BindingDB Entry 4895: Antipsychotic Agent Affinities for 5-HT6 and 5-HT7 Receptors

A 2001 study examined the binding affinities of 36 typical and atypical antipsychotic agents for cloned rat 5-HT6 and 5-HT7 receptors. The dataset, sourced from BindingDB, reports Ki values from experiments using transiently expressed COS-7 cells and stably transfected HEK-293 cells. It includes results for agents like clozapine, pimozide, and risperidone, with some affinities reported as low as 0.5 nM.

Use Cases

• Modeling structure-activity relationships based on reported Ki values for antipsychotic agents.
• Classifying typical vs. atypical antipsychotics based on their binding profiles to serotonin receptors.
• Screening for high-affinity drug candidates against 5-HT6 and 5-HT7 receptor targets.
• Analyzing receptor selectivity patterns among dopamine-selective and serotonin-binding antipsychotics.

Strengths

• Includes specific, quantitative Ki values for 36 distinct antipsychotic agents.
• Provides comparative binding data for two distinct serotonin receptor subtypes (5-HT6 and 5-HT7).
• Distinguishes between typical and atypical antipsychotic agents, as well as dopamine-selective agents.

Limitations

• Row count and column-level documentation are absent; field semantics must be inferred after download.
• Last update date is unknown; freshness unverified.
• Data may reflect experimental bias inherent to the specific cell lines and methods described.

Provenance

Source

BindingDB

Collection Method

Experimental data from receptor binding assays in transfected cell lines.

Time Range

Study likely from 2001 (inferred from journal publication date of the described research).

Freshness

Last updated date is unknown.

Geography

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