BAY1125976

BAY1125976 : Allosteric inhibitor of AKT2, AKT1

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(3 ratings)

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Information

AKT2
AKT1

Allosteric

up to 300 nM

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Probe Availability:

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

Off-Target Selectivity Assesments

Potency end-point : IC50 AKT3 427 nM @ 10mM ATP

Probe Selectivity in Vitro:

The selectivity of BAY 1125976 was assessed using two different kinase panels: the 230 kinase KinaseProfiler™ and the 468 kinase panel at DiscoveRx: FLT(D835Y), CKL1 and MKNK2 with 210, 310 and 330 nM, respectively

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP 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

In Cell Rating

In Model Organisms

(last updated: 12 Nov 2020 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 17 Nov 2020 )