Assay Detail
Binding
CHEMBL2168109
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Inhibition of HIV1 reverse transcriptase K103N mutant RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)10:1 and [3H]-dTTP substrate
8
Total Activities
8
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
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.82 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL308954 | ETRAVIRINE | 4.0 | 1 | 7.70 |
| CHEMBL2163488 | — | — | 1 | 7.50 |
| CHEMBL2163842 | — | — | 1 | 7.35 |
| CHEMBL2163845 | — | — | 1 | 6.79 |
| CHEMBL223228 | EFAVIRENZ | 4.0 | 1 | 6.40 |
| CHEMBL57 | NEVIRAPINE | 4.0 | 1 | 5.16 |
| CHEMBL2163848 | — | — | 1 | - |
| CHEMBL2163850 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL308954 | ETRAVIRINE | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2163488 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2163842 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL2163845 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL223228 | EFAVIRENZ | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL57 | NEVIRAPINE | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL2163848 | — | IC50 | > | 40.0 | nM | - |
| CHEMBL2163850 | — | IC50 | > | 10.0 | nM | - |