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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 |
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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]