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Assay Detail

CHEMBL2071987

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

Binding
Displacement of [125I]-c(RGDyK) from human integrin alphavbeta3 after 16 hrs by scintillation counting
6
Total Activities
3
Compounds Tested
2
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

Near-infrared fluorescent divalent RGD ligand for integrin αvβ₃-targeted optical imaging.
Ye Y, Akers W, Xu B, Bloch S, Odonkor C, Achilefu S.
Bioorg Med Chem Lett (2012) 22 : 5405 -5409
PubMed 22871580 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.79 9.55
Ki 3 9.40 10.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2071603 2 10.37
CHEMBL2071604 2 9.18
CHEMBL2071605 2 8.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2071603 Ki = 0.043 nM 10.37
CHEMBL2071603 IC50 = 0.281 nM 9.55
CHEMBL2071604 Ki = 0.663 nM 9.18
CHEMBL2071605 Ki = 2.27 nM 8.64
CHEMBL2071605 IC50 = 3.52 nM 8.45
CHEMBL2071604 IC50 = 4.305 nM 8.37