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ChEMBL ligand: CHEMBL2440787 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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TLR4/Toll-like receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5255] [GtoPdb: 1754] [UniProtKB: O00206] | ||||||||
ChEMBL | Antagonist activity at human TLR4 expressed in HEK blue cells coexpressing MD-2/CD14 assessed as inhibition of LPS-induced NF-kappaB activation-mediated SEAP production after 24 hrs | B | 4.49 | pIC50 | 32550 | nM | IC50 | Eur J Med Chem (2018) 154: 253-266 [PMID:29807331] |
RyR2 in Human [GtoPdb: 748] [UniProtKB: Q92736] | ||||||||
GtoPdb | Inhibition of R4496C mutant RyR2 (expressed in HEK293 cells)-mediated store-overload induced calcium release after 8 to 10 mins using a fura-2/AM dye-based fluorescence assay. | - | 4.77 | pIC50 | 16800 | nM | IC50 | J Med Chem (2013) 56: 8626-55 [PMID:24124794] |
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]