PF-04457845

Covalent Inhibitor of FAAH

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe PF-04457845 is in the process of SERP review.

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Information

FAAH

Covalent Inhibitor

40 nM

DOI - 10.1021/ml100190t

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: O00519

Target Class: Lipid metabolism

Target SubClass: Serine Hydrolase

Potency: IC50

Potency Value: 7.2 nM (human), 7.4 nM (Rat)

Potency Assay: glutamate dehydrogenase-coupled FAAH assay

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

Structure-activity relationship: yes

Target aliases:

Fatty-acid amide hydrolase 1, FAAH1, FAAH, FAAH1_H ...

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity profiling by competitive ABPP, shows no inhibition of ser. Hydrolases. Selectivity of PF-04457845 against the serine hydrolase superfamily of enzymes (>200 members in humans) @ 10 and 100 uM shows no off-targets. Outside target family: PF-04457845 exhibits a favourable selectivity profile when screened against a 68 target CEREP panel @ 10 uM. Low CYP inhibition IC50 ~10 uM.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

An excellent and very selective irreversible inhibitor of FAAH. Preincubation in vitro for 60 min is required to obtain maximum potency. Excellent brain penetration and efficacy with long duration of action after p.o, or i.p. dosing. Target engagement determined with fluorescent probe analogs.

(last updated: 6 May 2021 )