Binding affinities for histamine receptors 1 to 4: Systematic comparison of ligands from the Psychoactive Drug Screening Program Ki database and International Union of Basic and Clinical Pharmacology/British Pharmacological Society Guide to Pharmacology
Abstract
Histamine receptors (H1R-H4R) are G protein-coupled receptors with large physiological and therapeutic relevance. Despite extensive research, a systematic and cross-database overview of ligands is missing. This review integrates the Psychoactive Drug Screening Program (PDSP) Ki database and the International Union of Basic and Clinical Pharmacology/British Pharmacological Society (IUPHAR/BPS) Guide to Pharmacology, both having different scopes and curation principles, and evaluates concordance of HxR ligands across databases and experimental systems. Binding affinities (Ki) for 302 ligands targeting recombinant human HxR were extracted from the PDSP Ki database (accessed January 2026) and converted to pKi. A total of 302 ligands with relevant binding affinities were identified, including approved drugs and experimental compounds. Functional annotations and further binding affinities were retrieved from the IUPHAR/BPS Guide to Pharmacology and complementary literature, revealing missing or incomplete functional characterization for 69 ligands. Although most ligands were selective for a single HxR, others displayed multireceptor affinity. Cross-database comparisons found limited overlap in ligands, differences in primary literature, and pKi deviations. Comparisons with native human tissues and nonhuman species demonstrated substantial variability, with deviations of up to pKi 4.2 in human brain tissues and up to pKi 3.2 across species. This database-driven analysis highlights…
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