dapansutrile [Ligand Id: 10056] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3989943 (Dapansutrile, Dapansutrilo, OLT-1177, OLT1177)
  • NLRP3/NACHT, LRR and PYD domains-containing protein 3 in Mouse [ChEMBL: CHEMBL3779755] [GtoPdb: 1770] [UniProtKB: Q8R4B8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
NLRP3/NACHT, LRR and PYD domains-containing protein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3779755] [GtoPdb: 1770] [UniProtKB: Q8R4B8]
ChEMBL Inhibition of NLRP3 in mouse J774A.1 cells infected with FLA-ST assessed as inhibition of LPS- induced IL-1beta production by ELISA B 7 pIC50 100 nM IC50 Eur J Med Chem (2021) 219: 113417-113417 [PMID:33845232]
ChEMBL Inhibition of NLRP3 inflammasome activation in LPS-primed mouse J774A.1 cells assessed as reduction in IL-1beta level preincubated for 30 mins followed by addition of nigericin and measured after 40 mins by ELISA B 9 pIC50 1 nM IC50 Eur J Med Chem (2020) 185: 111822-111822 [PMID:31699536]
ChEMBL Inhibition of NLRP3 inflammasome activation in LPS-primed mouse J774.A1 cells assessed as reduction in IL-1beta level incubated for 1 hr followed by stimulation for 30 mins in presence of ATP by ELISA method B 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2021) 44: 128101-128101 [PMID:33984476]

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]