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ChEMBL Statistics
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Target Report Card

Target Name and Classification

Target ID CHEMBL1827
Preferred Name Phosphodiesterase 5A
Synonyms CGB-PDE | PDE5 | PDE5A | cGMP-binding cGMP-specific phosphodiesterase | cGMP-specific 3',5'-cyclic phosphodiesterase
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > phosphodiesterase > phosphodiesterase 5 > phosphodiesterase 5a

Target Components

Component Description Relationship Accession
cGMP-specific 3',5'-cyclic phosphodiesterase SINGLE PROTEIN O76074

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL2363066 3',5'-cyclic phosphodiesterase PROTEIN FAMILY
CHEMBL2111470 Phosphodiesterase 2 and 5 (PDE2 and PDE5) SELECTIVITY GROUP
CHEMBL2111400 Phosphodiesterase 3 and 5 (PDE3 and PDE5) SELECTIVITY GROUP
CHEMBL2097161 Phosphodiesterase, PDE1/PDE5 PROTEIN FAMILY
CHEMBL2095220 Phosphodiesterases; PDE5 & PDE6 SELECTIVITY GROUP
CHEMBL2111340 Phosphodiesterase 4 and 5 (PDE4 and PDE5) SELECTIVITY GROUP

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL779 TADALAFIL Phosphodiesterase 5A inhibitor 4 DailyMed
CHEMBL1339 VARDENAFIL HYDROCHLORIDE Phosphodiesterase 5A inhibitor 4 DailyMed
CHEMBL1737 SILDENAFIL CITRATE Phosphodiesterase 5A inhibitor 4 DailyMed
CHEMBL1963681 AVANAFIL Phosphodiesterase 5A inhibitor 4 FDA
CHEMBL2103849 UDENAFIL Phosphodiesterase 5A inhibitor 3 PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000138735
Ensembl ENSG00000138735
GO Cellular Component GO:0005575 (cellular_component)
GO:0005829 (cytosol)
GO Molecular Function GO:0000166 (nucleotide binding)
GO:0003824 (catalytic activity)
GO:0004112 (cyclic-nucleotide phosphodiesterase activity)
GO:0004114 (3',5'-cyclic-nucleotide phosphodiesterase activity)
GO:0005515 (protein binding)
GO:0008081 (phosphoric diester hydrolase activity)
GO:0016787 (hydrolase activity)
GO:0030553 (cGMP binding)
GO:0046872 (metal ion binding)
GO:0047555 (3',5'-cyclic-GMP phosphodiesterase activity)
GO Biological Process GO:0007165 (signal transduction)
GO:0008152 (metabolic process)
GO:0010613 (positive regulation of cardiac muscle hypertrophy)
GO:0030823 (regulation of cGMP metabolic process)
GO:0042130 (negative regulation of T cell proliferation)
GO:0043406 (positive regulation of MAP kinase activity)
GO:0046068 (cGMP metabolic process)
GO:0046069 (cGMP catabolic process)
GO:0055118 (negative regulation of cardiac muscle contraction)
GO:0055119 (relaxation of cardiac muscle)
GO:0060282 (positive regulation of oocyte development)
Wikipedia CGMP-specific_phosphodiesterase_type_5

Target Cross References - Protein

Human Protein Atlas ENSG00000138735
IntAct O76074
Guide to Pharmacology 1304
Open Targets ENSG00000138735
PharmGKB PA33132
Reactome R-HSA-418457 (cGMP effects.)
UniProt A0AV69 A8K2C4 O75026 O75887 O76074 Q86UI0 Q86V66 Q9Y6Z6

Target Cross References - Domain

InterPro IPR002073 (PDEase_catalytic_dom.)
IPR003018 (GAF.)
IPR003607 (HD/PDEase_dom.)
IPR023088 (PDEase.)
IPR023174 (PDEase_CS.)
IPR029016 (GAF-like_dom_sf.)
IPR036971 (PDEase_catalytic_dom_sf.)
Pfam PF00233 (PDEase_I)
PF01590 (GAF)

Target Cross References - Structure

PDBe 1RKP 1T9R 1T9S 1TBF 1UDT 1UDU 1UHO 1XOZ 1XP0 2CHM 2H40 2H42 2H44 2XSS 3B2R 3BJC 3HC8 3HDZ 3JWQ 3JWR 3LFV 3MF0 3SHY 3SHZ More...
CREDO 1RKP 1T9R 1T9S 1TBF 1UDT 1UDU 1UHO 1XOZ 1XP0 2CHM 2H40 2H42 2H44 2XSS 3B2R 3BJC 3HC8 3HDZ 3JWQ 3JWR 3LFV 3MF0 3SHY 3SHZ More...