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Target
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A
Ligand
BDBM50258896
Substrate
n/a
Meas. Tech.
ChEBML_1690776
IC50
>30000±n/a nM
Citation
 Mikami, S; Nakamura, S; Ashizawa, T; Nomura, I; Kawasaki, M; Sasaki, S; Oki, H; Kokubo, H; Hoffman, ID; Zou, H; Uchiyama, N; Nakashima, K; Kamiguchi, N; Imada, H; Suzuki, N; Iwashita, H; Taniguchi, T Discovery of Clinical Candidate N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915): A Highly Potent, Selective, and Brain-Penetrating Phosphodiesterase 2A Inhibitor for the Treatment of Cognitive Disorders. J Med Chem 60:7677-7702 (2017) [PubMed]  Article 
Target
Name:
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A
Synonyms:
Phosphodiesterase 3A (PDE3A) | Phosphodiesterase Type 3 (PDE3A) | Cyclic GMP-inhibited phosphodiesterase A | cGMP-inhibited 3,5-cyclic phosphodiesterase A | Phosphodiesterase 3A | Phosphodiesterase 3A (PDE3A1) | CGI-PDE A | cGMP-inhibited 3',5'-cyclic phosphodiesterase A | PDE3A_HUMAN | PDE3A | 3',5'-cyclic phosphodiesterase | Phosphodiesterase 3 (PDE3) | Phosphodiesterase 3 | Phosphodiesterase 3 and 5 (PDE3 and PDE5)
Type:
Enzyme
Mol. Mass.:
124966.46
Organism:
Human
Description:
Q14432
Residue:
1141
Sequence:
MAVPGDAARVRDKPVHSGVSQAPTAGRDCHHRADPASPRDSGCRGCWGDLVLQPLRSSRKLSSALCAGSLSFLLALLVRLVRGEVGCDLEQCKEAAAAEEEEAAPGAEGGVFPGPRGGAPGGGARLSPWLQPSALLFSLLCAFFWMGLYLLRAGVRLPLAVALLAACCGGEALVQIGLGVGEDHLLSLPAAGVVLSCLAAATWLVLRLRLGVLMIALTSAVRTVSLISLERFKVAWRPYLAYLAGVLGILLARYVEQILPQSAEAAPREHLGSQLIAGTKEDIPVFKRRRRSSSVVSAEMSGCSSKSHRRTSLPCIPREQLMGHSEWDHKRGPRGSQSSGTSITVDIAVMGEAHGLITDLLADPSLPPNVCTSLRAVSNLLSTQLTFQAIHKPRVNPVTSLSENYTCSDSEESSEKDKLAIPKRLRRSLPPGLLRRVSSTWTTTTSATGLPTLEPAPVRRDRSTSIKLQEAPSSSPDSWNNPVMMTLTKSRSFTSSYAISAANHVKAKKQSRPGALAKISPLSSPCSSPLQGTPASSLVSKISAVQFPESADTTAKQSLGSHRALTYTQSAPDLSPQILTPPVICSSCGRPYSQGNPADEPLERSGVATRTPSRTDDTAQVTSDYETNNNSDSSDIVQNEDETECLREPLRKASACSTYAPETMMFLDKPILAPEPLVMDNLDSIMEQLNTWNFPIFDLVENIGRKCGRILSQVSYRLFEDMGLFEAFKIPIREFMNYFHALEIGYRDIPYHNRIHATDVLHAVWYLTTQPIPGLSTVINDHGSTSDSDSDSGFTHGHMGYVFSKTYNVTDDKYGCLSGNIPALELMALYVAAAMHDYDHPGRTNAFLVATSAPQAVLYNDRSVLENHHAAAAWNLFMSRPEYNFLINLDHVEFKHFRFLVIEAILATDLKKHFDFVAKFNGKVNDDVGIDWTNENDRLLVCQMCIKLADINGPAKCKELHLQWTDGIVNEFYEQGDEEASLGLPISPFMDRSAPQLANLQESFISHIVGPLCNSYDSAGLMPGKWVEDSDESGDTDDPEEEEEEAPAPNEEETCENNESPKKKTFKRRKIYCQITQHLLQNHKMWKKVIEEEQRLAGIENQSLDQTPQSHSSEQIQAIKEEEEEKGKPRGEEIPTQKPDQ
  
Inhibitor
Name:
BDBM50258896
Synonyms:
CHEMBL4060569 | US11419874, TAK-915
Type:
Small organic molecule
Emp. Form.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD
Structure:
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