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Assay Detail

CHEMBL3868520

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

Binding
Agonist activity at LXR-beta in human whole blood assessed as ABCA1 gene induction by measuring ABCA1 mRNA level after 4 hrs by SYBR-Green dye-based Q-PCR analysis
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Oxysterols receptor LXR-beta (CHEMBL4093)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Highly Potent Liver X Receptor β Agonists.
Kick EK, Busch BB, Martin R, Stevens WC, Bollu V, Xie Y, Boren BC, Nyman MC, Nanao MH, Nguyen L, Plonowski A, Schulman IG, Yan G, Zhang H, Hou X, Valente MN, Narayanan R, Behnia K, Rodrigues AD, Brock B, Smalley J, Cantor GH, Lupisella J, Sleph P, Grimm D, Ostrowski J, Wexler RR, Kirchgessner T, Mohan R.
ACS Med Chem Lett (2016) 7 : 1207 -1212
PubMed 27994765 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 7.14 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3910597 1 8.30
CHEMBL3945199 BMS-852927 1.0 1 8.05
CHEMBL3935187 1 7.82
CHEMBL3945820 1 7.64
CHEMBL3917300 1 7.39
CHEMBL3980683 1 7.38
CHEMBL3941775 1 7.37
CHEMBL3926292 1 7.34
CHEMBL3944154 1 7.24
CHEMBL3953927 1 7.12
CHEMBL3960606 1 6.52
CHEMBL3913162 1 6.52
CHEMBL3890276 1 6.42
CHEMBL3963566 1 6.06
CHEMBL3360975 BMS-779788 1.0 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3910597 EC50 = 5.0 nM 8.30
CHEMBL3945199 BMS-852927 EC50 = 9.0 nM 8.05
CHEMBL3935187 EC50 = 15.0 nM 7.82
CHEMBL3945820 EC50 = 23.0 nM 7.64
CHEMBL3917300 EC50 = 41.0 nM 7.39
CHEMBL3980683 EC50 = 42.0 nM 7.38
CHEMBL3941775 EC50 = 43.0 nM 7.37
CHEMBL3926292 EC50 = 46.0 nM 7.34
CHEMBL3944154 EC50 = 57.0 nM 7.24
CHEMBL3953927 EC50 = 76.0 nM 7.12
CHEMBL3960606 EC50 = 300.0 nM 6.52
CHEMBL3913162 EC50 = 300.0 nM 6.52
CHEMBL3890276 EC50 = 380.0 nM 6.42
CHEMBL3963566 EC50 = 870.0 nM 6.06
CHEMBL3360975 BMS-779788 EC50 = 1200.0 nM 5.92