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Assay Detail

CHEMBL806019

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

Binding
Binding affinity against RXR gamma receptor using [3H]9-cis-RA as radioligand in CV-1 cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cercopithecidae
Cell Type CV-1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Retinoic acid receptor RXR-gamma (CHEMBL2004)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of novel RXR-selective modulators with improved pharmacological profile.
Michellys PY, Boehm MF, Chen JH, Grese TA, Karanewsky DS, Leibowitz MD, Liu S, Mais DA, Mapes CM, Reifel-Miller A, Ogilvie KM, Rungta D, Thompson AW, Tyhonas JS, Yumibe N, Ardecky RJ.
Bioorg Med Chem Lett (2003) 13 : 4071 -4075
PubMed 14592510 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.85 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL337393 1 8.55
CHEMBL130232 1 8.54
CHEMBL133915 1 8.25
CHEMBL130374 1 8.25
CHEMBL133896 1 8.11
CHEMBL422088 1 7.96
CHEMBL288436 1 7.92
CHEMBL335242 1 7.91
CHEMBL111217 1 7.88
CHEMBL424639 1 7.65
CHEMBL131122 1 7.63
CHEMBL131826 1 7.56
CHEMBL132568 1 7.56
CHEMBL130231 1 7.39
CHEMBL424269 1 7.34
CHEMBL42314 1 7.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL337393 Ki = 2.8 nM 8.55
CHEMBL130232 Ki = 2.9 nM 8.54
CHEMBL133915 Ki = 5.6 nM 8.25
CHEMBL130374 Ki = 5.6 nM 8.25
CHEMBL133896 Ki = 7.7 nM 8.11
CHEMBL422088 Ki = 10.9 nM 7.96
CHEMBL288436 Ki = 12.0 nM 7.92
CHEMBL335242 Ki = 12.4 nM 7.91
CHEMBL111217 Ki = 13.2 nM 7.88
CHEMBL424639 Ki = 22.5 nM 7.65
CHEMBL131122 Ki = 23.6 nM 7.63
CHEMBL131826 Ki = 27.8 nM 7.56
CHEMBL132568 Ki = 27.6 nM 7.56
CHEMBL130231 Ki = 40.3 nM 7.39
CHEMBL424269 Ki = 45.7 nM 7.34
CHEMBL42314 Ki = 84.0 nM 7.08