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Assay Detail

CHEMBL2014495

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

Binding
Inhibition of GST-tagged Human papillomavirus 16 protein E6 interaction with His-tagged human caspase 8 expressed in Escherichia coli after 1 hr incubation followed by overnight incubation by Alpha screening technique
5
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human papillomavirus type 16
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein E6 (CHEMBL2010633)
Type SINGLE PROTEIN
Organism Human papillomavirus type 16

Publication

Small molecule inhibitors of the HPV16-E6 interaction with caspase 8.
Yuan CH, Filippova M, Tungteakkhun SS, Duerksen-Hughes PJ, Krstenansky JL.
Bioorg Med Chem Lett (2012) 22 : 2125 -2129
PubMed 22300659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.74 6.07
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL164 MYRICETIN 1 6.07
CHEMBL28626 MORIN 1 5.40
CHEMBL150 KAEMPFEROL 1.0 2 -
CHEMBL50 QUERCETIN 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL164 MYRICETIN IC50 = 850.0 nM 6.07
CHEMBL28626 MORIN IC50 = 4000.0 nM 5.40
CHEMBL150 KAEMPFEROL Inhibition - % -
CHEMBL50 QUERCETIN IC50 > 20000.0 nM -
CHEMBL150 KAEMPFEROL IC50 > 20000.0 nM -