BAY-885

Inhibitor of MAPK7

Structure

Information

  • MAPK7
  • Inhibitor

In Vitro Validations

Uniprot ID: Q13164
Target Class: Protein kinase
Target SubClass: CMGC
Potency: IC50
Potency Value: 35 nM (@250 uM ATP)
Potency Assay: High-throughput TR-FRET-based kinase inhibition assay was used to identify potential ERK5 inhibitors
PDB ID for probe-target interaction (3D structure): 6HKM
Structure-activity relationship: yes see DOI:10.1021/acs.jmedchem.8b01606
Target aliases:
Mitogen-activated protein kinase 7, PRKM7, ERK5, B ...

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity against Eurofins kinase panel at 1 μM (350 kinases were tested). Residual kinase activity below 50% reported for FER (h): 38%, EPHB3 (h): 42%, EPHA5 (h): 57%. For other kinases, residual activity reported ≥ 80%.

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SERP ratings and comments


SERP Ratings

In Cell Rating

SERP Comments:

BAY-885 is an excellent inhibitor of ERK5.  It is potent, selective against other kinases and bromodomain-containing proteins, and active in cells.  There is not an inactive close analogue that is commercially available, so it could be useful to perform experiments of BAY-885 alongside the other commercially available ERK5 inhibitor, AX15836, for establishment of biology of ERK5’s kinase activity.

(last updated: 22 May 2020 )

SERP Ratings

In Cell Rating

SERP Comments:

1 uM is a reasonable maximum concentration to ensure ERK5 inhibition while not perturbing many other kinases. However, care should be taken in phenotypic assays to rule out inhibition of FER and ephrin kinases being responsible for observed phenotype at 1 uM.

(last updated: 4 Jul 2020 )

SERP Ratings

In Cell Rating

SERP Comments:

Key publication should be made public in a preprint server.
 
 

(last updated: 30 Jul 2020 )