Assay Detail
Binding
CHEMBL3116560
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIV-1 GST-tagged integrase-His6-tagged LEDGF complex expressed in Escherichia coli BL21(DE3) using [32P]-labeled U5B/U5A DNA as substrate assessed as inhibition of 3'-processing reaction after 2 hrs by PAGE analysis in presence of Mg2+
5
Total Activities
5
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
Specific features of HIV-1 integrase inhibition by bisphosphonate derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.16 | 5.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3116306 | — | — | 1 | 5.16 |
| CHEMBL3116308 | — | — | 1 | - |
| CHEMBL3116307 | — | — | 1 | - |
| CHEMBL3116305 | — | — | 1 | - |
| CHEMBL34249 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3116306 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3116308 | — | IC50 | - | — | - | |
| CHEMBL3116307 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL3116305 | — | IC50 | > | 250000.0 | nM | - |
| CHEMBL34249 | — | IC50 | > | 250000.0 | nM | - |