Assay Detail
Binding
CHEMBL1020340
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Inhibition of HIV1 reverse transcriptase p66/p51 K65R mutant expressed in Escherichia coli using calf thymus DNA substrate
4
Total Activities
4
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
In vitro suppression of K65R reverse transcriptase-mediated tenofovir- and adefovir-5'-diphosphate resistance conferred by the boranophosphonate derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 4.65 | 4.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2448397 | — | — | 1 | 4.92 |
| CHEMBL2448398 | — | — | 1 | 4.75 |
| CHEMBL1162433 | ADEFOVIR DIPHOSPHATE | -1.0 | 1 | 4.28 |
| CHEMBL1236349 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2448397 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2448398 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL1162433 | ADEFOVIR DIPHOSPHATE | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL1236349 | — | IC50 | = | 170000.0 | nM | - |