Assay Detail
Binding
CHEMBL998725
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Inhibition of HIV1 integrase by overall integration assay
22
Total Activities
22
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
Investigations on the 4-quinolone-3-carboxylic acid motif. 1. Synthesis and structure-activity relationship of a class of human immunodeficiency virus type 1 integrase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.30 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL204656 | ELVITEGRAVIR | 4.0 | 1 | 8.70 |
| CHEMBL522229 | — | — | 1 | 7.30 |
| CHEMBL458279 | — | — | 1 | 7.16 |
| CHEMBL458280 | — | — | 1 | 6.05 |
| CHEMBL497490 | — | — | 1 | 6.00 |
| CHEMBL497661 | — | — | 1 | 5.34 |
| CHEMBL511508 | — | — | 1 | 5.32 |
| CHEMBL526642 | — | — | 1 | 5.25 |
| CHEMBL497489 | — | — | 1 | 5.01 |
| CHEMBL497505 | — | — | 1 | 4.97 |
| CHEMBL497506 | — | — | 1 | 4.73 |
| CHEMBL498491 | — | — | 1 | 4.42 |
| CHEMBL498504 | — | — | 1 | 4.36 |
| CHEMBL496491 | — | — | 1 | 4.26 |
| CHEMBL497475 | — | — | 1 | 4.14 |
| CHEMBL496476 | — | — | 1 | 4.13 |
| CHEMBL526269 | — | — | 1 | 4.11 |
| CHEMBL458483 | — | — | 1 | 4.06 |
| CHEMBL444410 | — | — | 1 | - |
| CHEMBL498490 | — | — | 1 | - |
| CHEMBL498321 | — | — | 1 | - |
| CHEMBL497476 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL204656 | ELVITEGRAVIR | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL522229 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL458279 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL458280 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL497490 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL497661 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL511508 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL526642 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL497489 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL497505 | — | IC50 | = | 10800.0 | nM | 4.97 |
| CHEMBL497506 | — | IC50 | = | 18700.0 | nM | 4.73 |
| CHEMBL498491 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL498504 | — | IC50 | = | 43700.0 | nM | 4.36 |
| CHEMBL496491 | — | IC50 | = | 54900.0 | nM | 4.26 |
| CHEMBL497475 | — | IC50 | = | 71900.0 | nM | 4.14 |
| CHEMBL496476 | — | IC50 | = | 73900.0 | nM | 4.13 |
| CHEMBL526269 | — | IC50 | = | 77600.0 | nM | 4.11 |
| CHEMBL458483 | — | IC50 | = | 86900.0 | nM | 4.06 |
| CHEMBL444410 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL498490 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL498321 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL497476 | — | IC50 | > | 100000.0 | nM | - |