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Assay Detail

CHEMBL4006616

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 assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

6-Cyclohexylmethyl-3-hydroxypyrimidine-2,4-dione as an inhibitor scaffold of HIV reverase transcriptase: Impacts of the 3-OH on inhibiting RNase H and polymerase.
Tang J, Kirby KA, Huber AD, Casey MC, Ji J, Wilson DJ, Sarafianos SG, Wang Z.
Eur J Med Chem (2017) 128 : 168 -179
PubMed 28182989 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 6.92 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4065165 1 8.28
CHEMBL4080663 1 8.21
CHEMBL4098705 1 8.14
CHEMBL4101420 1 8.12
CHEMBL436546 1 7.96
CHEMBL4071987 1 7.96
CHEMBL4093701 1 7.85
CHEMBL4095043 1 7.58
CHEMBL4103727 1 7.41
CHEMBL4066126 1 7.41
CHEMBL4074733 1 7.32
CHEMBL4068668 1 7.23
CHEMBL4092759 1 7.19
CHEMBL4085004 1 6.68
CHEMBL4079480 1 6.38
CHEMBL4064119 1 6.37
CHEMBL4090318 1 6.10
CHEMBL4063363 1 6.08
CHEMBL4095984 1 5.62
CHEMBL4073514 1 5.62
CHEMBL4100350 1 5.39
CHEMBL4062311 1 5.28
CHEMBL4073756 1 5.00
CHEMBL4094347 1 -
CHEMBL4084111 1 -
CHEMBL4102096 1 -
CHEMBL4091873 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4065165 EC50 = 5.2 nM 8.28
CHEMBL4080663 EC50 = 6.2 nM 8.21
CHEMBL4098705 EC50 = 7.2 nM 8.14
CHEMBL4101420 EC50 = 7.5 nM 8.12
CHEMBL436546 EC50 = 11.0 nM 7.96
CHEMBL4071987 EC50 = 11.0 nM 7.96
CHEMBL4093701 EC50 = 14.0 nM 7.85
CHEMBL4095043 EC50 = 26.0 nM 7.58
CHEMBL4103727 EC50 = 39.0 nM 7.41
CHEMBL4066126 EC50 = 39.0 nM 7.41
CHEMBL4074733 EC50 = 48.0 nM 7.32
CHEMBL4068668 EC50 = 59.0 nM 7.23
CHEMBL4092759 EC50 = 65.0 nM 7.19
CHEMBL4085004 EC50 = 210.0 nM 6.68
CHEMBL4079480 EC50 = 420.0 nM 6.38
CHEMBL4064119 EC50 = 430.0 nM 6.37
CHEMBL4090318 EC50 = 800.0 nM 6.10
CHEMBL4063363 EC50 = 830.0 nM 6.08
CHEMBL4095984 EC50 = 2400.0 nM 5.62
CHEMBL4073514 EC50 = 2400.0 nM 5.62
CHEMBL4100350 EC50 = 4100.0 nM 5.39
CHEMBL4062311 EC50 = 5300.0 nM 5.28
CHEMBL4073756 EC50 = 10000.0 nM 5.00
CHEMBL4094347 EC50 > 15000.0 nM -
CHEMBL4084111 EC50 > 15000.0 nM -
CHEMBL4102096 EC50 > 15000.0 nM -
CHEMBL4091873 EC50 > 15000.0 nM -