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Target
cGMP-specific 3',5'-cyclic phosphodiesterase
Ligand
BDBM50134136
Substrate
n/a
Meas. Tech.
ChEMBL_155186 (CHEMBL761833)
IC50
10±n/a nM
Citation
 Daugan, A; Grondin, P; Ruault, C; Le Monnier de Gouville, AC; Coste, H; Linget, JM; Kirilovsky, J; Hyafil, F; Labaudinière, R The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues. J Med Chem 46:4533-42 (2003) [PubMed]  Article 
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:
BDBM50134136
Synonyms:
(R)-10-(4-Methoxy-phenyl)-2-methyl-3a,4,9,10-tetrahydro-2,9,10a-triaza-cyclopenta[b]fluorene-1,3-dione | CHEMBL142143
Type:
Small organic molecule
Emp. Form.:
C21H19N3O3
Mol. Mass.:
361.3939
SMILES:
COc1ccc(cc1)C1c2[nH]c3ccccc3c2Cc2c(O)n(C)c(=O)n12
Structure:
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