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Assay Detail

CHEMBL5153997

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

Binding
Activation of AhR in human HepG2 cells assessed as induction of XRE-dependent reporter activity incubated for 4 hrs by Renilla/Firefly based dual-luciferase reporter assay
1
Total Activities
1
Compounds Tested
1
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

The Highly Potent AhR Agonist Picoberin Modulates Hh-Dependent Osteoblast Differentiation.
Flegel J, Shaaban S, Jia ZJ, Schulte B, Lian Y, Krzyzanowski A, Metz M, Schneidewind T, Wesseler F, Flegel A, Reich A, Brause A, Xue G, Zhang M, Dötsch L, Stender ID, Hoffmann JE, Scheel R, Janning P, Rastinejad F, Schade D, Strohmann C, Antonchick AP, Sievers S, Moura-Alves P, Ziegler S, Waldmann H.
J Med Chem (2022) 65 : 16268 -16289
PubMed 36459434 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 8.49 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5186309 1 8.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5186309 EC50 = 3.2 nM 8.49