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 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]
