Reaction Details
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cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Ligand
BDBM50209536
Substrate
n/a
Meas. Tech.
ChEMBL_455270 (CHEMBL886046)
IC50
3±n/a nM
Citation
Cantin, LD; Magnuson, S; Gunn, D; Barucci, N; Breuhaus, M; Bullock, WH; Burke, J; Claus, TH; Daly, M; Decarr, L; Gore-Willse, A; Hoover-Litty, H; Kumarasinghe, ES; Li, Y; Liang, SX; Livingston, JN; Lowinger, T; Macdougall, M; Ogutu, HO; Olague, A; Ott-Morgan, R; Schoenleber, RW; Tersteegen, A; Wickens, P; Zhang, Z; Zhu, J; Zhu, L; Sweet, LJ PDE-10A inhibitors as insulin secretagogues. Bioorg Med Chem Lett 17:2869-73 (2007) [PubMed] Article More Info.:
Target
Name:
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Synonyms:
3',5'-cyclic phosphodiesterase | 3.1.4.17 | PDE10A | PDE10_HUMAN | Phosphodiesterase 10 (PDE10) | Phosphodiesterase 10A
Type:
Protein
Mol. Mass.:
88412.52
Organism:
Homo sapiens (Human)
Description:
Q9Y233
Residue:
1055
Sequence:
MASLEEPLAPRPQGPLPAAGDEPGCGPGKLRPEPRLSAAGGGSAAGPGPAPEWPGRGRAERAAPPRPPLSSAGRPSPAGGPGALSARGGGCGWVAARAPLALAFSSRVPSSSPSFFYFWPPPPPPPPSFLPSSSAFHLPVRLPGREGAAAAAAAGGGGDAGGGGGGGQEAAPLSVPTSSSHRGGGGSGGGRRRLFLSPALQGLLLPARAGPRPPPPPRLPLGQAARRAGSPGFPGAGPGGGGQTPRRPQGASFALAAAAALLFGSDMEDGPSNNASCFRRLTECFLSPSLTDEKVKAYLSLHPQVLDEFVSESVSAETVEKWLKRKNNKSEDESAPKEVSRYQDTNMQGVVYELNSYIEQRLDTGGDNQLLLYELSSIIKIATKADGFALYFLGECNNSLCIFTPPGIKEGKPRLIPAGPITQGTTVSAYVAKSRKTLLVEDILGDERFPRGTGLESGTRIQSVLCLPIVTAIGDLIGILELYRHWGKEAFCLSHQEVATANLAWASVAIHQVQVCRGLAKQTELNDFLLDVSKTYFDNIVAIDSLLEHIMIYAKNLVNADRCALFQVDHKNKELYSDLFDIGEEKEGKPVFKKTKEIRFSIEKGIAGQVARTGEVLNIPDAYADPRFNREVDLYTGYTTRNILCMPIVSRGSVIGVVQMVNKISGSAFSKTDENNFKMFAVFCALALHCANMYHRIRHSECIYRVTMEKLSYHSICTSEEWQGLMQFTLPVRLCKEIELFHFDIGPFENMWPGIFVYMVHRSCGTSCFELEKLCRFIMSVKKNYRRVPYHNWKHAVTVAHCMYAILQNNHTLFTDLERKGLLIACLCHDLDHRGFSNSYLQKFDHPLAALYSTSTMEQHHFSQTVSILQLEGHNIFSTLSSSEYEQVLEIIRKAIIATDLALYFGNRKQLEEMYQTGSLNLNNQSHRDRVIGLMMTACDLCSVTKLWPVTKLTANDIYAEFWAEGDEMKKLGIQPIPMMDRDKKDEVPQGQLGFYNAVAIPCYTTLTQILPPTEPLLKACRDNLSQWEKVIRGEETATWISSPSVAQKAAASED
Inhibitor
Name:
BDBM50209536
Synonyms:
4-[3-cyano-2-(2'-ethoxy-biphenyl-4-yl)-6-fluoro-quinolin-4-ylamino]-butyric acid | CHEMBL393646
Type:
Small organic molecule
Emp. Form.:
C28H24FN3O3
Mol. Mass.:
469.5069
SMILES:
CCOc1ccccc1-c1ccc(cc1)-c1nc2ccc(F)cc2c(NCCCC(O)=O)c1C#N
Structure:
