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Assay Detail

CHEMBL5588858

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

Binding
Agonist activity at GST tagged LXRbeta (unknown origin) using SRC1 as coactivator peptide incubated for 1 hr by coactivator recruitment based TR-FRET assay
25
Total Activities
25
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

Nonlipogenic ABCA1 Inducers (NLAI) for Alzheimer's Disease Validated in a Mouse Model Expressing Human <i>APOE3/APOE4</i>.
Velma GR, Laham MS, Lewandowski C, Valencia-Olvera AC, Balu D, Moore A, Ackerman-Berrier M, Rychetsky P, Penton C, Musku SR, Annadurai A, Sulaiman MI, Ma N, J Thatcher GR.
J Med Chem (2024) 67 : 15061 -15079
PubMed 39191400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 5.71 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62136 T091317 1 6.96
CHEMBL5597982 1 6.82
CHEMBL5596248 1 6.29
CHEMBL5597153 1 6.25
CHEMBL5596815 1 6.24
CHEMBL5597394 1 6.11
CHEMBL5598250 1 5.82
CHEMBL5596939 1 5.82
CHEMBL5596386 1 5.72
CHEMBL5597291 1 5.70
CHEMBL5598331 1 5.64
CHEMBL5597028 1 5.35
CHEMBL5596392 1 4.96
CHEMBL5590383 1 4.89
CHEMBL5590706 1 4.89
CHEMBL5597319 1 4.82
CHEMBL5596811 1 4.82
CHEMBL5596907 1 -
CHEMBL5596592 1 -
CHEMBL5597943 1 -
CHEMBL5598279 1 -
CHEMBL5596520 1 -
CHEMBL5597106 1 -
CHEMBL5598324 1 -
CHEMBL5590617 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62136 T091317 EC50 = 110.0 nM 6.96
CHEMBL5597982 EC50 = 150.0 nM 6.82
CHEMBL5596248 EC50 = 510.0 nM 6.29
CHEMBL5597153 EC50 = 560.0 nM 6.25
CHEMBL5596815 EC50 = 580.0 nM 6.24
CHEMBL5597394 EC50 = 770.0 nM 6.11
CHEMBL5598250 EC50 = 1500.0 nM 5.82
CHEMBL5596939 EC50 = 1500.0 nM 5.82
CHEMBL5596386 EC50 = 1900.0 nM 5.72
CHEMBL5597291 EC50 = 2000.0 nM 5.70
CHEMBL5598331 EC50 = 2300.0 nM 5.64
CHEMBL5597028 EC50 = 4500.0 nM 5.35
CHEMBL5596392 EC50 = 11000.0 nM 4.96
CHEMBL5590383 EC50 = 13000.0 nM 4.89
CHEMBL5590706 EC50 = 13000.0 nM 4.89
CHEMBL5597319 EC50 = 15000.0 nM 4.82
CHEMBL5596811 EC50 = 15000.0 nM 4.82
CHEMBL5596907 EC50 > 25000.0 nM -
CHEMBL5596592 EC50 > 25000.0 nM -
CHEMBL5597943 EC50 > 25000.0 nM -
CHEMBL5598279 EC50 > 25000.0 nM -
CHEMBL5596520 EC50 > 25000.0 nM -
CHEMBL5597106 EC50 > 25000.0 nM -
CHEMBL5598324 EC50 > 25000.0 nM -
CHEMBL5590617 EC50 > 25000.0 nM -