Assay Detail
Binding
CHEMBL4273393
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Inhibition of HIV integrase strand transfer activity using 5'-biotin/3'-Cy5-labeled DNA substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by HTS assay
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Human immunodeficiency virus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Human immunodeficiency virus type 1 integrase (CHEMBL3471) ↗| 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 | 6.01 | 7.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1229211 | DOLUTEGRAVIR | 4.0 | 1 | 7.17 |
| CHEMBL4292982 | — | — | 1 | 6.77 |
| CHEMBL4285242 | — | — | 1 | 6.62 |
| CHEMBL4276679 | — | — | 1 | 6.48 |
| CHEMBL4279266 | — | — | 1 | 6.31 |
| CHEMBL4291865 | — | — | 1 | 6.23 |
| CHEMBL254316 | RALTEGRAVIR | 4.0 | 1 | 6.19 |
| CHEMBL4289142 | — | — | 1 | 6.19 |
| CHEMBL4288722 | — | — | 1 | 6.12 |
| CHEMBL4278477 | — | — | 1 | 6.11 |
| CHEMBL4294846 | — | — | 1 | 6.10 |
| CHEMBL4277423 | — | — | 1 | 6.06 |
| CHEMBL4291548 | — | — | 1 | 6.06 |
| CHEMBL4277795 | — | — | 1 | 5.96 |
| CHEMBL4282218 | — | — | 1 | 5.96 |
| CHEMBL4288444 | — | — | 1 | 5.92 |
| CHEMBL4284247 | — | — | 1 | 5.89 |
| CHEMBL4288035 | — | — | 1 | 5.80 |
| CHEMBL4284648 | — | — | 1 | 5.57 |
| CHEMBL4292143 | — | — | 1 | 5.55 |
| CHEMBL4280139 | — | — | 1 | 5.47 |
| CHEMBL4276707 | — | — | 1 | 5.44 |
| CHEMBL4281951 | — | — | 1 | 5.17 |
| CHEMBL4286950 | — | — | 1 | 5.08 |
| CHEMBL4278348 | — | — | 1 | - |
| CHEMBL4280827 | — | — | 1 | - |
| CHEMBL4288759 | — | — | 1 | - |
| CHEMBL4280869 | — | — | 1 | - |
| CHEMBL4278516 | — | — | 1 | - |
| CHEMBL4289171 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1229211 | DOLUTEGRAVIR | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4292982 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4285242 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4276679 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4279266 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4291865 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL254316 | RALTEGRAVIR | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL4289142 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4288722 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL4278477 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL4294846 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4277423 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL4291548 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL4277795 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4282218 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4288444 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4284247 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4288035 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4284648 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4292143 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4280139 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4276707 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4281951 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL4286950 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL4289681 | — | IC50 | > | 140.0 | nM | - |
| CHEMBL4286262 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4293481 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4277847 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4285791 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4282386 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4289601 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4278928 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4286171 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4294074 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4282781 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4290671 | — | IC50 | - | — | - | |
| CHEMBL4281804 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4293068 | — | IC50 | > | 140.0 | nM | - |
| CHEMBL4281242 | — | IC50 | - | — | - | |
| CHEMBL4277935 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4288585 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4292590 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4281980 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4289171 | — | IC50 | - | — | - | |
| CHEMBL4278516 | — | IC50 | - | — | - | |
| CHEMBL4280869 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4288759 | — | IC50 | - | — | - | |
| CHEMBL4280827 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4278348 | — | IC50 | > | 140.0 | nM | - |