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Assay Detail

CHEMBL926068

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

Binding
Inhibition of human telomerase expressed in HEK293T cells treated before telomerase elongation by telomeric repeat amplification protocol assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Reevaluation of telomerase inhibition by quadruplex ligands and their mechanisms of action.
De Cian A, Cristofari G, Reichenbach P, De Lemos E, Monchaud D, Teulade-Fichou MP, Shin-Ya K, Lacroix L, Lingner J, Mergny JL.
Proc Natl Acad Sci U S A (2007) 104 : 17347 -17352
PubMed 17954919 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.78 9.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL443683 TELOMESTATIN 1 9.19
CHEMBL259739 1 8.82
CHEMBL336434 1 7.35
CHEMBL409247 1 7.28
CHEMBL65606 TMPYP4 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL443683 TELOMESTATIN IC50 = 0.64 nM 9.19
CHEMBL259739 IC50 = 1.5 nM 8.82
CHEMBL336434 IC50 = 45.0 nM 7.35
CHEMBL409247 IC50 = 52.0 nM 7.28
CHEMBL65606 TMPYP4 IC50 = 550.0 nM 6.26