VU591 [Ligand Id: 7696] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2146753 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kir1.1/ATP-sensitive inward rectifier potassium channel 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293292] [GtoPdb: 429] [UniProtKB: P48048] | ||||||||
| ChEMBL | Inhibition of human ROMK1 expressed in HEK293 cells after 20 mins by Thallos-AM dye based fluorescence assay | B | 6.1 | pIC50 | 794.33 | nM | IC50 | ACS Med Chem Lett (2018) 9: 125-130 [PMID:29456800] |
| ChEMBL | Inhibition of human ROMK1 expressed in HEK293 cells after 20 mins by Thallos-AM dye based fluorescence assay | B | 6.13 | pIC50 | 744 | nM | IC50 | ACS Med Chem Lett (2018) 9: 125-130 [PMID:29456800] |
| ChEMBL | Inhibition of ROMK S44D mutant expressed in HEK293 cells assessed as inhibition of thallium efflux incubated for 20 mins prior to thallium addition measured after 7 to 12 secs by fluorescence assay | B | 6.62 | pIC50 | 240 | nM | IC50 | ACS Med Chem Lett (2012) 3: 367-372 [PMID:24900480] |
| Kir1.1/ATP-sensitive inward rectifier potassium channel 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2146350] [GtoPdb: 429] [UniProtKB: P35560] | ||||||||
| GtoPdb | - | - | 6.6 | pKi | 240 | nM | Ki | Mol Pharmacol (2011) 79: 42-50 [PMID:20926757] |
| ChEMBL | Inhibition of rat ROMK1 expressed in HEK293 cells after 20 mins by Thallos-AM dye based fluorescence assay | B | 6.38 | pIC50 | 420 | nM | IC50 | ACS Med Chem Lett (2018) 9: 125-130 [PMID:29456800] |
| ChEMBL | Inhibition of rat ROMK1 expressed in HEK293 cells after 20 mins by Thallos-AM dye based fluorescence assay | B | 6.4 | pIC50 | 398.11 | nM | IC50 | ACS Med Chem Lett (2018) 9: 125-130 [PMID:29456800] |
| ChEMBL | Inhibition of rat ROMK1 expressed in HEK293 cells by Tl+ flux assay | B | 6.62 | pIC50 | 240 | nM | IC50 | J Med Chem (2019) 62: 8682-8694 [PMID:31034224] |
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]
