compound 6 [PMID: 29579323] [Ligand Id: 10039] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1408302
  • TRPM4/Transient receptor potential cation channel subfamily M member 4 in Human [ChEMBL: CHEMBL1628469] [GtoPdb: 496] [UniProtKB: Q8TD43]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
TRPM4/Transient receptor potential cation channel subfamily M member 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1628469] [GtoPdb: 496] [UniProtKB: Q8TD43]
ChEMBL Inhibition of Flag-tagged TRPM4 (unknown origin) expressed in HEK293 cells assessed as reduction in intracellular Na+ influx after 45 mins by ANG2 dye-based fluorescence assay B 6.4 pIC50 400 nM IC50 Eur J Med Chem (2019) 166: 167-177 [PMID:30708257]
GtoPdb - - 6.4 pIC50 400 nM IC50 Cancers (Basel) (2021) 13: [PMID:34771564]
GtoPdb In a fluorescence cell‐based screening assay that monitors Na+ influx using the intracellular Na+ specific dye Asante natrium green‐II. - 6.4 pIC50 400 nM IC50 Br J Pharmacol (2018) 175: 2504-2519 [PMID:29579323]

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]