compound 4 [PMID: 18163548] [Ligand Id: 6545] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL252937 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Anionic trypsin-1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3638328] [UniProtKB: P00762] | ||||||||
| ChEMBL | Enzyme Assay: Inhibition constant of the compound against Trypsin | B | 7.66 | pKi | 22 | nM | Ki | US-8476306-B2. Urokinase inhibitors, production and use thereof (2013) |
| plasminogen/Plasminogen in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3204] [GtoPdb: 2394] [UniProtKB: Q01177] | ||||||||
| ChEMBL | Enzyme Assay: Inhibition constant of the compound against Plasmin | B | 6.12 | pKi | 750 | nM | Ki | US-8476306-B2. Urokinase inhibitors, production and use thereof (2013) |
| coagulation factor II, thrombin/Thrombin in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3078] [GtoPdb: 2362] [UniProtKB: P18292] | ||||||||
| ChEMBL | Enzyme Assay: Inhibition constant of the compound against Thrombin | B | 4.85 | pKi | 14000 | nM | Ki | US-8476306-B2. Urokinase inhibitors, production and use thereof (2013) |
| transmembrane serine protease 11D/Transmembrane protease serine 11D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795138] [GtoPdb: 2420] [UniProtKB: O60235] | ||||||||
| ChEMBL | Inhibition of human recombinant airway trypsin-like protease HAT using D-cyclohexylalanine-Pro-Arg-AMC as substrate by fluorescence plate reader analysis | B | 7.11 | pKi | 78 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4860-4864 [PMID:21741839] |
| Urokinase plasminogen activator surface receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3638329] [UniProtKB: P49616] | ||||||||
| ChEMBL | Enzyme Assay: Inhibition constant of the compound against Plasminogen activator urokinase | B | 7.6 | pKi | 25 | nM | Ki | US-8476306-B2. Urokinase inhibitors, production and use thereof (2013) |
| plasminogen activator, urokinase/Urokinase-type plasminogen activator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3286] [GtoPdb: 2393] [UniProtKB: P00749] | ||||||||
| ChEMBL | Inhibition of human uPA | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2015) 58: 9238-9257 [PMID:26575094] |
| ChEMBL | Inhibition of uPA | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2008) 51: 183-186 [PMID:18163548] |
| GtoPdb | - | - | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2008) 51: 183-6 [PMID:18163548] |
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]
