| Reaction Details |
|---|
 | Report a problem with these data |
| Target | cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A |
|---|
| Ligand | BDBM50026820 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | ChEMBL_1438239 (CHEMBL3390271) |
|---|
| IC50 | 106±n/a nM |
|---|
| Citation |  Buijnsters, P; De Angelis, M; Langlois, X; Rombouts, FJ; Sanderson, W; Tresadern, G; Ritchie, A; Trabanco, AA; VanHoof, G; Roosbroeck, YV; Andrés, JI Structure-Based Design of a Potent, Selective, and Brain Penetrating PDE2 Inhibitor with Demonstrated Target Engagement. ACS Med Chem Lett5:1049-53 (2014) [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: | 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
|
|
|
|---|
| BDBM50026820 |
|---|
| n/a |
|---|
| Name | BDBM50026820 |
|---|
| Synonyms: | CHEMBL3331513 | US9669035, B-10 |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C22H22ClN5O2 |
|---|
| Mol. Mass. | 423.895 |
|---|
| SMILES | COc1ccc(Cl)c(c1)-c1nnc2c(C)nc3ccc(CN4CCOCC4)cc3n12 |
|---|
| Structure | 
|
|---|
Search and Browse
