Assay Detail
Binding
CHEMBL5609484
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Inhibition of recombinant wild-type HIV-1 reverse transcriptase incubated for 40 mins by fluorescence based assay
30
Total Activities
30
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 | Autocuration |
Target
Human immunodeficiency virus type 1 reverse transcriptase (CHEMBL247) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus 1 |
Publication
Structure-based discovery of novel piperidine-biphenyl-DAPY derivatives as non-nucleoside reverse transcriptase inhibitors featuring improved potency, safety, and selectivity: From piperazine-biphenyl-DAPYs to piperidine-biphenyl-DAPYs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.32 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL223228 | EFAVIRENZ | 4.0 | 1 | 7.89 |
| CHEMBL308954 | ETRAVIRINE | 4.0 | 1 | 7.54 |
| CHEMBL175691 | RILPIVIRINE | 4.0 | 1 | 7.46 |
| CHEMBL5612140 | — | — | 1 | 6.50 |
| CHEMBL5612668 | — | — | 1 | 6.49 |
| CHEMBL5613980 | — | — | 1 | 6.39 |
| CHEMBL5613406 | — | — | 1 | 6.29 |
| CHEMBL5612529 | — | — | 1 | 6.28 |
| CHEMBL5612747 | — | — | 1 | 6.28 |
| CHEMBL5612553 | — | — | 1 | 6.28 |
| CHEMBL5612507 | — | — | 1 | 6.27 |
| CHEMBL5612186 | — | — | 1 | 6.24 |
| CHEMBL5614187 | — | — | 1 | 6.22 |
| CHEMBL5612952 | — | — | 1 | 6.22 |
| CHEMBL5612637 | — | — | 1 | 6.21 |
| CHEMBL5613851 | — | — | 1 | 6.20 |
| CHEMBL5613811 | — | — | 1 | 6.17 |
| CHEMBL5613183 | — | — | 1 | 6.17 |
| CHEMBL5613123 | — | — | 1 | 6.16 |
| CHEMBL5612014 | — | — | 1 | 6.15 |
| CHEMBL5612205 | — | — | 1 | 6.14 |
| CHEMBL5613254 | — | — | 1 | 6.13 |
| CHEMBL5612631 | — | — | 1 | 6.13 |
| CHEMBL5612451 | — | — | 1 | 6.11 |
| CHEMBL5611942 | — | — | 1 | 6.11 |
| CHEMBL5613020 | — | — | 1 | 6.05 |
| CHEMBL5613691 | — | — | 1 | 6.00 |
| CHEMBL57 | NEVIRAPINE | 4.0 | 1 | 5.97 |
| CHEMBL5613297 | — | — | 1 | 5.89 |
| CHEMBL5614024 | — | — | 1 | 5.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL223228 | EFAVIRENZ | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL308954 | ETRAVIRINE | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL175691 | RILPIVIRINE | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5612140 | — | IC50 | = | 314.0 | nM | 6.50 |
| CHEMBL5612668 | — | IC50 | = | 327.0 | nM | 6.49 |
| CHEMBL5613980 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5613406 | — | IC50 | = | 514.0 | nM | 6.29 |
| CHEMBL5612529 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL5612747 | — | IC50 | = | 522.0 | nM | 6.28 |
| CHEMBL5612553 | — | IC50 | = | 527.0 | nM | 6.28 |
| CHEMBL5612507 | — | IC50 | = | 535.0 | nM | 6.27 |
| CHEMBL5612186 | — | IC50 | = | 582.0 | nM | 6.24 |
| CHEMBL5614187 | — | IC50 | = | 596.0 | nM | 6.22 |
| CHEMBL5612952 | — | IC50 | = | 598.0 | nM | 6.22 |
| CHEMBL5612637 | — | IC50 | = | 622.0 | nM | 6.21 |
| CHEMBL5613851 | — | IC50 | = | 634.0 | nM | 6.20 |
| CHEMBL5613811 | — | IC50 | = | 676.0 | nM | 6.17 |
| CHEMBL5613183 | — | IC50 | = | 669.0 | nM | 6.17 |
| CHEMBL5613123 | — | IC50 | = | 686.0 | nM | 6.16 |
| CHEMBL5612014 | — | IC50 | = | 713.0 | nM | 6.15 |
| CHEMBL5612205 | — | IC50 | = | 718.0 | nM | 6.14 |
| CHEMBL5613254 | — | IC50 | = | 744.0 | nM | 6.13 |
| CHEMBL5612631 | — | IC50 | = | 736.0 | nM | 6.13 |
| CHEMBL5612451 | — | IC50 | = | 782.0 | nM | 6.11 |
| CHEMBL5611942 | — | IC50 | = | 769.0 | nM | 6.11 |
| CHEMBL5613020 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL5613691 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL57 | NEVIRAPINE | IC50 | = | 1075.0 | nM | 5.97 |
| CHEMBL5613297 | — | IC50 | = | 1295.0 | nM | 5.89 |
| CHEMBL5614024 | — | IC50 | = | 2042.0 | nM | 5.69 |