Assay Detail
Binding
CHEMBL3240945
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Inhibition of HIV1 RNase H function of recombinant reverse transcriptase using an 18-nt 3'-fluorescein-labeled RNA annealed to complementary 18-nt 5'-dabsyl-labeled DNA as substrate after 10 mins by fluorescence spectrometer analysis
19
Total Activities
19
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
Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 4.92 | 5.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3238130 | — | — | 1 | 5.48 |
| CHEMBL496454 | — | — | 1 | 5.29 |
| CHEMBL3238134 | — | — | 1 | 5.24 |
| CHEMBL3238133 | — | — | 1 | 5.18 |
| CHEMBL3238132 | — | — | 1 | 5.17 |
| CHEMBL3238121 | — | — | 1 | 4.73 |
| CHEMBL3238122 | — | — | 1 | 4.58 |
| CHEMBL3238127 | — | — | 1 | 4.54 |
| CHEMBL204656 | ELVITEGRAVIR | 4.0 | 1 | 4.04 |
| CHEMBL3238123 | — | — | 1 | - |
| CHEMBL3238124 | — | — | 1 | - |
| CHEMBL3238125 | — | — | 1 | - |
| CHEMBL3238126 | — | — | 1 | - |
| CHEMBL3238128 | — | — | 1 | - |
| CHEMBL3238129 | — | — | 1 | - |
| CHEMBL3238131 | — | — | 1 | - |
| CHEMBL456365 | — | — | 1 | - |
| CHEMBL3238120 | — | — | 1 | - |
| CHEMBL254316 | RALTEGRAVIR | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3238130 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL496454 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL3238134 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL3238133 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL3238132 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL3238121 | — | IC50 | = | 18500.0 | nM | 4.73 |
| CHEMBL3238122 | — | IC50 | = | 26200.0 | nM | 4.58 |
| CHEMBL3238127 | — | IC50 | = | 28700.0 | nM | 4.54 |
| CHEMBL204656 | ELVITEGRAVIR | IC50 | = | 91000.0 | nM | 4.04 |
| CHEMBL3238123 | — | IC50 | - | — | - | |
| CHEMBL3238124 | — | IC50 | - | — | - | |
| CHEMBL3238125 | — | IC50 | - | — | - | |
| CHEMBL3238126 | — | IC50 | - | — | - | |
| CHEMBL3238128 | — | IC50 | - | — | - | |
| CHEMBL3238129 | — | IC50 | - | — | - | |
| CHEMBL3238131 | — | IC50 | - | — | - | |
| CHEMBL456365 | — | IC50 | - | — | - | |
| CHEMBL3238120 | — | IC50 | - | — | - | |
| CHEMBL254316 | RALTEGRAVIR | IC50 | > | 100000.0 | nM | - |