Assay Detail
Binding
CHEMBL4273398
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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.
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 | - |