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Assay Detail

CHEMBL3796330

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

Binding
Inhibition of Influenza A virus PR/8/34 6His-tagged PA (239 to 716 residues) interaction with GST-tagged PB1 (1 to 25 residues) expressed in Escherichia coli compound treated in PBS buffer measured after overnight incubation by ELISA
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Influenza A virus (A/Puerto Rico/8/1934(H1N1))
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

PA/PB1 (CHEMBL3137263)
Type PROTEIN-PROTEIN INTERACTION
Organism Influenza A virus (A/Puerto Rico/8/1934(H1N1))

Publication

4,6-Diphenylpyridines as Promising Novel Anti-Influenza Agents Targeting the PA-PB1 Protein-Protein Interaction: Structure-Activity Relationships Exploration with the Aid of Molecular Modeling.
Trist IM, Nannetti G, Tintori C, Fallacara AL, Deodato D, Mercorelli B, Palù G, Wijtmans M, Gospodova T, Edink E, Verheij M, de Esch I, Viteva L, Loregian A, Botta M.
J Med Chem (2016) 59 : 2688 -2703
PubMed 26924568 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 4.37 4.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3110332 1 4.45
CHEMBL3794203 1 4.28
CHEMBL1229 OSELTAMIVIR 4.0 1 -
CHEMBL1643 RIBAVIRIN 4.0 1 -
CHEMBL3792827 1 -
CHEMBL3794263 1 -
CHEMBL3792526 1 -
CHEMBL3792635 1 -
CHEMBL3793877 1 -
CHEMBL3792991 1 -
CHEMBL3794124 1 -
CHEMBL3794520 1 -
CHEMBL3794048 1 -
CHEMBL3794429 1 -
CHEMBL3793619 1 -
CHEMBL3794234 1 -
CHEMBL3792444 1 -
CHEMBL3793346 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3110332 IC50 = 35900.0 nM 4.45
CHEMBL3794203 IC50 = 52600.0 nM 4.28
CHEMBL1229 OSELTAMIVIR IC50 - -
CHEMBL1643 RIBAVIRIN IC50 - -
CHEMBL3792827 IC50 > 200000.0 nM -
CHEMBL3794263 IC50 = 165000.0 nM -
CHEMBL3792526 IC50 > 200000.0 nM -
CHEMBL3792635 IC50 > 200000.0 nM -
CHEMBL3793877 IC50 = 116000.0 nM -
CHEMBL3792991 IC50 = 140000.0 nM -
CHEMBL3794124 IC50 = 122000.0 nM -
CHEMBL3794520 IC50 = 190000.0 nM -
CHEMBL3794048 IC50 > 200000.0 nM -
CHEMBL3794429 IC50 > 200000.0 nM -
CHEMBL3793619 IC50 > 200000.0 nM -
CHEMBL3794234 IC50 = 177000.0 nM -
CHEMBL3792444 IC50 = 175000.0 nM -
CHEMBL3793346 IC50 = 195000.0 nM -