BI-4394

BI-4394 : Inhibitor of MMP13

Structure

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Information

MMP13

Inhibitor

Additional Data

SGC image SGC Chemical Probe Collection

Probe Availability:

MCULE

In Vitro Validations

Uniprot ID: P45452

Target Class: Enzyme

Target SubClass: Peptidase

Potency: IC50

Potency Value: 1 nM

Potency Assay: FRET assay

PDB ID for probe-target interaction (3D structure): 5BPA

Target aliases:

Collagenase 3, MMP13, MMP13_HUMAN, MMP-13, Matrix ...

DOI Reference: 10.1021/jm201129m

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family: Highly selective (> 1000-fold) against other matrix metalloproteinases: MMP1 (IC50 > 22 µM), MMP2 (18 µM), MMP3 (> 22 µM), MMP7 (> 22 µM), MMP8 (> 22 µM), MMP9 (8.9 µM), MMP10 (16 µM), MMP12 (> 22 µM) and MMP14 (8.3 µM). Selectivity outside target family: Invitrogen Panel - 18/56 kinases hit > 50 % inhibition at 10 µM, most potent off targets: AURKA (1.3 µM), MAPKAPK2 (1.1 µM), PRKAA1 (1.9 µM), PRKACA (1.6 µM); Clean GPCR scan.

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(last updated: 23 Feb 2022 )