3UI7: Discovery Of Orally Active Pyrazoloquinoline As A Potent Pde10 Inhibitor For The Management Of Schizophrenia

Citation:
Abstract
A series of pyrazoloquinoline analogs have been synthesized and shown to bind to PDE10 with high affinity. From the SAR study and our lead optimization efforts, compounds 16 and 27 were found to possess potent oral antipsychotic activity in the MK-801 induced hyperactive rat model.
PDB ID: 3UI7Download
MMDB ID: 95935
PDB Deposition Date: 2011/11/4
Updated in MMDB: 2011/12
Experimental Method:
x-ray diffraction
Resolution: 2.28  Å
Source Organism:
Similar Structures:
Biological Unit for 3UI7: monomeric; determined by author and by software (PISA)
Molecular Components in 3UI7
Label Count Molecule
Protein (1 molecule)
1
Camp and Camp-inhibited Cgmp 3',5'-cyclic Phosphodiesterase 10A(Gene symbol: PDE10A)
Molecule annotation
Chemicals (3 molecules)
1
1
2
1
3
1
* Click molecule labels to explore molecular sequence information.

Citing MMDB
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