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Assay Detail

CHEMBL3241282

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

Binding
Inhibition of vitronectin binding to human alphavbeta3 integrin receptor after 1 hr by competitive solid-phase binding ELISA
7
Total Activities
7
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

Pharmacophoric modifications lead to superpotent αvβ3 integrin ligands with suppressed α5β1 activity.
Neubauer S, Rechenmacher F, Brimioulle R, Di Leva FS, Bochen A, Sobahi TR, Schottelius M, Novellino E, Mas-Moruno C, Marinelli L, Kessler H.
J Med Chem (2014) 57 : 3410 -3417
PubMed 24654918 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.09 9.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429876 CILENGITIDE 3.0 1 9.27
CHEMBL3233260 1 9.19
CHEMBL3233259 1 9.07
CHEMBL3233263 1 8.80
CHEMBL3233262 1 7.12
CHEMBL3233258 1 6.96
CHEMBL3233261 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429876 CILENGITIDE IC50 = 0.54 nM 9.27
CHEMBL3233260 IC50 = 0.65 nM 9.19
CHEMBL3233259 IC50 = 0.86 nM 9.07
CHEMBL3233263 IC50 = 1.6 nM 8.80
CHEMBL3233262 IC50 = 75.1 nM 7.12
CHEMBL3233258 IC50 = 110.0 nM 6.96
CHEMBL3233261 IC50 = 638.0 nM 6.20