Assay Detail
Binding
CHEMBL1004782
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Inhibition of recombinant HIV1 integrase strand transfer activity by gel-based assay in presence of magnesium
23
Total Activities
23
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
Novel quinolinonyl diketo acid derivatives as HIV-1 integrase inhibitors: design, synthesis, and biological activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.12 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL497501 | — | — | 1 | 7.77 |
| CHEMBL498697 | — | — | 1 | 7.30 |
| CHEMBL512195 | — | — | 1 | 7.22 |
| CHEMBL498713 | — | — | 1 | 7.12 |
| CHEMBL497688 | — | — | 1 | 6.96 |
| CHEMBL498698 | — | — | 1 | 6.80 |
| CHEMBL496454 | — | — | 1 | 6.75 |
| CHEMBL504621 | — | — | 1 | 6.64 |
| CHEMBL496652 | — | — | 1 | 6.40 |
| CHEMBL458064 | — | — | 1 | 6.36 |
| CHEMBL524807 | — | — | 1 | 6.29 |
| CHEMBL458275 | — | — | 1 | 5.92 |
| CHEMBL456158 | — | — | 1 | 5.75 |
| CHEMBL496455 | — | — | 1 | 5.68 |
| CHEMBL456580 | — | — | 1 | 5.64 |
| CHEMBL456365 | — | — | 1 | 5.57 |
| CHEMBL457850 | — | — | 1 | 5.52 |
| CHEMBL456791 | — | — | 1 | 5.44 |
| CHEMBL456991 | — | — | 1 | 5.28 |
| CHEMBL514422 | — | — | 1 | 5.28 |
| CHEMBL492335 | — | — | 1 | 4.77 |
| CHEMBL497314 | — | — | 1 | 4.25 |
| CHEMBL497313 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL497501 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL498697 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL512195 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL498713 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL497688 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL498698 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL496454 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL504621 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL496652 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL458064 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL524807 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL458275 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL456158 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL496455 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL456580 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL456365 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL457850 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL456791 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL456991 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL514422 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL492335 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL497314 | — | IC50 | = | 56000.0 | nM | 4.25 |
| CHEMBL497313 | — | IC50 | = | 224000.0 | nM | - |