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Assay Detail

CHEMBL3377012

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

Binding
Binding affinity to LXRalpha-RXRalpha heterodimer (unknown origin) expressed in insect cells by scintillation proximity assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Publication

Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRβ.
Kick E, Martin R, Xie Y, Flatt B, Schweiger E, Wang TL, Busch B, Nyman M, Gu XH, Yan G, Wagner B, Nanao M, Nguyen L, Stout T, Plonowski A, Schulman I, Ostrowski J, Kirchgessner T, Wexler R, Mohan R.
Bioorg Med Chem Lett (2015) 25 : 372 -377
PubMed 25435151 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.97 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3360960 1 7.96
CHEMBL3360963 1 7.70
CHEMBL3360974 1 7.60
CHEMBL3360961 1 7.58
CHEMBL62136 T091317 1 7.51
CHEMBL3360962 1 7.44
CHEMBL3360970 1 7.21
CHEMBL3360973 1 7.18
CHEMBL3360964 1 7.17
CHEMBL3360975 BMS-779788 1.0 1 7.17
CHEMBL3360968 1 6.82
CHEMBL3360966 1 6.75
CHEMBL3360965 1 6.62
CHEMBL3360967 1 6.52
CHEMBL3360969 1 5.82
CHEMBL3360971 1 5.80
CHEMBL3360972 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3360960 Ki = 11.0 nM 7.96
CHEMBL3360963 Ki = 20.0 nM 7.70
CHEMBL3360974 Ki = 25.0 nM 7.60
CHEMBL3360961 Ki = 26.0 nM 7.58
CHEMBL62136 T091317 Ki = 31.0 nM 7.51
CHEMBL3360962 Ki = 36.0 nM 7.44
CHEMBL3360970 Ki = 61.0 nM 7.21
CHEMBL3360973 Ki = 66.0 nM 7.18
CHEMBL3360964 Ki = 68.0 nM 7.17
CHEMBL3360975 BMS-779788 Ki = 68.0 nM 7.17
CHEMBL3360968 Ki = 150.0 nM 6.82
CHEMBL3360966 Ki = 180.0 nM 6.75
CHEMBL3360965 Ki = 240.0 nM 6.62
CHEMBL3360967 Ki = 300.0 nM 6.52
CHEMBL3360969 Ki = 1500.0 nM 5.82
CHEMBL3360971 Ki = 1600.0 nM 5.80
CHEMBL3360972 Ki = 2500.0 nM 5.60