Assay Detail
Binding
CHEMBL4359415
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIV1 RT in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method
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 reverse transcriptase (CHEMBL247) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus 1 |
Publication
Structure-Based Bioisosterism Yields HIV-1 NNRTIs with Improved Drug-Resistance Profiles and Favorable Pharmacokinetic Properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.36 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL308954 | ETRAVIRINE | 4.0 | 1 | 7.92 |
| CHEMBL175691 | RILPIVIRINE | 4.0 | 1 | 7.82 |
| CHEMBL3929927 | — | — | 1 | 7.12 |
| CHEMBL4094163 | — | — | 1 | 7.00 |
| CHEMBL4526732 | — | — | 1 | 6.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL308954 | ETRAVIRINE | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL175691 | RILPIVIRINE | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3929927 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4094163 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4526732 | — | IC50 | = | 114.0 | nM | 6.94 |