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Assay Detail

CHEMBL3377019

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

Binding
Transactivation of LXR in human whole blood assessed as induction of ABCA1 after 4 hrs by SYBR-Green quantitative PCR analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Blood
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Liver X receptor (CHEMBL3706564)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRβ.
Kick E, Martin R, Xie Y, Flatt B, Schweiger E, Wang TL, Busch B, Nyman M, Gu XH, Yan G, Wagner B, Nanao M, Nguyen L, Stout T, Plonowski A, Schulman I, Ostrowski J, Kirchgessner T, Wexler R, Mohan R.
Bioorg Med Chem Lett (2015) 25 : 372 -377
PubMed 25435151 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 8.58 9.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3360966 1 9.32
CHEMBL3360975 BMS-779788 1.0 1 8.92
CHEMBL3360973 1 8.51
CHEMBL3360974 1 8.49
CHEMBL3360972 1 8.15
CHEMBL3360971 1 8.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3360966 EC50 = 0.48 nM 9.32
CHEMBL3360975 BMS-779788 EC50 = 1.2 nM 8.92
CHEMBL3360973 EC50 = 3.1 nM 8.51
CHEMBL3360974 EC50 = 3.2 nM 8.49
CHEMBL3360972 EC50 = 7.0 nM 8.15
CHEMBL3360971 EC50 = 8.3 nM 8.08