Assay Detail
Binding
CHEMBL2167934
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIV1 reverse transcriptase L100I 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 | 7.21 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2163488 | — | — | 1 | 8.10 |
| CHEMBL308954 | ETRAVIRINE | 4.0 | 1 | 8.00 |
| CHEMBL2163842 | — | — | 1 | 7.96 |
| CHEMBL2163845 | — | — | 1 | 7.62 |
| CHEMBL2163848 | — | — | 1 | 6.54 |
| CHEMBL57 | NEVIRAPINE | 4.0 | 1 | 5.05 |
| CHEMBL223228 | EFAVIRENZ | 4.0 | 1 | - |
| CHEMBL2163850 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2163488 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL308954 | ETRAVIRINE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2163842 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2163845 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2163848 | — | IC50 | = | 287.0 | nM | 6.54 |
| CHEMBL57 | NEVIRAPINE | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL223228 | EFAVIRENZ | IC50 | - | — | - | |
| CHEMBL2163850 | — | IC50 | > | 4.0 | nM | - |