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Assay Detail

CHEMBL4671306

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

Binding
Inhibition of human RANKL-induced osteoclastogenesis in RANKL cultured mouse bone marrow cells assessed as reduction in RANKL/M-CSF-induced TRAP activity preincubated with RANKL for 1 hr followed by cell addition and subsequent media replenishment every 48 hrs for 4 days
16
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Bone marrow cell
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tumor necrosis factor ligand superfamily member 11 (CHEMBL2364162)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Small-Molecule Inhibitors of Receptor Activator of Nuclear Factor-κB Ligand with a Superior Therapeutic Index.
Rinotas V,Papakyriakou A,Violitzi F,Papaneophytou C,Ouzouni MD,Alexiou P,Strongilos A,Couladouros E,Kontopidis G,Eliopoulos E,Douni E
J Med Chem (2020) 63 : 12043 -12059
PubMed 32955874 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.59 6.00
Inhibition 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL255489 2 6.00
CHEMBL4760595 1 5.85
CHEMBL3742191 2 5.73
CHEMBL4797434 1 5.72
CHEMBL4750116 1 5.70
CHEMBL4756975 2 5.60
CHEMBL4745590 1 5.57
CHEMBL3741720 2 5.54
CHEMBL3741275 2 5.29
CHEMBL4752672 1 5.29
CHEMBL4745373 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL255489 IC50 = 1000.0 nM 6.00
CHEMBL4760595 IC50 = 1400.0 nM 5.85
CHEMBL3742191 IC50 = 1880.0 nM 5.73
CHEMBL4797434 IC50 = 1900.0 nM 5.72
CHEMBL4750116 IC50 = 2000.0 nM 5.70
CHEMBL4756975 IC50 = 2500.0 nM 5.60
CHEMBL4745590 IC50 = 2700.0 nM 5.57
CHEMBL3741720 IC50 = 2860.0 nM 5.54
CHEMBL3741275 IC50 = 5070.0 nM 5.29
CHEMBL4752672 IC50 = 5100.0 nM 5.29
CHEMBL4745373 IC50 = 6400.0 nM 5.19
CHEMBL3742191 Inhibition - % -
CHEMBL255489 Inhibition - % -
CHEMBL3741720 Inhibition - % -
CHEMBL3741275 Inhibition - % -
CHEMBL4756975 Inhibition - % -