Assay Detail
Binding
CHEMBL804312
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HIV-1 reverse transcriptase inhibitory activity against Cys181 mutant using (poly)rC600*(oligo)dGT as template primer.
24
Total Activities
21
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
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.10 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL134278 | — | — | 3 | 8.40 |
| CHEMBL223228 | EFAVIRENZ | 4.0 | 1 | 8.22 |
| CHEMBL133559 | — | — | 1 | 8.10 |
| CHEMBL593 | DELAVIRDINE | 4.0 | 1 | 8.05 |
| CHEMBL134026 | — | — | 2 | 8.00 |
| CHEMBL541204 | — | — | 1 | 7.85 |
| CHEMBL132425 | — | — | 1 | 7.80 |
| CHEMBL135105 | — | — | 1 | 7.80 |
| CHEMBL133658 | — | — | 1 | 7.70 |
| CHEMBL131643 | — | — | 1 | 7.68 |
| CHEMBL57 | NEVIRAPINE | 4.0 | 1 | 6.94 |
| CHEMBL340047 | — | — | 1 | 6.89 |
| CHEMBL287317 | — | — | 1 | 6.85 |
| CHEMBL36424 | — | — | 1 | 6.62 |
| CHEMBL336426 | — | — | 1 | 6.58 |
| CHEMBL131972 | — | — | 1 | 6.00 |
| CHEMBL39665 | — | — | 1 | 5.82 |
| CHEMBL133779 | — | — | 1 | 5.37 |
| CHEMBL40562 | — | — | 1 | 5.00 |
| CHEMBL132259 | — | — | 1 | 4.90 |
| CHEMBL132122 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL134278 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL223228 | EFAVIRENZ | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL133559 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL593 | DELAVIRDINE | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL134026 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL541204 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL134026 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL135105 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL132425 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL134278 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL133658 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL131643 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL134278 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL57 | NEVIRAPINE | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL340047 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL287317 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL36424 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL336426 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL131972 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL39665 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL133779 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL40562 | — | IC50 | = | 10100.0 | nM | 5.00 |
| CHEMBL132259 | — | IC50 | = | 12700.0 | nM | 4.90 |
| CHEMBL132122 | — | IC50 | > | 50000.0 | nM | - |