Assay Detail
Binding
CHEMBL800979
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Inhibitory concentration against mutant reverse transcriptase of K103N was determined which is in turn resistant to pyridinones
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Human immunodeficiency virus type 1 reverse transcriptase (CHEMBL247) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus 1 |
Publication
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. 4. 2-Substituted dipyridodiazepinones as potent inhibitors of both wild-type and cysteine-181 HIV-1 reverse transcriptase enzymes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.68 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL144035 | — | — | 1 | 8.00 |
| CHEMBL81319 | — | — | 1 | 7.30 |
| CHEMBL145237 | — | — | 1 | 7.10 |
| CHEMBL144145 | — | — | 1 | 6.58 |
| CHEMBL142659 | — | — | 1 | 6.39 |
| CHEMBL142853 | — | — | 1 | 6.38 |
| CHEMBL288336 | — | — | 1 | 5.96 |
| CHEMBL57 | NEVIRAPINE | 4.0 | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL144035 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL81319 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL145237 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL144145 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL142659 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL142853 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL288336 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL57 | NEVIRAPINE | IC50 | = | 1900.0 | nM | 5.72 |