pralnacasan [Ligand Id: 6467] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL437526 (HMR3480, HMR-3480, HMR3480/VX-740, Pralnacasan, VX-740)
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
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 32:

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]