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 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]
