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Assay Detail

CHEMBL1109726

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

Binding
Displacement of [N-methyl-3H]T1317 from human biotinylated LXRbeta LBD after 3 hrs by LEAD seeker binding assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of tertiary sulfonamides as potent liver X receptor antagonists.
Zuercher WJ, Buckholz RG, Campobasso N, Collins JL, Galardi CM, Gampe RT, Hyatt SM, Merrihew SL, Moore JT, Oplinger JA, Reid PR, Spearing PK, Stanley TB, Stewart EL, Willson TM.
J Med Chem (2010) 53 : 3412 -3416
PubMed 20345102 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.58 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1091034 1 8.40
CHEMBL1093554 1 8.30
CHEMBL1093840 1 8.20
CHEMBL59030 1 8.10
CHEMBL1092952 1 8.00
CHEMBL1091976 1 7.90
CHEMBL1093523 1 7.80
CHEMBL62136 T091317 1 7.70
CHEMBL1093266 1 7.50
CHEMBL1093828 1 7.10
CHEMBL1090238 1 6.40
CHEMBL1090569 1 5.50
CHEMBL1091958 1 -
CHEMBL1090570 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1091034 IC50 = 3.981 nM 8.40
CHEMBL1093554 IC50 = 5.012 nM 8.30
CHEMBL1093840 IC50 = 6.31 nM 8.20
CHEMBL59030 IC50 = 7.943 nM 8.10
CHEMBL1092952 IC50 = 10.0 nM 8.00
CHEMBL1091976 IC50 = 12.59 nM 7.90
CHEMBL1093523 IC50 = 15.85 nM 7.80
CHEMBL62136 T091317 IC50 = 19.95 nM 7.70
CHEMBL1093266 IC50 = 31.62 nM 7.50
CHEMBL1093828 IC50 = 79.43 nM 7.10
CHEMBL1090238 IC50 = 398.11 nM 6.40
CHEMBL1090569 IC50 = 3162.28 nM 5.50
CHEMBL1091958 IC50 > 10000.0 nM -
CHEMBL1090570 IC50 > 10000.0 nM -