MONNA [Ligand Id: 12258] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4086165
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CaCC/Anoctamin-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2046267] [GtoPdb: 708] [UniProtKB: Q5XXA6]
ChEMBL Inhibition of human TMEM16A expressed in FRT cells assessed as reduction of ATP-induced in chloride conductance preincubated for 5 mins followed by ATP addition by short-circuit current assay B 5.8 pIC50 1600 nM IC50 J Med Chem (2017) 60: 4626-4635 [PMID:28493701]
ChEMBL Inhibition of TMEM16A (unknown origin) expressed in Xenopus laevis oocytes at -60 mV holding potential by voltage-clamp assay B 7.1 pIC50 80 nM IC50 J Med Chem (2017) 60: 4626-4635 [PMID:28493701]
GtoPdb Inhibition of TMEM16A current in Xenopus laevis oocytes by voltage-clamp assay. - 7.1 pIC50 80 nM IC50 J Med Chem (2017) 60: 4626-4635 [PMID:28493701]
Anoctamin-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105767] [UniProtKB: Q9NQ90]
ChEMBL Inhibition of human TMEM16B expressed in FRT cells co-expressing iodide sensitive fluorescent protein YFP-H148Q/I152L/F46L assessed as reduction in ATP-induced Ca2+ activation-mediated chloride current by measuring decrease in iodide influx preincubated for 10 mins followed by ATP/iodide addition by fluorescence assay B 4.89 pIC50 13000 nM IC50 J Med Chem (2017) 60: 4626-4635 [PMID:28493701]

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]