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Assay Detail

CHEMBL822770

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

Binding
Displacement of [125I]nonpeptide ligand (compound 7) from purified human recombinant alphaV-beta3
6
Total Activities
6
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

Nonpeptide alpha(v)beta(3) antagonists. 1. Transformation of a potent, integrin-selective alpha(IIb)beta(3) antagonist into a potent alpha(v)beta(3) antagonist.
Duggan ME, Duong LT, Fisher JE, Hamill TG, Hoffman WF, Huff JR, Ihle NC, Leu CT, Nagy RM, Perkins JJ, Rodan SB, Wesolowski G, Whitman DB, Zartman AE, Rodan GA, Hartman GD.
J Med Chem (2000) 43 : 3736 -3745
PubMed 11020288 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 9.32 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL123262 1 10.15
CHEMBL332914 1 10.10
CHEMBL123374 1 9.36
CHEMBL122000 1 9.03
CHEMBL333019 1 7.97
CHEMBL59562 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL123262 IC50 = 0.07 nM 10.15
CHEMBL332914 IC50 = 0.08 nM 10.10
CHEMBL123374 IC50 = 0.44 nM 9.36
CHEMBL122000 IC50 = 0.93 nM 9.03
CHEMBL333019 IC50 = 10.7 nM 7.97
CHEMBL59562 IC50 > 1000.0 nM -