Reaction Details |
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Target | cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A |
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Ligand | BDBM50130841 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1525202 (CHEMBL3635513) |
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IC50 | 4.3±n/a nM |
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Citation | Lingam, VS; Dahale, DH; Rathi, VE; Shingote, YB; Thakur, RR; Mindhe, AS; Kummari, S; Khairatkar-Joshi, N; Bajpai, M; Shah, DM; Sapalya, RS; Gullapalli, S; Gupta, PK; Gudi, GS; Jadhav, SB; Pattem, R; Thomas, A Design, Synthesis, and Pharmacological Evaluation of 5,6-Disubstituted Pyridin-2(1H)-one Derivatives as Phosphodiesterase 10A (PDE10A) Antagonists. J Med Chem58:8292-308 (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: | PDE10_RAT | Pde10a | Phosphodiesterase 10 | Phosphodiesterase 10A (PDE10A2) | Phosphodiesterase Type 10 (PDE10A) | Rat recombinant PDE10a (rPDE10a) |
Type: | Enzyme |
Mol. Mass.: | 90160.88 |
Organism: | Rattus norvegicus (rat) |
Description: | PDE10A was generated from the full-length recombinant rat clone transfected into Sf9 cells. |
Residue: | 794 |
Sequence: | MEDGPSNNASCFRRLTECFLSPSLTDEKVKAYLSLHPQVLDEFVSESVSAETVEKWLKRK
NNKAEDEPSPKEVSRYQDTNMQGVVYELNSYIEQRLDTGGDNHLLLYELSSIIRIATKAD
GFALYFLGECNNSLCVFTPPGMKEGQPRLIPAGPITQGTTISAYVAKSRKTLLVEDILGD
ERFPRGTGLESGTRIQSVLCLPIVTAIGDLIGILELYRHWGKEAFCLSHQEVATANLAWA
SVAIHQVQVCRGLAKQTELNDFLLDVSKTYFDNIVAIDSLLEHIMIYAKNLVNADRCALF
QVDHKNKELYSDLFDIGEEKEGKPVFKKTKEIRFSIEKGIAGQVARTGEVLNIPDAYADP
RFNREVDLYTGYTTRNILCMPIVSRGSVIGVVQMVNKISGSAFSKTDENNFKMFAVFCAL
ALHCANMYHRIRHSECIYRVTMEKLSYHSICTSEEWQGLMHFNLPARICRDIELFHFDIG
PFENMWPGIFVYMIHRSCGTSCFELEKLCRFIMSVKKNYRRVPYHNWKHAVTVAHCMYAI
LQNNNGLFTDLERKGLLIACLCHDLDHRGFSNSYLQKFDHPLAALYSTSTMEQHHFSQTV
SILQLEGHNIFSTLSSSEYEQVLEIIRKAIIATDLALYFGNRKQLEEMYQTGSLNLHNQS
HRDRVIGLMMTACDLCSVTKLWPVTKLTANDIYAEFWAEGDEMKKLGIQPIPMMDRDKRD
EVPQGQLGFYNAVAIPCYTTLTQILPPTEPLLKACRDNLNQWEKVIRGEETAMWISGPAT
SKSTSEKPTRKVDD
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BDBM50130841 |
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n/a |
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Name | BDBM50130841 |
Synonyms: | CHEMBL3634745 |
Type | Small organic molecule |
Emp. Form. | C27H19FN2O2 |
Mol. Mass. | 422.4504 |
SMILES | Fc1ccc(cc1)-c1[nH]c(=O)ccc1-c1ccc(OCc2ccc3ccccc3n2)cc1 |
Structure |
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