Reaction Details |
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Target | cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A |
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Ligand | BDBM50219268 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_457131 (CHEMBL940740) |
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IC50 | 130±n/a nM |
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Citation | Kuang, R; Shue, HJ; Blythin, DJ; Shih, NY; Gu, D; Chen, X; Schwerdt, J; Lin, L; Ting, PC; Zhu, X; Aslanian, R; Piwinski, JJ; Xiao, L; Prelusky, D; Wu, P; Zhang, J; Zhang, X; Celly, CS; Minnicozzi, M; Billah, M; Wang, P Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors. Bioorg Med Chem Lett17:5150-4 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A |
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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
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BDBM50219268 |
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n/a |
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Name | BDBM50219268 |
Synonyms: | CHEMBL399298 | tert-butyl (R)-1-(5-(aminomethyl)-2-(8-methoxy-2-(trifluoromethyl)quinolin-5-yl)oxazole-4-carbonyl)pyrrolidin-3-ylcarbamate |
Type | Small organic molecule |
Emp. Form. | C25H28F3N5O5 |
Mol. Mass. | 535.5155 |
SMILES | COc1ccc(-c2nc(C(=O)N3CC[C@H](C3)NC(=O)OC(C)(C)C)c(CN)o2)c2ccc(nc12)C(F)(F)F |
Structure |
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