Reaction Details |
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Target | cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A |
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Ligand | BDBM144390 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1849279 (CHEMBL4349820) |
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IC50 | 0.062000±n/a nM |
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Citation | Koizumi, Y; Tanaka, Y; Matsumura, T; Kadoh, Y; Miyoshi, H; Hongu, M; Takedomi, K; Kotera, J; Sasaki, T; Taniguchi, H; Watanabe, Y; Takakuwa, M; Kojima, K; Baba, N; Nakamura, I; Kawanishi, E Discovery of a pyrazolo[1,5-a]pyrimidine derivative (MT-3014) as a highly selective PDE10A inhibitor via core structure transformation from the stilbene moiety. Bioorg Med Chem27:3440-3450 (2019) [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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BDBM144390 |
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n/a |
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Name | BDBM144390 |
Synonyms: | US8969376, 1.006 |
Type | Small organic molecule |
Emp. Form. | C23H25F2N7O |
Mol. Mass. | 453.4877 |
SMILES | Cc1nc2ccc(F)cc2nc1-c1cc2nc(cc(NCC(C)(C)O)n2n1)N1CC[C@@H](F)C1 |r| |
Structure |
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