pralnacasan [Ligand Id: 6467] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL437526 (HMR-3480, HMR3480, HMR3480/VX-740, Pralnacasan, VX-740) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Caspase 1/Caspase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4801] [GtoPdb: 1617] [UniProtKB: P29466] | ||||||||
| GtoPdb | - | - | 9 | pKi | 1 | nM | Ki | Curr Top Med Chem (2005) 5: 1697-717 [PMID:16375749] |
| ChEMBL | Inhibition of caspase-1 in LPS stimulated human PMBC cells after 2 hrs by ELISA analysis | B | 6.38 | pIC50 | 420 | nM | IC50 | J Med Chem (2016) 59: 1691-1710 [PMID:26422006] |
| ChEMBL | Inhibition of ICE | B | 8.44 | pIC50 | 3.6 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4233-4236 [PMID:16782334] |
| ChEMBL | Inhibition of ICE | B | 8.44 | pIC50 | 3.6 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4728-4732 [PMID:16870441] |
| ChEMBL | Inhibition of caspase-1 using fluorogenic substrate and BMG Fluostar plate reader for 30 min at 37 degree C | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4291-4294 [PMID:16046125] |
| Caspase 3/Caspase-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2334] [GtoPdb: 1619] [UniProtKB: P42574] | ||||||||
| ChEMBL | Inhibition of Caspase 3 | B | 5.89 | pIC50 | 1300 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4728-4732 [PMID:16870441] |
| Caspase 8/Caspase-8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3776] [GtoPdb: 1624] [UniProtKB: Q14790] | ||||||||
| ChEMBL | Inhibition of caspase8 | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4233-4236 [PMID:16782334] |
| ChEMBL | Inhibition of Caspase 8 | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4728-4732 [PMID:16870441] |
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]
