Assay Detail
Binding
CHEMBL968064
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Inhibition of HIV1 recombinant integrase strand transfer activity
27
Total Activities
27
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
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.93 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL492465 | — | — | 1 | 8.70 |
| CHEMBL492464 | — | — | 1 | 8.52 |
| CHEMBL517136 | — | — | 1 | 8.40 |
| CHEMBL522374 | — | — | 1 | 8.40 |
| CHEMBL517428 | — | — | 1 | 8.40 |
| CHEMBL462045 | — | — | 1 | 8.22 |
| CHEMBL492667 | — | — | 1 | 8.15 |
| CHEMBL518491 | — | — | 1 | 8.15 |
| CHEMBL460771 | — | — | 1 | 8.15 |
| CHEMBL460977 | — | — | 1 | 8.10 |
| CHEMBL524164 | — | — | 1 | 8.10 |
| CHEMBL461405 | — | — | 1 | 8.05 |
| CHEMBL495331 | — | — | 1 | 8.00 |
| CHEMBL493295 | — | — | 1 | 7.92 |
| CHEMBL460770 | — | — | 1 | 7.82 |
| CHEMBL493920 | — | — | 1 | 7.82 |
| CHEMBL254316 | RALTEGRAVIR | 4.0 | 1 | 7.82 |
| CHEMBL495332 | — | — | 1 | 7.82 |
| CHEMBL505332 | — | — | 1 | 7.75 |
| CHEMBL461406 | — | — | 1 | 7.70 |
| CHEMBL510093 | — | — | 1 | 7.70 |
| CHEMBL461652 | — | — | 1 | 7.68 |
| CHEMBL492682 | — | — | 1 | 7.58 |
| CHEMBL386515 | — | — | 1 | 7.30 |
| CHEMBL386710 | — | — | 1 | 7.22 |
| CHEMBL493291 | — | — | 1 | 6.64 |
| CHEMBL492683 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL492465 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL492464 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL517136 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL522374 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL517428 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL462045 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL492667 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL518491 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL460771 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL460977 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL524164 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL461405 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL495331 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL493295 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL460770 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL493920 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL254316 | RALTEGRAVIR | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL495332 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL505332 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL461406 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL510093 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL461652 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL492682 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL386515 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL386710 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL493291 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL492683 | — | IC50 | > | 5000.0 | nM | - |