MILVEXIAN

Inhibitor of F11

Structure

SERP Rating

Probe MILVEXIAN is in the process of SERP review.

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Information

Inhibitor

1 µM

Probe Availability:

In Vitro Validations

Uniprot ID: P03951

Target Class: Enzyme

Target SubClass: Peptidase S1 family

Potency: Ki

Potency Value: 0.11 nM

Potency Assay: enzyme activity assay

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

Target aliases:

Coagulation factor XI, F11, FA11_HUMAN, PTA, FXI, ...

DOI Reference: 10.1021/acs.jmedchem.1c00613

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Milvexian was evaluated against a panel of relevant serine proteases.

Probe Selectivity in Vitro:

Ki values for evaluated serine proteases: factor XIa 0.11, factor VIIab 1200, factor IXa >27 000, factor Xa >13 000, factor XIIa >3000, plasma kallikrein 44, tissue kallikrein-1 >11 000, thrombin 1200, trypsin 720, activated protein C >21 000, plasmin 2650, TPA 2300, urokinase 3900, chymotrypsin 35, neutrophil elastase >8000, neutrophil cathepsin G >20 000, neutrophil proteinase 3 >12 000, mast cell chymase >13 000

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SERP ratings and comments

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