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 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]
