BCX-3607

BCX-3607 Inhibitor of FVII

Structure

SERP Rating

In Cells

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In Model Organisms

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Probe BCX-3607 is in the process of SERP review.

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Information

Inhibitor

In Vitro Validations

Uniprot ID: P08709

Target Class: Enzyme

Target SubClass: Peptidase

Potency: IC50

Potency Value: 4 nM

Potency Assay: Coagulation assay

PDB ID for probe-target interaction (3D structure): 2EC9

Target aliases:

Coagulation factor VII, F7, FA7_HUMAN, SPCA, Serum ...

DOI Reference: 10.1016/j.ejmech.2025.117708

Uniprot ID: P08709

Target Class: Enzyme

Target SubClass: Peptidase

Potency: IC50

Potency Value: 26 nM

Potency Assay: FVIIa-FX activity

PDB ID for probe-target interaction (3D structure): 2EC9

Target aliases:

Coagulation factor VII, F7, FA7_HUMAN, SPCA, Serum ...

DOI Reference: 10.1016/j.ejmech.2025.117708

In Cell Validations

No in Cell Validations available

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity was evaluated sampling BCX-3607 against human proteases, with the selectivity ratio, protease (i) IC50/FVIIa IC50, being represented as Si. BCX-3607 showed excellent selectivity (∼1000) against trypsin, thrombin, APC, and tPA.

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SERP ratings and comments

SERP Ratings

In Model Organisms

SERP Comments:

BCX-3607 is a 4 nM molecular inhibitor of TF FVIIa with a reasonable to good selectivity against related proteases like trypsin, thrombin, FXa or plasmin. The binding and interaction of BCX-3607 and FVIIa is confirmed by xray co-crystal structures and the delay in clotting time is supporting the claimed MoA. However, the cellular activity is weak and the PK profile of the compound does not qualifiy BCX-3607 for in vivo studies. The compound is probably suffering from a limited solubility and a very low fraction unbound, indicated by a very small volume of distribution. As alternative TF FVIIa inhibitors, PCI-27483 or BMS-593214 might be considered.

(last updated: 1 Aug 2025 )