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Assay Detail

CHEMBL642823

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

Binding
Inhibition of high affinity radioligand binding to human alphaV-beta3 integrin
9
Total Activities
9
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

Non-peptide alpha(v)beta(3) antagonists. Part 3: identification of potent RGD mimetics incorporating novel beta-amino acids as aspartic acid replacements.
Coleman PJ, Brashear KM, Hunt CA, Hoffman WF, Hutchinson JH, Breslin MJ, McVean CA, Askew BC, Hartman GD, Rodan SB, Rodan GA, Leu CT, Prueksaritanont T, Fernandez-Metzler C, Ma B, Libby LA, Merkle KM, Stump GL, Wallace AA, Lynch JJ, Lynch R, Duggan ME.
Bioorg Med Chem Lett (2002) 12 : 31 -34
PubMed 11738567 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 9.15 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL116123 1 10.40
CHEMBL114362 1 9.51
CHEMBL326724 1 9.49
CHEMBL116055 1 9.31
CHEMBL432980 1 9.24
CHEMBL114685 1 8.96
CHEMBL283795 1 8.74
CHEMBL323924 1 8.43
CHEMBL115130 1 8.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL116123 IC50 = 0.04 nM 10.40
CHEMBL114362 IC50 = 0.31 nM 9.51
CHEMBL326724 IC50 = 0.32 nM 9.49
CHEMBL116055 IC50 = 0.49 nM 9.31
CHEMBL432980 IC50 = 0.57 nM 9.24
CHEMBL114685 IC50 = 1.1 nM 8.96
CHEMBL283795 IC50 = 1.8 nM 8.74
CHEMBL323924 IC50 = 3.7 nM 8.43
CHEMBL115130 IC50 = 5.8 nM 8.24