SB-612111

SB-612111 : NOP antagonist of OPRL1

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(3 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Information

Protein target names: OPRL1

Mechanism of action: NOP antagonist

Recommended in-cell concentration:

300 nM, can be used up to 1 uM

Primary References:

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Probe Availability:

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, ...

In Cell Validations

In Vivo Data

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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 )