Brivanib

Brivanib : ATP competitive inhibitor of KDR

Structure

Information

  • KDR
  • ATP competitive
  • up to 10 uM
  • Reviewer recommended concentration: 1 µM

In Vitro Validations

Uniprot ID: P35968
Target Class: Kinase
Target SubClass: TK
Potency: IC50
Potency Value: 26 nM
Potency Assay: Kinase Assay using [γ-33P]-ATP IC50; 25 nM Ki
PDB ID for probe-target interaction (3D structure): --
Structure-activity relationship: yes
Target aliases:
Vascular endothelial growth factor receptor 2, VEG ...

DOI Reference: 10.1021/jm051106d

Uniprot ID: P35968
Target Class: Kinase
Target SubClass: TK
Potency: Ki
Potency Value: 25 nM
Potency Assay: Kinase Assay using [γ-33P]-ATP
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Vascular endothelial growth factor receptor 2, VEG ...

DOI Reference: 10.1021/jm051106d

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency end-point : IC50 FLK1 89 nM, FGFR1 148 nM
Probe Selectivity in Vitro:

Kinase Selectivity IC50 (nM): VEGFR-1 380, FGFR-1 148, PDGFR-β >6000, EGFR >1900, LCK >2500, PKCα >25000, JAK-3 >50000

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

Brivanib (BMS-540215) is a potent ATP-competitive inhibitor of KDR (VEGFR2) kinase. Due to limited selectivity data (only KDR plus seven additional kinases were tested), additional data would be necessary before considering this compound as a tool compound.

(last updated: 19 Oct 2025 )