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Assay Detail

CHEMBL4135245

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

Functional
Antiviral activity against HIV1 infected in human P4R5 cells assessed as reduction in viral infection preincubated with cells for 24 hrs followed by viral infection measured after 48 hrs by fluorescence based beta-galactosidase reporter gene based MAGI assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Confidence 1 — Organism
Curated By Intermediate

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

Design, synthesis and biological evaluations of N-Hydroxy thienopyrimidine-2,4-diones as inhibitors of HIV reverse transcriptase-associated RNase H.
Kankanala J, Kirby KA, Huber AD, Casey MC, Wilson DJ, Sarafianos SG, Wang Z.
Eur J Med Chem (2017) 141 : 149 -161
PubMed 29031062 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 5.20 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL254316 RALTEGRAVIR 4.0 1 7.52
CHEMBL4159305 1 5.42
CHEMBL4167216 1 5.35
CHEMBL4163088 1 5.13
CHEMBL4175467 1 5.05
CHEMBL183062 1 4.96
CHEMBL4176832 1 4.85
CHEMBL4170599 1 4.80
CHEMBL361350 1 4.75
CHEMBL4168270 1 4.68
CHEMBL4167025 1 4.66
CHEMBL4172336 1 -
CHEMBL4161705 1 -
CHEMBL4162103 1 -
CHEMBL183792 1 -
CHEMBL4170035 1 -
CHEMBL4175393 1 -
CHEMBL4161240 1 -
CHEMBL4176527 1 -
CHEMBL4163126 1 -
CHEMBL4171477 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL254316 RALTEGRAVIR EC50 = 30.0 nM 7.52
CHEMBL4159305 EC50 = 3800.0 nM 5.42
CHEMBL4167216 EC50 = 4500.0 nM 5.35
CHEMBL4163088 EC50 = 7400.0 nM 5.13
CHEMBL4175467 EC50 = 8900.0 nM 5.05
CHEMBL183062 EC50 = 11000.0 nM 4.96
CHEMBL4176832 EC50 = 14000.0 nM 4.85
CHEMBL4170599 EC50 = 16000.0 nM 4.80
CHEMBL361350 EC50 = 18000.0 nM 4.75
CHEMBL4168270 EC50 = 21000.0 nM 4.68
CHEMBL4167025 EC50 = 22000.0 nM 4.66
CHEMBL4172336 EC50 > 20000.0 nM -
CHEMBL4161705 EC50 > 20000.0 nM -
CHEMBL4162103 EC50 > 20000.0 nM -
CHEMBL183792 EC50 > 20000.0 nM -
CHEMBL4170035 EC50 > 20000.0 nM -
CHEMBL4175393 EC50 > 20000.0 nM -
CHEMBL4161240 EC50 > 20000.0 nM -
CHEMBL4176527 EC50 > 20000.0 nM -
CHEMBL4163126 EC50 > 20000.0 nM -
CHEMBL4171477 EC50 > 20000.0 nM -