Protein Information

General Information of the Protein

Protein ID	PT01176
Protein Name	cGMP-specific 3',5'-cyclic phosphodiesterase
Secondarily Protein Name	cGMP-binding cGMP-specific phosphodiesterase
Gene Name	PDE5A
Secondarily Gene Name	PDE5
Sequence	MERAGPSFGQQRQQQQPQQQKQQQRDQDSVEAWLDDHWDFTFSYFVRKATREMVNAWFAERVHTIPVCKEGIRGHTESCSCPLQQSPRADNSAPGTPTRKISASEFDRPLRPIVVKDSEGTVSFLSDSEKKEQMPLTPPRFDHDEGDQCSRLLELVKDISSHLDVTALCHKIFLHIHGLISADRYSLFLVCEDSSNDKFLISRLFDVAEGSTLEEVSNNCIRLEWNKGIVGHVAALGEPLNIKDAYEDPRFNAEVDQITGYKTQSILCMPIKNHREEVVGVAQAINKKSGNGGTFTEKDEKDFAAYLAFCGIVLHNAQLYETSLLENKRNQVLLDLASLIFEEQQSLEVILKKIAATIISFMQVQKCTIFIVDEDCSDSFSSVFHMECEELEKSSDTLTREHDANKINYMYAQYVKNTMEPLNIPDVSKDKRFPWTTENTGNVNQQCIRSLLCTPIKNGKKNKVIGVCQLVNKMEENTGKVKPFNRNDEQFLEAFVIFCGLGIQNTQMYEAVERAMAKQMVTLEVLSYHASAAEEETRELQSLAAAVVPSAQTLKITDFSFSDFELSDLETALCTIRMFTDLNLVQNFQMKHEVLCRWILSVKKNYRKNVAYHNWRHAFNTAQCMFAALKAGKIQNKLTDLEILALLIAALSHDLDHRGVNNSYIQRSEHPLAQLYCHSIMEHHHFDQCLMILNSPGNQILSGLSIEEYKTTLKIIKQAILATDLALYIKRRGEFFELIRKNQFNLEDPHQKELFLAMLMTACDLSAITKPWPIQQRIAELVATEFFDQGDRERKELNIEPTDLMNREKKNKIPSMQVGFIDAICLQLYEALTHVSEDCFPLLDGCRKNRQKWQALAEQQEKMLINGESGQAKRN Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Enzyme > Phosphodiesterase > Phosphodiesterase 5 > Phosphodiesterase 5A
Function	Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. This phosphodiesterase catalyzes the specific hydrolysis of cGMP to 5'-GMP (PubMed:9714779, PubMed:15489334). Specifically regulates nitric-oxide-generated cGMP (PubMed:15489334). Show/Hide
Uniprot ID	Primary ID: O76074 Secondarily ID: A0AV69 A8K2C4 O75026 O75887 Q86UI0 Q86V66 Q9Y6Z6 Show/Hide
Ensembl ID	ENSG00000138735
HGNC ID	HGNC:8784

