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Assay Detail

CHEMBL917191

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Binding
Inhibition of human telomerase from HEK293 cell extracts by Flash-Plate assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Catecholic flavonoids acting as telomerase inhibitors.
Menichincheri M, Ballinari D, Bargiotti A, Bonomini L, Ceccarelli W, D'Alessio R, Fretta A, Moll J, Polucci P, Soncini C, Tibolla M, Trosset JY, Vanotti E.
J Med Chem (2004) 47 : 6466 -6475
PubMed 15588081 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 5.50 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225211 1 6.89
CHEMBL222541 1 6.70
CHEMBL376279 1 6.33
CHEMBL222354 1 6.22
CHEMBL426182 1 6.10
CHEMBL222132 1 6.09
CHEMBL222757 1 5.92
CHEMBL225618 1 5.77
CHEMBL222547 1 5.66
CHEMBL420982 1 5.52
CHEMBL222539 1 5.44
CHEMBL390725 1 5.40
CHEMBL222557 1 5.22
CHEMBL222490 1 5.13
CHEMBL225228 1 5.11
CHEMBL225227 1 4.96
CHEMBL221503 1 4.93
CHEMBL222381 1 4.72
CHEMBL225572 1 4.66
CHEMBL75267 7,8-DIHYDROXYFLAVONE 1 4.44
CHEMBL225513 1 4.30
CHEMBL222238 1 -
CHEMBL436311 1 -
CHEMBL373745 1 -
CHEMBL448169 1 -
CHEMBL225649 1 -
CHEMBL321555 1 -
CHEMBL222556 1 -
CHEMBL222211 1 -
CHEMBL301624 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225211 IC50 = 130.0 nM 6.89
CHEMBL222541 IC50 = 200.0 nM 6.70
CHEMBL376279 IC50 = 470.0 nM 6.33
CHEMBL222354 IC50 = 600.0 nM 6.22
CHEMBL426182 IC50 = 800.0 nM 6.10
CHEMBL222132 IC50 = 820.0 nM 6.09
CHEMBL222757 IC50 = 1200.0 nM 5.92
CHEMBL225618 IC50 = 1700.0 nM 5.77
CHEMBL222547 IC50 = 2200.0 nM 5.66
CHEMBL420982 IC50 = 3000.0 nM 5.52
CHEMBL222539 IC50 = 3600.0 nM 5.44
CHEMBL390725 IC50 = 4000.0 nM 5.40
CHEMBL222557 IC50 = 6000.0 nM 5.22
CHEMBL222490 IC50 = 7400.0 nM 5.13
CHEMBL225228 IC50 = 7800.0 nM 5.11
CHEMBL225227 IC50 = 11000.0 nM 4.96
CHEMBL221503 IC50 = 11700.0 nM 4.93
CHEMBL222381 IC50 = 19000.0 nM 4.72
CHEMBL225572 IC50 = 22100.0 nM 4.66
CHEMBL75267 7,8-DIHYDROXYFLAVONE IC50 = 36000.0 nM 4.44
CHEMBL225513 IC50 = 50000.0 nM 4.30
CHEMBL222238 IC50 > 40000.0 nM -
CHEMBL436311 IC50 > 40000.0 nM -
CHEMBL373745 IC50 > 40000.0 nM -
CHEMBL448169 IC50 > 40000.0 nM -
CHEMBL225649 IC50 > 40000.0 nM -
CHEMBL321555 IC50 > 40000.0 nM -
CHEMBL222556 IC50 > 40000.0 nM -
CHEMBL222211 IC50 > 40000.0 nM -
CHEMBL301624 IC50 > 40000.0 nM -