Assay Detail
Binding
CHEMBL1259305
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Inhibition of HIV1 integrase 3'-strand transfer
35
Total Activities
35
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
Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: selection of the scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.33 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL522653 | — | — | 1 | 7.60 |
| CHEMBL1258612 | — | — | 1 | 7.12 |
| CHEMBL1257580 | — | — | 1 | 7.10 |
| CHEMBL1257819 | — | — | 1 | 7.07 |
| CHEMBL1258162 | — | — | 1 | 6.96 |
| CHEMBL1258046 | — | — | 1 | 6.89 |
| CHEMBL1257935 | — | — | 1 | 6.89 |
| CHEMBL518520 | RALTEGRAVIR POTASSIUM | 4.0 | 1 | 6.89 |
| CHEMBL1257936 | — | — | 1 | 6.87 |
| CHEMBL1257575 | — | — | 1 | 6.77 |
| CHEMBL1258045 | — | — | 1 | 6.71 |
| CHEMBL1257576 | — | — | 1 | 6.61 |
| CHEMBL1257697 | — | — | 1 | 6.56 |
| CHEMBL1257696 | — | — | 1 | 6.37 |
| CHEMBL1258501 | — | — | 1 | 6.35 |
| CHEMBL499184 | — | — | 1 | 6.23 |
| CHEMBL1258956 | — | — | 1 | 6.20 |
| CHEMBL1257818 | — | — | 1 | 6.12 |
| CHEMBL1257223 | — | — | 1 | 5.95 |
| CHEMBL1258958 | — | — | 1 | 5.37 |
| CHEMBL1257345 | — | — | 1 | 5.29 |
| CHEMBL1258840 | — | — | 1 | 4.87 |
| CHEMBL1258720 | — | — | 1 | 4.69 |
| CHEMBL1258957 | — | — | 1 | 4.48 |
| CHEMBL1257224 | — | — | 1 | - |
| CHEMBL1257344 | — | — | 1 | - |
| CHEMBL1258842 | — | — | 1 | - |
| CHEMBL1258841 | — | — | 1 | - |
| CHEMBL1258721 | — | — | 1 | - |
| CHEMBL1258613 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL522653 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1258612 | — | IC50 | = | 76.8 | nM | 7.12 |
| CHEMBL1257580 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1257819 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL1258162 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1258046 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1257935 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL518520 | RALTEGRAVIR POTASSIUM | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1257936 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL1257575 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1258045 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL1257576 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL1257697 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL1257696 | — | IC50 | = | 429.0 | nM | 6.37 |
| CHEMBL1258501 | — | IC50 | = | 445.0 | nM | 6.35 |
| CHEMBL499184 | — | IC50 | = | 587.0 | nM | 6.23 |
| CHEMBL1258956 | — | IC50 | = | 626.0 | nM | 6.20 |
| CHEMBL1257818 | — | IC50 | = | 755.0 | nM | 6.12 |
| CHEMBL1257223 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL1258958 | — | IC50 | = | 4250.0 | nM | 5.37 |
| CHEMBL1257345 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL1258840 | — | IC50 | = | 13650.0 | nM | 4.87 |
| CHEMBL1258720 | — | IC50 | = | 20250.0 | nM | 4.69 |
| CHEMBL1258957 | — | IC50 | = | 33250.0 | nM | 4.48 |
| CHEMBL1258278 | — | IC50 | - | — | - | |
| CHEMBL1258277 | — | IC50 | - | — | - | |
| CHEMBL1258163 | — | IC50 | - | — | - | |
| CHEMBL1257456 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1257455 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1258613 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1258721 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1258841 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1258842 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1257344 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1257224 | — | IC50 | > | 50000.0 | nM | - |