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Assay Detail

CHEMBL3418582

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

Binding
Inhibition of telomerase in human MGC803 cell extracts after 24 hrs by TRAP-PCR-ELISA
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MGC-803
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design and synthesis of celastrol derivatives as anticancer agents.
Tang WJ, Wang J, Tong X, Shi JB, Liu XH, Li J.
Eur J Med Chem (2015) 95 : 166 -173
PubMed 25812966 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.60 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3417316 1 6.96
CHEMBL3417317 1 6.47
CHEMBL27323 1 6.39
CHEMBL301982 CELASTROL 1 6.11
CHEMBL3417322 1 5.85
CHEMBL3417321 1 5.70
CHEMBL3417319 1 5.10
CHEMBL3417314 1 4.82
CHEMBL3417320 1 4.82
CHEMBL3417313 1 4.73
CHEMBL3417315 1 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3417316 IC50 = 110.0 nM 6.96
CHEMBL3417317 IC50 = 340.0 nM 6.47
CHEMBL27323 IC50 = 410.0 nM 6.39
CHEMBL301982 CELASTROL IC50 = 780.0 nM 6.11
CHEMBL3417322 IC50 = 1410.0 nM 5.85
CHEMBL3417321 IC50 = 2010.0 nM 5.70
CHEMBL3417319 IC50 = 8010.0 nM 5.10
CHEMBL3417314 IC50 = 15100.0 nM 4.82
CHEMBL3417320 IC50 = 15170.0 nM 4.82
CHEMBL3417313 IC50 = 18550.0 nM 4.73
CHEMBL3417315 IC50 = 21010.0 nM 4.68