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Target
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A
Ligand
BDBM50151635
Substrate
n/a
Meas. Tech.
ChEMBL_306338 (CHEMBL828158)
IC50
11800±n/a nM
Citation
 Bernardelli, P; Lorthiois, E; Vergne, F; Oliveira, C; Mafroud, AK; Proust, E; Pham, N; Ducrot, P; Moreau, F; Idrissi, M; Tertre, A; Bertin, B; Coupe, M; Chevalier, E; Descours, A; Berlioz-Seux, F; Berna, P; Li, M Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 2: Optimization of 5,8-disubstituted derivatives. Bioorg Med Chem Lett 14:4627-31 (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:
BDBM50151635
Synonyms:
8''-chloro-5''-(1H-1,2,3,4-tetraazol-5-ylmethoxy)spiro[cyclohexane-1,4''-(1'',2'',3'',4''-tetrahydroquinazoline)]-2''-one | CHEMBL184861
Type:
Small organic molecule
Emp. Form.:
C15H17ClN6O2
Mol. Mass.:
348.787
SMILES:
Clc1ccc(OCc2nnn[nH]2)c2c1NC(=O)NC21CCCCC1
Structure:
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