Assay Detail
Binding
CHEMBL1016229
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIV1 integrase 3'-end processing activity
6
Total Activities
6
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, synthesis, and biological evaluation of a series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.23 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL204656 | ELVITEGRAVIR | 4.0 | 1 | 7.30 |
| CHEMBL414850 | — | — | 1 | 6.92 |
| CHEMBL456326 | — | — | 1 | 6.12 |
| CHEMBL254316 | RALTEGRAVIR | 4.0 | 1 | 6.05 |
| CHEMBL444646 | — | — | 1 | 5.85 |
| CHEMBL512021 | — | — | 1 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL204656 | ELVITEGRAVIR | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL414850 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL456326 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL254316 | RALTEGRAVIR | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL444646 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL512021 | — | IC50 | = | 7790.0 | nM | 5.11 |