Assay Detail
Binding
CHEMBL1816188
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Inhibition of HIV1 recombinant integrase 3'-processing and strand transfer activity using 21-mer U5B/U5A duplex oligonucleotides after 1 hr
12
Total Activities
12
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 integrase (CHEMBL3471) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus 1 |
Publication
Ethyl malonate amides: a diketo acid offspring fragment for HIV integrase inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.77 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL254316 | RALTEGRAVIR | 4.0 | 1 | 8.30 |
| CHEMBL36640 | — | — | 1 | 6.16 |
| CHEMBL1813126 | — | — | 1 | 5.70 |
| CHEMBL1813127 | — | — | 1 | 4.38 |
| CHEMBL1456957 | — | — | 1 | 4.30 |
| CHEMBL1813133 | — | — | 1 | - |
| CHEMBL1813132 | — | — | 1 | - |
| CHEMBL1813131 | — | — | 1 | - |
| CHEMBL1813130 | — | — | 1 | - |
| CHEMBL1813129 | — | — | 1 | - |
| CHEMBL1813128 | — | — | 1 | - |
| CHEMBL1813134 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL254316 | RALTEGRAVIR | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL36640 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1813126 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1813127 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL1456957 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL1813133 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1813132 | — | IC50 | - | — | - | |
| CHEMBL1813131 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL1813130 | — | IC50 | - | — | - | |
| CHEMBL1813129 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1813128 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1813134 | — | IC50 | = | 500000.0 | nM | - |