Assay Detail
Binding
CHEMBL1062363
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIV1 recombinant integrase strand transfer activity treated after enzyme assembly and washing
49
Total Activities
49
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
N-(4-Fluorobenzyl)-3-hydroxy-9,9-dimethyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrazino[1,2-a]pyrimidine-2-carboxamides a novel class of potent HIV-1 integrase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 49 | 8.03 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL556894 | — | — | 1 | 8.70 |
| CHEMBL549422 | — | — | 1 | 8.70 |
| CHEMBL559395 | — | — | 1 | 8.52 |
| CHEMBL550051 | — | — | 1 | 8.52 |
| CHEMBL558051 | — | — | 1 | 8.40 |
| CHEMBL559537 | — | — | 1 | 8.30 |
| CHEMBL557854 | — | — | 1 | 8.30 |
| CHEMBL552065 | — | — | 1 | 8.30 |
| CHEMBL558641 | — | — | 1 | 8.30 |
| CHEMBL563502 | — | — | 1 | 8.30 |
| CHEMBL554284 | — | — | 1 | 8.30 |
| CHEMBL550985 | — | — | 1 | 8.30 |
| CHEMBL560387 | — | — | 1 | 8.30 |
| CHEMBL560251 | — | — | 1 | 8.22 |
| CHEMBL561467 | — | — | 1 | 8.22 |
| CHEMBL564212 | — | — | 1 | 8.22 |
| CHEMBL560322 | — | — | 1 | 8.22 |
| CHEMBL550784 | — | — | 1 | 8.22 |
| CHEMBL549831 | — | — | 1 | 8.22 |
| CHEMBL559306 | — | — | 1 | 8.22 |
| CHEMBL561987 | — | — | 1 | 8.15 |
| CHEMBL557646 | — | — | 1 | 8.15 |
| CHEMBL561729 | — | — | 1 | 8.15 |
| CHEMBL557308 | — | — | 1 | 8.15 |
| CHEMBL558121 | — | — | 1 | 8.15 |
| CHEMBL563631 | — | — | 1 | 8.10 |
| CHEMBL562327 | — | — | 1 | 8.10 |
| CHEMBL551808 | — | — | 1 | 8.10 |
| CHEMBL550997 | — | — | 1 | 8.10 |
| CHEMBL552202 | — | — | 1 | 8.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL556894 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL549422 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL559395 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL550051 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL558051 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL552065 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL557854 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL558641 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL563502 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL559537 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL554284 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL550985 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL560387 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL559306 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL549831 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL560251 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL550784 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL560322 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL564212 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL561467 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL558121 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL557308 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL557646 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL561987 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL561729 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL563631 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL562327 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL551808 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL550997 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL552202 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL552264 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL564823 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL554737 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL551325 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL552177 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL518520 | RALTEGRAVIR POTASSIUM | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL550108 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL550394 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL563270 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL552327 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL560185 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL551402 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL550590 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL554745 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL563963 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL552176 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL560265 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL562760 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL551401 | — | IC50 | = | 76.0 | nM | 7.12 |