Target Information

Target General Information

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Target ID

T82266 (Former ID: TTDS00160)

Target Name

Voltage-gated L-type calcium channel (L-CaC)

Synonyms

L-type voltage-dependent Ca(2+) channel; L-type Ca2+ channel; L-type Ca(2+) channel

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Gene Name

NO-GeName

Target Type

Successful target

[1]

Disease

[+] 4 Target-related Diseases

Angina pectoris [ICD-11: BA40]

Hypertension [ICD-11: BA00-BA04]

Neuropathy [ICD-11: 8C0Z]

Oesophagus motility disorder [ICD-11: DA21]

BioChemical Class

Voltage-gated ion channel

UniProt ID

NOUNIPROTAC

Drugs and Modes of Action

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Approved Drug(s)

[+] 5 Approved Drugs

Clevidipine butyrate

Drug Info

Approved

Hypertension

[2], [3]

Epalrestat

Drug Info

Approved

Diabetic neuropathy

[4]

Nifedipine

Drug Info

Approved

Angina pectoris

[5], [6]

Otilonium bromide

Drug Info

Approved

Gastric motility disorder

[7]

Levamlodipine

Drug Info

Phase 4

Hypertension

[8], [9]

Clinical Trial Drug(s)

[+] 5 Clinical Trial Drugs

Cilnidipine

Drug Info

Phase 3

High blood pressure

[10], [11]

Pinaverium bromide

Drug Info

Phase 3

Irritable bowel syndrome

[1]

MEM-1003

Drug Info

Phase 2a

Bipolar disorder

[12]

BAY-Y-5959

Drug Info

Phase 2

Cardiovascular disease

[13]

Gallopamil

Drug Info

Phase 2

Asthma

[14]

Discontinued Drug(s)

[+] 1 Discontinued Drugs

Furnidipine

Drug Info

Discontinued in Phase 3

Nerve injury

[15]

Mode of Action

[+] 4 Modes of Action

Inhibitor

[+] 1 Inhibitor drugs

Clevidipine butyrate

Drug Info

[16]

Blocker

[+] 23 Blocker drugs

Epalrestat

Drug Info

[17]

Otilonium bromide

Drug Info

[1]

Cilnidipine

Drug Info

[20], [21]

Pinaverium bromide

Drug Info

[1]

Gallopamil

Drug Info

[24], [25]

Ajinomoto 1

Drug Info

[17]

Ajinomoto 2

Drug Info

[17]

Ajinomoto 3

Drug Info

[17]

Dihydropyridines

Drug Info

[21]

Euro-Celtique 1

Drug Info

[17]

Euro-Celtique 2

Drug Info

[17]

Euro-Celtique 3

Drug Info

[17]

Euro-Celtique 4

Drug Info

[17]

Neuromed 2

Drug Info

[17]

Neuromed 5

Drug Info

[17]

Ono 1

Drug Info

[17]

Ono 3

Drug Info

[17]

Parke-Davis 1

Drug Info

[17]

Parke-Davis 9

Drug Info

[17]

PD173212

Drug Info

[17]

PD176078

Drug Info

[17]

SQ32,910

Drug Info

[25]

[3H](-)devapamil

Drug Info

[24], [25]

Modulator

[+] 5 Modulator drugs

Nifedipine

Drug Info

[18]

Levamlodipine

Drug Info

[19]

MEM-1003

Drug Info

[22]

BAY-Y-5959

Drug Info

[23]

Furnidipine

Drug Info

[26]

Activator

[+] 2 Activator drugs

Bay K 8644

Drug Info

[25]

S 202 791

Drug Info

[25]

Chemical Structure based Activity Landscape of Target

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Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"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

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Co-Targets

Co-Targets Info

Target Poor or Non Binders

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Target Poor or Non Binders

Target Poor or Non Binders Info

Target-Related Models and Studies

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Target Validation

Target Validation Info

References

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REF 1

Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.

REF 2

2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.

REF 3

Clevidipine: a short-acting intravenous dihydropyridine calcium channel blocker for the management of hypertension. Pharmacotherapy. 2010 May;30(5):515-28.

REF 4

Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.

REF 5

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: 2514).

REF 6

Are sildenafil and theophylline effective in the prevention of high-altitude pulmonary edema Med Hypotheses. 2002 Aug;59(2):223-5.

REF 7

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 8

ClinicalTrials.gov (NCT01131546) Efficacy and Safety of Levamlodipine Besylate Compared to Amlodipine Maleate in Patients With Essential Hypertension. U.S. National Institutes of Health.

REF 9

Quantification of pedal edema during treatment with S(-)-amlodipine nicotinate versus amlodipine besylate in female Korean patients with mild to moderate hypertension: a 12-week, multicenter, randomized, double-blind, active-controlled, phase IV clinical trial. Clin Ther. 2012 Sep;34(9):1940-7.

REF 10

REF 11

ClinicalTrials.gov (NCT02145104) Efficacy/Safety of Cilnidipine Plus Valsartan Versus Valsartan in Patients With Hypertension. U.S. National Institutes of Health.

REF 12

Emerging drugs for bipolar disorder. Expert Opin Emerg Drugs. 2006 Nov;11(4):621-34.

REF 13

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004756)

REF 14

ClinicalTrials.gov (NCT00896428) Effects of Gallopamil in Severe Asthma (REMODEL'ASTHME) in University Hospital, Bordeaux.

REF 15

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002558)

REF 16

Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.

REF 17

Recent updates of N-type calcium channel blockers with therapeutic potential for neuropathic pain and stroke. Curr Top Med Chem. 2009;9(4):377-95.

REF 18

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

REF 19

Effects of (S)-amlodipine and (R)-amlodipine on L-type calcium channel current of rat ventricular myocytes and cytosolic calcium of aortic smooth muscle cells. Pharmazie. 2008 Jun;63(6):470-4.

REF 20

N- and L-type calcium channel antagonist improves glomerular dynamics, reverses severe nephrosclerosis, and inhibits apoptosis and proliferation in an l-NAME/SHR model. J Hypertens. 2002 May;20(5):993-1000.

REF 21

Pharmacology of N-type Ca2+ channels distributed in cardiovascular system (Review). Int J Mol Med. 1999 May;3(5):455-66.

REF 22

Efficacy of MEM 1003, a novel calcium channel blocker, in delay and trace eyeblink conditioning in older rabbits. Neurobiol Aging. 2007 May;28(5):766-73.

REF 23

Hemodynamic effects of a calcium channel promoter, BAY y 5959, are preserved after chronic administration in ischemic heart failure in conscious dogs. J Pharmacol Exp Ther. 1998 Aug;286(2):760-6.

REF 24

Role of apoptosis in the kidney after reperfusion. Orv Hetil. 2008 Feb 17;149(7):305-15.

REF 25

Molecular determinants of drug binding and action on L-type calcium channels. Annu Rev Pharmacol Toxicol. 1997;37:361-96.

REF 26

Q-type Ca2+ channels are located closer to secretory sites than L-type channels: functional evidence in chromaffin cells. Pflugers Arch. 1998 Mar;435(4):472-8.

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