Target Information
| Target General Information | Top | |||||
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| Target ID |
T39078
(Former ID: TTDS00145)
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| Target Name |
Calcium-activated potassium channel (KCN)
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| Synonyms |
Ca-activated K channel
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| Gene Name |
NO-GeName
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Acute pain [ICD-11: MG31] | |||||
| 2 | Neurological toxicity disorder [ICD-11: 8D43] | |||||
| Function |
Forms a voltage-independent potassium channel that is activated by intracellular calcium. activation is followed by membrane hyperpolarization which promotes calcium influx. The channel is blocked by clotrimazole and charybdotoxin.
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| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Chlorzoxazone | Drug Info | Approved | Acute pain | [4], [5], [6] | |
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | ICA-17043 | Drug Info | Phase 2 | Alzheimer disease | [7] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Activator | [+] 1 Activator drugs | + | ||||
| 1 | Chlorzoxazone | Drug Info | [1] | |||
| Inhibitor | [+] 19 Inhibitor drugs | + | ||||
| 1 | ICA-17043 | Drug Info | [8] | |||
| 2 | (2-fluorophenyl)-(4-fluorophenyl)phenylacetamide | Drug Info | [8] | |||
| 3 | 1-((2-chlorophenyl)diphenylmethyl)-1H-pyrazole | Drug Info | [9] | |||
| 4 | 2,2,2-tris-(3-fluorophenyl)-acetamide | Drug Info | [8] | |||
| 5 | 2,2,2-tris-(4-fluorophenyl)-acetamide | Drug Info | [8] | |||
| 6 | 2,2-bis-(3-fluorophenyl)-2-phenylacetamide | Drug Info | [8] | |||
| 7 | 2-(2,4-difluorophenyl)-2,2-diphenylacetamide | Drug Info | [8] | |||
| 8 | 2-(2-chlorophenyl)-2,2-diphenylethanamide | Drug Info | [8] | |||
| 9 | 2-fluorophenyl-2,2-diphenylacetamide | Drug Info | [8] | |||
| 10 | 2-trityl-4,5-dihydrooxazole | Drug Info | [8] | |||
| 11 | 4-(4-phenoxybutoxy)-7H-furo[3,2-g]chromen-7-one | Drug Info | [9] | |||
| 12 | 4-fluorophenyl-2,2-diphenylacetamide | Drug Info | [8] | |||
| 13 | 5-tosyl-5H-dibenzo[b,d]azepin-7(6H)-one | Drug Info | [9] | |||
| 14 | Bis(4-fluorophenyl)-2-fluorophenylacetamide | Drug Info | [8] | |||
| 15 | N,N-dimethyl-2,2,2-triphenylacetamide | Drug Info | [8] | |||
| 16 | N-ethyl-2,2,2-triphenylacetamide | Drug Info | [8] | |||
| 17 | N-methyl-2,2,2-triphenylacetamide | Drug Info | [8] | |||
| 18 | Triphenylacetic acid methyl ester | Drug Info | [8] | |||
| 19 | TRIPHENYLMETHANAMINE | Drug Info | [8] | |||
| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| Target QSAR Model | ||||||
| References | Top | |||||
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| REF 1 | Chlorzoxazone inhibits contraction of rat thoracic aorta. Eur J Pharmacol. 2006 Sep 18;545(2-3):161-6. | |||||
| REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2328). | |||||
| REF 3 | Reversible inhibition of the platelet procoagulant response through manipulation of the Gardos channel. Blood. 2006 Oct 1;108(7):2223-8. | |||||
| REF 4 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2322). | |||||
| REF 5 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 6 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040113. | |||||
| REF 7 | Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357. | |||||
| REF 8 | Novel inhibitors of the Gardos channel for the treatment of sickle cell disease. J Med Chem. 2008 Feb 28;51(4):976-82. | |||||
| REF 9 | Inhibitors of potassium channels KV1.3 and IK-1 as immunosuppressants. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2299-304. | |||||
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