Assay Detail
Binding
CHEMBL4432973
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full length C-terminal His-tagged HIV1 integrase expressed in Escherichia coli BL21(DE3) cells assessed as inhibition of recombinant C-terminal FLAG-tagged LEDGF/p75-induced integration of viral 32-mer blunt-ended U5 DNA into pBR322 DNA preincubated with enzyme for 30 mins followed by viral and target DNA addition and subsequent addition of LEDGF/p75 after 5 mins measured after 90 mins by HTRF assay
8
Total Activities
8
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
Indole-based allosteric inhibitors of HIV-1 integrase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 4.81 | 5.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3259891 | — | — | 1 | 5.89 |
| CHEMBL4448648 | — | — | 1 | 5.35 |
| CHEMBL4460215 | — | — | 1 | 4.50 |
| CHEMBL4532605 | — | — | 1 | 4.50 |
| CHEMBL4586384 | — | — | 1 | 4.36 |
| CHEMBL4573753 | — | — | 1 | 4.23 |
| CHEMBL4513790 | — | — | 1 | - |
| CHEMBL4462745 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3259891 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4448648 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4460215 | — | IC50 | = | 31300.0 | nM | 4.50 |
| CHEMBL4532605 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL4586384 | — | IC50 | = | 44100.0 | nM | 4.36 |
| CHEMBL4573753 | — | IC50 | = | 59100.0 | nM | 4.23 |
| CHEMBL4513790 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4462745 | — | IC50 | > | 100000.0 | nM | - |