tranexamic acid [Ligand Id: 6573] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL877 (Acide tranexamique, Acido tranexamico, Amcha, CL 65336, CL-65336, CL65336, Cyclocapron, Cyclo-f, Cyclokapron, Cyklo-f heavy period relief, Cyklokapron, Espercil, Exacyl, Femstrual, Haematrix, LB-1148, LB1148, Lysteda, Menstralite, NSC-291305, Rikavarin, RP-18429, Tranexamic acid, Trans AMCHA, TRANS AMCHA, TRANS-AMCHA, Transamin)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
plasminogen/Plasminogen in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1801] [GtoPdb: 2394] [UniProtKB: P00747]
ChEMBL Binding affinity to human plasma N-terminal truncated Lys-plasminogen by surface plasmon resonance analysis B 4.44 pKd 36000 nM Kd ACS Med Chem Lett (2014) 5: 538-543 [PMID:24900876]
ChEMBL Binding affinity to human plasma N-terminal truncated Lys-plasminogen K1 domain by surface plasmon resonance analysis B 5.66 pKd 2200 nM Kd ACS Med Chem Lett (2014) 5: 538-543 [PMID:24900876]
ChEMBL Binding affinity to human plasma full length Glu-plasminogen K1 domain by surface plasmon resonance analysis B 5.96 pKd 1100 nM Kd ACS Med Chem Lett (2014) 5: 538-543 [PMID:24900876]
ChEMBL Binding affinity to plasminogen K1 domain (unknown origin) B 5.96 pKd 1100 nM Kd J Med Chem (2020) 63: 1445-1472 [PMID:31658420]
GtoPdb - - 3.6 pIC50 241000 nM IC50 J Thromb Haemost (2007) 5: 2113-8 [PMID:17666018]
ChEMBL Inhibition of human plasmin assessed as inhibition of fibrinolysis in presence of fibrinogen B 4.3 pIC50 50000 nM IC50 Bioorg Med Chem (2016) 24: 545-553 [PMID:26732532]
ChEMBL Binding affinity to human full length Glu-plasminogen in buffer assessed as inhibition of interaction with fibrin preincubated for 15 mins followed by thrombin addition measured every 2 mins for 15 hrs by Spectra-Max reader analysis in presence of tPA B 4.92 pIC50 12000 nM IC50 ACS Med Chem Lett (2014) 5: 538-543 [PMID:24900876]
ChEMBL Inhibition of human Glu-plasminogen/fibrinogen interaction in HEPES buffer assessed as inhibition of lysis of thrombin-induced clot preincubated for 15 mins prior to thrombin addition measured for 15 hrs by clot-lysis buffer assay B 4.94 pIC50 11500 nM IC50 J Med Chem (2013) 56: 3273-3280 [PMID:23521080]
ChEMBL Inhibition of plasminogen/fibrinogen interaction in pooled citreated human platelet-poor plasma assessed as inhibition of lysis of CaCl2/t-PA-induced clot by microtiter plate analysis B 5.51 pIC50 3100 nM IC50 J Med Chem (2013) 56: 3273-3280 [PMID:23521080]
ChEMBL Binding affinity to full length Glu-plasminogen in human plasma assessed as inhibition of interaction with fibrin in presence of tPA B 5.51 pIC50 3100 nM IC50 ACS Med Chem Lett (2014) 5: 538-543 [PMID:24900876]

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]