Assay Detail
Binding
CHEMBL753040
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Inhibition of the NNRTI HIV-1 enzyme by 50% using enzyme assay.
24
Total Activities
24
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
Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.75 | 7.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL106783 | — | — | 1 | 7.93 |
| CHEMBL320282 | — | — | 1 | 7.93 |
| CHEMBL320379 | — | — | 1 | 7.78 |
| CHEMBL268871 | L-697661 | — | 1 | 7.72 |
| CHEMBL106694 | — | — | 1 | 7.61 |
| CHEMBL106997 | — | — | 1 | 7.59 |
| CHEMBL104349 | — | — | 1 | 7.58 |
| CHEMBL105863 | — | — | 1 | 7.44 |
| CHEMBL325343 | — | — | 1 | 7.39 |
| CHEMBL322004 | — | — | 1 | 7.36 |
| CHEMBL223228 | EFAVIRENZ | 4.0 | 1 | 7.33 |
| CHEMBL104658 | — | — | 1 | 6.98 |
| CHEMBL107693 | — | — | 1 | 6.89 |
| CHEMBL321174 | — | — | 1 | 6.74 |
| CHEMBL105400 | — | — | 1 | 6.73 |
| CHEMBL413751 | — | — | 1 | 6.21 |
| CHEMBL106646 | — | — | 1 | 6.11 |
| CHEMBL105630 | — | — | 1 | 5.87 |
| CHEMBL106659 | — | — | 1 | 5.74 |
| CHEMBL321786 | — | — | 1 | 5.71 |
| CHEMBL105826 | — | — | 1 | 5.57 |
| CHEMBL107899 | — | — | 1 | 5.42 |
| CHEMBL104738 | — | — | 1 | 5.21 |
| CHEMBL107946 | — | — | 1 | 5.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL106783 | — | IC50 | = | 11.69 | nM | 7.93 |
| CHEMBL320282 | — | IC50 | = | 11.82 | nM | 7.93 |
| CHEMBL320379 | — | IC50 | = | 16.68 | nM | 7.78 |
| CHEMBL268871 | L-697661 | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL106694 | — | IC50 | = | 24.34 | nM | 7.61 |
| CHEMBL106997 | — | IC50 | = | 25.56 | nM | 7.59 |
| CHEMBL104349 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL105863 | — | IC50 | = | 36.01 | nM | 7.44 |
| CHEMBL325343 | — | IC50 | = | 41.1 | nM | 7.39 |
| CHEMBL322004 | — | IC50 | = | 43.89 | nM | 7.36 |
| CHEMBL223228 | EFAVIRENZ | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL104658 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL107693 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL321174 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL105400 | — | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL413751 | — | IC50 | = | 613.0 | nM | 6.21 |
| CHEMBL106646 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL105630 | — | IC50 | = | 1348.0 | nM | 5.87 |
| CHEMBL106659 | — | IC50 | = | 1842.0 | nM | 5.74 |
| CHEMBL321786 | — | IC50 | = | 1951.0 | nM | 5.71 |
| CHEMBL105826 | — | IC50 | = | 2696.0 | nM | 5.57 |
| CHEMBL107899 | — | IC50 | = | 3843.0 | nM | 5.42 |
| CHEMBL104738 | — | IC50 | = | 6093.0 | nM | 5.21 |
| CHEMBL107946 | — | IC50 | = | 8115.0 | nM | 5.09 |