Assay Detail
Binding
CHEMBL1015285
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Inhibition of HIV1 recombinant integrase strand transfer activity
21
Total Activities
21
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 | Autocuration |
Target
Human immunodeficiency virus type 1 integrase (CHEMBL3471) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus 1 |
Publication
The use of oxadiazole and triazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 1: Establishing the pharmacophore.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.52 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL454633 | — | — | 1 | 8.70 |
| CHEMBL452588 | — | — | 1 | 7.96 |
| CHEMBL199145 | — | — | 1 | 7.92 |
| CHEMBL414850 | — | — | 1 | 7.89 |
| CHEMBL491150 | — | — | 1 | 7.38 |
| CHEMBL455437 | — | — | 1 | 6.89 |
| CHEMBL522630 | — | — | 1 | 6.89 |
| CHEMBL523974 | — | — | 1 | 6.89 |
| CHEMBL455438 | — | — | 1 | 6.44 |
| CHEMBL523303 | — | — | 1 | 6.19 |
| CHEMBL510677 | — | — | 1 | 6.02 |
| CHEMBL490971 | — | — | 1 | 5.99 |
| CHEMBL491149 | — | — | 1 | 5.62 |
| CHEMBL490972 | — | — | 1 | 5.55 |
| CHEMBL523302 | — | — | 1 | 5.46 |
| CHEMBL490970 | — | — | 1 | 5.34 |
| CHEMBL523468 | — | — | 1 | 5.20 |
| CHEMBL491685 | — | — | 1 | 5.10 |
| CHEMBL453399 | — | — | 1 | - |
| CHEMBL453400 | — | — | 1 | - |
| CHEMBL499839 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL454633 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL452588 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL199145 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL414850 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL491150 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL455437 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL522630 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL523974 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL455438 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL523303 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL510677 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL490971 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL491149 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL490972 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL523302 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL490970 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL523468 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL491685 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL453399 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL453400 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL499839 | — | IC50 | > | 100000.0 | nM | - |