Assay Detail
Binding
CHEMBL5611633
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 6His-tagged recombinant HIV-1 integrase/biotinylated HIV-1 transactivation response element RNA interaction assessed as fluorescence quenching preincubated with integrase for 2 hrs followed by RNA addition and measured after 1 hrs by ALPHAscreen based AlphaLISA
15
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Human immunodeficiency virus 1 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 8 | 5.82 | 6.12 |
| Inhibition | 7 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5613849 | — | — | 1 | 6.12 |
| CHEMBL497501 | — | — | 1 | 6.08 |
| CHEMBL5612575 | — | — | 1 | 5.98 |
| CHEMBL2236594 | — | — | 1 | 5.88 |
| CHEMBL5613927 | — | — | 1 | 5.80 |
| CHEMBL5612913 | — | — | 1 | 5.70 |
| CHEMBL2236593 | — | — | 1 | 5.65 |
| CHEMBL5613277 | — | — | 1 | 5.38 |
| CHEMBL5613097 | — | — | 1 | - |
| CHEMBL5171239 | — | — | 1 | - |
| CHEMBL5613898 | — | — | 1 | - |
| CHEMBL5173288 | — | — | 1 | - |
| CHEMBL5613833 | — | — | 1 | - |
| CHEMBL5172754 | — | — | 1 | - |
| CHEMBL5612322 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5613849 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL497501 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL5612575 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL2236594 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL5613927 | — | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL5612913 | — | IC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL2236593 | — | IC50 | = | 2220.0 | nM | 5.65 |
| CHEMBL5613277 | — | IC50 | = | 4190.0 | nM | 5.38 |
| CHEMBL5613097 | — | Inhibition | - | % | - | |
| CHEMBL5171239 | — | Inhibition | - | % | - | |
| CHEMBL5613898 | — | Inhibition | - | % | - | |
| CHEMBL5173288 | — | Inhibition | - | % | - | |
| CHEMBL5613833 | — | Inhibition | - | % | - | |
| CHEMBL5172754 | — | Inhibition | - | % | - | |
| CHEMBL5612322 | — | Inhibition | - | % | - |