Assay Detail
Binding
CHEMBL802599
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Inhibitory activity against HIV-1 Y181C Reverse transcriptase (RT)
68
Total Activities
68
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
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 | 68 | 6.27 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL81319 | — | — | 1 | 7.40 |
| CHEMBL142853 | — | — | 1 | 7.30 |
| CHEMBL422123 | — | — | 1 | 7.22 |
| CHEMBL145237 | — | — | 1 | 7.22 |
| CHEMBL357221 | — | — | 1 | 7.16 |
| CHEMBL344289 | — | — | 1 | 6.96 |
| CHEMBL144145 | — | — | 1 | 6.92 |
| CHEMBL144652 | — | — | 1 | 6.80 |
| CHEMBL144653 | — | — | 1 | 6.75 |
| CHEMBL356779 | — | — | 1 | 6.72 |
| CHEMBL422659 | — | — | 1 | 6.68 |
| CHEMBL288336 | — | — | 1 | 6.68 |
| CHEMBL144290 | — | — | 1 | 6.68 |
| CHEMBL357183 | — | — | 1 | 6.62 |
| CHEMBL142659 | — | — | 1 | 6.58 |
| CHEMBL144035 | — | — | 1 | 6.57 |
| CHEMBL144561 | — | — | 1 | 6.54 |
| CHEMBL146550 | — | — | 1 | 6.52 |
| CHEMBL355918 | — | — | 1 | 6.50 |
| CHEMBL344288 | — | — | 1 | 6.38 |
| CHEMBL145193 | — | — | 1 | 6.38 |
| CHEMBL145736 | — | — | 1 | 6.36 |
| CHEMBL356998 | — | — | 1 | 6.25 |
| CHEMBL343883 | — | — | 1 | 6.25 |
| CHEMBL144866 | — | — | 1 | 6.25 |
| CHEMBL145397 | — | — | 1 | 6.22 |
| CHEMBL144852 | — | — | 1 | 6.19 |
| CHEMBL144773 | — | — | 1 | 6.17 |
| CHEMBL342068 | — | — | 1 | 6.15 |
| CHEMBL358555 | — | — | 1 | 6.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL81319 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL142853 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL145237 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL422123 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL357221 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL344289 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL144145 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL144652 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL144653 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL356779 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL422659 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL288336 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL144290 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL357183 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL142659 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL144035 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL144561 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL146550 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL355918 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL344288 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL145193 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL145736 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL356998 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL343883 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL144866 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL145397 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL144852 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL144773 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL342068 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL358555 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL145322 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL343007 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL142837 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL342056 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL145199 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL144820 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL358564 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL143107 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL15411 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL288305 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL144378 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL359187 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL342771 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL358947 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL37628 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL144522 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL37343 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL143976 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL145004 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL57 | NEVIRAPINE | IC50 | = | 2600.0 | nM | 5.58 |