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Assay Detail

CHEMBL3377014

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

Binding
Transactivation of LXRalpha (unknown origin) expressed in CV1 cells by luciferase reporter gene assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Oxysterols receptor LXR-alpha (CHEMBL2808)
Type SINGLE PROTEIN
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 17 7.05 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3360960 1 8.40
CHEMBL3360963 1 7.75
CHEMBL3360961 1 7.70
CHEMBL62136 T091317 1 7.55
CHEMBL3360970 1 7.28
CHEMBL3360968 1 7.19
CHEMBL3360974 1 7.07
CHEMBL3360965 1 6.92
CHEMBL3360964 1 6.85
CHEMBL3360973 1 6.70
CHEMBL3360966 1 6.66
CHEMBL3360975 BMS-779788 1.0 1 6.64
CHEMBL3360967 1 6.50
CHEMBL3360969 1 6.27
CHEMBL3360962 1 6.24
CHEMBL3360971 1 -
CHEMBL3360972 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3360960 EC50 = 4.0 nM 8.40
CHEMBL3360963 EC50 = 18.0 nM 7.75
CHEMBL3360961 EC50 = 20.0 nM 7.70
CHEMBL62136 T091317 EC50 = 28.0 nM 7.55
CHEMBL3360970 EC50 = 52.0 nM 7.28
CHEMBL3360968 EC50 = 65.0 nM 7.19
CHEMBL3360974 EC50 = 85.0 nM 7.07
CHEMBL3360965 EC50 = 120.0 nM 6.92
CHEMBL3360964 EC50 = 140.0 nM 6.85
CHEMBL3360973 EC50 = 200.0 nM 6.70
CHEMBL3360966 EC50 = 220.0 nM 6.66
CHEMBL3360975 BMS-779788 EC50 = 230.0 nM 6.64
CHEMBL3360967 EC50 = 320.0 nM 6.50
CHEMBL3360969 EC50 = 540.0 nM 6.27
CHEMBL3360962 EC50 = 570.0 nM 6.24
CHEMBL3360971 EC50 > 10000.0 nM -
CHEMBL3360972 EC50 > 10000.0 nM -