Assay Detail
Binding
CHEMBL802885
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In vitro inhibitory activity against HIV-1 mutant Reverse transcriptase containing the single amino acid substitution K103N
10
Total Activities
10
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
Pyrrolobenzoxazepinone derivatives as non-nucleoside HIV-1 RT inhibitors: further structure-activity relationship studies and identification of more potent broad-spectrum HIV-1 RT inhibitors with antiviral activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.44 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL140665 | — | — | 1 | 7.66 |
| CHEMBL336441 | — | — | 1 | 7.52 |
| CHEMBL138969 | — | — | 1 | 7.35 |
| CHEMBL344257 | — | — | 1 | 7.16 |
| CHEMBL137838 | — | — | 1 | 6.52 |
| CHEMBL141223 | — | — | 1 | 6.40 |
| CHEMBL139532 | — | — | 1 | 5.96 |
| CHEMBL141371 | — | — | 1 | 5.57 |
| CHEMBL57 | NEVIRAPINE | 4.0 | 1 | 5.16 |
| CHEMBL329653 | — | — | 1 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL140665 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL336441 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL138969 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL344257 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL137838 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL141223 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL139532 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL141371 | — | Ki | = | 2700.0 | nM | 5.57 |
| CHEMBL57 | NEVIRAPINE | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL329653 | — | Ki | = | 7700.0 | nM | 5.11 |