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 34:

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]