Assay Detail
Binding
CHEMBL5585776
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Allosteric inhibition of HIV-1 integrase by ELISA based IN-DNA assembly/Strand transfer assay
15
Total Activities
15
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 and synthesis of novel and potent allosteric HIV-1 integrase inhibitors with a spirocyclic moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.60 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5597897 | — | — | 1 | 8.85 |
| CHEMBL5597978 | — | — | 1 | 8.74 |
| CHEMBL5597609 | — | — | 1 | 8.70 |
| CHEMBL5596288 | — | — | 1 | 8.66 |
| CHEMBL5596381 | — | — | 1 | 8.24 |
| CHEMBL5597870 | — | — | 1 | 8.08 |
| CHEMBL5277931 | — | — | 1 | 7.92 |
| CHEMBL5596946 | — | — | 1 | 7.70 |
| CHEMBL5596570 | — | — | 1 | 7.30 |
| CHEMBL5596874 | — | — | 1 | 7.28 |
| CHEMBL5596283 | — | — | 1 | 7.27 |
| CHEMBL5597523 | — | — | 1 | 6.80 |
| CHEMBL5596955 | — | — | 1 | 6.37 |
| CHEMBL5591004 | — | — | 1 | 6.31 |
| CHEMBL5598287 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5597897 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5597978 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5597609 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5596288 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5596381 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL5597870 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL5277931 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5596946 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5596570 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5596874 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5596283 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5597523 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5596955 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL5591004 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL5598287 | — | IC50 | = | 1800.0 | nM | 5.75 |