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Assay Detail

CHEMBL806017

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

Binding
Displacement of [3H]9-cis-RA from Retinoic X receptor beta
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Retinoic acid receptor RXR-beta (CHEMBL1870)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and structure-activity relationship of novel RXR-selective modulators.
Michellys PY, D'Arrigo J, Grese TA, Karanewsky DS, Leibowitz MD, Mais DA, Mapes CM, Reifel-Miller A, Rungta D, Boehm MF.
Bioorg Med Chem Lett (2004) 14 : 1593 -1598
PubMed 15006411 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.68 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41422 1 8.40
CHEMBL288436 1 8.12
CHEMBL41260 1 8.00
CHEMBL41146 1 8.00
CHEMBL41890 1 7.96
CHEMBL2372524 1 7.92
CHEMBL43238 1 7.92
CHEMBL291034 1 7.92
CHEMBL41742 1 7.82
CHEMBL42314 1 7.75
CHEMBL44420 1 7.48
CHEMBL290761 1 7.26
CHEMBL290246 1 7.19
CHEMBL39206 1 6.85
CHEMBL265051 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41422 Ki = 4.0 nM 8.40
CHEMBL288436 Ki = 7.5 nM 8.12
CHEMBL41260 Ki = 10.0 nM 8.00
CHEMBL41146 Ki = 10.0 nM 8.00
CHEMBL41890 Ki = 11.0 nM 7.96
CHEMBL2372524 Ki = 12.0 nM 7.92
CHEMBL43238 Ki = 12.0 nM 7.92
CHEMBL291034 Ki = 12.0 nM 7.92
CHEMBL41742 Ki = 15.0 nM 7.82
CHEMBL42314 Ki = 18.0 nM 7.75
CHEMBL44420 Ki = 33.0 nM 7.48
CHEMBL290761 Ki = 55.0 nM 7.26
CHEMBL290246 Ki = 64.5 nM 7.19
CHEMBL39206 Ki = 142.0 nM 6.85
CHEMBL265051 Ki = 261.0 nM 6.58