ZK756326 is a full agonist of CCR8（Chemokine receptor 8） with an IC50 of 1.8 μM, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1.
ZK 756326 effectively blocks the attachment of the CCL1, with an IC50 of 1.8 μM. It acts as a complete agonist for CCR8, inducing a dose-dependent rise in intracellular calcium and diminishing the receptor's responsiveness to CCL1. ZK 756326 also prompts extracellular acidification in cells that express human CCR8. To assess the specificity of ZK 756326 for CCR8, binding competition assays are conducted on a range of other G-protein-coupled receptors. In these tests, ZK 756326, at a concentration of 50 μM, demonstrates more than 28-fold specificity for CCR8 over 26 other GPCRs, which all show IC50 values above 50 μM. However, ZK 756326 exhibits less specificity against serotonergic receptors 5-HT1A, 5-HT2B, 5-HT2C, 5-HT5A, 5-HT6, and the adrenergic receptor α2A, with respective IC50 values of 5.4, 4.4, 34.8, 16, 5.9, and less than 20 μM (with 65% inhibition at 20 μM). Given that ZK 756326 displays no agonist activity at concentrations up to 10 μM on 5-HT1A in a GTPγS binding assay, it is unlikely to act as an agonist on these biogenic amine receptors[1].
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