Assay Detail
Binding
CHEMBL1262283
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 20 nM [3H]GSK304649 from Human immunodeficiency virus 1 integrase by scintillation proximity assay
5
Total Activities
4
Compounds Tested
2
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
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.90 | 7.96 |
| Kd | 1 | 8.48 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL414850 | — | — | 2 | 8.48 |
| CHEMBL1256978 | GSK-364735 | 2.0 | 1 | 7.96 |
| CHEMBL204656 | ELVITEGRAVIR | 4.0 | 1 | 7.96 |
| CHEMBL254316 | RALTEGRAVIR | 4.0 | 1 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL414850 | — | Kd | = | 3.3 | nM | 8.48 |
| CHEMBL1256978 | GSK-364735 | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL204656 | ELVITEGRAVIR | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL414850 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL254316 | RALTEGRAVIR | IC50 | = | 16.0 | nM | 7.80 |