Assay Detail
Binding
CHEMBL921484
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Inhibition of HIV1 integrase strand transfer activity
13
Total Activities
13
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
A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.34 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL254316 | RALTEGRAVIR | 4.0 | 1 | 8.15 |
| CHEMBL204656 | ELVITEGRAVIR | 4.0 | 1 | 7.82 |
| CHEMBL260185 | — | — | 1 | 7.52 |
| CHEMBL259011 | — | — | 1 | 6.85 |
| CHEMBL261714 | — | — | 1 | 6.72 |
| CHEMBL261541 | — | — | 1 | 6.66 |
| CHEMBL409643 | — | — | 1 | 6.57 |
| CHEMBL260398 | — | — | 1 | 6.18 |
| CHEMBL259012 | — | — | 1 | 5.63 |
| CHEMBL260619 | — | — | 1 | 5.63 |
| CHEMBL405652 | — | — | 1 | 5.58 |
| CHEMBL406929 | — | — | 1 | 5.12 |
| CHEMBL263887 | — | — | 1 | 4.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL254316 | RALTEGRAVIR | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL204656 | ELVITEGRAVIR | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL260185 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL259011 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL261714 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL261541 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL409643 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL260398 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL259012 | — | IC50 | = | 2330.0 | nM | 5.63 |
| CHEMBL260619 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL405652 | — | IC50 | = | 2640.0 | nM | 5.58 |
| CHEMBL406929 | — | IC50 | = | 7550.0 | nM | 5.12 |
| CHEMBL263887 | — | IC50 | = | 92300.0 | nM | 4.04 |