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PF3644022

ATP-competitive inhbitor of MAPKAPK2

Structure

Information

  • MAPKAPK2
  • ATP-competitive inhbitor
  • 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

Off-Target Selectivity Assesments

Potency end-point : IC50 MK3 53 nM, PRAK 53 nM, MNK2 148 nM, AMPK 117 nM, BrSK1 187 nM, BrSK2 90 nM, CAMK2 70 nM, DRAK1 71 nM, PIM1 88 nM, ASK1 60 nM, MER 76 nM
Potency assay (off target): At 1 uM, PF3644022 inhibited 16 kinases > 50% out of a panel of 200.
Probe Selectivity in Cell:
PF36644022 did not interfere with the phosphorylation of substrates for p38alpha or JNK.
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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 )