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Assay Detail

CHEMBL710256

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

Binding
Ligand-dependent recruitment of steroid receptor co-activator 1 (SRC1) to Liver X receptor-alpha
12
Total Activities
12
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

Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines.
Collins JL, Fivush AM, Watson MA, Galardi CM, Lewis MC, Moore LB, Parks DJ, Wilson JG, Tippin TK, Binz JG, Plunket KD, Morgan DG, Beaudet EJ, Whitney KD, Kliewer SA, Willson TM.
J Med Chem (2002) 45 : 1963 -1966
PubMed 11985463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 6.78 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL58076 1 7.35
CHEMBL62136 T091317 1 7.22
CHEMBL60393 1 7.07
CHEMBL61766 1 7.07
CHEMBL434302 24(S),25-EPOXYCHOLESTEROL 1 7.02
CHEMBL59030 1 6.90
CHEMBL61124 1 6.72
CHEMBL59359 1 6.60
CHEMBL62135 1 6.58
CHEMBL61528 1 6.58
CHEMBL59082 1 6.18
CHEMBL60079 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL58076 EC50 = 45.0 nM 7.35
CHEMBL62136 T091317 EC50 = 60.0 nM 7.22
CHEMBL60393 EC50 = 85.0 nM 7.07
CHEMBL61766 EC50 = 85.0 nM 7.07
CHEMBL434302 24(S),25-EPOXYCHOLESTEROL EC50 = 95.0 nM 7.02
CHEMBL59030 EC50 = 125.0 nM 6.90
CHEMBL61124 EC50 = 190.0 nM 6.72
CHEMBL59359 EC50 = 250.0 nM 6.60
CHEMBL62135 EC50 = 260.0 nM 6.58
CHEMBL61528 EC50 = 260.0 nM 6.58
CHEMBL59082 EC50 = 660.0 nM 6.18
CHEMBL60079 EC50 = 860.0 nM 6.07