BB2-50F [Ligand Id: 13072] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4213248
  • 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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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
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  • coagulation factor II, thrombin/Thrombin in Human [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
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  • plasminogen activator, tissue type/Tissue-type plasminogen activator in Human [ChEMBL: CHEMBL1873] [GtoPdb: 2392] [UniProtKB: P00750]
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  • plasminogen activator, urokinase/Urokinase-type plasminogen activator in Human [ChEMBL: CHEMBL3286] [GtoPdb: 2393] [UniProtKB: P00749]
  • plasminogen activator, urokinase/Urokinase-type plasminogen activator in Mouse [ChEMBL: CHEMBL1075311] [GtoPdb: 2393] [UniProtKB: P06869]
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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 Inhibition of factor 10a (unknown origin) using chromogenic H-D-Ile-L-Pro-L-Arg-p-nitoraniline as substrate by fluorescence assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2018) 61: 8299-8320 [PMID:30130401]
coagulation factor XI/Coagulation factor XI in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2820] [GtoPdb: 2360] [UniProtKB: P03951]
ChEMBL Inhibition of factor 11a (unknown origin) using chromogenic L-pyroGlu-L-Pro-L-Arg-p-nitroaniline as substrate by fluorescence assay B 4.51 pIC50 31000 nM IC50 J Med Chem (2018) 61: 8299-8320 [PMID:30130401]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of recombinant human ERG expressed in CHO cells incubated for 12 mins by whole cell voltage clamp method B 5.52 pIC50 <3000 nM IC50 Bioorg Med Chem (2021) 37: 116116-116116 [PMID:33799173]
kallikrein B1/Plasma kallikrein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2000] [GtoPdb: 2379] [UniProtKB: P03952]
ChEMBL Inhibition of human plasma kallikrein using chromogenic L-pyroGlu-L-Pro-L-Arg-p-nitroaniline as substrate by fluorescence assay B 4.95 pIC50 11300 nM IC50 J Med Chem (2018) 61: 8299-8320 [PMID:30130401]
plasminogen/Plasminogen in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1801] [GtoPdb: 2394] [UniProtKB: P00747]
ChEMBL Inhibition of plasmin (unknown origin) using chromogenic H-D-Ile-L-Pro-L-Arg-p-nitoraniline as substrate by fluorescence assay B 5 pIC50 >10000 nM IC50 J Med Chem (2018) 61: 8299-8320 [PMID:30130401]
Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
ChEMBL Inhibition of recombinant human Nav1.5alpha expressed in HEK293 cells incubated for 10 mins by voltage clamp method B 5.52 pIC50 <3000 nM IC50 Bioorg Med Chem (2021) 37: 116116-116116 [PMID:33799173]
coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
ChEMBL Inhibition of thrombin (unknown origin) using chromogenic H-D-Ile-L-Pro-L-Arg-p-nitoraniline as substrate by fluorescence assay B 5 pIC50 >10000 nM IC50 J Med Chem (2018) 61: 8299-8320 [PMID:30130401]
plasminogen activator, tissue type/Tissue-type plasminogen activator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1873] [GtoPdb: 2392] [UniProtKB: P00750]
ChEMBL Inhibition of tPA (unknown origin) using chromogenic H-D-Ile-L-Pro-L-Arg-p-nitoraniline as substrate by fluorescence assay B 5 pIC50 >10000 nM IC50 J Med Chem (2018) 61: 8299-8320 [PMID:30130401]
plasminogen activator, urokinase/Urokinase-type plasminogen activator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3286] [GtoPdb: 2393] [UniProtKB: P00749]
ChEMBL Inhibition of human kidney uPA using Z-Gly-Gly-Arg-AMC as substrate measured over 15 mins by fluorescence assay B 6.74 pKi 183 nM Ki J Med Chem (2018) 61: 8299-8320 [PMID:30130401]
GtoPdb - - 6.74 pKi 183 nM Ki J Med Chem (2018) 61: 8299-8320 [PMID:30130401]
ChEMBL Inhibition of human kidney uPA using chromogenic H-D-Ile-L-Pro-L-Arg-p-nitoraniline as substrate by fluorescence assay B 6.28 pIC50 530 nM IC50 J Med Chem (2018) 61: 8299-8320 [PMID:30130401]
plasminogen activator, urokinase/Urokinase-type plasminogen activator in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075311] [GtoPdb: 2393] [UniProtKB: P06869]
ChEMBL Inhibition of mouse uPA using Z-Gly-Gly-Arg-AMC as substrate after 15 mins by fluorescence assay B 5.74 pKi 1802 nM Ki J Med Chem (2018) 61: 8299-8320 [PMID:30130401]
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 Inhibition of activated protein C (unknown origin) using chromogenic L-pyroGlu-L-Pro-L-Arg-p-nitroaniline as substrate by fluorescence assay B 4.3 pIC50 >50000 nM IC50 J Med Chem (2018) 61: 8299-8320 [PMID:30130401]

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]