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Assay Detail

CHEMBL823263

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

Binding
Displacement of a non-peptide radioligand from human recombinant alphaV-beta3 integrin
10
Total Activities
10
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. Part 2: constrained glycyl amides derived from the RGD tripeptide.
Meissner RS, Perkins JJ, Duong LT, Hartman GD, Hoffman WF, Huff JR, Ihle NC, Leu CT, Nagy RM, Naylor-Olsen A, Rodan GA, Rodan SB, Whitman DB, Wesolowski GA, Duggan ME.
Bioorg Med Chem Lett (2002) 12 : 25 -29
PubMed 11738566 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.47 9.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL300008 1 9.46
CHEMBL329081 1 9.03
CHEMBL416669 1 8.92
CHEMBL53822 1 8.89
CHEMBL95987 1 8.54
CHEMBL95750 1 8.06
CHEMBL99287 1 7.92
CHEMBL82927 1 6.96
CHEMBL100246 1 -
CHEMBL313763 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL300008 IC50 = 0.35 nM 9.46
CHEMBL329081 IC50 = 0.94 nM 9.03
CHEMBL416669 IC50 = 1.2 nM 8.92
CHEMBL53822 IC50 = 1.3 nM 8.89
CHEMBL95987 IC50 = 2.9 nM 8.54
CHEMBL95750 IC50 = 8.8 nM 8.06
CHEMBL99287 IC50 = 12.0 nM 7.92
CHEMBL82927 IC50 = 111.0 nM 6.96
CHEMBL100246 IC50 > 10000.0 nM -
CHEMBL313763 IC50 > 10000.0 nM -