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] |
| ChEMBL | Inhibition of human furin expressed in HEK293 cells using pGlu-Arg-Thr-LysArg-AMC as substrate and measured by fluorescence based assay | B | 9.18 | pKi | 0.66 | nM | Ki | J Med Chem (2022) 65: 2747-2784 [PMID:34340303] |
| 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 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]
