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Assay Detail

CHEMBL803373

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

Binding
Binding affinity against RAR alpha receptor using [3H]ATRA 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 alpha (CHEMBL2055)
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 5.54 7.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42314 1 7.27
CHEMBL288436 1 5.81
CHEMBL132568 1 5.60
CHEMBL424269 1 5.56
CHEMBL131826 1 5.43
CHEMBL133915 1 5.34
CHEMBL130374 1 5.34
CHEMBL335242 1 5.33
CHEMBL424639 1 5.33
CHEMBL130231 1 5.18
CHEMBL422088 1 5.17
CHEMBL111217 1 5.08
CHEMBL337393 1 -
CHEMBL131122 1 -
CHEMBL130232 1 -
CHEMBL133896 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42314 Ki = 54.0 nM 7.27
CHEMBL288436 Ki = 1550.0 nM 5.81
CHEMBL132568 Ki = 2500.0 nM 5.60
CHEMBL424269 Ki = 2750.0 nM 5.56
CHEMBL131826 Ki = 3730.0 nM 5.43
CHEMBL133915 Ki = 4555.0 nM 5.34
CHEMBL130374 Ki = 4555.0 nM 5.34
CHEMBL335242 Ki = 4663.0 nM 5.33
CHEMBL424639 Ki = 4659.0 nM 5.33
CHEMBL130231 Ki = 6592.0 nM 5.18
CHEMBL422088 Ki = 6756.0 nM 5.17
CHEMBL111217 Ki = 8300.0 nM 5.08
CHEMBL337393 Ki > 10000.0 nM -
CHEMBL131122 Ki > 10000.0 nM -
CHEMBL130232 Ki > 10000.0 nM -
CHEMBL133896 Ki > 10000.0 nM -