VU0240551 [Ligand Id: 4665] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1491962 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Basolateral Na-K-Cl symporter/Solute carrier family 12 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1615383] [GtoPdb: 969] [UniProtKB: P55011] | ||||||||
| ChEMBL | Antagonist activity at NKKC1 expressed in human HEK293 cells assessed as [86Rb] uptake after 30 mins by scintillation counting | F | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4532-4535 [PMID:22727639] |
| K-Cl cotransporter 2/Solute carrier family 12 member 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1615384] [GtoPdb: 972] [UniProtKB: Q9H2X9] | ||||||||
| ChEMBL | Antagonist activity at KCC2 expressed in human HEK293 cells assessed as decrease in Tl-stimulated fluorescence increase after 8 mins by fluorescence analysis | F | 6.25 | pIC50 | 568 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4532-4535 [PMID:22727639] |
| GtoPdb | - | - | 6.25 | pIC50 | 560 | nM | IC50 | Proc Natl Acad Sci USA (2009) 106: 5383-8 [PMID:19279215] |
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]
