Chemical Probes logo

SB-612111

SB-612111 : NOP antagonist of OPRL1

Structure

Information

  • OPRL1
  • Antagonist
  • 300 nM, can be used up to 1 uM

In Vitro Validations

Uniprot ID: P41146
Target Class: GPCR
Target SubClass: Opioid receptor
Potency: Ki
Potency Value: 0.33 ± 0.03 nM
Potency Assay: Competitive radioligand binding assays using membranes prepared from clonal cell lines
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Nociceptin receptor, ORL1, OOR, OPRL1, OPRX_HUMAN, ...

DOI Reference: 10.1124/jpet.103.055848

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency end-point : Ki ORL-1 57.6 ± 8.0 nM
Potency assay (off target): Competitive radioligand binding assays using membranes prepared from clonal cell lines
Probe Selectivity in Vitro:

SB-612111 is highly selective versus μ-(174-fold), δ-(6391-fold), and κ (486-fold)-opioid receptors. Ki nM:  μ- 57.6 ± 8.0,  δ- 2109 ± 570, κ- 160.5 ± 22.4. SB-612111 was tested at a concentration of 10 μM by CEREP in a broad profile of radioligand binding assays specific for different classes of receptors, ion channels, and enzymes. The highest measured affinity interaction of SB-612111, to the β3-adrenergic receptor, was >260-fold weaker than its interaction with the ORL-1 receptor.

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

Note:  SB-612111 appears to be slowly reversible.  From Spagnolo 2007 “Apart from antagonist potency, the reversibility test conducted in the mouse vas deferens experiments demonstrated another important difference between SB-612111 and (±)J113397. In fact, (±)J-113397 effects could be reversed by washing the tissues, whereas those of SB-612111 were not affected even after 3 h of washing.”

(last updated: 25 Jul 2021 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 4 Aug 2021 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 5 Aug 2021 )