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Assay Detail

CHEMBL1007709

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

Binding
Agonist activity at human recombinant LXRalpha expressed in Escherichia coli BL21 cells assessed as association of recombinant SRC1 to LXRalpha ligand binding domain by HTRF assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BL21
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Diterpenoid, steroid, and triterpenoid agonists of liver X receptors from diversified terrestrial plants and marine sources.
Jayasuriya H, Herath KB, Ondeyka JG, Guan Z, Borris RP, Tiwari S, de Jong W, Chavez F, Moss J, Stevenson DW, Beck HT, Slattery M, Zamora N, Schulman M, Ali A, Sharma N, MacNaul K, Hayes N, Menke JG, Singh SB.
J Nat Prod (2005) 68 : 1247 -1252
PubMed 16124770 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 7.14 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL506838 ACETYL PODOCARPIC ACID ANHYDRIDE 1 9.00
CHEMBL486808 1 7.52
CHEMBL23296 1 7.46
CHEMBL486198 1 7.30
CHEMBL520370 1 6.77
CHEMBL512490 1 6.75
CHEMBL194642 1 6.68
CHEMBL470040 1 6.41
CHEMBL486197 1 6.35
CHEMBL269277 BETULINIC ACID 1.0 1 -
CHEMBL519222 1 -
CHEMBL485990 1 -
CHEMBL487001 ROSACEA ACID B 1 -
CHEMBL421115 PODOCARIC ACID 1 -
CHEMBL470041 VIPERIDONE 1 -
CHEMBL521375 1 -
CHEMBL422904 22(R)-HYDROXYCHOLESTEROL 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL506838 ACETYL PODOCARPIC ACID ANHYDRIDE EC50 = 1.0 nM 9.00
CHEMBL486808 EC50 = 30.0 nM 7.52
CHEMBL23296 EC50 = 35.0 nM 7.46
CHEMBL486198 EC50 = 50.0 nM 7.30
CHEMBL520370 EC50 = 170.0 nM 6.77
CHEMBL512490 EC50 = 180.0 nM 6.75
CHEMBL194642 EC50 = 210.0 nM 6.68
CHEMBL470040 EC50 = 390.0 nM 6.41
CHEMBL486197 EC50 = 450.0 nM 6.35
CHEMBL269277 BETULINIC ACID EC50 > 50000.0 nM -
CHEMBL519222 EC50 - -
CHEMBL485990 EC50 - -
CHEMBL487001 ROSACEA ACID B EC50 > 50000.0 nM -
CHEMBL421115 PODOCARIC ACID EC50 > 50000.0 nM -
CHEMBL470041 VIPERIDONE EC50 > 15000.0 nM -
CHEMBL521375 EC50 > 50000.0 nM -
CHEMBL422904 22(R)-HYDROXYCHOLESTEROL EC50 > 15000.0 nM -