Map of Molecular Bioactivity Related to the Protein

Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity

Table of Molecular Bioactivities Related to the Protein

Cell Line ID: CL000053 , COS-7

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0264367 Compound Info	3,7-Bis(2-hydroxyethyl)icaritin Show/Hide	C25H28O8	1
1	IC50 = 74 nM Bioactivity Info	TI LI LO TS
CP0010658 Compound Info	5-[2-ethoxy-5-(4-methyl-1-piperazinylsulfonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one Show/Hide	C22H30N6O4S	1
1	IC50 = 75 nM Bioactivity Info	TI LI LO TS
CP0160450 Compound Info	5,7-dihydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-enyl)-3-[(2S,3S,4S,5S,6R)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxychromen-4-one Show/Hide	C27H30O10	1
1	IC50 = 160 nM Bioactivity Info	TI LI LO TS
CP0354149 Compound Info	7-(2-Hydroxyethyl)-3-O-rhamnosylicariin Show/Hide	C29H34O11	1
1	IC50 = 360 nM Bioactivity Info	TI LI LO TS
CP0460413 Compound Info	2-(3,4-Dihydroxy-phenyl)-3,5,7-trihydroxy-8-(3-methyl-but-2-enyl)-chromen-4-one Show/Hide	C20H18O7	1
1	IC50 = 700 nM Bioactivity Info	TI LI LO TS
CP0401808 Compound Info	5,7-Dihydroxy-2-(4-hydroxy-phenyl)-8-(3-methyl-but-2-enyl)-chromen-4-one Show/Hide	C20H18O5	1
1	IC50 = 1290 nM Bioactivity Info	TI LI LO TS
CP0347682 Compound Info	3-hydroxy-7-o-beta-glucose-8-prenyl-4'-methoxy Chrysin Show/Hide	C21H20O6	1
1	IC50 = 2200 nM Bioactivity Info	TI LI LO TS
CP0262424 Compound Info	CHEBI:78420 Show/Hide	C33H40O15	1
1	IC50 = 5900 nM Bioactivity Info	TI LI LO TS
CP0209727 Compound Info	SOPHORAFLAVANONE B Show/Hide	C20H20O5	1
1	IC50 = 16230 nM Bioactivity Info	TI LI LO TS
CP0262440 Compound Info	3,7-dimethanesulfonyl-8-prenyl-4'-methoxy Chrysin Show/Hide	C21H20O6	1
1	IC50 = 45500 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000013 , Sf9

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0175962 Compound Info	3-(5-ethylfuran-2-yl)-2-(5-pyridin-2-ylpyrimidin-2-yl)-3,4-dihydro-1H-pyrrolo[3,4-b]quinolin-9-one Show/Hide	C26H21N5O2	1
1	IC50 = 0.53 nM
CP0117113 Compound Info	3-(5-ethylthiophen-2-yl)-2-(5-pyridin-2-ylpyrimidin-2-yl)-3,4-dihydro-1H-pyrrolo[3,4-b]quinolin-9-one Show/Hide	C26H21N5OS	1
1	IC50 = 0.6 nM
CP0000847 Compound Info	(2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.0^{3,8}.0^{11,16}]heptadeca-1(10),11(16),12,14-tetraene-4,7-dione Show/Hide	C22H19N3O4	10
1	IC50 = 1.2 nM
2	IC50 = 3 nM
3	IC50 = 3.162 nM
4	IC50 = 4 nM
5	IC50 = 5 nM
6	IC50 = 5.012 nM
7	IC50 = 6.7 nM
8	IC50 = 9.4 nM
9	Ki = 5.2 nM
10	Ki = 10 nM
CP0010658 Compound Info	5-[2-ethoxy-5-(4-methyl-1-piperazinylsulfonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one Show/Hide	C22H30N6O4S	17
1	IC50 = 1.4 nM
2	IC50 = 1.6 nM
3	IC50 = 2.2 nM
4	IC50 = 3 nM
5	IC50 = 3.5 nM
6	IC50 = 3.9 nM
7	IC50 = 3.981 nM
8	IC50 = 5.22 nM
9	IC50 = 5.6 nM
10	IC50 = 6.6 nM
11	IC50 = 8.5 nM
12	IC50 = 20 nM
13	IC50 = 12590 nM
14	Ki = 1.6 nM
15	Ki = 1.87 nM
16	Ki = 1.91 nM
17	Ki = 10 nM
CP0116540 Compound Info	4-ethoxy-N-(6-hydroxyhexyl)-3-(1-methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)benzenesulfonamide Show/Hide	C23H33N5O5S	1
1	IC50 = 1.5 nM
CP0086283 Compound Info	4,5-diethyl-2-[5-(4-methylpiperazin-1-yl)sulfonyl-2-propoxyphenyl]-1H-pyrimidin-6-one Show/Hide	C22H32N4O4S	1
1	IC50 = 1.6 nM
CP0012955 Compound Info	5-[[4-ethoxy-3-(1-methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)phenyl]methyl]-N-hydroxyfuran-2-carboxamide Show/Hide	C23H25N5O5	1
1	IC50 = 3 nM
CP0201347 Compound Info	5-[[4-ethoxy-3-(5-methyl-4-oxo-7-propyl-3H-imidazo[5,1-f][1,2,4]triazin-2-yl)phenyl]methyl]-N-hydroxythiophene-2-carboxamide Show/Hide	C23H25N5O4S	1
1	IC50 = 3 nM
CP0012519 Compound Info	5-[[4-ethoxy-3-(1-methyl-7-oxo-3-propyl-6H-pyrazolo[4,3-d]pyrimidin-5-yl)phenyl]methyl]-N-hydroxythiophene-2-carboxamide Show/Hide	C23H25N5O4S	1
1	IC50 = 11 nM
CP0218821 Compound Info	4-[3-(4-methoxyphenyl)-5-phenyl-3,4-dihydropyrazol-2-yl]benzoic acid Show/Hide	C23H20N2O3	1
1	IC50 = 1200 nM
CP0053897 Compound Info	US9388139, 9 Show/Hide	C24H22N2O4	1
1	IC50 = 1800 nM
CP0340455 Compound Info	US9388139, 1 Show/Hide	C21H24N2O3	1
1	IC50 = 2020 nM
CP0177639 Compound Info	US9388139, 27 Show/Hide	C23H19FN2O3	1
1	IC50 = 3100 nM
CP0250532 Compound Info	US9388139, 8 Show/Hide	C24H22N2O4	1
1	IC50 = 3200 nM
CP0244231 Compound Info	US9388139, 10 Show/Hide	C25H24N2O5	1
1	IC50 = 6900 nM
CP0053899 Compound Info	US9388139, 23 Show/Hide	C21H24N2O2	1
1	IC50 = 8400 nM
CP0011191 Compound Info	4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzene-1-sulfonamide Show/Hide	C17H14F3N3O2S	1
1	IC50 = 36000 nM

