Reaction Details
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cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A [432-779]
Ligand
BDBM14773
Substrate
BDBM10851
Meas. Tech.
Phosphodiesterase (PDE) Inhibition Assay
IC50
73000±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 More Info.:
Target
Name:
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A [432-779]
Synonyms:
PDE10_HUMAN | PDE10A | cAMP and cAMP-inhibited cGMP 3,5-cyclic phosphodiesterase 10A | Phosphodiesterase Type 10 (PDE10A)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
40036.62
Organism:
Human
Description:
Recombinant catalytic domain (M432-D779) of human PDE10A.
Residue:
348
Sequence:
MEKLSYHSICTSEEWQGLMQFTLPVRLCKEIELFHFDIGPFENMWPGIFVYMVHRSCGTSCFELEKLCRFIMSVKKNYRRVPYHNWKHAVTVAHCMYAILQNNHTLFTDLERKGLLIACLCHDLDHRGFSNSYLQKFDHPLAALYSTSTMEQHHFSQTVSILQLEGHNIFSTLSSSEYEQVLEIIRKAIIATDLALYFGNRKQLEEMYQTGSLNLNNQSHRDRVIGLMMTACDLCSVTKLWPVTKLTANDIYAEFWAEGDEMKKLGIQPIPMMDRDKKDEVPQGQLGFYNAVAIPCYTTLTQILPPTEPLLKACRDNLSQWEKVIRGEETATWISSPSVAQKAAASED
Inhibitor
Name:
BDBM14773
Synonyms:
Ariflo | 4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexane-1-carboxylic acid | SB207499 | 4-cyano-4-(3-cyclopentyloxy-4-methoxy-phenyl)cyclohexane-1-carboxylic acid | Cilomilast
Type:
Small organic molecule
Emp. Form.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD
Substrate
Name:
BDBM10851
Synonyms:
(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 | cid_23902375 | Cyclic adenosine monophosphate | (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 | ADENOSINE-3 ,5 -CYCLIC-MONOPHOSPHATE | cAMP
Type:
Small organic molecule
Emp. Form.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD

