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Target
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A
Ligand
BDBM50238419
Substrate
n/a
Meas. Tech.
ChEMBL_1663231 (CHEMBL4012912)
IC50
50119±n/a nM
Citation
 Thomson, DW; Wagner, AJ; Bantscheff, M; Benson, RE; Dittus, L; Duempelfeld, B; Drewes, G; Krause, J; Moore, JT; Mueller, K; Poeckel, D; Rau, C; Salzer, E; Shewchuk, L; Hopf, C; Emery, JG; Muelbaier, M Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines. J Med Chem 60:5455-5471 (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:
BDBM50238419
Synonyms:
CHEMBL4060134
Type:
Small organic molecule
Emp. Form.:
C24H22N10O2
Mol. Mass.:
482.19
SMILES:
Cn1cnc(c1)C(=O)N1CCN(CC1)C(=O)c1ccc(Nc2nc3ccccc3n3nnnc23)cc1
Structure:
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