Assay Detail
Binding
CHEMBL954258
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIV1 reverse transcriptase p66/p51 Y181I mutant
27
Total Activities
27
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
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 5.51 | 7.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL398174 | — | — | 1 | 7.54 |
| CHEMBL85059 | — | — | 1 | 6.85 |
| CHEMBL126603 | — | — | 1 | 5.78 |
| CHEMBL469562 | — | — | 1 | 5.74 |
| CHEMBL502565 | — | — | 1 | 5.71 |
| CHEMBL512673 | — | — | 1 | 5.66 |
| CHEMBL470404 | — | — | 1 | 5.61 |
| CHEMBL127012 | — | — | 1 | 5.60 |
| CHEMBL470403 | — | — | 1 | 5.54 |
| CHEMBL511290 | — | — | 1 | 5.38 |
| CHEMBL469358 | — | — | 1 | 5.38 |
| CHEMBL469985 | — | — | 1 | 5.30 |
| CHEMBL472217 | — | — | 1 | 5.26 |
| CHEMBL511963 | — | — | 1 | 5.20 |
| CHEMBL513080 | — | — | 1 | 5.14 |
| CHEMBL502566 | — | — | 1 | 5.07 |
| CHEMBL469986 | — | — | 1 | 5.07 |
| CHEMBL512486 | — | — | 1 | 4.92 |
| CHEMBL469569 | — | — | 1 | 4.80 |
| CHEMBL485180 | — | — | 1 | 4.58 |
| CHEMBL469804 | — | — | 1 | - |
| CHEMBL470007 | — | — | 1 | - |
| CHEMBL470630 | — | — | 1 | - |
| CHEMBL524360 | — | — | 1 | - |
| CHEMBL502297 | — | — | 1 | - |
| CHEMBL521183 | — | — | 1 | - |
| CHEMBL383700 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL398174 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL85059 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL126603 | — | IC50 | = | 1645.0 | nM | 5.78 |
| CHEMBL469562 | — | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL502565 | — | IC50 | = | 1944.0 | nM | 5.71 |
| CHEMBL512673 | — | IC50 | = | 2211.0 | nM | 5.66 |
| CHEMBL470404 | — | IC50 | = | 2459.0 | nM | 5.61 |
| CHEMBL127012 | — | IC50 | = | 2493.0 | nM | 5.60 |
| CHEMBL470403 | — | IC50 | = | 2909.0 | nM | 5.54 |
| CHEMBL511290 | — | IC50 | = | 4211.0 | nM | 5.38 |
| CHEMBL469358 | — | IC50 | = | 4137.0 | nM | 5.38 |
| CHEMBL469985 | — | IC50 | = | 5055.0 | nM | 5.30 |
| CHEMBL472217 | — | IC50 | = | 5534.0 | nM | 5.26 |
| CHEMBL511963 | — | IC50 | = | 6277.0 | nM | 5.20 |
| CHEMBL513080 | — | IC50 | = | 7165.0 | nM | 5.14 |
| CHEMBL502566 | — | IC50 | = | 8550.0 | nM | 5.07 |
| CHEMBL469986 | — | IC50 | = | 8566.0 | nM | 5.07 |
| CHEMBL512486 | — | IC50 | = | 11920.0 | nM | 4.92 |
| CHEMBL469569 | — | IC50 | = | 15830.0 | nM | 4.80 |
| CHEMBL485180 | — | IC50 | = | 26220.0 | nM | 4.58 |
| CHEMBL469804 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL470007 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL470630 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL524360 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL502297 | — | IC50 | - | — | - | |
| CHEMBL521183 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL383700 | — | IC50 | - | — | - |