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Assay Detail

CHEMBL3420249

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

Binding
Inhibition of Influenza A virus (A/udorn/1972(H3N2)) M2 V27A mutant channel expressed in Xenopus oocyte plasma membranes after 2 mins by two-electrode voltage clamp assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Influenza A virus (A/udorn/1972(H3N2))
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Matrix protein 2 (CHEMBL2052)
Type SINGLE PROTEIN
Organism Influenza A virus (A/Udorn/307/1972(H3N2))

Publication

New polycyclic dual inhibitors of the wild type and the V27A mutant M2 channel of the influenza A virus with unexpected binding mode.
Rey-Carrizo M, Gazzarrini S, Llabrés S, Frigolé-Vivas M, Juárez-Jiménez J, Font-Bardia M, Naesens L, Moroni A, Luque FJ, Vázquez S.
Eur J Med Chem (2015) 96 : 318 -329
PubMed 25899336 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 4.63 4.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3415948 1 4.76
CHEMBL3305169 1 4.65
CHEMBL3415949 1 4.49
CHEMBL3415952 1 -
CHEMBL3415951 1 -
CHEMBL3415950 1 -
CHEMBL3415947 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3415948 IC50 = 17200.0 nM 4.76
CHEMBL3305169 IC50 = 22600.0 nM 4.65
CHEMBL3415949 IC50 = 32200.0 nM 4.49
CHEMBL3415952 IC50 - -
CHEMBL3415951 IC50 - -
CHEMBL3415950 IC50 - -
CHEMBL3415947 IC50 = 184600.0 nM -