Assay Detail
Binding
CHEMBL3294262
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant HIV-1 integrase strand transfer activity using 32P 5' end-labeled linear 21'mer as substrate preincubated for 30 mins prior to substrate challenge by phosphorimaging analysis
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 | 4.90 | 6.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8260 | BAICALEIN | 2.0 | 1 | 6.11 |
| CHEMBL3288712 | — | — | 1 | 5.40 |
| CHEMBL3288714 | — | — | 1 | 5.16 |
| CHEMBL3288958 | — | — | 1 | 5.12 |
| CHEMBL50 | QUERCETIN | 3.0 | 1 | 5.10 |
| CHEMBL151 | LUTEOLIN | 2.0 | 1 | 5.05 |
| CHEMBL3288946 | — | — | 1 | 4.46 |
| CHEMBL3288950 | — | — | 1 | 4.30 |
| CHEMBL3288955 | — | — | 1 | 4.16 |
| CHEMBL3288954 | — | — | 1 | 4.10 |
| CHEMBL3288713 | — | — | 1 | - |
| CHEMBL3288943 | — | — | 1 | - |
| CHEMBL3288944 | — | — | 1 | - |
| CHEMBL3288945 | — | — | 1 | - |
| CHEMBL28 | APIGENIN | — | 1 | - |
| CHEMBL3288947 | — | — | 1 | - |
| CHEMBL3288948 | — | — | 1 | - |
| CHEMBL117 | CHRYSIN | — | 1 | - |
| CHEMBL3288949 | — | — | 1 | - |
| CHEMBL3288951 | — | — | 1 | - |
| CHEMBL9352 | NARINGENIN | — | 1 | - |
| CHEMBL3288959 | — | — | 1 | - |
| CHEMBL3286423 | — | — | 1 | - |
| CHEMBL3288957 | — | — | 1 | - |
| CHEMBL3288956 | — | — | 1 | - |
| CHEMBL44 | GENISTEIN | 2.0 | 1 | - |
| CHEMBL3288953 | — | — | 1 | - |
| CHEMBL3288960 | — | — | 1 | - |
| CHEMBL3288952 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8260 | BAICALEIN | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL3288712 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3288714 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3288958 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL50 | QUERCETIN | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL151 | LUTEOLIN | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL3288946 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL3288950 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL3288955 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL3288954 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL3288713 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288943 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3288944 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288945 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL28 | APIGENIN | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288947 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288948 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL117 | CHRYSIN | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288949 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288951 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL9352 | NARINGENIN | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288959 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3286423 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288957 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288956 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL44 | GENISTEIN | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288953 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3288960 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3288952 | — | IC50 | > | 100000.0 | nM | - |