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Assay Detail

CHEMBL2329944

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

Binding
Inhibition of CX3CL1-stimulated CX3CR1 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
8
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

C-X-C chemokine receptor type 1 (CHEMBL4029)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Colloidal aggregation causes inhibition of G protein-coupled receptors.
Sassano MF, Doak AK, Roth BL, Shoichet BK.
J Med Chem (2013) 56 : 2406 -2414
PubMed 23437772 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.90 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64391 ITRACONAZOLE 4.0 2 7.00
CHEMBL2324200 Tetra-iodophenolphthalein 2 5.70
CHEMBL104 CLOTRIMAZOLE 4.0 2 5.70
CHEMBL50 QUERCETIN 3.0 2 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64391 ITRACONAZOLE IC50 = 100.0 nM 7.00
CHEMBL64391 ITRACONAZOLE IC50 = 158.49 nM 6.80
CHEMBL2324200 Tetra-iodophenolphthalein IC50 = 1995.26 nM 5.70
CHEMBL104 CLOTRIMAZOLE IC50 = 2000.0 nM 5.70
CHEMBL104 CLOTRIMAZOLE IC50 = 1995.26 nM 5.70
CHEMBL2324200 Tetra-iodophenolphthalein IC50 = 2200.0 nM 5.66
CHEMBL50 QUERCETIN IC50 = 4500.0 nM 5.35
CHEMBL50 QUERCETIN IC50 = 5011.87 nM 5.30