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Target
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A
Ligand
BDBM14769
Substrate
n/a
Meas. Tech.
Enzymatic Assay
pH
7.5±0
Temperature
297.15±0 K
IC50
5e+2±n/a nM
Citation
 Wang, H; Kunz, S; Chen, G; Seebeck, T; Wan, Y; Robinson, H; Martinelli, S; Ke, H Biological and structural characterization of Trypanosoma cruzi phosphodiesterase C and Implications for design of parasite selective inhibitors. J Biol Chem 287:11788-97 (2012) [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:
BDBM14769
Synonyms:
6-(3,4-Dimethoxy-phenyl)-4,5-dimethyl-4,5-dihydro-2H-pyridazin-3-one | 6-(4-(difluoromethoxy)-3-methoxyphenyl)pyridazin-3(2H)-one | 6-(4-Difluoromethoxy-3-methoxy-phenyl)-2H-pyridazin-3-one | 6-[4-(difluoromethoxy)-3-methoxyphenyl]-2,3-dihydropyridazin-3-one | CHEMBL313842 | Zaradaverine | Zardaverine
Type:
Small organic molecule
Emp. Form.:
C12H10F2N2O3
Mol. Mass.:
268.2162
SMILES:
COc1cc(ccc1OC(F)F)-c1ccc(=O)[nH]n1
Structure:
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