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Assay Detail

CHEMBL840260

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Binding
Concentration required to inhibit 50% of telomerase activity
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Evaluation of by disubstituted acridone derivatives as telomerase inhibitors: the importance of G-quadruplex binding.
Harrison RJ, Reszka AP, Haider SM, Romagnoli B, Morrell J, Read MA, Gowan SM, Incles CM, Kelland LR, Neidle S.
Bioorg Med Chem Lett (2004) 14 : 5845 -5849
PubMed 15501053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 5.79 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL184103 1 7.05
CHEMBL361868 1 6.70
CHEMBL184289 1 6.70
CHEMBL186346 1 6.70
CHEMBL186019 1 6.40
CHEMBL186971 1 6.22
CHEMBL186933 1 6.16
CHEMBL184711 1 5.77
CHEMBL365070 1 5.77
CHEMBL187257 1 5.72
CHEMBL186489 1 5.72
CHEMBL425350 1 5.72
CHEMBL185718 1 5.64
CHEMBL365069 1 5.64
CHEMBL186848 1 5.64
CHEMBL184503 1 5.64
CHEMBL187238 1 5.55
CHEMBL186509 1 5.37
CHEMBL187966 1 5.31
CHEMBL186037 1 5.28
CHEMBL187202 1 5.24
CHEMBL186994 1 5.24
CHEMBL362887 1 5.24
CHEMBL187955 1 5.23
CHEMBL185975 1 5.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL184103 EC50 = 90.0 nM 7.05
CHEMBL361868 EC50 = 200.0 nM 6.70
CHEMBL184289 EC50 = 200.0 nM 6.70
CHEMBL186346 EC50 = 200.0 nM 6.70
CHEMBL186019 EC50 = 400.0 nM 6.40
CHEMBL186971 EC50 = 600.0 nM 6.22
CHEMBL186933 EC50 = 700.0 nM 6.16
CHEMBL184711 EC50 = 1700.0 nM 5.77
CHEMBL365070 EC50 = 1700.0 nM 5.77
CHEMBL187257 EC50 = 1900.0 nM 5.72
CHEMBL186489 EC50 = 1900.0 nM 5.72
CHEMBL425350 EC50 = 1900.0 nM 5.72
CHEMBL185718 EC50 = 2300.0 nM 5.64
CHEMBL365069 EC50 = 2300.0 nM 5.64
CHEMBL186848 EC50 = 2300.0 nM 5.64
CHEMBL184503 EC50 = 2300.0 nM 5.64
CHEMBL187238 EC50 = 2800.0 nM 5.55
CHEMBL186509 EC50 = 4300.0 nM 5.37
CHEMBL187966 EC50 = 4900.0 nM 5.31
CHEMBL186037 EC50 = 5200.0 nM 5.28
CHEMBL187202 EC50 = 5800.0 nM 5.24
CHEMBL186994 EC50 = 5800.0 nM 5.24
CHEMBL362887 EC50 = 5700.0 nM 5.24
CHEMBL187955 EC50 = 5900.0 nM 5.23
CHEMBL185975 EC50 = 8100.0 nM 5.09