Assay Detail
Binding
CHEMBL4135244
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Inhibition of HIV1 integrase pre-incubated for 10 mins before DNA substrate addition and measured after 30 mins
20
Total Activities
20
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 integrase (CHEMBL3471) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus 1 |
Publication
Design, synthesis and biological evaluations of N-Hydroxy thienopyrimidine-2,4-diones as inhibitors of HIV reverse transcriptase-associated RNase H.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.24 | 6.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL254316 | RALTEGRAVIR | 4.0 | 1 | 6.19 |
| CHEMBL4176832 | — | — | 1 | 5.89 |
| CHEMBL4170599 | — | — | 1 | 5.70 |
| CHEMBL4163088 | — | — | 1 | 5.68 |
| CHEMBL4161705 | — | — | 1 | 5.66 |
| CHEMBL4168270 | — | — | 1 | 5.44 |
| CHEMBL183062 | — | — | 1 | 5.35 |
| CHEMBL4172336 | — | — | 1 | 5.30 |
| CHEMBL4167025 | — | — | 1 | 5.25 |
| CHEMBL4175393 | — | — | 1 | 5.10 |
| CHEMBL4163126 | — | — | 1 | 5.08 |
| CHEMBL4175467 | — | — | 1 | 5.08 |
| CHEMBL4159305 | — | — | 1 | 4.96 |
| CHEMBL183792 | — | — | 1 | 4.92 |
| CHEMBL4176527 | — | — | 1 | 4.77 |
| CHEMBL4170035 | — | — | 1 | 4.77 |
| CHEMBL4162103 | — | — | 1 | 4.64 |
| CHEMBL361350 | — | — | 1 | 4.46 |
| CHEMBL4161240 | — | — | 1 | - |
| CHEMBL4171477 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL254316 | RALTEGRAVIR | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL4176832 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4170599 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4163088 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4161705 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4168270 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL183062 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4172336 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4167025 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4175393 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL4163126 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL4175467 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL4159305 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL183792 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4176527 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4170035 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4162103 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL361350 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL4161240 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4171477 | — | IC50 | > | 100000.0 | nM | - |