BAY-405

BAY-405 : ATP competitive inhibitor of MAP4K

Structure

SERP Rating

Probe BAY-405 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

MAP4K1

ATP competitive

up to 5 uM

Probe Availability:

MedKoo

In Vitro Validations

Uniprot ID: Q92918

Target Class: Kinase

Target SubClass: STE

Potency: IC50

Potency Value: 6.2 nM

Potency Assay: MAP4K1 binding competition assay

PDB ID for probe-target interaction (3D structure): 8PAR

Target aliases:

Mitogen-activated protein kinase kinase kinase kin ...

DOI Reference: 10.1021/acs.jmedchem.4c01325

Uniprot ID: Q92918

Target Class: Kinase

Target SubClass: STE

Potency: IC50

Potency Value: 11 nM

Potency Assay: Kinase inhibition assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Mitogen-activated protein kinase kinase kinase kin ...

DOI Reference: 10.1021/acs.jmedchem.4c01325

Uniprot ID: Q92918

Target Class: Kinase

Target SubClass: STE

Potency: Kd

Potency Value: 19.7 nM

Potency Assay: SPR

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Mitogen-activated protein kinase kinase kinase kin ...

DOI Reference: 10.1021/acs.jmedchem.4c01325

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Possesses a ROCK2 selectivity ratio of 130 in the biochemical assay and an overall selectivity score of S = 0.080 (80%, 1 μM) against an external kinase panel consisting of 373 kinases. Excellent selectivity was realized against a range of kinases involved in cell cycle regulation, whose inhibition may be associated with decreased ability of T-cells to efficiently proliferate (e.g., CDKs, PLKs, Aurora kinases, checkpoint kinases). Good selectivity was observed against kinases involved in TCR signaling (e.g., ZAP70, Lck, Fyn, Itk, Jak1/2/3 ). The impact of BAY-405 on MAP4K3, a kinase closely related to MAP4K1, showed a modest selectivity ratio of 6.5.

Potency assay, off target (cells): The binding of BAY-405 with submicromolar Kd was confirmed in a cell lysate proteomics-based kinase selectivity assay

I have extra information to add

SERP ratings and comments

No SERP comments found for BAY-405