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Assay Detail

CHEMBL933518

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

Binding
Displacement of [125I]echistatin from human placental integrin alphaVbeta3 receptor
4
Total Activities
4
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

Synthesis, SAR and in vitro evaluation of new cyclic Arg-Gly-Asp pseudopentapeptides containing a s-cis peptide bond as integrin alphavbeta3 and alphavbeta5 ligands.
Salvati M, Cordero FM, Pisaneschi F, Melani F, Gratteri P, Cini N, Bottoncetti A, Brandi A.
Bioorg Med Chem (2008) 16 : 4262 -4271
PubMed 18343671 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.89 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429876 CILENGITIDE 3.0 1 7.72
CHEMBL408195 1 7.46
CHEMBL411941 CYCLORGDFV 1 6.71
CHEMBL265445 1 5.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429876 CILENGITIDE IC50 = 18.9 nM 7.72
CHEMBL408195 IC50 = 34.4 nM 7.46
CHEMBL411941 CYCLORGDFV IC50 = 196.0 nM 6.71
CHEMBL265445 IC50 = 2150.0 nM 5.67