cromakalim [Ligand Id: 2413] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL49035 (BRL 34915, BRL-34915, BRL34915, Cromakalim) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Mitochondrial complex V; ATP synthase in Bovine (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL612444] [UniProtKB: P00829, P05630, P05631, P05632] | ||||||||
| ChEMBL | Inhibitory concentration towards rat mitochondrial F1F0 ATP hydrolase using a pyruvate kinase / lactate dehydrogenase system | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2004) 47: 1081-1084 [PMID:14971888] |
| ABCC9/Sulfonylurea receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1971] [GtoPdb: 2746] [UniProtKB: O60706] | ||||||||
| ChEMBL | Channel opening activity at SUR2B/Kir6.2 potassium ATP channel in human TE671 cells assessed as isometric force by FLIPR | B | 5.9 | pEC50 | 1250 | nM | EC50 | Bioorg Med Chem (2009) 17: 855-866 [PMID:19101153] |
| ABCC9/ATP-binding cassette, sub-family C (CFTR/MRP), member 8/Kir6.2/Kir6.1/Sulfonylurea receptors; K-ATP channels in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2095152] [GtoPdb: 2746, 2594, 442, 441] [UniProtKB: O60706, Q09428, Q14654, Q15842] | ||||||||
| ChEMBL | IC50 evaluated by measuring contraction and relaxation of guinea pig bladder strips with KCl and glibenclamide respectively | F | 6.24 | pIC50 | 570 | nM | IC50 | J Med Chem (1996) 39: 4592-4601 [PMID:8917648] |
| ChEMBL | Contraction and relaxation of guinea pig portal vein with KCl and glibenclamide respectively | F | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (1996) 39: 4592-4601 [PMID:8917648] |
| ChEMBL | PEC50 for functional potassium channel opening activity in isolated bladder strips | F | 6.34 | pEC50 | 457.09 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 1481-1484 [PMID:12031324] |
| ChEMBL | Potent effective concentration was evaluated for KATP channel opening activity in pig bladder strips | F | 6.34 | pEC50 | 457.09 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1741-1744 [PMID:12729655] |
| ChEMBL | Potassium channel opening activity determined in cultured guinea pig urinary bladder cells | F | 6.37 | pEC50 | 425 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 1481-1484 [PMID:12031324] |
| Kv1.7 in Mouse [GtoPdb: 544] [UniProtKB: Q17ST2] | ||||||||
| GtoPdb | - | - | 3.3 | pIC50 | - | - | - | J Biol Chem (1998) 273: 5851-7 [PMID:9488722] |
| Kv3.1 in Mouse [GtoPdb: 548] [UniProtKB: P15388] | ||||||||
| GtoPdb | - | - | 3.6 | pIC50 | - | - | - | Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498] |
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]
