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Assay Detail

CHEMBL800654

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

Functional
Effective concentration required for agonistic activity in CV-1 cells expressing RXR-alpha
8
Total Activities
8
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 8 6.60 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL88740 1 8.70
CHEMBL430651 1 7.19
CHEMBL91979 1 6.63
CHEMBL314745 1 6.04
CHEMBL328507 1 5.99
CHEMBL420808 1 5.84
CHEMBL93571 1 5.84
CHEMBL414218 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL88740 EC50 = 2.0 nM 8.70
CHEMBL430651 EC50 = 65.0 nM 7.19
CHEMBL91979 EC50 = 235.0 nM 6.63
CHEMBL314745 EC50 = 914.0 nM 6.04
CHEMBL328507 EC50 = 1024.0 nM 5.99
CHEMBL420808 EC50 = 1442.0 nM 5.84
CHEMBL93571 EC50 = 1438.0 nM 5.84
CHEMBL414218 EC50 - nM -