clemizole [Ligand Id: 10285] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1407943 (AL 20 [AS HYDROCHLORIDE], Clemizole, Clemizole hydrochloride, AL-20 FREE BASE, NSC-46261)
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  • TRPC3/Short transient receptor potential channel 3 in Human [ChEMBL: CHEMBL2417348] [GtoPdb: 488] [UniProtKB: Q13507]
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  • TRPC4 in Human [GtoPdb: 489] [UniProtKB: Q9UBN4]
  • TRPC4/Short transient receptor potential channel 4 in Mouse [ChEMBL: CHEMBL1741219] [GtoPdb: 489] [UniProtKB: Q9QUQ5]
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  • TRPC5 in Human [GtoPdb: 490] [UniProtKB: Q9UL62]
  • TRPC5/Short transient receptor potential channel 5 in Mouse [ChEMBL: CHEMBL4523481] [GtoPdb: 490] [UniProtKB: Q9QX29]
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  • TRPC6/Short transient receptor potential channel 6 in Human [ChEMBL: CHEMBL2417347] [GtoPdb: 491] [UniProtKB: Q9Y210]
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  • TRPC7/Short transient receptor potential channel 7 in Mouse [ChEMBL: CHEMBL4523502] [GtoPdb: 492] [UniProtKB: Q9WVC5]
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  • TRPV2/Transient receptor potential cation channel subfamily V member 2 in Rat [ChEMBL: CHEMBL2863] [GtoPdb: 508] [UniProtKB: Q9WUD2]
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  • TRPV4/Transient receptor potential cation channel subfamily V member 4 in Mouse [ChEMBL: CHEMBL6126] [GtoPdb: 510] [UniProtKB: Q9EPK8]
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]