Assay Detail
Binding
CHEMBL4273391
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Inhibition of HIV1 reverse transcriptase RNaseH activity using 3'-fluorescein/5'-Dabcyl labeled HTS-1 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-Arylthio-3-hydroxypyrimidine-2,4-diones potently inhibited HIV reverse transcriptase-associated RNase H with antiviral activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 49 | 7.90 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4276679 | — | — | 1 | 8.40 |
| CHEMBL4278348 | — | — | 1 | 8.40 |
| CHEMBL4292982 | — | — | 1 | 8.40 |
| CHEMBL4277935 | — | — | 1 | 8.30 |
| CHEMBL4288585 | — | — | 1 | 8.30 |
| CHEMBL4289601 | — | — | 1 | 8.30 |
| CHEMBL4277847 | — | — | 1 | 8.30 |
| CHEMBL4286262 | — | — | 1 | 8.30 |
| CHEMBL4293068 | — | — | 1 | 8.30 |
| CHEMBL4293481 | — | — | 1 | 8.22 |
| CHEMBL4285791 | — | — | 1 | 8.22 |
| CHEMBL4285242 | — | — | 1 | 8.22 |
| CHEMBL4278928 | — | — | 1 | 8.22 |
| CHEMBL4282781 | — | — | 1 | 8.22 |
| CHEMBL4281804 | — | — | 1 | 8.15 |
| CHEMBL4294846 | — | — | 1 | 8.15 |
| CHEMBL4282386 | — | — | 1 | 8.15 |
| CHEMBL4289681 | — | — | 1 | 8.15 |
| CHEMBL4277795 | — | — | 1 | 8.10 |
| CHEMBL4286171 | — | — | 1 | 8.10 |
| CHEMBL4288722 | — | — | 1 | 8.00 |
| CHEMBL4284247 | — | — | 1 | 8.00 |
| CHEMBL4281242 | — | — | 1 | 8.00 |
| CHEMBL4288444 | — | — | 1 | 7.96 |
| CHEMBL4291865 | — | — | 1 | 7.96 |
| CHEMBL4288035 | — | — | 1 | 7.96 |
| CHEMBL4280139 | — | — | 1 | 7.92 |
| CHEMBL4276707 | — | — | 1 | 7.92 |
| CHEMBL4289142 | — | — | 1 | 7.92 |
| CHEMBL4281980 | — | — | 1 | 7.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4276679 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4292982 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4278348 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4277935 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4288585 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4289601 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4277847 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4286262 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4293068 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4282781 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4278928 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4285242 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4285791 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4293481 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4289681 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4281804 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4282386 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4294846 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4277795 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4286171 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4288722 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4284247 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4281242 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4288035 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4291865 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4288444 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4280139 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4276707 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4289142 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4281980 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4277423 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4292590 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4291548 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4284648 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4279266 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4278477 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4282218 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4286950 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4280827 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4292143 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4281951 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4294074 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4289171 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4290671 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4278516 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4280869 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4288759 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL254316 | RALTEGRAVIR | IC50 | > | 10000.0 | nM | - |
| CHEMBL1229211 | DOLUTEGRAVIR | IC50 | > | 10000.0 | nM | - |