Target Information
| Target General Information | Top | |||||
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| Target ID |
T86192
(Former ID: TTDI01791)
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| Target Name |
Voltage-gated potassium channel Kv7 (KCNQ)
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| Synonyms |
Voltage-gated potassium channel subunit Kv7; Potassium voltage-gated channel subfamily KQT; Kv7; KVLQT; KQT-like; IKs producing slow voltage-gated potassium channel subunit alpha KvLQT; IKs producing slow voltage-gated potassium channel alpha subunit KvLQT
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| Gene Name |
NO-GeName
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Behcet disease [ICD-11: 4A62] | |||||
| BioChemical Class |
Voltage-gated ion channel
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| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Retigabine | Drug Info | Approved | Behcet disease | [2] | |
| Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
| 1 | CNSB-001 | Drug Info | Phase 2 | Neuropathic pain | [3] | |
| 2 | Flupirtine | Drug Info | Phase 2 | Fibromyalgia | [4], [5] | |
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | DMP-543 | Drug Info | Discontinued in Phase 2 | Parkinson disease | [6] | |
| Mode of Action | [+] 3 Modes of Action | + | ||||
| Activator | [+] 1 Activator drugs | + | ||||
| 1 | Retigabine | Drug Info | [7] | |||
| Agonist | [+] 1 Agonist drugs | + | ||||
| 1 | CNSB-001 | Drug Info | [1] | |||
| Modulator | [+] 2 Modulator drugs | + | ||||
| 1 | Flupirtine | Drug Info | [8] | |||
| 2 | DMP-543 | Drug Info | [9] | |||
| 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 | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 6 KEGG Pathways | + | ||||
| 1 | Adrenergic signaling in cardiomyocytes | |||||
| 2 | Cholinergic synapse | |||||
| 3 | Gastric acid secretion | |||||
| 4 | Pancreatic secretion | |||||
| 5 | Protein digestion and absorption | |||||
| 6 | Vibrio cholerae infection | |||||
| References | Top | |||||
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| REF 1 | The Kv7 potassium channel activator flupirtine affects clinical excitability parameters of myelinated axons in isolated rat sural nerve. J Peripher Nerv Syst. 2010 Mar;15(1):63-72. | |||||
| REF 2 | Clinical pipeline report, company report or official report of GlaxoSmithKline. | |||||
| REF 3 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029018) | |||||
| 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: 2598). | |||||
| REF 5 | ClinicalTrials.gov (NCT00623415) Flupirtine as Oral Treatment in Multiple Sclerosis. U.S. National Institutes of Health. | |||||
| REF 6 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009278) | |||||
| REF 7 | Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357. | |||||
| REF 8 | Treatment with the Kv7 potassium channel activator flupirtine is beneficial in two independent mouse models of pulmonary hypertension. Br J Pharmacol. 2009 August; 157(7): 1241-1249. | |||||
| REF 9 | KV7 channels regulate muscle tone and nonadrenergic noncholinergic relaxation of the rat gastric fundus.Pharmacol Res.2011 Oct;64(4):397-409. | |||||
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