Assay Detail
Binding
CHEMBL804313
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HIV-1 reverse transcriptase inhibitory activity against Ile 100 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 | 6.77 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL593 | DELAVIRDINE | 4.0 | 1 | 8.05 |
| CHEMBL135105 | — | — | 1 | 7.89 |
| CHEMBL134026 | — | — | 2 | 7.85 |
| CHEMBL134278 | — | — | 3 | 7.85 |
| CHEMBL133559 | — | — | 1 | 7.75 |
| CHEMBL133658 | — | — | 1 | 7.57 |
| CHEMBL132425 | — | — | 1 | 7.50 |
| CHEMBL223228 | EFAVIRENZ | 4.0 | 1 | 7.30 |
| CHEMBL131643 | — | — | 1 | 7.28 |
| CHEMBL541204 | — | — | 1 | 7.09 |
| CHEMBL57 | NEVIRAPINE | 4.0 | 1 | 6.89 |
| CHEMBL336426 | — | — | 1 | 6.85 |
| CHEMBL287317 | — | — | 1 | 6.85 |
| CHEMBL340047 | — | — | 1 | 6.70 |
| CHEMBL131972 | — | — | 1 | 6.00 |
| CHEMBL36424 | — | — | 1 | 5.78 |
| CHEMBL133779 | — | — | 1 | 5.39 |
| CHEMBL40562 | — | — | 1 | 4.95 |
| CHEMBL132122 | — | — | 1 | 4.77 |
| CHEMBL132259 | — | — | 1 | 4.58 |
| CHEMBL39665 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL593 | DELAVIRDINE | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL135105 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL134026 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL134278 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL133559 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL133658 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL132425 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL223228 | EFAVIRENZ | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL131643 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL134278 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL541204 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL134278 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL57 | NEVIRAPINE | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL287317 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL336426 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL134026 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL340047 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL131972 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL36424 | — | IC50 | = | 1680.0 | nM | 5.78 |
| CHEMBL133779 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL40562 | — | IC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL132122 | — | IC50 | = | 17100.0 | nM | 4.77 |
| CHEMBL132259 | — | IC50 | = | 26200.0 | nM | 4.58 |
| CHEMBL39665 | — | IC50 | > | 2500.0 | nM | - |