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Assay Detail

CHEMBL2175309

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

Binding
Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction by telomeric repeat amplification protocol
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A new strategy for detection and development of tractable telomerase inhibitors.
Cohn EP, Wu KL, Pettus TR, Reich NO.
J Med Chem (2012) 55 : 3678 -3686
PubMed 22413845 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.01 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2170855 1 7.22
CHEMBL222541 1 6.64
CHEMBL297453 EPIGALOCATECHIN GALLATE 3.0 1 5.93
CHEMBL2170857 1 5.88
CHEMBL27323 1 5.44
CHEMBL2170856 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2170855 IC50 = 60.0 nM 7.22
CHEMBL222541 IC50 = 230.0 nM 6.64
CHEMBL297453 EPIGALOCATECHIN GALLATE IC50 = 1180.0 nM 5.93
CHEMBL2170857 IC50 = 1320.0 nM 5.88
CHEMBL27323 IC50 = 3600.0 nM 5.44
CHEMBL2170856 IC50 = 12100.0 nM 4.92