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Target
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A
Ligand
BDBM50151605
Substrate
n/a
Meas. Tech.
ChEMBL_306668 (CHEMBL832269)
IC50
29300±n/a nM
Citation
 Lorthiois, E; Bernardelli, P; Vergne, F; Oliveira, C; Mafroud, AK; Proust, E; Heuze, L; Moreau, F; Idrissi, M; Tertre, A; Bertin, B; Coupe, M; Wrigglesworth, R; Descours, A; Soulard, P; Berna, P Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 1. Bioorg Med Chem Lett 14:4623-6 (2004) [PubMed]  Article 
Target
Name:
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A
Synonyms:
3',5'-cyclic phosphodiesterase | CGI-PDE A | Cyclic GMP-inhibited phosphodiesterase A | PDE3A | PDE3A_HUMAN | Phosphodiesterase 3 | Phosphodiesterase 3 (PDE3) | Phosphodiesterase 3 and 5 (PDE3 and PDE5) | Phosphodiesterase 3A | Phosphodiesterase 3A (PDE3A) | Phosphodiesterase 3A (PDE3A1) | Phosphodiesterase Type 3 (PDE3A) | cGMP-inhibited 3',5'-cyclic phosphodiesterase A | cGMP-inhibited 3,5-cyclic phosphodiesterase A
Type:
Enzyme
Mol. Mass.:
124966.46
Organism:
Homo sapiens (Human)
Description:
Q14432
Residue:
1141
Sequence:
MAVPGDAARVRDKPVHSGVSQAPTAGRDCHHRADPASPRDSGCRGCWGDLVLQPLRSSRKLSSALCAGSLSFLLALLVRLVRGEVGCDLEQCKEAAAAEEEEAAPGAEGGVFPGPRGGAPGGGARLSPWLQPSALLFSLLCAFFWMGLYLLRAGVRLPLAVALLAACCGGEALVQIGLGVGEDHLLSLPAAGVVLSCLAAATWLVLRLRLGVLMIALTSAVRTVSLISLERFKVAWRPYLAYLAGVLGILLARYVEQILPQSAEAAPREHLGSQLIAGTKEDIPVFKRRRRSSSVVSAEMSGCSSKSHRRTSLPCIPREQLMGHSEWDHKRGPRGSQSSGTSITVDIAVMGEAHGLITDLLADPSLPPNVCTSLRAVSNLLSTQLTFQAIHKPRVNPVTSLSENYTCSDSEESSEKDKLAIPKRLRRSLPPGLLRRVSSTWTTTTSATGLPTLEPAPVRRDRSTSIKLQEAPSSSPDSWNNPVMMTLTKSRSFTSSYAISAANHVKAKKQSRPGALAKISPLSSPCSSPLQGTPASSLVSKISAVQFPESADTTAKQSLGSHRALTYTQSAPDLSPQILTPPVICSSCGRPYSQGNPADEPLERSGVATRTPSRTDDTAQVTSDYETNNNSDSSDIVQNEDETECLREPLRKASACSTYAPETMMFLDKPILAPEPLVMDNLDSIMEQLNTWNFPIFDLVENIGRKCGRILSQVSYRLFEDMGLFEAFKIPIREFMNYFHALEIGYRDIPYHNRIHATDVLHAVWYLTTQPIPGLSTVINDHGSTSDSDSDSGFTHGHMGYVFSKTYNVTDDKYGCLSGNIPALELMALYVAAAMHDYDHPGRTNAFLVATSAPQAVLYNDRSVLENHHAAAAWNLFMSRPEYNFLINLDHVEFKHFRFLVIEAILATDLKKHFDFVAKFNGKVNDDVGIDWTNENDRLLVCQMCIKLADINGPAKCKELHLQWTDGIVNEFYEQGDEEASLGLPISPFMDRSAPQLANLQESFISHIVGPLCNSYDSAGLMPGKWVEDSDESGDTDDPEEEEEEAPAPNEEETCENNESPKKKTFKRRKIYCQITQHLLQNHKMWKKVIEEEQRLAGIENQSLDQTPQSHSSEQIQAIKEEEEEKGKPRGEEIPTQKPDQ
  
Inhibitor
Name:
BDBM50151605
Synonyms:
4-[8''-chloro-2''-oxospiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-6-yl]phenyl-4-methylhexahydro-1-pyrazinylmethanone | CHEMBL183465
Type:
Small organic molecule
Emp. Form.:
C25H29ClN4O2
Mol. Mass.:
452.976
SMILES:
CN1CCN(CC1)C(=O)c1ccc(cc1)-c1cc(Cl)c2NC(=O)NC3(CCCCC3)c2c1
Structure:
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