emlenoflast [Ligand Id: 12172] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4650350 (Emlenoflast, Inzomelid, Izd-174, Izd174, MCC-7840, MCC7840) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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| NLRP3/NACHT, LRR and PYD domains-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741208] [GtoPdb: 1770] [UniProtKB: Q96P20] | ||||||||
| GtoPdb | Measuring inhibition of IL-1β production by LPS primed, ATP-activated human primary microglial cells | - | 6.85 | pIC50 | 142 | nM | IC50 | WO2021089781A1. Treatment or prevention of psychiatric brain disorders using the nlrp3 inhibitor n-((1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-1 -isopropyl-1 h-pyrazole-3-sulfonamide (2021) |
| ChEMBL | Inhibition of NLRP3 inflammasome activation in LPS-activated human THP-1 cells assessed as inhibition of nigericin induced IL-1beta secretion preincubated with LPS for 3 hrs followed by compound addition for 40 mins and further stimulated with nigericin for 40 mins by ELISA method | B | 7.4 | pIC50 | 39.5 | nM | IC50 | J Med Chem (2024) 67: 7516-7538 [PMID:38686671] |
| 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 BMDMs assessed as reduction in LPS/ATP-induced IL-1beta release preincubated for 30 mins in presence of LPS followed by ATP addition and measured after 1 hr by ELISA | B | 7.8 | pIC50 | 16 | nM | IC50 | Eur J Med Chem (2023) 260: 115750-115750 [PMID:37639823] |
| ChEMBL | Inhibition of NLRP3 inflammasome activation in LPS/ATP-induced C57BL/6 mouse BMDMs assessed as reduction in IL-1beta secretion preincubated with LPS for 4 hrs followed by compound addition for 30 mins and further stimulated with ATP for 30 mins by ELISA | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2024) 67: 9406-9430 [PMID:38751194] |
ChEMBL data shown on this page come from version 36:
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]
