General Information of Drug Therapeutic Target (DTT) (ID: TT1VOHK)

DTT Name Potassium channel unspecific (KC)
Gene Name KC
DTT Type
Successful target
[1]
UniProt ID
NOUNIPROTAC
TTD ID
T67952

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
10 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amifampridine DMK08L3 LambertEaton myasthenic syndrome 8C62 Approved [2]
Amiodarone DMUTEX3 Tachyarrhythmias BC71 Approved [1]
Dalfampridine DMM0PDO Multiple sclerosis 8A40 Approved [3]
Diazoxide DML1538 Congenital hyperinsulinism 5A4Y Approved [1]
Dofetilide DMPN1TW Sinus rhythm disorder BC9Y Approved [1]
Dronedarone DMA8FS5 Angina pectoris BA40 Approved [4]
Ibutilide DMKXY2R Atrial fibrillation BC81.3 Approved [1]
Minoxidil DMA2Z4F Alopecia ED70 Approved [1]
Nateglinide DMLK2QH Diabetic complication 5A2Y Approved [1]
Pinacidil DMRADYL High blood pressure BA00 Approved [1]
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⏷ Show the Full List of 10 Approved Drug(s)
16 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Andolast DMX36BH Rhinitis FA20 Phase 3 [5]
Azimilide DMUIBV8 Atrial fibrillation BC81.3 Phase 3 [6]
ATI-2042 DMWP59B Atrial fibrillation BC81.3 Phase 2 [7]
AZD-7009 DMIBXK0 Atrial fibrillation BC81.3 Phase 2 [8]
Bimakalim DMBRL19 Angina pectoris BA40 Phase 2 [9]
HBI-3000 DM74ZKN Heart arrhythmia BC65 Phase 2 [10]
K-201 DMZCVD7 Atopic dermatitis EA80 Phase 2 [11]
MSH-1001 DMUM370 Ocular hypertension 9C61.01 Phase 2 [12]
RP-49356 DM4N6PF Hypertension BA00-BA04 Phase 2 [13]
YM-934 DM7KR4C Angina pectoris BA40 Phase 2 [14]
AVE0118 DMSR91U Obstructive sleep apnea 7A41 Phase 1 [15]
CLP-1004 DM2QBMI Hypertension BA00-BA04 Phase 1 [16]
Iptakalim DMHW1LI Hypertension BA00-BA04 Phase 1 [17]
Nibentan DM8J3WE Cardiac arrhythmias BC9Z Phase 1 [18]
NS-8 DMX8LY4 Urinary incontinence MF50.2 Phase 1 [19]
UK-66914 DMO8Z1D Cardiac arrhythmias BC9Z Phase 1 [20]
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⏷ Show the Full List of 16 Clinical Trial Drug(s)
46 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Levcromakalim DMNS4TK Chronic obstructive pulmonary disease CA22 Discontinued in Preregistration [21]
Acecainide DMKM543 Solid tumour/cancer 2A00-2F9Z Discontinued in Phase 3 [22]
Alinidine DMV2Y6L Angina pectoris BA40 Discontinued in Phase 3 [23]
Almokalant DMV3PEA Cardiac arrhythmias BC9Z Discontinued in Phase 3 [24]
BMS-204352 DMFZNLH Nerve injury ND56.4 Discontinued in Phase 3 [25]
Ambasilide DMA57O4 Cardiac arrhythmias BC9Z Discontinued in Phase 2 [26]
BMS-180448 DMVBGIT Angina pectoris BA40 Discontinued in Phase 2 [27]
BRL-32872A DMRKBIU Cardiac arrhythmias BC9Z Discontinued in Phase 2 [28]
BRL-55834 DM0WG4U Chronic obstructive pulmonary disease CA22 Discontinued in Phase 2 [29]
E-4031 DMU872N Cardiac arrhythmias BC9Z Discontinued in Phase 2 [30]
JTV-506 DMM8UNL Angina pectoris BA40 Discontinued in Phase 2 [31]
KCO-912 DMC30N4 Chronic obstructive pulmonary disease CA22 Discontinued in Phase 2 [32]
