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Assay Detail

CHEMBL800656

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

Functional
Effective concentration for antagonistic activity against RXR-alpha expressed in CV-1 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Retinoic acid receptor RXR-alpha (CHEMBL2061)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of benzofused heterocyclic RXR modulators.
Gernert DL, Neel DA, Boehm MF, Leibowitz MD, Mais DA, Michellys PY, Rungta D, Reifel-Miller A, Grese TA.
Bioorg Med Chem Lett (2004) 14 : 2759 -2763
PubMed 15125928 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.02 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL414218 1 8.40
CHEMBL92243 1 8.19
CHEMBL92798 1 7.68
CHEMBL93246 1 7.58
CHEMBL92447 1 7.52
CHEMBL430651 1 7.18
CHEMBL421748 1 5.81
CHEMBL93128 1 5.40
CHEMBL264746 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL414218 EC50 = 4.0 nM 8.40
CHEMBL92243 EC50 = 6.4 nM 8.19
CHEMBL92798 EC50 = 21.1 nM 7.68
CHEMBL93246 EC50 = 26.4 nM 7.58
CHEMBL92447 EC50 = 30.1 nM 7.52
CHEMBL430651 EC50 = 66.3 nM 7.18
CHEMBL421748 EC50 = 1533.0 nM 5.81
CHEMBL93128 EC50 = 3976.3 nM 5.40
CHEMBL264746 EC50 = 4154.0 nM 5.38