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Assay Detail

CHEMBL830070

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

Binding
Inhibitory activity against alpha v beta-3 receptor using scintillation proximity assay (SPAV3)
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Integrin alpha-V/beta-3 (CHEMBL1907598)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis.
Coleman PJ, Brashear KM, Askew BC, Hutchinson JH, McVean CA, Duong LT, Feuston BP, Fernandez-Metzler C, Gentile MA, Hartman GD, Kimmel DB, Leu CT, Lipfert L, Merkle K, Pennypacker B, Prueksaritanont T, Rodan GA, Wesolowski GA, Rodan SB, Duggan ME.
J Med Chem (2004) 47 : 4829 -4837
PubMed 15369386 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 9.21 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL186552 1 10.15
CHEMBL187289 1 10.10
CHEMBL186126 1 9.96
CHEMBL189201 1 9.70
CHEMBL425717 1 9.68
CHEMBL361936 1 9.28
CHEMBL180489 1 9.19
CHEMBL188406 1 9.03
CHEMBL150678 1 8.48
CHEMBL183998 1 8.14
CHEMBL83649 1 7.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL186552 IC50 = 0.07 nM 10.15
CHEMBL187289 IC50 = 0.08 nM 10.10
CHEMBL186126 IC50 = 0.11 nM 9.96
CHEMBL189201 IC50 = 0.2 nM 9.70
CHEMBL425717 IC50 = 0.21 nM 9.68
CHEMBL361936 IC50 = 0.52 nM 9.28
CHEMBL180489 IC50 = 0.65 nM 9.19
CHEMBL188406 IC50 = 0.93 nM 9.03
CHEMBL150678 IC50 = 3.3 nM 8.48
CHEMBL183998 IC50 = 7.2 nM 8.14
CHEMBL83649 IC50 = 22.7 nM 7.64