KW-7158 DMJNSML Urinary incontinence MF50.2 Discontinued in Phase 2 [33]
P-1075 DM02ANM Hypertension BA00-BA04 Discontinued in Phase 2 [34]
Risotilide DMNRGB7 Heart arrhythmia BC65 Discontinued in Phase 2 [35]
Y-27152 DMO90RN Angina pectoris BA40 Discontinued in Phase 2 [36]
ZD-0947 DMS95DX Overactive bladder GC50.0 Discontinued in Phase 2 [37]
ZD-6169 DMVBL25 Urinary incontinence MF50.2 Discontinued in Phase 2 [37]
Emakalim DM2V5XP Angina pectoris BA40 Discontinued in Phase 1 [38]
KR-30450 DMMD6LR Hypertension BA00-BA04 Discontinued in Phase 1 [39]
NTC-801 DM1QZKS Atrial fibrillation BC81.3 Discontinued in Phase 1 [40]
Rilmakalim DMBQZTO Chronic obstructive pulmonary disease CA22 Discontinued in Phase 1 [41]
Ro-31-6930 DMAJDPN Hypertension BA00-BA04 Discontinued in Phase 1 [42]
SDZ-PCO-400 DMZHOYM Asthma CA23 Discontinued in Phase 1 [43]
SR-47063 DMAICVN Cardiac arrhythmias BC9Z Discontinued in Phase 1 [44]
Symakalim DMSPBJ9 Hypertension BA00-BA04 Discontinued in Phase 1 [45]
AL-0671 DMRYJ40 Arteriosclerosis BD40 Terminated [46]
AWD-23-111 DMD8ZM1 Heart arrhythmia BC65 Terminated [47]
E-4080 DMZ1JKX Angina pectoris BA40 Terminated [48]
ICI-181037 DM0XU4P Heart arrhythmia BC65 Terminated [49]
KC-399 DMD0FNH Alopecia ED70 Terminated [50]
Ki-1769 DMQXPJB Hypertension BA00-BA04 Terminated [51]
NS-004 DMCHLJ4 Hypertension BA00-BA04 Terminated [52]
NS-1546 DM75DZ1 Major depressive disorder 6A70.3 Terminated [53]
NS-1608 DMYV9M1 Cerebrovascular ischaemia 8B1Z Terminated [54]
Org-20781 DM95QG2 Heart arrhythmia BC65 Terminated [55]
RP-66784 DM2GV78 Angina pectoris BA40 Terminated [56]
S-1389 DMDQGFR Heart arrhythmia BC65 Terminated [57]
SB-237376 DMBCANZ Arrhythmia BC9Z Terminated [58]
TCV-295 DMCFGS6 Hypertension BA00-BA04 Terminated [59]
TERIKALANT DM2X5R6 Cardiac arrhythmias BC9Z Terminated [60]
UR-8225 DMJC82N Asthma CA23 Terminated [61]
UR-8308 DM6C7WJ Asthma CA23 Terminated [62]
UR-8328 DM4KOTA Asthma CA23 Terminated [63]
WAY-123223 DMMOS8G Heart arrhythmia BC65 Terminated [64]
YM-099 DMDXLG2 Hypertension BA00-BA04 Terminated [65]
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⏷ Show the Full List of 46 Discontinued Drug(s)
8 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
CGS-7181 DMZKS6Q Discovery agent N.A. Investigative [66]
HMR1883 DMNXR17 Discovery agent N.A. Investigative [67]
L 691121 DMB73Y4 Discovery agent N.A. Investigative [68]
MJ-451 DMMP6YH Discovery agent N.A. Investigative [69]
RP-66471 DMR4O3I Discovery agent N.A. Investigative [70]
Trecetilide fumarate DME94KO Cardiac arrhythmias BC9Z Investigative [71]
WAY-125971 DMCSZG0 Discovery agent N.A. Investigative [64]
Y-26763 DMZKPSQ Discovery agent N.A. Investigative [72]
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⏷ Show the Full List of 8 Investigative Drug(s)

References

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4 Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
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6 Azimilide. Drugs. 2000 Feb;59(2):271-7; discussion 278-9.
