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Assay Detail

CHEMBL4006613

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Binding
Inhibition of RNase H activity of full length HIV reverse transcriptase using RNA-DNA duplex HTS-1 substrate
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
IC50 27 5.45 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4079480 1 5.96
CHEMBL4100350 1 5.77
CHEMBL4064119 1 5.68
CHEMBL4102096 1 5.66
CHEMBL4095984 1 5.57
CHEMBL4091873 1 5.51
CHEMBL4073756 1 5.41
CHEMBL4084111 1 5.34
CHEMBL4095043 1 5.28
CHEMBL4068668 1 5.26
CHEMBL4103727 1 5.24
CHEMBL4094347 1 5.12
CHEMBL4073514 1 5.00
CHEMBL436546 1 -
CHEMBL4065165 1 -
CHEMBL4098705 1 -
CHEMBL4080663 1 -
CHEMBL4101420 1 -
CHEMBL4074733 1 -
CHEMBL4093701 1 -
CHEMBL4066126 1 -
CHEMBL4071987 1 -
CHEMBL4092759 1 -
CHEMBL4063363 1 -
CHEMBL4085004 1 -
CHEMBL4090318 1 -
CHEMBL4062311 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4079480 IC50 = 1100.0 nM 5.96
CHEMBL4100350 IC50 = 1700.0 nM 5.77
CHEMBL4064119 IC50 = 2100.0 nM 5.68
CHEMBL4102096 IC50 = 2200.0 nM 5.66
CHEMBL4095984 IC50 = 2700.0 nM 5.57
CHEMBL4091873 IC50 = 3100.0 nM 5.51
CHEMBL4073756 IC50 = 3900.0 nM 5.41
CHEMBL4084111 IC50 = 4600.0 nM 5.34
CHEMBL4095043 IC50 = 5200.0 nM 5.28
CHEMBL4068668 IC50 = 5500.0 nM 5.26
CHEMBL4103727 IC50 = 5800.0 nM 5.24
CHEMBL4094347 IC50 = 7600.0 nM 5.12
CHEMBL4073514 IC50 = 10000.0 nM 5.00
CHEMBL436546 IC50 > 10000.0 nM -
CHEMBL4065165 IC50 > 10000.0 nM -
CHEMBL4098705 IC50 > 10000.0 nM -
CHEMBL4080663 IC50 > 10000.0 nM -
CHEMBL4101420 IC50 > 10000.0 nM -
CHEMBL4074733 IC50 > 10000.0 nM -
CHEMBL4093701 IC50 > 10000.0 nM -
CHEMBL4066126 IC50 > 10000.0 nM -
CHEMBL4071987 IC50 > 10000.0 nM -
CHEMBL4092759 IC50 > 10000.0 nM -
CHEMBL4063363 IC50 > 10000.0 nM -
CHEMBL4085004 IC50 > 10000.0 nM -
CHEMBL4090318 IC50 > 10000.0 nM -
CHEMBL4062311 IC50 > 10000.0 nM -