Assay Detail
Binding
CHEMBL3294266
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Inhibition of His6-tagged HIV-1 integrase assessed as decrease in integrase-Flag-LEDGF/p75 interaction preincubated with enzyme for 30 mins followed by addition of Flag-LEDGF/p75 for 1 hr by AlphaScreen assay
29
Total Activities
29
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
Design and discovery of flavonoid-based HIV-1 integrase inhibitors targeting both the active site and the interaction with LEDGF/p75.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 5.92 | 6.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3286423 | — | — | 1 | 6.42 |
| CHEMBL151 | LUTEOLIN | 2.0 | 1 | 6.35 |
| CHEMBL50 | QUERCETIN | 3.0 | 1 | 6.22 |
| CHEMBL3288712 | — | — | 1 | 6.03 |
| CHEMBL3288713 | — | — | 1 | 6.01 |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | 5.96 |
| CHEMBL3288960 | — | — | 1 | 5.85 |
| CHEMBL117 | CHRYSIN | — | 1 | 5.85 |
| CHEMBL28 | APIGENIN | — | 1 | 5.82 |
| CHEMBL3288945 | — | — | 1 | 5.80 |
| CHEMBL3288948 | — | — | 1 | 5.77 |
| CHEMBL3288956 | — | — | 1 | 5.77 |
| CHEMBL9352 | NARINGENIN | — | 1 | 5.77 |
| CHEMBL3288958 | — | — | 1 | 5.75 |
| CHEMBL3288959 | — | — | 1 | 5.75 |
| CHEMBL8260 | BAICALEIN | 2.0 | 1 | 5.57 |
| CHEMBL3288951 | — | — | 1 | - |
| CHEMBL3288950 | — | — | 1 | - |
| CHEMBL3288952 | — | — | 1 | - |
| CHEMBL3288953 | — | — | 1 | - |
| CHEMBL3288943 | — | — | 1 | - |
| CHEMBL3288954 | — | — | 1 | - |
| CHEMBL3288955 | — | — | 1 | - |
| CHEMBL3288949 | — | — | 1 | - |
| CHEMBL3288957 | — | — | 1 | - |
| CHEMBL3288714 | — | — | 1 | - |
| CHEMBL3288944 | — | — | 1 | - |
| CHEMBL3288947 | — | — | 1 | - |
| CHEMBL3288946 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3286423 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL151 | LUTEOLIN | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL50 | QUERCETIN | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3288712 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL3288713 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL44 | GENISTEIN | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3288960 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL117 | CHRYSIN | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL28 | APIGENIN | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3288945 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3288948 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3288956 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL9352 | NARINGENIN | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3288958 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3288959 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL8260 | BAICALEIN | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3288951 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288950 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288952 | — | IC50 | - | — | - | |
| CHEMBL3288953 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288943 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288954 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288955 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288949 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288957 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288714 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288944 | — | IC50 | - | — | - | |
| CHEMBL3288947 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288946 | — | IC50 | > | 20000.0 | nM | - |