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Assay Detail

CHEMBL801376

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

Binding
Binding affinity for Retinoic acid receptor RXR-gamma was determined by competing with 3[H]-9-cis-RA
17
Total Activities
17
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-gamma (CHEMBL4277)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.
Michellys PY, Ardecky RJ, Chen JH, D'Arrigo J, Grese TA, Karanewsky DS, Leibowitz MD, Liu S, Mais DA, Mapes CM, Montrose-Rafizadeh C, Ogilvie KM, Reifel-Miller A, Rungta D, Thompson AW, Tyhonas JS, Boehm MF.
J Med Chem (2003) 46 : 4087 -4103
PubMed 12954061 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.88 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL340074 1 8.72
CHEMBL340555 1 8.60
CHEMBL339298 1 8.31
CHEMBL133176 1 8.31
CHEMBL335751 1 8.18
CHEMBL129887 1 8.16
CHEMBL336086 1 8.12
CHEMBL131561 1 8.00
CHEMBL42314 1 7.92
CHEMBL335762 1 7.86
CHEMBL337719 1 7.80
CHEMBL288436 1 7.75
CHEMBL132488 1 7.74
CHEMBL445634 1 7.31
CHEMBL130577 1 7.20
CHEMBL130230 1 7.13
CHEMBL129976 1 6.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL340074 Ki = 1.9 nM 8.72
CHEMBL340555 Ki = 2.5 nM 8.60
CHEMBL339298 Ki = 4.9 nM 8.31
CHEMBL133176 Ki = 4.9 nM 8.31
CHEMBL335751 Ki = 6.6 nM 8.18
CHEMBL129887 Ki = 6.9 nM 8.16
CHEMBL336086 Ki = 7.6 nM 8.12
CHEMBL131561 Ki = 10.0 nM 8.00
CHEMBL42314 Ki = 12.0 nM 7.92
CHEMBL335762 Ki = 13.9 nM 7.86
CHEMBL337719 Ki = 15.9 nM 7.80
CHEMBL288436 Ki = 18.0 nM 7.75
CHEMBL132488 Ki = 18.1 nM 7.74
CHEMBL445634 Ki = 48.6 nM 7.31
CHEMBL130577 Ki = 63.2 nM 7.20
CHEMBL130230 Ki = 73.9 nM 7.13
CHEMBL129976 Ki = 154.7 nM 6.81