Assay Detail
Binding
CHEMBL1060098
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Inhibition of recombinant HIV-1 integrase strand transfer activity
29
Total Activities
27
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
Dihydroxy-pyrimidine and N-methylpyrimidone HIV-integrase inhibitors: improving cell based activity by the quaternarization of a chiral center.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.37 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL549592 | — | — | 1 | 8.40 |
| CHEMBL394786 | — | — | 1 | 8.22 |
| CHEMBL563757 | — | — | 1 | 7.85 |
| CHEMBL564267 | — | — | 3 | 7.82 |
| CHEMBL254316 | RALTEGRAVIR | 4.0 | 1 | 7.82 |
| CHEMBL563898 | — | — | 1 | 7.70 |
| CHEMBL562595 | — | — | 1 | 7.70 |
| CHEMBL243365 | — | — | 1 | 7.70 |
| CHEMBL550202 | — | — | 1 | 7.70 |
| CHEMBL565220 | — | — | 1 | 7.70 |
| CHEMBL550674 | — | — | 1 | 7.70 |
| CHEMBL243150 | — | — | 1 | 7.52 |
| CHEMBL560944 | — | — | 1 | 7.52 |
| CHEMBL563628 | — | — | 1 | 7.40 |
| CHEMBL559493 | — | — | 1 | 7.30 |
| CHEMBL559494 | — | — | 1 | 7.22 |
| CHEMBL226764 | — | — | 1 | 7.16 |
| CHEMBL554522 | — | — | 1 | 7.10 |
| CHEMBL549798 | — | — | 1 | 7.05 |
| CHEMBL551942 | — | — | 1 | 7.00 |
| CHEMBL559492 | — | — | 1 | 7.00 |
| CHEMBL564984 | — | — | 1 | 6.92 |
| CHEMBL227497 | — | — | 1 | 6.89 |
| CHEMBL407451 | — | — | 1 | 6.66 |
| CHEMBL549309 | — | — | 1 | 6.60 |
| CHEMBL216389 | — | — | 1 | 6.36 |
| CHEMBL562482 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL549592 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL394786 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL563757 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL564267 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL254316 | RALTEGRAVIR | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL243365 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL563898 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL562595 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL550202 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL564267 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL565220 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL550674 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL564267 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL560944 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL243150 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL563628 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL559493 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL559494 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL226764 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL554522 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL549798 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL551942 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL559492 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL564984 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL227497 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL407451 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL549309 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL216389 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL562482 | — | IC50 | = | 550.0 | nM | 6.26 |