Modification of the clozapine structure by parallel synthesis.

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Su J, Tang H, McKittrick BA, Burnett DA, Zhang H, Smith-Torhan A, Fawzi A, Lachowicz J

Modification of the clozapine structure by parallel synthesis.

Bioorg Med Chem Lett. 2006 Sep 1;16(17):4548-53. Epub 2006 Jun 27.

PubMed ID

16806922 [ View in PubMed

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Abstract

A structure-activity study based on the core structure of clozapine 1b was accomplished by utilizing high-throughput synthesis. Several focused libraries were designed and synthesized to quickly develop SAR. The results indicate that by varying different regions of clozapine, both D(1)-selective and D(2)-selective compounds can be obtained.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Clozapine	Dopamine D1 receptor	Ki (nM)	132	N/A	N/A	Details
Clozapine	Dopamine D2 receptor	Ki (nM)	208	N/A	N/A	Details