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Assay Detail

CHEMBL933864

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 low affinity state by solid phase assay
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 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 8 6.49 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL411863 1 7.62
CHEMBL437072 1 6.75
CHEMBL410050 1 6.60
CHEMBL406680 1 6.49
CHEMBL270690 1 6.26
CHEMBL406912 1 6.22
CHEMBL2372171 1 6.08
CHEMBL270683 1 5.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL411863 IC50 = 23.7 nM 7.62
CHEMBL437072 IC50 = 178.0 nM 6.75
CHEMBL410050 IC50 = 251.0 nM 6.60
CHEMBL406680 IC50 = 327.0 nM 6.49
CHEMBL270690 IC50 = 550.0 nM 6.26
CHEMBL406912 IC50 = 600.0 nM 6.22
CHEMBL2372171 IC50 = 840.0 nM 6.08
CHEMBL270683 IC50 = 1350.0 nM 5.87