Assay Detail
Functional
CHEMBL834149
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Effective concentration of the compound to inhibit HIV-1 mutant L100I+K103N replication in HIV-infected MT-4 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MT4 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 6.40 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL308954 | ETRAVIRINE | 4.0 | 1 | 7.72 |
| CHEMBL70517 | — | — | 1 | 7.43 |
| CHEMBL439757 | — | — | 1 | 7.31 |
| CHEMBL71882 | — | — | 1 | 6.46 |
| CHEMBL72335 | — | — | 1 | 6.10 |
| CHEMBL70442 | — | — | 1 | 5.96 |
| CHEMBL71728 | — | — | 1 | 5.89 |
| CHEMBL73008 | — | — | 1 | 5.60 |
| CHEMBL305803 | — | — | 1 | 5.09 |
| CHEMBL305838 | — | — | 1 | - |
| CHEMBL70663 | DAPIVIRINE | 3.0 | 1 | - |
| CHEMBL223228 | EFAVIRENZ | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL308954 | ETRAVIRINE | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL70517 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL439757 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL71882 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL72335 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL70442 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL71728 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL73008 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL305803 | — | EC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL305838 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL70663 | DAPIVIRINE | EC50 | > | 10000.0 | nM | - |
| CHEMBL223228 | EFAVIRENZ | EC50 | > | 10000.0 | nM | - |