Assay Detail
Binding
CHEMBL5611630
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Inhibition of HIV-1 integrase catalytic activity incubated for 1 hrs in absence of LEDGF/p75 by HTRF assay
15
Total Activities
15
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
Quinolinonyl Derivatives as Dual Inhibitors of the HIV-1 Integrase Catalytic Site and Integrase-RNA interactions.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.90 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL497501 | — | — | 1 | 7.16 |
| CHEMBL5613927 | — | — | 1 | 7.11 |
| CHEMBL5613849 | — | — | 1 | 6.74 |
| CHEMBL5612575 | — | — | 1 | 6.32 |
| CHEMBL5613097 | — | — | 1 | 6.13 |
| CHEMBL5613277 | — | — | 1 | 6.11 |
| CHEMBL5612913 | — | — | 1 | 6.10 |
| CHEMBL2236593 | — | — | 1 | 5.63 |
| CHEMBL2236594 | — | — | 1 | 5.50 |
| CHEMBL5613833 | — | — | 1 | 5.20 |
| CHEMBL5173288 | — | — | 1 | 4.44 |
| CHEMBL5172754 | — | — | 1 | 4.38 |
| CHEMBL5171239 | — | — | 1 | - |
| CHEMBL5613898 | — | — | 1 | - |
| CHEMBL5612322 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL497501 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5613927 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5613849 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL5612575 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL5613097 | — | IC50 | = | 741.0 | nM | 6.13 |
| CHEMBL5613277 | — | IC50 | = | 782.0 | nM | 6.11 |
| CHEMBL5612913 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL2236593 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL2236594 | — | IC50 | = | 3140.0 | nM | 5.50 |
| CHEMBL5613833 | — | IC50 | = | 6280.0 | nM | 5.20 |
| CHEMBL5173288 | — | IC50 | = | 36500.0 | nM | 4.44 |
| CHEMBL5172754 | — | IC50 | = | 41900.0 | nM | 4.38 |
| CHEMBL5171239 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL5613898 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL5612322 | — | IC50 | > | 200000.0 | nM | - |