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Assay Detail

CHEMBL882881

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

Binding
Effective concentration in recombinant human LXRalpha ligand binding domain in homogeneous time-resolved fluorescence assay
25
Total Activities
25
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

Design, synthesis, and structure-activity relationship of podocarpic acid amides as liver X receptor agonists for potential treatment of atherosclerosis.
Liu W, Chen S, Dropinski J, Colwell L, Robins M, Szymonifka M, Hayes N, Sharma N, MacNaul K, Hernandez M, Burton C, Sparrow CP, Menke JG, Singh SB.
Bioorg Med Chem Lett (2005) 15 : 4574 -4578
PubMed 16125384 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 6.72 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL365544 1 9.00
CHEMBL191965 1 8.70
CHEMBL372612 1 7.30
CHEMBL194733 1 7.16
CHEMBL371990 1 6.85
CHEMBL196340 1 6.82
CHEMBL194573 1 6.77
CHEMBL194353 1 6.77
CHEMBL199255 1 6.66
CHEMBL194642 1 6.64
CHEMBL197522 1 6.62
CHEMBL382942 1 6.55
CHEMBL194409 1 6.50
CHEMBL370175 1 6.50
CHEMBL365750 1 6.44
CHEMBL197265 1 6.37
CHEMBL196335 1 6.12
CHEMBL194679 1 5.82
CHEMBL424831 1 5.51
CHEMBL196145 1 5.28
CHEMBL426289 1 -
CHEMBL194192 1 -
CHEMBL196106 1 -
CHEMBL427183 1 -
CHEMBL194866 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL365544 EC50 = 1.0 nM 9.00
CHEMBL191965 EC50 = 2.0 nM 8.70
CHEMBL372612 EC50 = 50.0 nM 7.30
CHEMBL194733 EC50 = 70.0 nM 7.16
CHEMBL371990 EC50 = 140.0 nM 6.85
CHEMBL196340 EC50 = 150.0 nM 6.82
CHEMBL194573 EC50 = 170.0 nM 6.77
CHEMBL194353 EC50 = 170.0 nM 6.77
CHEMBL199255 EC50 = 220.0 nM 6.66
CHEMBL194642 EC50 = 230.0 nM 6.64
CHEMBL197522 EC50 = 240.0 nM 6.62
CHEMBL382942 EC50 = 280.0 nM 6.55
CHEMBL194409 EC50 = 320.0 nM 6.50
CHEMBL370175 EC50 = 320.0 nM 6.50
CHEMBL365750 EC50 = 360.0 nM 6.44
CHEMBL197265 EC50 = 430.0 nM 6.37
CHEMBL196335 EC50 = 760.0 nM 6.12
CHEMBL194679 EC50 = 1500.0 nM 5.82
CHEMBL424831 EC50 = 3100.0 nM 5.51
CHEMBL196145 EC50 = 5200.0 nM 5.28
CHEMBL426289 EC50 > 50000.0 nM -
CHEMBL194192 EC50 > 50000.0 nM -
CHEMBL196106 EC50 > 50000.0 nM -
CHEMBL427183 EC50 > 15000.0 nM -
CHEMBL194866 EC50 > 50000.0 nM -