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Assay Detail

CHEMBL4681218

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of fibronectin binding to human recombinant alphaVbeta3 expressed in HEK293 cells incubated for 1 hr by scintillation-proximity assay based competitive solid-phase binding assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SK-MEL-24
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Integrin alpha-V/beta-3 (CHEMBL1907598)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins.
Baiula M,Galletti P,Martelli G,Soldati R,Belvisi L,Civera M,Dattoli SD,Spampinato SM,Giacomini D
J Med Chem (2016) 59 : 9721 -9742
PubMed 27726366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 8.03 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3289605 1 8.92
CHEMBL411941 CYCLORGDFV 1 8.85
CHEMBL4461771 1 8.72
CHEMBL3289604 1 8.25
CHEMBL4794300 1 8.00
CHEMBL4764510 1 6.94
CHEMBL4461668 1 6.54
CHEMBL4777693 1 -
CHEMBL4797755 1 -
CHEMBL4589062 1 -
CHEMBL4586928 1 -
CHEMBL916 TIROFIBAN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3289605 IC50 = 1.2 nM 8.92
CHEMBL411941 CYCLORGDFV IC50 = 1.4 nM 8.85
CHEMBL4461771 IC50 = 1.9 nM 8.72
CHEMBL3289604 IC50 = 5.6 nM 8.25
CHEMBL4794300 IC50 = 9.9 nM 8.00
CHEMBL4764510 IC50 = 116.0 nM 6.94
CHEMBL4461668 IC50 = 285.0 nM 6.54
CHEMBL4777693 IC50 > 1000.0 nM -
CHEMBL4797755 IC50 > 1000.0 nM -
CHEMBL4589062 IC50 > 1000.0 nM -
CHEMBL4586928 IC50 > 1000.0 nM -
CHEMBL916 TIROFIBAN IC50 - -