Target Information

Target General Information

Top

Target ID

T92138 (Former ID: TTDC00315)

Target Name

Phosphodiesterase (PDE)

Synonyms

Human phosphodiesterase

Click to Show/Hide

Gene Name

NO-GeName

Target Type

Clinical trial target

[1]

Disease

[+] 2 Target-related Diseases

Angina pectoris [ICD-11: BA40]

Psoriasis [ICD-11: EA90]

Function

Participates in processes of transmission and amplification of the visual signal. cGMP-PDEs are the effector molecules in G-protein-mediated phototransduction in vertebrate rods and cones.

Click to Show/Hide

BioChemical Class

Phosphoric diester hydrolase

UniProt ID

NOUNIPROTAC

Drugs and Modes of Action

Top

Clinical Trial Drug(s)

[+] 2 Clinical Trial Drugs

M-518101

Drug Info

Phase 3

Psoriasis vulgaris

[2]

NM-702

Drug Info

Phase 3

Angina pectoris

[3]

Discontinued Drug(s)

[+] 9 Discontinued Drugs

Piroximone

Drug Info

Discontinued in Phase 3

Cardiac failure

[4]

AA-2379

Drug Info

Discontinued in Phase 2

Inflammation

[5]

HN-10200

Drug Info

Discontinued in Phase 2

Cardiac failure

[6]

TIBENELAST

Drug Info

Discontinued in Phase 2

Asthma

[7]

ALBIFYLLINE

Drug Info

Discontinued in Phase 1

Sepsis

[8]

BBB-022

Drug Info

Terminated

Cerebrovascular ischaemia

[9]

Isomazole

Drug Info

Terminated

Asthma

[10]

JTT-608

Drug Info

Terminated

Diabetic complication

[11]

Sch-45752

Drug Info

Terminated

Asthma

[12]

Mode of Action

[+] 1 Modes of Action

Inhibitor

[+] 12 Inhibitor drugs

M-518101

Drug Info

[13]

NM-702

Drug Info

[1]

Piroximone

Drug Info

[14]

AA-2379

Drug Info

[15]

HN-10200

Drug Info

[16]

TIBENELAST

Drug Info

[17]

ALBIFYLLINE

Drug Info

[18]

BBB-022

Drug Info

[19]

Isomazole

Drug Info

[20]

JTT-608

Drug Info

[21]

Sch-45752

Drug Info

[22]

DPN-205-734

Drug Info

[23]

Drug Property Profile of Target

Top

(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

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

References

Top

REF 1

The novel phosphodiesterase inhibitor NM-702 improves claudication-limited exercise performance in patients with peripheral arterial disease. J Am Coll Cardiol. 2006 Dec 19;48(12):2539-45.

REF 2

ClinicalTrials.gov (NCT01989429) Efficacy Study Comparing Topical M518101 and Vitamin D3 in Adult Psoriasis Patients. U.S. National Institutes of Health.

REF 3

Application of adaptive design and decision making to a phase II trial of a phosphodiesterase inhibitor for the treatment of intermittent claudication. Trials. 2011; 12: 134.

REF 4

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000260)

REF 5

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000920)

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 800001592)

REF 7

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000078)

REF 8

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003224)

REF 9

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009640)

REF 10

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000373)

REF 11

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011585)

REF 12

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002639)

REF 13

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 14

Circulatory effects of the PDE-inhibitors piroximone and enoximone. Br J Clin Pharmacol. 1993 Oct;36(4):309-14.

REF 15

Inhibitory effects of methyl 7-butyl-4,5,6,7-tetrahydro-3-methylamino-4,6-dioxo-5-propyl- 2H-pyrazolo[3,4-d]pyrimidine-2-carboxylate (AA-2379) on lysosomal enzyme and arachidonic acid release from rat polymorphonuclear leukocytes and its mode of action. Agents Actions. 1989 Nov;28(3-4):248-55.

REF 16

HN-10200 causes endothelium-independent relaxations in isolated canine arteries. Cardiovasc Drugs Ther. 1992 Apr;6(2):159-65.

REF 17

Effect of tibenelast (a phosphodiesterase inhibitor) and theophylline on isoproterenol-stimulated heart rate, cyclic AMP and norepinephrine levels. Pharmacology. 1993;46(3):142-7.

REF 18

Enhanced tumor necrosis factor suppression and cyclic adenosine monophosphate accumulation by combination of phosphodiesterase inhibitors and prostanoids. Eur J Immunol. 1995 Jan;25(1):147-53.

REF 19

Matrix metalloproteinase inhibition prevents oxidative stress-associated blood-brain barrier disruption after transient focal cerebral ischemia. J Cereb Blood Flow Metab. 2001 Dec;21(12):1393-400.

REF 20

Effects of isomazole on force of contraction and phosphodiesterase isoenzymes I-IV in nonfailing and failing human hearts. J Cardiovasc Pharmacol. 1991 Sep;18(3):386-97.

REF 21

JTT-608 controls blood glucose by enhancement of glucose-stimulated insulin secretion in normal and diabetes mellitus rats. Eur J Pharmacol. 1999 Feb 12;367(1):91-9.

REF 22

SCH 45752--an inhibitor of calmodulin-sensitive cyclic nucleotide phosphodiesterase activity. J Antibiot (Tokyo). 1993 Feb;46(2):207-13.

REF 23

Pharmacological actions of DPN 205-734, a novel cardiotonic agent. J Cardiovasc Pharmacol. 1988 Oct;12(4):451-60.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.

Prof. Feng ZHU

Prof. Yuzong CHEN