7 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
8 Rapid slowing of the atrial fibrillatory rate after administration of AZD7009 predicts conversion of atrial fibrillation. J Electrocardiol. 2014 May-Jun;47(3):316-23.
9 Lack of anti-ischemic efficacy of the potassium channel opener bimakalim in patients with stable angina pectoris. Cardiovasc Drugs Ther. 2004 Jan;18(1):37-46.
10 Electrophysiological properties of HBI-3000: a new antiarrhythmic agent with multiple-channel blocking properties in human ventricular myocytes. J Cardiovasc Pharmacol. 2011 Jan;57(1):79-85.
11 Cardiac ryanodine receptor in metabolic syndrome: is JTV519 (K201) future therapy
12 KR-31378, a potassium-channel opener, induces the protection of retinal ganglion cells in rat retinal ischemic models. J Pharmacol Sci. 2009 Apr;109(4):511-7.
13 Effects of pinacidil, RP 49356 and nicorandil on ATP-sensitive potassium channels in insulin-secreting cells. Br J Pharmacol. 1990 Mar;99(3):487-92.
14 Potassium channel opener, YM 934, inhibits neurogenic plasma leakage in guinea pig airways. Am J Respir Crit Care Med. 1994 Nov;150(5 Pt 1):1379-83.
15 Neurogenic contraction induced by the antiarrhythmic compound, AVE 0118, in rat small mesenteric arteries.Basic Clin Pharmacol Toxicol.2014 Oct;115(4):315-20.
16 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036783)
17 Iptakalim: A novel multi-utility potassium channel opener. J Pharmacol Pharmacother. 2012 Jan;3(1):12-4.
18 Nibentan -- a drug for pharmacological cardioversion of persistent atrial fibrillation. Kardiologiia. 2005;45(3):19-23.
19 Stimulation of large-conductance calcium-activated potassium channels inhibits neurogenic contraction of human bladder from patients with urinary symptoms and reverses acetic acid-induced bladder hyperactivity in rats. Eur J Pharmacol. 2014 Jul 15;735:68-76.
20 Electrophysiologic properties of UK-66,914, a novel class III antiarrhythmic agent. J Cardiovasc Pharmacol. 1991 Mar;17(3):376-85.
21 The potassium channel opener levcromakalim causes expansive remodelling of experimental vein grafts. J Vasc Surg. 2006 Jul;44(1):159-65.
22 Acecainide (N-acetylprocainamide). A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in cardiac arrhythmias. Drugs. 1990 May;39(5):720-40.
23 Decrease in bradycardic effect of AQ-A 39 and alinidine in guinea-pig sinoatrial node depolarized by high external K+-concentration. Naunyn Schmiedebergs Arch Pharmacol. 1984 Dec;328(2):210-3.
24 Effect of almokalant, a selective potassium channel blocker, on the termination and inducibility of paroxysmal supraventricular tachycardias: a study in patients with Wolff-Parkinson-White syndrome and atrioventricular nodal reentrant tachycardia.Almokalant PSVT Study Group.J Cardiovasc Pharmacol.1995 Aug;26(2):198-206.
25 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
26 Ambasilide prolongs the action potential and blocks multiple potassium currents in human atrium. J Cardiovasc Pharmacol. 1999 May;33(5):762-71.
27 The novel cardioprotective agent BMS-180448 activates a potassium conductance in cardiac and vascular smooth muscle. Naunyn Schmiedebergs Arch Pharmacol. 1996 Oct;354(4):444-51.
