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Assay Detail

CHEMBL3998013

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

Binding
Activation of PXR in human LS180 cells assessed as P-gp induction by measuring intracellular accumulation of rhodamine 123 preincubated for 48 hrs followed by rhodamine 123 addition after 40 mins and measured after 90 mins by fluorescence assay
4
Total Activities
4
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

Nuclear receptor subfamily 1 group I member 2 (CHEMBL3401)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Medchemcomm (2016) 7 : 1910 -1915
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 6.42 6.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL374478 RIFAMPIN 4.0 1 6.65
CHEMBL4084567 1 6.57
CHEMBL4095208 1 6.54
CHEMBL458767 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL374478 RIFAMPIN EC50 = 226.0 nM 6.65
CHEMBL4084567 EC50 = 271.0 nM 6.57
CHEMBL4095208 EC50 = 290.0 nM 6.54
CHEMBL458767 EC50 = 1250.0 nM 5.90