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Target
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A [432-779]
Ligand
BDBM14361
Substrate
BDBM10851
Meas. Tech.
Phosphodiesterase (PDE) Inhibition Assay
IC50
140000±n/a nM
Citation
 Card, GL; England, BP; Suzuki, Y; Fong, D; Powell, B; Lee, B; Luu, C; Tabrizizad, M; Gillette, S; Ibrahim, PN; Artis, DR; Bollag, G; Milburn, MV; Kim, SH; Schlessinger, J; Zhang, KY Structural basis for the activity of drugs that inhibit phosphodiesterases. Structure 12:2233-47 (2004) [PubMed]  Article 
Target
Name:
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A [432-779]
Synonyms:
PDE10A | PDE10_HUMAN | Phosphodiesterase Type 10 (PDE10A) | cAMP and cAMP-inhibited cGMP 3,5-cyclic phosphodiesterase 10A
Type:
Enzyme Catalytic Domain
Mol. Mass.:
40036.62
Organism:
Homo sapiens (Human)
Description:
Recombinant catalytic domain (M432-D779) of human PDE10A.
Residue:
348
Sequence:
MEKLSYHSICTSEEWQGLMQFTLPVRLCKEIELFHFDIGPFENMWPGIFVYMVHRSCGTSCFELEKLCRFIMSVKKNYRRVPYHNWKHAVTVAHCMYAILQNNHTLFTDLERKGLLIACLCHDLDHRGFSNSYLQKFDHPLAALYSTSTMEQHHFSQTVSILQLEGHNIFSTLSSSEYEQVLEIIRKAIIATDLALYFGNRKQLEEMYQTGSLNLNNQSHRDRVIGLMMTACDLCSVTKLWPVTKLTANDIYAEFWAEGDEMKKLGIQPIPMMDRDKKDEVPQGQLGFYNAVAIPCYTTLTQILPPTEPLLKACRDNLSQWEKVIRGEETATWISSPSVAQKAAASED
  
Inhibitor
Name:
BDBM14361
Synonyms:
(R,S)-Rolipram | 4-(3-cyclopentyloxy-4-methoxy-phenyl)pyrrolidin-2-one | 4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrrolidin-2-one | Adeo | CHEMBL63 | Rolipram
Type:
Small organic molecule
Emp. Form.:
C16H21NO3
Mol. Mass.:
275.3428
SMILES:
COc1ccc(cc1OC1CCCC1)C1CNC(=O)C1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM10851
Synonyms:
(4aR,6R,7R,7aS)-6-(6-amino-9H-purin-9-yl)-2,7-dihydroxy-hexahydro-1,3,5,2-furo[3,2-d][1,3,2]dioxaphosphinin-2-one | (4aR,6R,7R,7aS)-6-(6-amino-9H-purin-9-yl)tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinine-2,7-diol 2-oxide | ADENOSINE-3 ,5 -CYCLIC-MONOPHOSPHATE | Cyclic adenosine monophosphate | cAMP | cid_23902375
Type:
Small organic molecule
Emp. Form.:
C10H12N5O6P
Mol. Mass.:
329.2059
SMILES:
Nc1ncnc2n(cnc12)[C@@H]1O[C@@H]2COP(O)(=O)O[C@H]2[C@H]1O
Structure:
Search PDB for entries with ligand similarity: