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Target
cGMP-specific 3',5'-cyclic phosphodiesterase
Ligand
BDBM50059049
Substrate
n/a
Meas. Tech.
ChEMBL_155185 (CHEMBL761832)
IC50
120±n/a nM
Citation
Ahn, HS; Bercovici, A; Boykow, G; Bronnenkant, A; Chackalamannil, S; Chow, J; Cleven, R; Cook, J; Czarniecki, M; Domalski, C; Fawzi, A; Green, M; Gündes, A; Ho, G; Laudicina, M; Lindo, N; Ma, K; Manna, M; McKittrick, B; Mirzai, B; Nechuta, T; Neustadt, B; Puchalski, C; Pula, K; Zhang, H Potent tetracyclic guanine inhibitors of PDE1 and PDE5 cyclic guanosine monophosphate phosphodiesterases with oral antihypertensive activity. J Med Chem 40:2196-210 (1997) [PubMed] Article
More Info.:
Target
Name:
cGMP-specific 3',5'-cyclic phosphodiesterase
Synonyms:
PDE5 | PDE5A | PDE5A_BOVIN | Phosphodiesterase 5A
Type:
PROTEIN
Mol. Mass.:
98615.45
Organism:
Bos taurus
Description:
ChEMBL_155186
Residue:
865
Sequence:
MERAGPGSARPQQQWDQDSVEAWLDDHWDFTFSYFVRKGTREMVNAWFAERVHTIPVCKEGIKGHTESCSCPLQPSPRAESSVPGTPTRKISASEFDRPLRPIVIKDSEGTVSFLSDSDKKEQMPLTSPRFDNDEGDQCSRLLELVKDISSHLDVTALCHKIFLHIHGLISADRYSLFLVCEDSSNDKFLISRLFDVAEGSTLEEASNNCIRLEWNKGIVGHVAAFGEPLNIKDAYEDPRFNAEVDQITGYKTQSILCMPIKNHREEVVGVAQAINKKSGNGGTFTEKDEKDFAAYLAFCGIVLHNAQLYETSLLENKRNQVLLDLASLIFEEQQSLEVILKKIAATIISFMQVQKCTIFIVDEDCSDSFSSVFHMECEELEKSSDTLTRERDANRINYMYAQYVKNTMEPLNIPDVSKDKRFPWTNENMGNINQQCIRSLLCTPIKNGKKNKVIGVCQLVNKMEETTGKVKAFNRNDEQFLEAFVIFCGLGIQNTQMYEAVERAMAKQMVTLEVLSYHASAAEEETRELQSLAAAVVPSAQTLKITDFSFSDFELSDLETALCTIRMFTDLNLVQNFQMKHEVLCKWILSVKKNYRKNVAYHNWRHAFNTAQCMFAALKAGKIQKRLTDLEILALLIAALSHDLDHRGVNNSYIQRSEHPLAQLYCHSIMEHHHFDQCLMILNSPGNQILSGLSIEEYKTTLKIIKQAILATDLALYIKRRGEFFELIMKNQFNLEDPHQKELFLAMLMTACDLSAITKPWPIQQRIAELVATEFFDQGDRERKELNIEPADLMNREKKNKIPSMQVGFIDAICLQLYEALTHVSEDCFPLLDGCRKNRQKWQALAEQQEKTLINGESSQTKRN
Inhibitor
Name:
BDBM50059049
Synonyms:
5'-Methyl-2'-(cyclopentylmethyl)-3'-(phenylmethyl)spiro[cyclopentane-1,7'(8'H)-[3H]imidazo[2,1-b]purin]-4(5'H)-one | CHEMBL305989
Type:
Small organic molecule
Emp. Form.:
C25H31N5O
Mol. Mass.:
417.5465
SMILES:
CN1C2=NC3(CCCC3)CN2c2nc(CC3CCCC3)n(Cc3ccccc3)c2C1=O |t:2|