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Assay Detail

CHEMBL866015

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

Binding
Inhibition of [125I]echistatin binding to integrin alphaVbeta3 receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery of small molecule integrin alphavbeta3 antagonists as novel anticancer agents.
Dayam R, Aiello F, Deng J, Wu Y, Garofalo A, Chen X, Neamati N.
J Med Chem (2006) 49 : 4526 -4534
PubMed 16854058 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.67 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378530 1 10.52
CHEMBL212414 1 7.75
CHEMBL212315 1 7.62
CHEMBL426146 1 7.28
CHEMBL211163 1 6.62
CHEMBL377411 1 6.22
CHEMBL211589 1 -
CHEMBL214002 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378530 IC50 = 0.03 nM 10.52
CHEMBL212414 IC50 = 18.0 nM 7.75
CHEMBL212315 IC50 = 24.0 nM 7.62
CHEMBL426146 IC50 = 52.0 nM 7.28
CHEMBL211163 IC50 = 240.0 nM 6.62
CHEMBL377411 IC50 = 605.0 nM 6.22
CHEMBL211589 IC50 > 1000.0 nM -
CHEMBL214002 IC50 > 1000.0 nM -