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Assay Detail

CHEMBL4617427

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

Binding
Agonist activity at AhR in human HepG2 cells assessed as induction of CYP1A1 expression after 24 hrs by ethoxyresorufin-O-deethylase assay
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HepG2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Aryl hydrocarbon receptor (CHEMBL3201)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of FICZ analogues as agonists of aryl hydrocarbon receptor.
Wu H, Liu B, Yang K, Winston-McPherson GN, Leisten ED, Vezina CM, Ricke WA, Peterson RE, Tang W.
Bioorg Med Chem Lett (2020) 30 : 126959 -126959
PubMed 31952965 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 9.14 9.59
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4646273 2 9.59
CHEMBL472031 2 8.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4646273 EC50 = 0.26 nM 9.59
CHEMBL472031 EC50 = 2.04 nM 8.69
CHEMBL4646273 Activity - -
CHEMBL472031 Activity - -