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Assay Detail

CHEMBL933853

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

Binding
Displacement of [125I]echistatin from human integrin alpha-V-beta-3 receptor by solid phase assay
11
Total Activities
11
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 subnanomolar arginine-glycine-aspartate-based alphaVbeta3/alphaVbeta5 integrin binders embedding 4-aminoproline residues.
Zanardi F, Burreddu P, Rassu G, Auzzas L, Battistini L, Curti C, Sartori A, Nicastro G, Menchi G, Cini N, Bottoncetti A, Raspanti S, Casiraghi G.
J Med Chem (2008) 51 : 1771 -1782
PubMed 18303826 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.94 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269913 1 9.59
CHEMBL437072 1 8.55
CHEMBL411863 1 8.36
CHEMBL406912 1 8.29
CHEMBL392303 1 8.25
CHEMBL410050 1 8.25
CHEMBL270690 1 8.15
CHEMBL429876 CILENGITIDE 3.0 1 7.72
CHEMBL270683 1 7.12
CHEMBL406680 1 6.76
CHEMBL2372171 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269913 IC50 = 0.26 nM 9.59
CHEMBL437072 IC50 = 2.84 nM 8.55
CHEMBL411863 IC50 = 4.4 nM 8.36
CHEMBL406912 IC50 = 5.15 nM 8.29
CHEMBL392303 IC50 = 5.64 nM 8.25
CHEMBL410050 IC50 = 5.6 nM 8.25
CHEMBL270690 IC50 = 7.01 nM 8.15
CHEMBL429876 CILENGITIDE IC50 = 18.9 nM 7.72
CHEMBL270683 IC50 = 75.14 nM 7.12
CHEMBL406680 IC50 = 174.0 nM 6.76
CHEMBL2372171 IC50 = 530.0 nM 6.28