Reaction Details |
| Report a problem with these data |
Target | cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A |
---|
Ligand | BDBM99037 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_1437292 (CHEMBL3384795) |
---|
IC50 | 2.6±n/a nM |
---|
Citation | Rzasa, RM; Frohn, MJ; Andrews, KL; Chmait, S; Chen, N; Clarine, JG; Davis, C; Eastwood, HA; Horne, DB; Hu, E; Jones, AD; Kaller, MR; Kunz, RK; Miller, S; Monenschein, H; Nguyen, T; Pickrell, AJ; Porter, A; Reichelt, A; Zhao, X; Treanor, JJ; Allen, JR Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility. Bioorg Med Chem22:6570-85 (2015) [PubMed] Article |
---|
More Info.: | Get all data from this article, Assay Method |
---|
|
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A |
---|
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: | MASLEEPLAPRPQGPLPAAGDEPGCGPGKLRPEPRLSAAGGGSAAGPGPAPEWPGRGRAE
RAAPPRPPLSSAGRPSPAGGPGALSARGGGCGWVAARAPLALAFSSRVPSSSPSFFYFWP
PPPPPPPSFLPSSSAFHLPVRLPGREGAAAAAAAGGGGDAGGGGGGGQEAAPLSVPTSSS
HRGGGGSGGGRRRLFLSPALQGLLLPARAGPRPPPPPRLPLGQAARRAGSPGFPGAGPGG
GGQTPRRPQGASFALAAAAALLFGSDMEDGPSNNASCFRRLTECFLSPSLTDEKVKAYLS
LHPQVLDEFVSESVSAETVEKWLKRKNNKSEDESAPKEVSRYQDTNMQGVVYELNSYIEQ
RLDTGGDNQLLLYELSSIIKIATKADGFALYFLGECNNSLCIFTPPGIKEGKPRLIPAGP
ITQGTTVSAYVAKSRKTLLVEDILGDERFPRGTGLESGTRIQSVLCLPIVTAIGDLIGIL
ELYRHWGKEAFCLSHQEVATANLAWASVAIHQVQVCRGLAKQTELNDFLLDVSKTYFDNI
VAIDSLLEHIMIYAKNLVNADRCALFQVDHKNKELYSDLFDIGEEKEGKPVFKKTKEIRF
SIEKGIAGQVARTGEVLNIPDAYADPRFNREVDLYTGYTTRNILCMPIVSRGSVIGVVQM
VNKISGSAFSKTDENNFKMFAVFCALALHCANMYHRIRHSECIYRVTMEKLSYHSICTSE
EWQGLMQFTLPVRLCKEIELFHFDIGPFENMWPGIFVYMVHRSCGTSCFELEKLCRFIMS
VKKNYRRVPYHNWKHAVTVAHCMYAILQNNHTLFTDLERKGLLIACLCHDLDHRGFSNSY
LQKFDHPLAALYSTSTMEQHHFSQTVSILQLEGHNIFSTLSSSEYEQVLEIIRKAIIATD
LALYFGNRKQLEEMYQTGSLNLNNQSHRDRVIGLMMTACDLCSVTKLWPVTKLTANDIYA
EFWAEGDEMKKLGIQPIPMMDRDKKDEVPQGQLGFYNAVAIPCYTTLTQILPPTEPLLKA
CRDNLSQWEKVIRGEETATWISSPSVAQKAAASED
|
|
|
BDBM99037 |
---|
n/a |
---|
Name | BDBM99037 |
Synonyms: | US8497265, 677 |
Type | Small organic molecule |
Emp. Form. | C27H27N5O2 |
Mol. Mass. | 453.5356 |
SMILES | CC(=O)N1CCC(CC1)c1nc2ccccc2nc1OC1CN(C1)c1ccc2ccccc2n1 |
Structure |
|