28 Combined potassium and calcium channel blocking activities as a basis for antiarrhythmic efficacy with low proarrhythmic risk: experimental profile... J Pharmacol Exp Ther. 1996 Feb;276(2):637-46.
29 Comparison of the airways relaxant and hypotensive potencies of the potassium channel activators BRL 55834 and levcromakalim (BRL 38227) in vivo in guinea-pigs and rats. Br J Pharmacol. 1993 Aug;109(4):1133-9.
30 Comparison of the IKr blockers moxifloxacin, dofetilide and E-4031 in five screening models of pro-arrhythmia reveals lack of specificity of isolated cardiomyocytes.Br J Pharmacol.2012 Jan;165(2):467-78.
31 Effects of the new potassium channel opener JTV-506 on coronary vessels in vitro and in vivo. Arzneimittelforschung. 1999 Mar;49(3):199-206.
32 KCO912: a potent and selective opener of ATP-dependent potassium (K(ATP)) channels which suppresses airways hyperreactivity at doses devoid of card... Naunyn Schmiedebergs Arch Pharmacol. 2002 Mar;365(3):220-30.
33 KW-7158 [(2S)-(+)-3,3,3-trifluoro-2-hydroxy-2-methyl-N-(5,5,10-trioxo-4,10-dihydrothieno[3,2-c][1]benzothiepin-9-yl)propanamide] enhances A-type K+... J Pharmacol Exp Ther. 2004 Jul;310(1):159-68.
34 The effects of potassium channel opener P1075 on the human saphenous vein and human internal mammary artery. J Cardiovasc Pharmacol. 2011 Jun;57(6):648-55.
35 Electrophysiological effects of left ventricular hypertrophy. Effect of calcium and potassium channel blockade. Circulation. 1991 Jun;83(6):2067-75.
36 Pharmacokinetics and safety of a novel, long-acting, prodrug-type potassium channel opener, Y-27152, in healthy volunteers. J Clin Pharmacol. 1996 May;36(5):439-51.
37 Effects of ZD6169 and ZD0947, 2 potassium adenosine triphosphate channel openers, on bladder function of spinalized rats. J Urol. 2002 Aug;168(2):837-42.
38 Therapeutic potential of potassium channel activators in coronary heart disease. Eur Heart J. 1994 Aug;15 Suppl C:82-8.
39 Cardioprotective effects of KR-30450, a novel K+(ATP) opener, and its major metabolite KR-30818 on isolated rat hearts. Jpn J Pharmacol. 1998 Jan;76(1):65-73.
40 Effects of the selective KACh channel blocker NTC-801 on atrial fibrillation in a canine model of atrial tachypacing: comparison with class Ic and III drugs. J Cardiovasc Pharmacol. 2014 May;63(5):421-7.
41 Hypotonic stress increases efficacy of rilmakalim, but not pinacidil, to activate ATP-sensitive K(+) current in guinea pig ventricular myocytes. J Pharmacol Sci. 2004 Jun;95(2):189-95.
42 Evaluation of the bronchodilator properties of Ro 31-6930, a novel potassium channel opener, in the guinea-pig. Br J Pharmacol. 1990 Jun;100(2):289-94.
43 Effects of a potassium channel opener (SDZ PCO 400) on guinea-pig and human pulmonary airways. Br J Pharmacol. 1992 Jun;106(2):423-9.
44 Vasorelaxant effects of the potassium channel opener SR 47063 on the isolated human saphenous vein and rat aorta. Braz J Med Biol Res. 2000 Aug;33(8):961-6.
45 Synthesis and antihypertensive activity of 4-(diazabicyclo[4.1.0]-heptenyloxy)benzopyran derivatives and their analogues. Chem Pharm Bull (Tokyo). 1998 Apr;46(4):602-9.
46 A possible mechanism of action of a new potassium channel opener, AL0671, on lipid metabolism in obese Zucker rats. J Pharmacol Exp Ther. 1994 Dec;271(3):1666-71.
