NAPHTHYRIDINONE

NAPHTHYRIDINONE : Inverse Agonist of CNR1

Structure

SERP Rating

Probe NAPHTHYRIDINONE is in the process of SERP review.

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Information

CNR1

Inverse Agonist

up to 1 uM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: P21554

Target Class: GPCR

Target SubClass: Cannabinoid Receptor

Potency: IC50

Potency Value: 7.5 nM

Potency Assay: Radioligand Binding Assay (CNR1)

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

Target aliases:

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

DOI Reference: 10.1016/j.bmcl.2005.10.028

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

CNR2 is on the order of 1000-fold less potent with 4.6 µM. Shows off-target activity in the GPCR scan: the closest hits are GABA/PBR (Ki = 82 nM) and TMEM97 (Sigma2 receptor) Ki= 605 nM. Outside target family: Screened against a customized panel of assorted radioligand binding and enzymatic assays (MDS Pharma Services, Taipei, Taiwan): no inhibition at 10 µM in 152 of 168 assays. All off-targets are > 100-fold less potent.

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