BAY-7598

Inhibitor of MMP12

Structure

SERP Rating

Probe BAY-7598 is in the process of SERP review.

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Information

MMP12

Inhibitor

< 10 nM

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

In Vitro Validations

Uniprot ID: P39900

Target Class: Enzyme

Target SubClass: Metallopeptidase

Potency: IC50

Potency Value: 0.085 nM

Potency Assay: Biochemical assay

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

Target aliases:

Macrophage metalloelastase, HME, MMP12, MMP12_HUMA ...

Other Reference: SGC

Uniprot ID: P39900

Target Class: Enzyme

Target SubClass: Metallopeptidase

Potency: Kd

Potency Value: 0.004 nM

Potency Assay: Biophysical assay (SPR biosensor-based assay)

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

Target aliases:

Macrophage metalloelastase, HME, MMP12, MMP12_HUMA ...

Other Reference: SGC

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

> 100 fold selectivity vs all other human MMPs tested (> 40 fold selectivity of rodent ortholog MMP12 vs all rodent MMPs tested), closest off-targets: MMP10 (IC50 = 13 nM), MMP8 (IC50 = 15 nM). No relevant activity in panel of 68 off-targets (@ 10 µM compound conc.); clean GPCR scan

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SERP ratings and comments

No SERP comments found for BAY-7598