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Assay Detail

CHEMBL1692770

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

Binding
Inhibition of human Telomerase activity in cell free system by TRAP assay
4
Total Activities
4
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

N-cyclic bay-substituted perylene G-quadruplex ligands have selective antiproliferative effects on cancer cells and induce telomere damage.
Casagrande V, Salvati E, Alvino A, Bianco A, Ciammaichella A, D'Angelo C, Ginnari-Satriani L, Serrilli AM, Iachettini S, Leonetti C, Neidle S, Ortaggi G, Porru M, Rizzo A, Franceschin M, Biroccio A.
J Med Chem (2011) 54 : 1140 -1156
PubMed 21280624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.17 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL443683 TELOMESTATIN 1 9.15
CHEMBL1689442 1 5.52
CHEMBL1689438 1 5.00
CHEMBL1689441 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL443683 TELOMESTATIN IC50 = 0.7 nM 9.15
CHEMBL1689442 IC50 = 3000.0 nM 5.52
CHEMBL1689438 IC50 = 10000.0 nM 5.00
CHEMBL1689441 IC50 = 10000.0 nM 5.00