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Assay Detail

CHEMBL4221124

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

Binding
Inhibition of human TLR4 signaling expressed in HEK-Blue cells co-expressing MD2/CD14 assessed as reduction in LPS-induced NF-kappaB activation-mediated SEAP production preincubated for 2 hrs followed by LPS stimulation for 20 hrs by colorimetric assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Toll-like receptor 4 (CHEMBL5255)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout.
Huang J, Zhou Z, Zhou M, Miao M, Li H, Hu Q.
Bioorg Med Chem (2018) 26 : 1653 -1664
PubMed 29472126 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.23 6.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4228510 1 6.27
CHEMBL225157 RESATORVID 3.0 1 6.17
CHEMBL4228911 1 5.27
CHEMBL4227459 1 4.72
CHEMBL4229108 1 4.59
CHEMBL4225876 1 4.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4228510 IC50 = 540.0 nM 6.27
CHEMBL225157 RESATORVID IC50 = 680.0 nM 6.17
CHEMBL4228911 IC50 = 5420.0 nM 5.27
CHEMBL4227459 IC50 = 19250.0 nM 4.72
CHEMBL4229108 IC50 = 25900.0 nM 4.59
CHEMBL4225876 IC50 = 45650.0 nM 4.34