CY-09 [Ligand Id: 10057] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL488823 |
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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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741208] [GtoPdb: 1770] [UniProtKB: Q96P20] | ||||||||
| GtoPdb | MST assay for the affinity between CY-09 and purified GFP-NLRP3 protein. | - | 6.3 | pKd | 500 | nM | Kd | J Exp Med (2017) 214: 3219-3238 [PMID:29021150] |
| ChEMBL | Inhibition of NLRP3 inflammasome (unknown origin) activation in LPS-primed bone marrow derived macrophage cells assessed as effect on IL-1beta production in presence of nigericin by ELISA | B | 5.62 | pIC50 | 2400 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127021-127021 [PMID:32057583] |
| 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 inflammasome activation in LPS/nigericin-treated mouse BMDM cells assessed as inhibition of LPS and nigericin-induced IL-1beta production pre-treated for 1 hr measured after 1 hr of stimulation by ELISA | B | 6 | pIC50 | 1000 | nM | IC50 | Eur J Med Chem (2021) 219: 113417-113417 [PMID:33845232] |
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]
