OL-135

OL-135 : Inhibitor of FAAH2

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 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.

Probe OL-135 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

FAAH2
FAAH

Inhibitor

up to 10 uM

Probe Availability:

In Vitro Validations

Uniprot ID: Q6GMR7

Target Class: Enzyme

Target SubClass: Amidase

Potency: Ki

Potency Value: 4.7 nM

Potency Assay: Competitive radioligand displacement

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

Target aliases:

Fatty-acid amide hydrolase 2, AMDD, FAAH2, FAAH2_H ...

DOI Reference: 10.1021/jm049614v

Uniprot ID: Q6GMR7

Target Class: Enzyme

Target SubClass: Amidase

Potency: IC50

Potency Value: 13.4 nM

Potency Assay: Competitive ABPP assay

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

Target aliases:

Fatty-acid amide hydrolase 2, AMDD, FAAH2, FAAH2_H ...

DOI Reference: 10.1074/jbc.M606646200

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity was assessed against KIAA and TGH with IC50 >100 and 0.6 uM. Also in proteomics analysis, OL-135 didn't bind AAD, CD-1, LPL and MAGL as reported in DOI: 10.1124/jpet.104.069401.

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

OL-135 displayed inhibitory activity against recombinant human Fatty-acid amide hydrolase (FAAH) in cell-free assays at low nanomolar concentrations. In T84 cells, it showed inhibitory activity against FAAH at high nanomolar concentrations. Through proteomic investigations, OL-135 was found to selectively inhibit FAAH compared to other hydrolases. OL-135 was also reported to produce several pharmacological activities in vivo after intravenous or intraperitoneal administration (10 mg/kg).

(last updated: 29 Aug 2022 )