ChEMBL ligand: CHEMBL2440787
TLR4/Toll-like receptor 4 in Human [ChEMBL: CHEMBL5255] [GtoPdb: 1754] [UniProtKB: O00206] There should be some charts here, you may need to enable JavaScript!
RyR2 in Human [GtoPdb: 748] [UniProtKB: Q92736] 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
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 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]