Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4273398

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

Binding
Inhibition of recombinant HIV1 reverse transcriptase RNase H expressed in Escherichia coli JM109 using RNA/DNA duplex substrate HTS1 as substrate
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Human immunodeficiency virus type 1 reverse transcriptase (CHEMBL247)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

6-Biphenylmethyl-3-hydroxypyrimidine-2,4-diones potently and selectively inhibited HIV reverse transcriptase-associated RNase H.
Wang L, Tang J, Huber AD, Casey MC, Kirby KA, Wilson DJ, Kankanala J, Parniak MA, Sarafianos SG, Wang Z.
Eur J Med Chem (2018) 156 : 680 -691
PubMed 30031978 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 6.55 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4285516 1 8.12
CHEMBL4283283 1 8.11
CHEMBL4291139 1 8.06
CHEMBL4294172 1 8.04
CHEMBL4280134 1 8.03
CHEMBL4277572 1 7.96
CHEMBL4277884 1 7.96
CHEMBL4284329 1 7.92
CHEMBL4285821 1 7.89
CHEMBL4283583 1 7.82
CHEMBL4290770 1 7.82
CHEMBL4286946 1 7.80
CHEMBL4291563 1 7.80
CHEMBL4281820 1 7.80
CHEMBL4294970 1 7.75
CHEMBL4279822 1 7.70
CHEMBL4290358 1 7.60
CHEMBL4282486 1 7.55
CHEMBL4280927 1 7.43
CHEMBL4287728 1 7.42
CHEMBL4280616 1 7.33
CHEMBL4279014 1 7.07
CHEMBL4291913 1 6.66
CHEMBL4281296 1 6.60
CHEMBL4293081 1 6.37
CHEMBL1767306 1 6.05
CHEMBL1767172 1 6.05
CHEMBL1767178 1 5.75
CHEMBL1767171 1 5.75
CHEMBL1651642 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4285516 IC50 = 7.6 nM 8.12
CHEMBL4283283 IC50 = 7.7 nM 8.11
CHEMBL4291139 IC50 = 8.8 nM 8.06
CHEMBL4294172 IC50 = 9.2 nM 8.04
CHEMBL4280134 IC50 = 9.4 nM 8.03
CHEMBL4277572 IC50 = 11.0 nM 7.96
CHEMBL4277884 IC50 = 11.0 nM 7.96
CHEMBL4284329 IC50 = 12.0 nM 7.92
CHEMBL4285821 IC50 = 13.0 nM 7.89
CHEMBL4283583 IC50 = 15.0 nM 7.82
CHEMBL4290770 IC50 = 15.0 nM 7.82
CHEMBL4281820 IC50 = 16.0 nM 7.80
CHEMBL4291563 IC50 = 16.0 nM 7.80
CHEMBL4286946 IC50 = 16.0 nM 7.80
CHEMBL4294970 IC50 = 18.0 nM 7.75
CHEMBL4279822 IC50 = 20.0 nM 7.70
CHEMBL4290358 IC50 = 25.0 nM 7.60
CHEMBL4282486 IC50 = 28.0 nM 7.55
CHEMBL4280927 IC50 = 37.0 nM 7.43
CHEMBL4287728 IC50 = 38.0 nM 7.42
CHEMBL4280616 IC50 = 47.0 nM 7.33
CHEMBL4279014 IC50 = 85.0 nM 7.07
CHEMBL4291913 IC50 = 220.0 nM 6.66
CHEMBL4281296 IC50 = 250.0 nM 6.60
CHEMBL4293081 IC50 = 430.0 nM 6.37
CHEMBL1767172 IC50 = 900.0 nM 6.05
CHEMBL1767306 IC50 = 900.0 nM 6.05
CHEMBL1767178 IC50 = 1800.0 nM 5.75
CHEMBL1767171 IC50 = 1800.0 nM 5.75
CHEMBL1651642 IC50 = 2100.0 nM 5.68
CHEMBL4285262 IC50 = 2100.0 nM 5.68
CHEMBL1651640 IC50 = 2500.0 nM 5.60
CHEMBL1767176 IC50 = 2800.0 nM 5.55
CHEMBL1767181 IC50 = 3800.0 nM 5.42
CHEMBL4288609 IC50 = 5200.0 nM 5.28
CHEMBL4292026 IC50 = 6200.0 nM 5.21
CHEMBL1649606 IC50 = 6200.0 nM 5.21
CHEMBL1767180 IC50 = 6600.0 nM 5.18
CHEMBL4281403 IC50 = 6700.0 nM 5.17
CHEMBL1651645 IC50 = 6800.0 nM 5.17
CHEMBL1767174 IC50 = 7000.0 nM 5.16
CHEMBL1767312 IC50 = 10000.0 nM 5.00
CHEMBL1767175 IC50 = 11000.0 nM 4.96
CHEMBL1767313 IC50 = 13000.0 nM 4.89
CHEMBL1767314 IC50 = 15000.0 nM 4.82
CHEMBL1767311 IC50 = 15000.0 nM 4.82
CHEMBL4288318 IC50 = 17000.0 nM 4.77
CHEMBL4277948 IC50 > 5000.0 nM -
CHEMBL1651646 IC50 > 25000.0 nM -