Ki Summary

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Target

cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A [432-779]

Ligand

BDBM14776

Substrate/Competitor

BDBM10851

Meas. Tech.

Phosphodiesterase (PDE) Inhibition Assay

IC50

880±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. Structure12:2233-47 (2004) [PubMed] Article

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Get all data from this article, Solution Info, Assay Method

cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A [432-779]

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:

MEKLSYHSICTSEEWQGLMQFTLPVRLCKEIELFHFDIGPFENMWPGIFVYMVHRSCGTS
CFELEKLCRFIMSVKKNYRRVPYHNWKHAVTVAHCMYAILQNNHTLFTDLERKGLLIACL
CHDLDHRGFSNSYLQKFDHPLAALYSTSTMEQHHFSQTVSILQLEGHNIFSTLSSSEYEQ
VLEIIRKAIIATDLALYFGNRKQLEEMYQTGSLNLNNQSHRDRVIGLMMTACDLCSVTKL
WPVTKLTANDIYAEFWAEGDEMKKLGIQPIPMMDRDKKDEVPQGQLGFYNAVAIPCYTTL
TQILPPTEPLLKACRDNLSQWEKVIRGEETATWISSPSVAQKAAASED

BDBM14776

BDBM10851

Name

BDBM14776

Synonyms:

2-{2-ethoxy-5-[(4-ethylpiperazine-1-)sulfonyl]phenyl}-5-methyl-7-propyl-3H,4H-imidazo[1,5-a][1,2,4]triazin-4-one | CHEMBL1520 | Vardenafil | citric acid;2-[2-ethoxy-5-(4-ethylpiperazino)sulfonyl-phenyl]-5-methyl-7-propyl-1H-imidazo[5,1-f][1,2,4]triazin-4-one

Type

Small organic molecule

Emp. Form.

C23H32N6O4S

Mol. Mass.

488.603

SMILES

CCCc1nc(C)c2n1nc([nH]c2=O)-c1cc(ccc1OCC)S(=O)(=O)N1CCN(CC)CC1

Structure