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ChEMBL ligand: CHEMBL877 (Amcha, CL 65336, CL-65336, 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 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]