Clinical Information about the Protein

Target 1 ( Phosphodiesterase 5A (PDE5A) )

Target Type	Successful Target
Disease	9 Target-related Diseases				9
1	Erectile dysfunction [ICD-11: HA01.1]
2	Hypertension [ICD-11: BA00-BA04]
3	Spasm [ICD-11: MB47.3]
4	Hereditary angioedema [ICD-11: 4A00.14]
5	Colorectal cancer [ICD-11: 2B91.Z]
6	Raynaud disease [ICD-11: BD42.0]
7	Allergy [ICD-11: 4A80-4A85]
8	Cardiovascular disease [ICD-11: BA00-BE2Z]
9	Asthma [ICD-11: CA23]
Approved Drug(s)	7 Approved Drugs				7
1	Avanafil	Drug Info	Approved	Erectile dysfunction
2	Dipyridamole	Drug Info	Approved	Hypertension
3	Papaverine	Drug Info	Approved	Spasm
4	Rhucin	Drug Info	Approved	Hereditary angioedema
5	Tadalafil	Drug Info	Approved	Erectile dysfunction
6	Udenafil	Drug Info	Approved	Erectile dysfunction
7	Vardenafil	Drug Info	Approved	Erectile dysfunction
Clinical Trial Drug(s)	3 Clinical Trial Drugs				3
1	EXISULIND	Drug Info	Phase 3	Colorectal cancer
2	PF-489791	Drug Info	Phase 2	Raynaud disease
3	UK-371800	Drug Info	Phase 1	Erectile dysfunction
Discontinued Drug(s)	4 Discontinued Drugs				4
1	BRL-61063	Drug Info	Discontinued in Phase 2	Allergy
2	E-4021	Drug Info	Discontinued in Phase 2	Cardiovascular disease
3	UK-369003	Drug Info	Discontinued in Phase 1/2	Erectile dysfunction
4	SKF-96231	Drug Info	Terminated	Asthma

Target 2 ( HUMAN phosphodiesterase type 5 (PDE5) )

Target Type	Unknown Type Target
Disease	1 Target-related Disease				1
1	Erectile dysfunction [ICD-11: HA01.1]
Clinical Trial Drug(s)	1 Clinical Trial Drug				1
1	Sildenafil	Drug Info	Approved	Erectile dysfunction

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han