factors Va and VIIIa/Vitamin K-dependent protein C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4444] [GtoPdb: 2396] [UniProtKB: P04070]
ChEMBL Competitive inhibition of human APC using S-2366 as substrate B 7.4 pKi 40 nM Ki Bioorg Med Chem Lett (2014) 24: 821-827 [PMID:24418773]
GtoPdb - - 7.4 pKi 40 nM Ki Bioorg Med Chem Lett (2014) 24: 821-7 [PMID:24418773]
ChEMBL Inhibition of human APC using S-2366 as substrate preincubated for 300 seconds followed by substrate addition measured after 40 mins by spectrophotometric analysis B 6.89 pIC50 130 nM IC50 Bioorg Med Chem Lett (2014) 24: 821-827 [PMID:24418773]

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]