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Assay Detail

CHEMBL4681202

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

Binding
Agonist activity at alphaVbeta3 in human SK-MEL-24 cells assessed as increase in cell adhesion to fibronectin pre-incubated for 30 mins before fibronectin and further incubated for 1 hr by nitrophenyl-N-acetyl-beta-D-glucosaminide substrate based chromogenic 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
EC50 12 7.32 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3289605 1 7.96
CHEMBL3289604 1 7.26
CHEMBL4764510 1 6.73
CHEMBL3289606 1 -
CHEMBL4777693 1 -
CHEMBL4782288 1 -
CHEMBL4797755 1 -
CHEMBL4755971 1 -
CHEMBL4589062 1 -
CHEMBL4586928 1 -
CHEMBL88478 1 -
CHEMBL916 TIROFIBAN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3289605 EC50 = 11.0 nM 7.96
CHEMBL3289604 EC50 = 55.0 nM 7.26
CHEMBL4764510 EC50 = 187.0 nM 6.73
CHEMBL3289606 EC50 > 5000.0 nM -
CHEMBL4777693 EC50 > 5000.0 nM -
CHEMBL4782288 EC50 > 5000.0 nM -
CHEMBL4797755 EC50 > 5000.0 nM -
CHEMBL4755971 EC50 > 5000.0 nM -
CHEMBL4589062 EC50 > 5000.0 nM -
CHEMBL4586928 EC50 > 5000.0 nM -
CHEMBL88478 EC50 - -
CHEMBL916 TIROFIBAN EC50 - -