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Assay Detail

CHEMBL5736505

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Binding
ligand sensing assay (LiSA): As used herein, reference to the activity of an LXR agonist at LXRα and LXRβ refer to the activity as measured using the ligand sensing assay (LiSA) described in Spencer et al. Journal of Medicinal Chemistry 2001, 44, 886-897, incorporated herein by reference.
18
Total Activities
6
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Treatment and diagnosis of melanoma
(2021)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.91 7.70
kon 6 - -
k_off 6 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62136 T091317 3 7.70
CHEMBL5775096 3 7.13
CHEMBL456237 LXR-623 1.0 3 6.75
CHEMBL59030 3 6.70
CHEMBL3360975 BMS-779788 1.0 3 6.26
CHEMBL3945199 BMS-852927 1.0 3 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62136 T091317 EC50 = 20.0 nM 7.70
CHEMBL5775096 EC50 = 74.0 nM 7.13
CHEMBL456237 LXR-623 EC50 = 179.0 nM 6.75
CHEMBL59030 EC50 = 200.0 nM 6.70
CHEMBL3360975 BMS-779788 EC50 = 550.0 nM 6.26
CHEMBL59030 kon = - -
CHEMBL59030 k_off = - s-1 -
CHEMBL5775096 kon = - -
CHEMBL5775096 k_off = - s-1 -
CHEMBL62136 T091317 kon = - -
CHEMBL62136 T091317 k_off = - s-1 -
CHEMBL456237 LXR-623 kon = - -
CHEMBL456237 LXR-623 k_off = - s-1 -
CHEMBL3945199 BMS-852927 EC50 < 100.0 nM -
CHEMBL3945199 BMS-852927 kon = - -
CHEMBL3945199 BMS-852927 k_off = - s-1 -
CHEMBL3360975 BMS-779788 kon = - -
CHEMBL3360975 BMS-779788 k_off = - s-1 -