Assay Detail
Binding
CHEMBL3418042
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIV1 reverse transcriptase L100I/K103N mutant associated RNase H domain activity assessed as reduction in reduction in DNA 3' end directed cleavage using HTS-1 RNA/DNA duplex substrate by fluorescence assay
7
Total Activities
7
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
Design, synthesis, biochemical, and antiviral evaluations of C6 benzyl and C6 biarylmethyl substituted 2-hydroxylisoquinoline-1,3-diones: dual inhibition against HIV reverse transcriptase-associated RNase H and polymerase with antiviral activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.84 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3414871 | — | — | 1 | 6.52 |
| CHEMBL3414868 | — | — | 1 | 6.10 |
| CHEMBL3414865 | — | — | 1 | 6.00 |
| CHEMBL3414870 | — | — | 1 | 5.85 |
| CHEMBL3414869 | — | — | 1 | 5.72 |
| CHEMBL3414867 | — | — | 1 | 5.60 |
| CHEMBL3414860 | — | — | 1 | 5.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3414871 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3414868 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3414865 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3414870 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3414869 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3414867 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3414860 | — | IC50 | = | 8700.0 | nM | 5.06 |