VIP36

VIP36 : Agonist of CNR1

Structure

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Information

CNR1

Agonist

up to 100 nM

In Vitro Validations

Uniprot ID: P21554

Target Class: GPCR

Target SubClass: Cannabinoid receptor

Potency: Ki

Potency Value: 22 nM

Potency Assay: radioligand competition assay

PDB ID for probe-target interaction (3D structure): 9b54

Target aliases:

Cannabinoid receptor 1, CNR, CNR1, CNR1_HUMAN, CB1 ...

DOI Reference: 10.1038/s41586-025-08618-7

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): Functional selectivity for CB1 over CB2 receptors was also confirmed by in-cell cAMP and biochemical guanosine triphosphate (GTP) turnover assays

Potency assay (off target): Selectivity over a broad range of targets was tested in binding assays (approximately 45 CNS targets) and functional assays (320 targets) through the National Institute of Mental Health’s Psychoactive Drug Screening Program screening, as well as CardioAlert, such as human Ether-à-go-go-Related Gene (hERG) and 5HT2B. Other identified off-targets included µOR and somatostatin receptor 4 (SSTR4). Follow-up assays revealed that VIP36 had reasonable to high selectivity for CB1 over all probed targets.

Potency assay, off target (cells): No measurable potency and low efficacy were observed in BRET Gi1 assays on MOR. No measurable efficacy and potency observed for VIP36 in 5-HT2b receptor.

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