Reaction Details |
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Target | cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A |
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Ligand | BDBM50129267 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1523367 (CHEMBL3630287) |
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IC50 | 0.940000±n/a nM |
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Citation | Yoshikawa, M; Kamisaki, H; Kunitomo, J; Oki, H; Kokubo, H; Suzuki, A; Ikemoto, T; Nakashima, K; Kamiguchi, N; Harada, A; Kimura, H; Taniguchi, T Design and synthesis of a novel 2-oxindole scaffold as a highly potent and brain-penetrant phosphodiesterase 10A inhibitor. Bioorg Med Chem23:7138-49 (2015) [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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BDBM50129267 |
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n/a |
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Name | BDBM50129267 |
Synonyms: | CHEMBL3629540 |
Type | Small organic molecule |
Emp. Form. | C23H18FN5O4 |
Mol. Mass. | 447.4185 |
SMILES | COc1cn(nc(-c2ccnn2-c2ccccc2)c1=O)-c1ccc(cc1F)N1CCOC1=O |
Structure |
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