BAY1125976

Allosteric Inhibitor of AKT2, AKT1

Structure

Information

Protein target names: AKT2, AKT1

Mechanism of action: Allosteric Inhibitor

Recommended in-cell concentration:
up to 300 nM

In Vitro Validations

Uniprot ID: P31751
Target Class: Kinase
Target SubClass: AGC
Potency: IC 50
Potency Value: 18/36 nM Hi/Lo ATP
Potency Assay: TR‐FRET‐based in vitro kinase assays
PDB ID for probe-target interaction (3D structure): --
Target aliases:
RAC-beta serine/threonine-protein kinase, AKT2, AK ...

DOI Reference: 10.1002/ijc.30457

In Cell Validations

In Vivo Data

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SERP ratings and comments


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Comments:

There are several inhibitors of this class, including  Miransertib (ARQ092), MK2206, and  Borussertib.  Miransertib has some advantages with PK (particularly longer half-life:  https://pubs.acs.org/doi/full/10.1021/acs.jmedchem.6b00619) and borussertib is a covalaent inhibitor and may offer some PD advantages depending on AKT1/2 turnover in a given cell type.

(last updated: 4 Nov 2020 )

SERP Ratings

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(last updated: 12 Nov 2020 )

SERP Ratings

In Cell Rating
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(last updated: 17 Nov 2020 )