TMinh-23 [Ligand Id: 13561] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4074929 |
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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 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 | 7.08 | pIC50 | 83 | nM | IC50 | J Med Chem (2017) 60: 4626-4635 [PMID:28493701] |
| GtoPdb | - | - | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2017) 60: 4626-4635 [PMID:28493701] |
| 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 | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2017) 60: 4626-4635 [PMID:28493701] |
| ChEMBL | Inhibition of ANO1 channel (unknown origin) | B | 7.52 | pIC50 | 30 | nM | IC50 | Eur J Med Chem (2020) 208: 112688-112688 [PMID:32906067] |
| ChEMBL | Inhibition of YFP tagged ANO1 (unknown origin) expressed in FRT cells incubated for 24 hrs by fluorescence plate reader assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Eur J Med Chem (2022) 237: 114413-114413 [PMID:35512566] |
| CaCC/Anoctamin-1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105874] [GtoPdb: 708] [UniProtKB: Q8BHY3] | ||||||||
| ChEMBL | Inhibition of GFP-fused mouse ANO1 channel expressed in HEK293A cells assessed as inhibition of ATP-induced channel current amplitude at membrane potential of +80 mV by patch clamp electrophysiology assay | B | 7.3 | pIC50 | 50 | nM | IC50 | Eur J Med Chem (2020) 208: 112688-112688 [PMID:32906067] |
| 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 | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2017) 60: 4626-4635 [PMID:28493701] |
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]
