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Assay Detail

CHEMBL2427719

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

Binding
Inhibition of telomerase (unknown origin) by TRAP assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Toward the design of new DNA G-quadruplex ligands through rational analysis of polymorphism and binding data.
Artese A, Costa G, Distinto S, Moraca F, Ortuso F, Parrotta L, Alcaro S.
Eur J Med Chem (2013) 68 : 139 -149
PubMed 23974014 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.30 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1078511 1 7.75
CHEMBL2425367 1 7.55
CHEMBL335819 1 7.22
CHEMBL1997011 1 7.00
CHEMBL2111043 ISOMETAMIDIUM 2.0 1 7.00
CHEMBL2425366 1 6.89
CHEMBL2425365 1 6.66
CHEMBL219728 1 6.36
CHEMBL274335 1 6.30
CHEMBL2425364 1 6.12
CHEMBL2425363 1 5.89
CHEMBL343445 1 5.75
CHEMBL2425362 1 5.27
CHEMBL119096 CRYPTOLEPINE 1 5.03
CHEMBL2425361 1 5.00
CHEMBL327101 MERIDINE 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1078511 IC50 = 18.0 nM 7.75
CHEMBL2425367 IC50 = 28.0 nM 7.55
CHEMBL335819 IC50 = 60.0 nM 7.22
CHEMBL1997011 IC50 = 100.0 nM 7.00
CHEMBL2111043 ISOMETAMIDIUM IC50 = 100.0 nM 7.00
CHEMBL2425366 IC50 = 130.0 nM 6.89
CHEMBL2425365 IC50 = 220.0 nM 6.66
CHEMBL219728 IC50 = 440.0 nM 6.36
CHEMBL274335 IC50 = 500.0 nM 6.30
CHEMBL2425364 IC50 = 750.0 nM 6.12
CHEMBL2425363 IC50 = 1300.0 nM 5.89
CHEMBL343445 IC50 = 1800.0 nM 5.75
CHEMBL2425362 IC50 = 5400.0 nM 5.27
CHEMBL119096 CRYPTOLEPINE IC50 = 9400.0 nM 5.03
CHEMBL2425361 IC50 = 10000.0 nM 5.00
CHEMBL327101 MERIDINE IC50 = 11000.0 nM 4.96