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Assay Detail

CHEMBL3300520

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

Binding
Inhibition of vitronectin binding to human alphaVbeta5 integrin after 1 hr by ELISA
4
Total Activities
4
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-5 (CHEMBL2096675)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides.
Hegemann JD, De Simone M, Zimmermann M, Knappe TA, Xie X, Di Leva FS, Marinelli L, Novellino E, Zahler S, Kessler H, Marahiel MA.
J Med Chem (2014) 57 : 5829 -5834
PubMed 24949551 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.46 5.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429876 CILENGITIDE 3.0 1 5.27
CHEMBL313763 1 4.42
CHEMBL3298392 1 4.10
CHEMBL303561 1 4.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429876 CILENGITIDE IC50 = 5400.0 nM 5.27
CHEMBL313763 IC50 = 38000.0 nM 4.42
CHEMBL3298392 IC50 = 80000.0 nM 4.10
CHEMBL303561 IC50 = 92000.0 nM 4.04