Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2330504

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

Binding
Activation of human RXRalpha activity expressed in COS1 cells after 12 hrs by RXRE-luciferase reporter gene assay
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Design, synthesis, and biological evaluation of indenoisoquinoline rexinoids with chemopreventive potential.
Conda-Sheridan M, Park EJ, Beck DE, Reddy PV, Nguyen TX, Hu B, Chen L, White JJ, van Breemen RB, Pezzuto JM, Cushman M.
J Med Chem (2013) 56 : 2581 -2605
PubMed 23472886 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 39 5.14 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288436 1 7.40
CHEMBL2172208 1 5.38
CHEMBL2172212 1 5.36
CHEMBL242857 1 5.32
CHEMBL2326683 1 5.16
CHEMBL2322964 1 5.08
CHEMBL213072 1 5.06
CHEMBL2322955 1 5.04
CHEMBL425544 1 5.02
CHEMBL2324622 1 5.00
CHEMBL2322288 1 4.97
CHEMBL1181663 1 4.95
CHEMBL1182248 1 4.91
CHEMBL2172210 1 4.82
CHEMBL1181674 1 4.80
CHEMBL1185123 1 4.79
CHEMBL2322286 1 4.73
CHEMBL2323836 1 4.71
CHEMBL2322954 1 -
CHEMBL2172206 1 -
CHEMBL242413 1 -
CHEMBL121622 1 -
CHEMBL244759 1 -
CHEMBL2172218 1 -
CHEMBL2172214 1 -
CHEMBL2172216 1 -
CHEMBL2312904 1 -
CHEMBL2172209 1 -
CHEMBL382475 1 -
CHEMBL2322957 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288436 EC50 = 40.0 nM 7.40
CHEMBL2172208 EC50 = 4220.0 nM 5.38
CHEMBL2172212 EC50 = 4400.0 nM 5.36
CHEMBL242857 EC50 = 4840.0 nM 5.32
CHEMBL2326683 EC50 = 7000.0 nM 5.16
CHEMBL2322964 EC50 = 8400.0 nM 5.08
CHEMBL213072 EC50 = 8660.0 nM 5.06
CHEMBL2322955 EC50 = 9220.0 nM 5.04
CHEMBL425544 EC50 = 9600.0 nM 5.02
CHEMBL2324622 EC50 = 10010.0 nM 5.00
CHEMBL2322288 EC50 = 10720.0 nM 4.97
CHEMBL1181663 EC50 = 11300.0 nM 4.95
CHEMBL1182248 EC50 = 12200.0 nM 4.91
CHEMBL2172210 EC50 = 15200.0 nM 4.82
CHEMBL1181674 EC50 = 15900.0 nM 4.80
CHEMBL1185123 EC50 = 16400.0 nM 4.79
CHEMBL2322286 EC50 = 18440.0 nM 4.73
CHEMBL2323836 EC50 = 19460.0 nM 4.71
CHEMBL2312571 EC50 > 44500.0 nM -
CHEMBL2322965 EC50 - -
CHEMBL2323837 EC50 - -
CHEMBL2321897 EC50 - -
CHEMBL2323838 EC50 - -
CHEMBL2322285 EC50 - -
CHEMBL2322290 EC50 - -
CHEMBL207901 EC50 - -
CHEMBL2322956 EC50 - -
CHEMBL2322957 EC50 - -
CHEMBL382475 EC50 - -
CHEMBL2172209 EC50 - -
CHEMBL2312904 EC50 > 20700.0 nM -
CHEMBL2172216 EC50 - -
CHEMBL2172214 EC50 > 34700.0 nM -
CHEMBL2172218 EC50 - -
CHEMBL244759 EC50 - -
CHEMBL121622 EC50 - -
CHEMBL242413 EC50 - -
CHEMBL2172206 EC50 - -
CHEMBL2322954 EC50 - -