47 The new antiarrhythmic substance AWD 23-111 inhibits the delayed rectifier potassium current (IK) in guinea pig ventricular myocytes. Pharmazie. 1999 Jan;54(1):61-8.
48 Ionic currents involved in vasodilating actions of E4080, a newly synthesized bradycardia-inducing agent, in dispersed smooth muscle cells of the rabbit portal vein. J Pharmacol Exp Ther. 1991 Dec;259(3):1396-403.
49 ICI 181,037: a novel eukalemic diuretic with antiarrhythmic activity. Jpn J Pharmacol. 1991 Nov;57(3):263-77.
50 Action of KC-399, a newly synthesized potassium channel opener, on mechanical activity and 86Rb efflux in rat aorta. J Cardiovasc Pharmacol. 1994 Feb;23(2):220-6.
51 Vasorelaxant action of Ki1769, a new pyridinecarboximidamide, in isolated porcine coronary artery. Eur J Pharmacol. 1993 Sep 14;241(2-3):177-81.
52 Effects of K+ channel inhibitors and antagonists on NS-004 evoked relaxations in guinea-pig isolated trachea. Fundam Clin Pharmacol. 1997;11(1):78-82.
53 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006187)
54 Modulation of the Ca(2+)-dependent K+ channel, hslo, by the substituted diphenylurea NS 1608, paxilline and internal Ca2+. Neuropharmacology. 1996;35(7):903-14.
55 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003350)
56 Syntheses and biological activities of potent potassium channel openers derived from (+/-)-2-oxo-1-pyridin-3-yl-cyclohexanecarbothioic acid methylamide: new potassium channel openers. J Med Chem. 1993 May 28;36(11):1604-12.
57 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000214)
58 Electrophysiologic effects of SB-237376: a new antiarrhythmic compound with dual potassium and calcium channel blocking action. J Cardiovasc Pharmacol. 2003 Mar;41(3):414-21.
59 Antihypertensive and cardiovascular effects of a new potassium channel opener, TCV-295, in rats and dogs. J Cardiovasc Pharmacol. 1994 Dec;24(6):929-36.
60 Terikalant, an inward-rectifier potassium channel blocker, does not abolish the cardioprotection induced by ischemic preconditioning in the rat. J Mol Cell Cardiol. 1998 Sep;30(9):1817-25.
61 Effects of the novel potassium channel opener, UR-8225, on contractile responses in rat isolated smooth muscle. Br J Pharmacol. 1993 Nov;110(3):1165-71.
62 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005294)
63 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005293)
64 Synthesis and selective class III antiarrhythmic activity of novel N-heteroaralkyl-substituted 1-(aryloxy)-2-propanolamine and related propylamine derivatives. J Med Chem. 1991 Nov;34(11):3212-28.
65 Potassium channel-opening and vasorelaxant profiles of a novel compound YM099 in rat isolated portal vein and rabbit isolated aorta. Arch Int Pharmacodyn Ther. 1994 May-Jun;327(3):330-43.
66 Molecular mechanism of pharmacological activation of BK channels
67 Clamikalant (Aventis). IDrugs. 2000 Nov;3(11):1353-7.
68 Embryotoxic effects of L-691,121, a class III antiarrhythmic agent, in rats. Arch Toxicol. 1994;69(1):65-71.
69 Pharmacological characteristics of MJ-451, a new benzopyran- derived ATP-sensitive potassium channel opener, in guinea pig isolated trachea. Pharmacology. 1998 Dec;57(6):314-22.
70 Potassium channel opener, RP 66471, induces membrane depolarization of rat liver mitochondria. Biochem Biophys Res Commun. 1995 Feb 6;207(1):126-32.
71 IKr channel blockers: novel antiarrhythmic agents. Curr Med Chem Cardiovasc Hematol Agents. 2003 Oct;1(3):203-23.
72 Y-26763: ATP-sensitive K+ channel activation and the inhibition of insulin release from human pancreatic beta-cells. Eur J Pharmacol. 2004 Feb 20;486(2):133-9.