Dup-714 [Ligand Id: 8760] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL290376 (DuP-714)
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  • plasminogen activator, tissue type/Tissue-type plasminogen activator in Human [ChEMBL: CHEMBL1873] [GtoPdb: 2392] [UniProtKB: P00750]
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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 In vitro for inhibition of plasmin B 8.29 pKi 5.1 nM Ki Bioorg Med Chem Lett (1996) 6: 2913-2918
coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
ChEMBL Binding affinity against Thrombin. B 10.39 pKd 0.04 nM Kd J Med Chem (2000) 43: 305-341 [PMID:10669559]
ChEMBL Inhibition of Coagulation factor II B 10.38 pKi 0.04 nM Ki Bioorg Med Chem Lett (1999) 9: 925-930 [PMID:10230612]
ChEMBL Inhibition constant for binding with thrombin was determined B 10.39 pKi 0.04 nM Ki J Med Chem (1993) 36: 1831-1838 [PMID:8515421]
ChEMBL In vitro for inhibition of thrombin. B 10.39 pKi 0.04 nM Ki Bioorg Med Chem Lett (1996) 6: 2913-2918
GtoPdb Affinity for thrombin active site. - 10.39 pKi 0.04 nM Ki Bioorg Med Chem Lett (1996) 6: 2913–2918
ChEMBL Inhibition of thrombin B 10.4 pKi 0.04 nM Ki Bioorg Med Chem Lett (1997) 7: 1595-1600
ChEMBL Inhibition of compound against thrombin mediated platelet activation and fibrinogen cleavage. B 10.4 pKi 0.04 nM Ki J Med Chem (2000) 43: 305-341 [PMID:10669559]
Thrombin in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4471] [UniProtKB: P00735]
ChEMBL Concentration necessary to double time for clot formation induced by bovine thrombin B 7.26 pKi 55 nM Ki Bioorg Med Chem Lett (1996) 6: 2913-2918
plasminogen activator, tissue type/Tissue-type plasminogen activator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1873] [GtoPdb: 2392] [UniProtKB: P00750]
GtoPdb - - 8.24 pKi 5.7 nM Ki Bioorg Med Chem Lett (1996) 6: 2913–2918
ChEMBL Compound was tested in vitro for inhibition of tissue plasminogen activator B 8.24 pKi 5.7 nM Ki Bioorg Med Chem Lett (1996) 6: 2913-2918
serine protease 1/Trypsin I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL209] [GtoPdb: 2397] [UniProtKB: P07477]
ChEMBL Inhibitory activity against trypsin B 8.05 pKi 9 nM Ki Bioorg Med Chem Lett (1999) 9: 925-930 [PMID:10230612]
ChEMBL Inhibition of trypsin B 10.35 pKi 0.04 nM Ki Bioorg Med Chem Lett (1997) 7: 1595-1600
ChEMBL Binding affinity against Trypsin B 10.35 pKi 0.04 nM Ki J Med Chem (2000) 43: 305-341 [PMID:10669559]
ChEMBL Compound was tested in vitro for inhibition of trypsin B 10.35 pKi 0.04 nM Ki Bioorg Med Chem Lett (1996) 6: 2913-2918

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]