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Assay Detail

CHEMBL4255723

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

Binding
Binding affinity to Influenza A virus A/Udorn/72 wild-type M2 proton channel expressed in Xenopus laevis oocytes at pH 5.5 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

Unraveling the Binding, Proton Blockage, and Inhibition of Influenza M2 WT and S31N by Rimantadine Variants.
Drakopoulos A, Tzitzoglaki C, McGuire K, Hoffmann A, Konstantinidi A, Kolokouris D, Ma C, Freudenberger K, Hutterer J, Gauglitz G, Wang J, Schmidtke M, Busath DD, Kolocouris A.
ACS Med Chem Lett (2018) 9 : 198 -203
PubMed 29541360 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 5.01 5.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1235691 1 5.50
CHEMBL3392935 1 5.41
CHEMBL959 RIMANTADINE 4.0 1 5.16
CHEMBL660 AMANTADINE 4.0 1 5.05
CHEMBL4277543 1 4.89
CHEMBL4292664 1 4.06
CHEMBL4284791 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1235691 Kd = 3200.0 nM 5.50
CHEMBL3392935 Kd = 3900.0 nM 5.41
CHEMBL959 RIMANTADINE Kd = 7000.0 nM 5.16
CHEMBL660 AMANTADINE Kd = 9000.0 nM 5.05
CHEMBL4277543 Kd = 13000.0 nM 4.89
CHEMBL4292664 Kd = 88000.0 nM 4.06
CHEMBL4284791 Kd - -