ERKi

ERKi : Inhibitor of MAPK1, MAPK3

Structure

SERP Rating

In Cells

(3 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.

Information

MAPK1
MAPK3

Inhibitor

1 uM
Reviewer recommended concentration: 1-5 µM may be more suitable in some cell lines

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: P28482

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 1.8 nM

Potency Assay: ERK Biochemical Assay

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

Target aliases:

, Mitogen-activated protein kinase 1, PRKM2, PRKM1 ...

DOI Reference: 10.7554/eLife.34311

Uniprot ID: P28482

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 4 nM

Potency Assay: Invitrogen kinase screen (MAPK1)

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

Target aliases:

, Mitogen-activated protein kinase 1, PRKM2, PRKM1 ...

DOI Reference: 10.7554/eLife.34311

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family: Invitrogen kinase panel. Closest off targets: GSK3A = 0.21 µM, SGK1 = 0.27 µM, GSK3B = 0.54 µM, GRK2 (ADRBK1) = 0.59 µM, TBK1 = 0.77 µM, CDK2 = 0.79 µM, STK26 (MST4) = 0.88 µM, CLK2 = 0.94 µM, PRKG2 = 0.95 µM, CDK5 = 1.2 µM, ROCK1 = 1.2 µM, ROCK2 = 1.4 µM, MARK2 = 1.4 µM. Selectivity outside target family: Profiled in a panel of 116 enzymes and receptors at MDS Pharma/Taiwan: only one unconfirmed hit, PDE3A (61% @ 10 µM) is > 1000-fold MAPK1/3 potency; Clean GPCR scan

Probe Selectivity in Cell:

NanoBRET results: GSK3A, SGK1, GSK3B, GRK2 and TBK1 (IC50 > 20µM)

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

ERKi is a suitable probe for interrogating ERK1/2 activity in cell culture models. It should provide value as an orthogonal probe alongside other ERK ligands such as SCH772984 as more data becomes available.

(last updated: 2 Feb 2022 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

This is a good additional probe for ERK. As with almost all kinase probes, it's best to also test ERK inhibitors from different scaffolds to ensure any effects are target related.

(last updated: 16 Feb 2022 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

The assumption is that the probe is ATP competitive. May be used in parallel with orthogonal probe SCH772984. Good selectivity; and reassuring to see that the enantiomer is inactive. Insufficient evidence to endorse as an in vivo probe - particularly low PO %F in rat.

(last updated: 7 Aug 2023 )