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Assay Detail

CHEMBL2175533

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

Functional
Agonist activity at human RXRalpha expressed in african green monkey COS1 cells assessed as induction of RXRE transcriptional activity after 12 hrs by luciferase reporter gene assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type COS-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Identification, synthesis, and biological evaluation of the metabolites of 3-amino-6-(3'-aminopropyl)-5H-indeno[1,2-c]isoquinoline-5,11-(6H)dione (AM6-36), a promising rexinoid lead compound for the development of cancer chemotherapeutic and chemopreventive agents.
Chen L, Conda-Sheridan M, Reddy PV, Morrell A, Park EJ, Kondratyuk TP, Pezzuto JM, van Breemen RB, Cushman M.
J Med Chem (2012) 55 : 5965 -5981
PubMed 22712432 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 5.07 5.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2172212 1 5.47
CHEMBL2172208 1 5.12
CHEMBL2172210 1 5.00
CHEMBL2172299 1 4.68
CHEMBL2172214 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2172212 EC50 = 3370.0 nM 5.47
CHEMBL2172208 EC50 = 7650.0 nM 5.12
CHEMBL2172210 EC50 = 9960.0 nM 5.00
CHEMBL2172299 EC50 = 20910.0 nM 4.68
CHEMBL2172214 EC50 > 41400.0 nM -