PF3644022

ATP-competitive inhbitor of MAPKAPK2

Structure

Information

Protein target names: MAPKAPK2

Mechanism of action: ATP-competitive inhbitor

Recommended in-cell concentration:
200-900 nM

In Vitro Validations

Uniprot ID: P49137
Target Class: Kinase
Target SubClass: CAMK
Potency: Ki
Potency Value: 3 nM
PDB ID for probe-target interaction (3D structure): --
Target aliases:
MAP kinase-activated protein kinase 2, MAPKAPK2, M ...

DOI Reference: 10.1124/jpet.110.166173

Uniprot ID: P49137
Target Class: Kinase
Target SubClass: CAMK
Potency: Kd
Potency Value: 5.9 nM
PDB ID for probe-target interaction (3D structure): 3FYJ 6T8X
Target aliases:
MAP kinase-activated protein kinase 2, MAPKAPK2, M ...

DOI Reference: 10.1124/jpet.110.166173

Uniprot ID: P49137
Target Class: Kinase
Target SubClass: CAMK
Potency: IC50
Potency Value: 5.2 nM
PDB ID for probe-target interaction (3D structure): 3FYJ 6T8X
Target aliases:
MAP kinase-activated protein kinase 2, MAPKAPK2, M ...

DOI Reference: 10.1124/jpet.110.166173

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 16 May 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

PF3644022 is not a super selective chemical probe. It may, however, represent one of the better choices for studying MAPKAPK2, as a selective chemical probe is not currently available in the literature.

(last updated: 15 Jun 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

This compound was originally described by Pfizer in a publication in 2010 (J Pharmacol Exp Ther. 2010 Jun; 333(3): 797-807). It has high potency towards MK2 (Ki = 3 nM) as well as PRAK (IC50 = 5 nM), MK2 (IC50 = 53 nM) and MNK2 (IC50 = 148 nM). It did not have significant activity against most of the ~200 other kinases against which it was profiled. It had significant activity (IC50 <100 nM) against the following kinases: BRSK2, CAMKII, DRAK1, PIM1, PRAK, ASK1, and MER. It is not known to what extent it has activity outside the kinome.

(last updated: 9 Sept 2016 )