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Assay Detail

CHEMBL4329323

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

Binding
Inhibition of PB2 in Influenza A virus (A/Weiss/1943(H1N1)) infected in MDCK cells assessed as reduction in virus induced cell death after 5 days by CCK-8 assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Influenza A virus (A/Weiss/1943(H1N1))
Cell Type MDCK
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Polymerase basic protein 2 (CHEMBL3317339)
Type SINGLE PROTEIN
Organism Influenza A virus (strain A/Puerto Rico/8/1934 H1N1)

Publication

Design, synthesis and biological evaluation of novel, orally bioavailable pyrimidine-fused heterocycles as influenza PB2 inhibitors.
Xiong J, Wang J, Hu G, Zhao W, Li J.
Eur J Med Chem (2019) 162 : 249 -265
PubMed 30448415 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 33 8.11 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4593027 1 10.22
CHEMBL4472219 1 9.70
CHEMBL4568323 1 9.70
CHEMBL4570851 1 9.40
CHEMBL4434862 1 9.30
CHEMBL4466462 1 9.30
CHEMBL3318007 PIMODIVIR 3.0 1 9.22
CHEMBL4547565 1 8.85
CHEMBL4469158 1 8.59
CHEMBL4470294 1 8.55
CHEMBL4435833 1 8.52
CHEMBL4444973 1 8.40
CHEMBL4529778 1 8.35
CHEMBL4468219 1 8.28
CHEMBL4469921 1 8.26
CHEMBL4459959 1 8.02
CHEMBL4524775 1 8.00
CHEMBL4567115 1 8.00
CHEMBL4530239 1 7.96
CHEMBL4522400 1 7.96
CHEMBL4527175 1 7.92
CHEMBL4562249 1 7.92
CHEMBL4567152 1 7.89
CHEMBL4514982 1 7.85
CHEMBL4464813 1 7.70
CHEMBL4542293 1 7.62
CHEMBL4580408 1 7.16
CHEMBL4538856 1 6.96
CHEMBL4589525 1 6.72
CHEMBL4513835 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4593027 EC50 = 0.06 nM 10.22
CHEMBL4472219 EC50 = 0.2 nM 9.70
CHEMBL4568323 EC50 = 0.2 nM 9.70
CHEMBL4570851 EC50 = 0.4 nM 9.40
CHEMBL4434862 EC50 = 0.5 nM 9.30
CHEMBL4466462 EC50 = 0.5 nM 9.30
CHEMBL3318007 PIMODIVIR EC50 = 0.6 nM 9.22
CHEMBL4547565 EC50 = 1.4 nM 8.85
CHEMBL4469158 EC50 = 2.6 nM 8.59
CHEMBL4470294 EC50 = 2.8 nM 8.55
CHEMBL4435833 EC50 = 3.0 nM 8.52
CHEMBL4444973 EC50 = 4.0 nM 8.40
CHEMBL4529778 EC50 = 4.5 nM 8.35
CHEMBL4468219 EC50 = 5.3 nM 8.28
CHEMBL4469921 EC50 = 5.5 nM 8.26
CHEMBL4459959 EC50 = 9.6 nM 8.02
CHEMBL4524775 EC50 = 10.0 nM 8.00
CHEMBL4567115 EC50 = 10.0 nM 8.00
CHEMBL4530239 EC50 = 11.0 nM 7.96
CHEMBL4522400 EC50 = 11.0 nM 7.96
CHEMBL4527175 EC50 = 12.0 nM 7.92
CHEMBL4562249 EC50 = 12.0 nM 7.92
CHEMBL4567152 EC50 = 13.0 nM 7.89
CHEMBL4514982 EC50 = 14.0 nM 7.85
CHEMBL4464813 EC50 = 20.0 nM 7.70
CHEMBL4542293 EC50 = 24.0 nM 7.62
CHEMBL4580408 EC50 = 70.0 nM 7.16
CHEMBL4538856 EC50 = 110.0 nM 6.96
CHEMBL4589525 EC50 = 190.0 nM 6.72
CHEMBL4513835 EC50 = 220.0 nM 6.66
CHEMBL4453678 EC50 = 230.0 nM 6.64
CHEMBL4548835 EC50 = 450.0 nM 6.35
CHEMBL4519832 EC50 = 2000.0 nM 5.70