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Assay Detail

CHEMBL903630

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

Binding
Inhibition of human telomerase by TRAP assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-based design of benzylamino-acridine compounds as G-quadruplex DNA telomere targeting agents.
Martins C, Gunaratnam M, Stuart J, Makwana V, Greciano O, Reszka AP, Kelland LR, Neidle S.
Bioorg Med Chem Lett (2007) 17 : 2293 -2298
PubMed 17276687 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 6.50 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL397746 1 7.52
CHEMBL336434 1 6.92
CHEMBL239793 1 6.64
CHEMBL397768 1 6.62
CHEMBL397767 1 6.46
CHEMBL396326 1 6.44
CHEMBL396113 1 6.41
CHEMBL396325 1 6.36
CHEMBL1162066 1 6.07
CHEMBL239791 1 6.06
CHEMBL239789 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL397746 EC50 = 30.0 nM 7.52
CHEMBL336434 EC50 = 120.0 nM 6.92
CHEMBL239793 EC50 = 230.0 nM 6.64
CHEMBL397768 EC50 = 240.0 nM 6.62
CHEMBL397767 EC50 = 350.0 nM 6.46
CHEMBL396326 EC50 = 360.0 nM 6.44
CHEMBL396113 EC50 = 390.0 nM 6.41
CHEMBL396325 EC50 = 440.0 nM 6.36
CHEMBL1162066 EC50 = 860.0 nM 6.07
CHEMBL239791 EC50 = 880.0 nM 6.06
CHEMBL239789 EC50 = 1000.0 nM 6.00