Assay Detail
Functional
CHEMBL5140100
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiviral activity against HIV-1 harboring K103N mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Human immunodeficiency virus 1 |
| Cell Type | MT4 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Target
Human immunodeficiency virus 1 (CHEMBL378) ↗| Type | ORGANISM |
| Organism | Human immunodeficiency virus 1 |
Publication
Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 6.94 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL308954 | ETRAVIRINE | 4.0 | 1 | 8.52 |
| CHEMBL129 | ZIDOVUDINE | 4.0 | 1 | 8.22 |
| CHEMBL85059 | — | — | 1 | 7.77 |
| CHEMBL5190166 | — | — | 1 | 7.25 |
| CHEMBL223228 | EFAVIRENZ | 4.0 | 1 | 7.01 |
| CHEMBL5202157 | — | — | 1 | 6.85 |
| CHEMBL5199217 | — | — | 1 | 6.85 |
| CHEMBL5186616 | — | — | 1 | 6.82 |
| CHEMBL5201311 | — | — | 1 | 6.72 |
| CHEMBL5180167 | — | — | 1 | 6.68 |
| CHEMBL5199747 | — | — | 1 | 6.48 |
| CHEMBL5171297 | — | — | 1 | 6.36 |
| CHEMBL5205695 | — | — | 1 | 6.24 |
| CHEMBL57 | NEVIRAPINE | 4.0 | 1 | 5.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL308954 | ETRAVIRINE | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL129 | ZIDOVUDINE | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL85059 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5190166 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL223228 | EFAVIRENZ | EC50 | = | 97.0 | nM | 7.01 |
| CHEMBL5202157 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5199217 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5186616 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5201311 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5180167 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5199747 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5171297 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5205695 | — | EC50 | = | 570.0 | nM | 6.24 |
| CHEMBL57 | NEVIRAPINE | EC50 | = | 3551.0 | nM | 5.45 |