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Target
Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'
Ligand
BDBM50459162
Substrate
n/a
Meas. Tech.
ChEMBL_1765665 (CHEMBL4200912)
IC50
1.2±n/a nM
Citation
 Wu, D; Huang, Y; Chen, Y; Huang, YY; Geng, H; Zhang, T; Zhang, C; Li, Z; Guo, L; Chen, J; Luo, HB Optimization of Chromeno[2,3- c]pyrrol-9(2 H)-ones as Highly Potent, Selective, and Orally Bioavailable PDE5 Inhibitors: Structure-Activity Relationship, X-ray Crystal Structure, and Pharmacodynamic Effect on Pulmonary Arterial Hypertension. J Med Chem 61:8468-8473 (2018) [PubMed]  Article 
Target
Name:
Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha'
Synonyms:
3',5'-cyclic phosphodiesterase | PDE6C | PDE6C_HUMAN | PDEA2 | Phosphodiesterase 6C | Phosphodiesterase 6C (PDE6C)
Type:
Protein
Mol. Mass.:
99132.02
Organism:
Homo sapiens (Human)
Description:
P51160
Residue:
858
Sequence:
MGEINQVAVEKYLEENPQFAKEYFDRKLRVEVLGEIFKNSQVPVQSSMSFSELTQVEESALCLELLWTVQEEGGTPEQGVHRALQRLAHLLQADRCSMFLCRSRNGIPEVASRLLDVTPTSKFEDNLVGPDKEVVFPLDIGIVGWAAHTKKTHNVPDVKKNSHFSDFMDKQTGYVTKNLLATPIVVGKEVLAVIMAVNKVNASEFSKQDEEVFSKYLNFVSIILRLHHTSYMYNIESRRSQILMWSANKVFEELTDVERQFHKALYTVRSYLNCERYSIGLLDMTKEKEFYDEWPIKLGEVEPYKGPKTPDGREVNFYKIIDYILHGKEEIKVIPTPPADHWTLISGLPTYVAENGFICNMMNAPADEYFTFQKGPVDETGWVIKNVLSLPIVNKKEDIVGVATFYNRKDGKPFDEHDEYITETLTQFLGWSLLNTDTYDKMNKLENRKDIAQEMLMNQTKATPEEIKSILKFQEKLNVDVIDDCEEKQLVAILKEDLPDPRSAELYEFRFSDFPLTEHGLIKCGIRLFFEINVVEKFKVPVEVLTRWMYTVRKGYRAVTYHNWRHGFNVGQTMFTLLMTGRLKKYYTDLEAFAMLAAAFCHDIDHRGTNNLYQMKSTSPLARLHGSSILERHHLEYSKTLLQDESLNIFQNLNKRQFETVIHLFEVAIIATDLALYFKKRTMFQKIVDACEQMQTEEEAIKYVTVDPTKKEIIMAMMMTACDLSAITKPWEVQSQVALMVANEFWEQGDLERTVLQQQPIPMMDRNKRDELPKLQVGFIDFVCTFVYKEFSRFHKEITPMLSGLQNNRVEWKSLADEYDAKMKVIEEEAKKQEGGAEKAAEDSGGGDDKKSKTCLML
  
Inhibitor
Name:
BDBM50459162
Synonyms:
CHEMBL4218772
Type:
Small organic molecule
Emp. Form.:
C25H21N3O6S
Mol. Mass.:
491.516
SMILES:
COCCNc1cc(O)c2c(c1)oc1c(Cc3ccc4OCOc4c3)[nH]c(-c3nccs3)c1c2=O
Structure:
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