phenylacetyl-Arg-Val-Arg-4-amidinobenzylamide [Ligand Id: 6564] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL566340 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| coagulation factor X/Coagulation factor X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742] | ||||||||
| ChEMBL | Inhibition of factor 10a | B | 4.4 | pKi | 40000 | nM | Ki | J Med Chem (2010) 53: 1067-1075 [PMID:20038105] |
| furin, paired basic amino acid cleaving enzyme/Furin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2611] [GtoPdb: 2366] [UniProtKB: P09958] | ||||||||
| ChEMBL | Inhibition of human furin by fluorescence assay | B | 9.09 | pKi | 0.81 | nM | Ki | J Med Chem (2010) 53: 1067-1075 [PMID:20038105] |
| ChEMBL | Inhibition of recombinant human furin expressed in CHO cells using pyroGlu- Arg-Thr-Lys-Arg-AMC as the substrate after 30 mins | B | 9.09 | pKi | 0.81 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4695-4697 [PMID:21757345] |
| GtoPdb | - | - | 9.1 | pKi | 0.81 | nM | Ki | J Med Chem (2010) 53: 1067-75 [PMID:20038105] |
| plasminogen/Plasminogen in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1801] [GtoPdb: 2394] [UniProtKB: P00747] | ||||||||
| ChEMBL | Inhibition of plasmin | B | 5.22 | pKi | 6000 | nM | Ki | J Med Chem (2010) 53: 1067-1075 [PMID:20038105] |
| proprotein convertase subtilisin/kexin type 1/Prohormone convertase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3182] [GtoPdb: 2382] [UniProtKB: P29120] | ||||||||
| GtoPdb | - | - | 9.12 | pKi | 0.75 | nM | Ki | J Med Chem (2010) 53: 1067-75 [PMID:20038105] |
| ChEMBL | Inhibition of human PC1/3 expressed in Drosophila schneider 2 cells by fluorescence assay | B | 9.12 | pKi | 0.75 | nM | Ki | J Med Chem (2010) 53: 1067-1075 [PMID:20038105] |
| proprotein convertase subtilisin/kexin type 2/Prohormone convertase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2433] [GtoPdb: 2383] [UniProtKB: P16519] | ||||||||
| ChEMBL | Inhibition of human PC2 expressed in Drosophila schneider 2 cells by fluorescence assay | B | 6.51 | pKi | 312 | nM | Ki | J Med Chem (2010) 53: 1067-1075 [PMID:20038105] |
| proprotein convertase subtilisin/kexin type 5/Subtilisin/kexin type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2826] [GtoPdb: 2385] [UniProtKB: Q92824] | ||||||||
| ChEMBL | Inhibition of human PC5/6 expressed in Drosophila schneider 2 cells by fluorescence assay | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (2010) 53: 1067-1075 [PMID:20038105] |
| GtoPdb | - | - | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (2010) 53: 1067-75 [PMID:20038105] |
| proprotein convertase subtilisin/kexin type 6/Subtilisin/kexin type 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2951] [GtoPdb: 2386] [UniProtKB: P29122] | ||||||||
| GtoPdb | - | - | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (2010) 53: 1067-75 [PMID:20038105] |
| ChEMBL | Inhibition of human PACE4 expressed in Drosophila schneider 2 cells by fluorescence assay | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (2010) 53: 1067-1075 [PMID:20038105] |
| proprotein convertase subtilisin/kexin type 7/Subtilisin/kexin type 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2232] [GtoPdb: 2387] [UniProtKB: Q16549] | ||||||||
| ChEMBL | Inhibition of human PC7 expressed in Drosophila schneider 2 cells by fluorescence assay | B | 5.21 | pKi | 6154 | nM | Ki | J Med Chem (2010) 53: 1067-1075 [PMID:20038105] |
| coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734] | ||||||||
| ChEMBL | Inhibition of thrombin | B | 4.64 | pKi | 23000 | nM | Ki | J Med Chem (2010) 53: 1067-1075 [PMID:20038105] |
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]
