Assay Detail
Binding
CHEMBL2411983
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Inhibition of HIV1 integrase overall inhibition using 5'-digoxigenin-labeled 5'-GACCCTTTTAGTCAGTGTGGAAAATCTCTAGCAGT-3' as substrate after 1 hr by ELISA
19
Total Activities
19
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
4-Substituted 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as a Novel Class of HIV-1 Integrase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.89 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2407278 | — | — | 1 | 8.00 |
| CHEMBL254316 | RALTEGRAVIR | 4.0 | 1 | 8.00 |
| CHEMBL2407277 | — | — | 1 | 7.70 |
| CHEMBL2407272 | — | — | 1 | 7.52 |
| CHEMBL2407284 | — | — | 1 | 7.46 |
| CHEMBL2407283 | — | — | 1 | 7.46 |
| CHEMBL2407287 | — | — | 1 | 7.25 |
| CHEMBL2407281 | — | — | 1 | 7.12 |
| CHEMBL2407280 | — | — | 1 | 7.10 |
| CHEMBL2407286 | — | — | 1 | 6.69 |
| CHEMBL2407285 | — | — | 1 | 6.63 |
| CHEMBL2407276 | — | — | 1 | 6.51 |
| CHEMBL2407273 | — | — | 1 | 6.30 |
| CHEMBL2407274 | — | — | 1 | 6.17 |
| CHEMBL2407279 | — | — | 1 | 6.10 |
| CHEMBL2407282 | — | — | 1 | 5.92 |
| CHEMBL2407275 | — | — | 1 | 5.28 |
| CHEMBL2407288 | — | — | 1 | - |
| CHEMBL2407289 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2407278 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL254316 | RALTEGRAVIR | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2407277 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2407272 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2407284 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2407283 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2407287 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL2407281 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL2407280 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2407286 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL2407285 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL2407276 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL2407273 | — | IC50 | = | 495.0 | nM | 6.30 |
| CHEMBL2407274 | — | IC50 | = | 673.0 | nM | 6.17 |
| CHEMBL2407279 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL2407282 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL2407275 | — | IC50 | = | 5210.0 | nM | 5.28 |
| CHEMBL2407288 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL2407289 | — | IC50 | = | 199000.0 | nM | - |