Assay Detail
Binding
CHEMBL4187326
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Inhibition of reverse transcriptase K103N mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay
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 | Intermediate |
Target
Human immunodeficiency virus type 1 reverse transcriptase (CHEMBL247) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus 1 |
Publication
Structural optimization of N1-aryl-benzimidazoles for the discovery of new non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 5.93 | 7.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL223228 | EFAVIRENZ | 4.0 | 1 | 7.54 |
| CHEMBL4203336 | — | — | 1 | 6.17 |
| CHEMBL4211084 | — | — | 1 | 6.02 |
| CHEMBL4218333 | — | — | 1 | 5.92 |
| CHEMBL57 | NEVIRAPINE | 4.0 | 1 | 5.02 |
| CHEMBL4207026 | — | — | 1 | 4.93 |
| CHEMBL4211907 | — | — | 1 | - |
| CHEMBL4218422 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL223228 | EFAVIRENZ | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4203336 | — | EC50 | = | 670.0 | nM | 6.17 |
| CHEMBL4211084 | — | EC50 | = | 960.0 | nM | 6.02 |
| CHEMBL4218333 | — | EC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL57 | NEVIRAPINE | EC50 | = | 9590.0 | nM | 5.02 |
| CHEMBL4207026 | — | EC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL4211907 | — | EC50 | > | 3130.0 | nM | - |
| CHEMBL4218422 | — | EC50 | > | 33940.0 | nM | - |