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Assay Detail

CHEMBL4337894

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Binding
Inhibition of Influenza A virus RNA-dependent RNA polymerase PA N-terminal endonuclease using [6-FAM]AATCGCAGGCAGCACTC[TAM] substrate and measured over 45 mins by fluorescence based assay
ChEMBL ↗
44
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Influenza A virus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Polymerase acidic protein (CHEMBL1169598) ↗
Type SINGLE PROTEIN
Organism Influenza A virus (A/Puerto Rico/8/1934(H1N1))

Publication

SAR Exploration of Tight-Binding Inhibitors of Influenza Virus PA Endonuclease.
Credille CV, Morrison CN, Stokes RW, Dick BL, Feng Y, Sun J, Chen Y, Cohen SM.
J Med Chem (2019) 62 : 9438 -9449
PubMed 31536340 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 8.28 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4551356 — — 2 10.30
CHEMBL4555466 — — 2 10.00
CHEMBL4444029 — — 2 9.90
CHEMBL4591220 — — 2 9.60
CHEMBL4440338 — — 2 8.64
CHEMBL4570983 — — 2 8.64
CHEMBL4530222 — — 2 8.50
CHEMBL4550646 — — 2 8.50
CHEMBL4553243 — — 2 8.32
CHEMBL4469796 — — 2 8.30
CHEMBL4460007 — — 2 8.22
CHEMBL4453833 — — 2 8.20
CHEMBL4535893 — — 2 8.14
CHEMBL4438546 — — 2 7.90
CHEMBL4170746 — — 2 7.80
CHEMBL4476501 — — 2 7.60
CHEMBL4459575 — — 2 -
CHEMBL4588964 — — 2 -
CHEMBL4539596 — — 2 -
CHEMBL4440123 — — 2 -
CHEMBL4545631 — — 2 -
CHEMBL4563716 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4551356 — IC50 = 0.05012 nM 10.30
CHEMBL4555466 — IC50 = 0.1 nM 10.00
CHEMBL4444029 — IC50 = 0.1259 nM 9.90
CHEMBL4591220 — IC50 = 0.2512 nM 9.60
CHEMBL4440338 — IC50 = 2.3 nM 8.64
CHEMBL4570983 — IC50 = 2.3 nM 8.64
CHEMBL4440338 — IC50 = 2.512 nM 8.60
CHEMBL4570983 — IC50 = 2.512 nM 8.60
CHEMBL4550646 — IC50 = 3.162 nM 8.50
CHEMBL4530222 — IC50 = 3.162 nM 8.50
CHEMBL4550646 — IC50 = 3.2 nM 8.49
CHEMBL4530222 — IC50 = 3.2 nM 8.49
CHEMBL4553243 — IC50 = 4.8 nM 8.32
CHEMBL4469796 — IC50 = 5.012 nM 8.30
CHEMBL4553243 — IC50 = 5.012 nM 8.30
CHEMBL4469796 — IC50 = 5.6 nM 8.25
CHEMBL4460007 — IC50 = 6.0 nM 8.22
CHEMBL4453833 — IC50 = 6.3 nM 8.20
CHEMBL4453833 — IC50 = 6.31 nM 8.20
CHEMBL4460007 — IC50 = 6.31 nM 8.20
CHEMBL4535893 — IC50 = 7.2 nM 8.14
CHEMBL4535893 — IC50 = 7.943 nM 8.10
CHEMBL4438546 — IC50 = 12.59 nM 7.90
CHEMBL4438546 — IC50 = 14.0 nM 7.85
CHEMBL4170746 — IC50 = 15.85 nM 7.80
CHEMBL4170746 — IC50 = 17.0 nM 7.77
CHEMBL4476501 — IC50 = 25.0 nM 7.60
CHEMBL4476501 — IC50 = 25.12 nM 7.60
CHEMBL4551356 — IC50 = 47.0 nM 7.33
CHEMBL4555466 — IC50 = 110.0 nM 6.96
CHEMBL4444029 — IC50 = 120.0 nM 6.92
CHEMBL4591220 — IC50 = 230.0 nM 6.64
CHEMBL4545631 — IC50 < 1.995 nM -
CHEMBL4545631 — IC50 < 2.0 nM -
CHEMBL4539596 — IC50 < 2.0 nM -
CHEMBL4588964 — IC50 < 2.0 nM -
CHEMBL4539596 — IC50 < 1.995 nM -
CHEMBL4588964 — IC50 < 1.995 nM -
CHEMBL4440123 — IC50 < 2.0 nM -
CHEMBL4459575 — IC50 < 1.995 nM -
CHEMBL4563716 — IC50 < 2.0 nM -
CHEMBL4440123 — IC50 < 1.995 nM -
CHEMBL4563716 — IC50 < 1.995 nM -
CHEMBL4459575 — IC50 < 2.0 nM -