JNJ-42226314

J-42226314 : Competitive reversible inhibitor of MGLL

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 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 JNJ-42226314 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

MGLL

Competitive

up to 10 µM
Reviewer recommended concentration: 100 nM to 1µM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: Q99685

Target Class: Enzyme

Target SubClass: Lipase

Potency: IC50

Potency Value: < 5 nM

Potency Assay: Fluorometric Assay (Inhibition of 4MU-B cleavage)

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

Target aliases:

Monoglyceride lipase, MGLL, MGLL_HUMAN, MAGL, MGL, ...

DOI Reference: 10.1016/j.bmcl.2020.127243

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Serine protease panel (15 proteases) at 10 µM: clean Panel of endocannabinoid related targets: Closest hit is hFAAH with IC50 > 4 µM Outside target family: Kinase Panel: 50 targets, 10 µM ATP at 10 µM, all < 20% inhibition CEREP panel of 50 binding assays at 10 µM (ion channels, receptors, including CB1 and CB2): binding > 50%: rat OPRK1 (66%), rat HTR1B HTR1B (56%), rat chloride ion channel (55%), human SLC6A3 (54%). Follow up in cellular assays (10 µM): OPRK1 (no activity), HTR1B (inhibition 50%) and inhibited dopamine uptake by 35%.

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 26 Oct 2023 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 2 Nov 2023 )