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Assay Detail

CHEMBL807687

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

Binding
Binding affinity against RAR gamma receptor using [3H]ATRA as radioligand in CV-1 cells
15
Total Activities
15
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 gamma (CHEMBL2003)
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 15 5.03 5.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL422088 1 5.06
CHEMBL288436 1 5.00
CHEMBL111217 1 -
CHEMBL130231 1 -
CHEMBL337393 1 -
CHEMBL131826 1 -
CHEMBL335242 1 -
CHEMBL130232 1 -
CHEMBL133915 1 -
CHEMBL42314 1 -
CHEMBL133896 1 -
CHEMBL424269 1 -
CHEMBL132568 1 -
CHEMBL130374 1 -
CHEMBL424639 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL422088 Ki = 8764.0 nM 5.06
CHEMBL288436 Ki = 9901.0 nM 5.00
CHEMBL111217 Ki > 10000.0 nM -
CHEMBL130231 Ki > 10000.0 nM -
CHEMBL337393 Ki > 10000.0 nM -
CHEMBL131826 Ki > 10000.0 nM -
CHEMBL335242 Ki > 10000.0 nM -
CHEMBL130232 Ki > 10000.0 nM -
CHEMBL133915 Ki > 10000.0 nM -
CHEMBL42314 Ki > 9513.0 nM -
CHEMBL133896 Ki > 10000.0 nM -
CHEMBL424269 Ki > 10000.0 nM -
CHEMBL132568 Ki > 1000.0 nM -
CHEMBL130374 Ki > 10000.0 nM -
CHEMBL424639 Ki > 10000.0 nM -