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

CHEMBL864040

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

Functional
Inhibition of telomerase activity from human A2780 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A2780
Confidence 9 — Direct single protein target
Curated By Expert

Target

Telomerase reverse transcriptase (CHEMBL2916)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Trisubstituted acridines as G-quadruplex telomere targeting agents. Effects of extensions of the 3,6- and 9-side chains on quadruplex binding, telomerase activity, and cell proliferation.
Moore MJ, Schultes CM, Cuesta J, Cuenca F, Gunaratnam M, Tanious FA, Wilson WD, Neidle S.
J Med Chem (2006) 49 : 582 -599
PubMed 16420044 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 6.45 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201766 1 7.17
CHEMBL201697 1 7.00
CHEMBL336434 1 6.95
CHEMBL202769 1 6.93
CHEMBL383282 1 6.84
CHEMBL264477 1 6.78
CHEMBL202717 1 6.59
CHEMBL203366 1 6.49
CHEMBL202167 1 5.71
CHEMBL202820 1 5.28
CHEMBL202562 1 5.16
CHEMBL381966 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201766 EC50 = 67.0 nM 7.17
CHEMBL201697 EC50 = 99.0 nM 7.00
CHEMBL336434 EC50 = 113.0 nM 6.95
CHEMBL202769 EC50 = 117.0 nM 6.93
CHEMBL383282 EC50 = 146.0 nM 6.84
CHEMBL264477 EC50 = 167.0 nM 6.78
CHEMBL202717 EC50 = 255.0 nM 6.59
CHEMBL203366 EC50 = 326.0 nM 6.49
CHEMBL202167 EC50 = 1930.0 nM 5.71
CHEMBL202820 EC50 = 5200.0 nM 5.28
CHEMBL202562 EC50 = 6910.0 nM 5.16
CHEMBL381966 EC50 > 20000.0 nM -