clemizole [Ligand Id: 10285] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1407943 (AL 20 [AS HYDROCHLORIDE], AL-20 FREE BASE, Clemizole, Clemizole hydrochloride, NSC-46261) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Heat sensitive channel TRPV3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879847] [UniProtKB: Q4QYD9] | ||||||||
| ChEMBL | Inhibition of YFP-tagged rat TRPV3 expressed in HEK293 cells assessed as reduction in calcium level by fluo-4 dye based fluorescence assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2019) 62: 7589-7602 [PMID:30943030] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Potassium Channel Assay: Drugs belonging to different classes have been shown to be associated with QT prolongation and in some cases serious ventricular arrhythmias. The most common mechanism for these adverse events is the inhibition of one or more cardiac potassium channels, in particular hERG. This current is important for cardiac myocyte repolarization and is a common target for drugs that prolong the QT interval. Test articles in this study were therefore characterized to determine their ability to inhibit the hERG channel. Ion channel activity was measured using a stably transfected Chinese Hamster Ovary (CHO) cell line expressing the hERG mRNA. The pharmacology of this cloned channel expressed in the CHO cell line is very similar to that observed in native tissue. | B | 6 | pIC50 | <1000 | nM | IC50 | US-8975247-B2. Methods and compositions of treating a flaviviridae family viral infection (2015) |
| TRPC3/Short transient receptor potential channel 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2417348] [GtoPdb: 488] [UniProtKB: Q13507] | ||||||||
| GtoPdb | - | - | 5.04 | pIC50 | 9100 | nM | IC50 | Mol Pharmacol (2014) 86: 514-21 [PMID:25140002] |
| ChEMBL | Inhibition of YFP-tagged human TRPC3 expressed in thapsigargin treated HEK293 cells assessed as reduction in amix-induced calcium level by fluo-4 dye based fluorescence assay | B | 5.04 | pIC50 | 9100 | nM | IC50 | J Med Chem (2019) 62: 7589-7602 [PMID:30943030] |
| TRPC4 in Human [GtoPdb: 489] [UniProtKB: Q9UBN4] | ||||||||
| GtoPdb | - | - | 5.19 | pIC50 | 6400 | nM | IC50 | Mol Pharmacol (2014) 86: 514-21 [PMID:25140002] |
| TRPC4/Short transient receptor potential channel 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741219] [GtoPdb: 489] [UniProtKB: Q9QUQ5] | ||||||||
| ChEMBL | Inhibition of YFP-tagged mouse TRPC4 beta expressed in thapsigargin treated HEK293 cells co-expressing M3 receptor assessed as reduction in carbachol-induced calcium level by fluo-4 dye based fluorescence assay | B | 5.19 | pIC50 | 6400 | nM | IC50 | J Med Chem (2019) 62: 7589-7602 [PMID:30943030] |
| TRPC5 in Human [GtoPdb: 490] [UniProtKB: Q9UL62] | ||||||||
| GtoPdb | - | - | 5.96 | pIC50 | 1100 | nM | IC50 | Mol Pharmacol (2014) 86: 514-21 [PMID:25140002] |
| TRPC5/Short transient receptor potential channel 5 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523481] [GtoPdb: 490] [UniProtKB: Q9QX29] | ||||||||
| ChEMBL | Inhibition of mouse TRPC5 expressed in thapsigargin treated HEK293/TREx cells assessed as reduction in intracellular calcium level in presence of GPCR agonist by fluorescence method | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Med Chem (2019) 62: 7589-7602 [PMID:30943030] |
| TRPC6/Short transient receptor potential channel 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2417347] [GtoPdb: 491] [UniProtKB: Q9Y210] | ||||||||
| ChEMBL | Inhibition of YFP-tagged human TRPC6 expressed in thapsigargin treated HEK293 cells assessed as reduction in amix-induced calcium level by fluo-4 dye based fluorescence assay | B | 4.95 | pIC50 | 11300 | nM | IC50 | J Med Chem (2019) 62: 7589-7602 [PMID:30943030] |
| GtoPdb | - | - | 5.89 | pIC50 | - | - | - | Mol Pharmacol (2014) 86: 514-21 [PMID:25140002] |
| TRPC7/Short transient receptor potential channel 7 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523502] [GtoPdb: 492] [UniProtKB: Q9WVC5] | ||||||||
| ChEMBL | Inhibition of YFP-tagged mouse TRPC7 expressed in thapsigargin treated HEK293 cells assessed as reduction in amix-induced calcium level by fluo-4 dye based fluorescence assay | B | 4.58 | pIC50 | 26500 | nM | IC50 | J Med Chem (2019) 62: 7589-7602 [PMID:30943030] |
| TRPV2/Transient receptor potential cation channel subfamily V member 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2863] [GtoPdb: 508] [UniProtKB: Q9WUD2] | ||||||||
| ChEMBL | Inhibition of YFP-tagged rat TRPV2 expressed in HEK293 cells assessed as reduction in calcium level by fluo-4 dye based fluorescence assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2019) 62: 7589-7602 [PMID:30943030] |
| TRPV4/Transient receptor potential cation channel subfamily V member 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6126] [GtoPdb: 510] [UniProtKB: Q9EPK8] | ||||||||
| ChEMBL | Inhibition of YFP-tagged mouse TRPV4 expressed in HEK293 cells assessed as reduction in calcium level by fluo-4 dye based fluorescence assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2019) 62: 7589-7602 [PMID:30943030] |
| TRPV1/Vanilloid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433] | ||||||||
| ChEMBL | Inhibition of CFP-tagged rat TRPV1 expressed in HEK293 cells assessed as reduction in calcium level by fluo-4 dye based fluorescence assay | B | 4.7 | pIC50 | >20000 | nM | IC50 | J Med Chem (2019) 62: 7589-7602 [PMID:30943030] |
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]
