Assay Detail
Binding
CHEMBL4359416
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIV1 RT L100I mutant 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 | 7.24 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL308954 | ETRAVIRINE | 4.0 | 1 | 7.89 |
| CHEMBL175691 | RILPIVIRINE | 4.0 | 1 | 7.62 |
| CHEMBL3929927 | — | — | 1 | 7.04 |
| CHEMBL4094163 | — | — | 1 | 7.00 |
| CHEMBL4526732 | — | — | 1 | 6.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL308954 | ETRAVIRINE | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL175691 | RILPIVIRINE | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3929927 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4094163 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4526732 | — | IC50 | = | 228.0 | nM | 6.64 |