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Assay Detail

CHEMBL812000

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

Binding
Ability to inhibit human telomerase in a modified cell-free TRAP assay using extracts from A2780 cell line
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type A2780
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Human telomerase inhibition by substituted acridine derivatives.
Harrison RJ, Gowan SM, Kelland LR, Neidle S.
Bioorg Med Chem Lett (1999) 9 : 2463 -2468
PubMed 10498189 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.40 5.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL309919 1 5.87
CHEMBL431404 1 5.58
CHEMBL81747 1 5.57
CHEMBL81268 1 5.55
CHEMBL82008 1 5.51
CHEMBL311055 1 5.39
CHEMBL83173 1 5.36
CHEMBL79900 1 5.28
CHEMBL81271 1 5.27
CHEMBL309982 1 5.24
CHEMBL81516 1 5.10
CHEMBL311072 1 5.09
CHEMBL79536 1 -
CHEMBL421143 1 -
CHEMBL310569 1 -
CHEMBL310838 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL309919 IC50 = 1350.0 nM 5.87
CHEMBL431404 IC50 = 2600.0 nM 5.58
CHEMBL81747 IC50 = 2700.0 nM 5.57
CHEMBL81268 IC50 = 2800.0 nM 5.55
CHEMBL82008 IC50 = 3100.0 nM 5.51
CHEMBL311055 IC50 = 4100.0 nM 5.39
CHEMBL83173 IC50 = 4400.0 nM 5.36
CHEMBL79900 IC50 = 5200.0 nM 5.28
CHEMBL81271 IC50 = 5400.0 nM 5.27
CHEMBL309982 IC50 = 5800.0 nM 5.24
CHEMBL81516 IC50 = 8000.0 nM 5.10
CHEMBL311072 IC50 = 8200.0 nM 5.09
CHEMBL79536 IC50 > 50000.0 nM -
CHEMBL421143 IC50 > 50000.0 nM -
CHEMBL310569 IC50 > 50000.0 nM -
CHEMBL310838 IC50 > 50000.0 nM -