Assay Detail
Binding
CHEMBL882853
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Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution K103N
13
Total Activities
13
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 | Expert |
Target
Human immunodeficiency virus type 1 reverse transcriptase (CHEMBL247) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus 1 |
Publication
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 6.58 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL107342 | — | — | 1 | 7.68 |
| CHEMBL108221 | — | — | 1 | 7.00 |
| CHEMBL110091 | — | — | 1 | 6.82 |
| CHEMBL105916 | — | — | 1 | 6.80 |
| CHEMBL223228 | EFAVIRENZ | 4.0 | 1 | 6.80 |
| CHEMBL105976 | — | — | 1 | 6.68 |
| CHEMBL320557 | — | — | 1 | 6.62 |
| CHEMBL107535 | — | — | 1 | 6.60 |
| CHEMBL418833 | — | — | 1 | 6.46 |
| CHEMBL107099 | — | — | 1 | 6.40 |
| CHEMBL317406 | — | — | 1 | 6.35 |
| CHEMBL418812 | — | — | 1 | 6.19 |
| CHEMBL57 | NEVIRAPINE | 4.0 | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL107342 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL108221 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL110091 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL105916 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL223228 | EFAVIRENZ | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL105976 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL320557 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL107535 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL418833 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL107099 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL317406 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL418812 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL57 | NEVIRAPINE | Ki | = | 7000.0 | nM | 5.16 |