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Assay Detail

CHEMBL828112

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

Binding
Displacement of [3H2]-F3-methyl AA (1) from liver X receptor-alpha in SPA assay
6
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Oxysterols receptor LXR-alpha (CHEMBL2808)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters.
Singh SB, Ondeyka JG, Liu W, Chen S, Chen TS, Li X, Bouffard A, Dropinski J, Jones AB, McCormick S, Hayes N, Wang J, Sharma N, Macnaul K, Hernandez M, Chao YS, Baffic J, Lam MH, Burton C, Sparrow CP, Menke JG.
Bioorg Med Chem Lett (2005) 15 : 2824 -2828
PubMed 15911262 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.26 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL365544 1 9.00
CHEMBL555373 1 8.70
CHEMBL191965 1 8.70
CHEMBL23296 2 7.45
CHEMBL421115 PODOCARIC ACID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL365544 IC50 = 1.0 nM 9.00
CHEMBL555373 IC50 = 2.0 nM 8.70
CHEMBL191965 IC50 = 2.0 nM 8.70
CHEMBL23296 IC50 = 35.4 nM 7.45
CHEMBL23296 IC50 = 35.4 nM 7.45
CHEMBL421115 PODOCARIC ACID IC50 > 50000.0 nM -