Assay Detail
Binding
CHEMBL990225
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIV1 integrase 3' processing/strand transfer coupled activity
9
Total Activities
9
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
The complestatins as HIV-1 integrase inhibitors. Efficient isolation, structure elucidation, and inhibitory activities of isocomplestatin, chloropeptin I, new complestatins, A and B, and acid-hydrolysis products of chloropeptin I.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.84 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL506605 | ISOCOMPLESTATIN | — | 1 | 6.70 |
| CHEMBL525803 | CHLOROPEPTIN | — | 1 | 6.40 |
| CHEMBL448564 | — | — | 1 | 6.30 |
| CHEMBL507121 | — | — | 1 | 6.22 |
| CHEMBL524665 | COMPLESTATINS A | — | 1 | 6.10 |
| CHEMBL524869 | COMPLESTATIN B | — | 1 | 5.77 |
| CHEMBL505739 | — | — | 1 | 5.42 |
| CHEMBL448271 | — | — | 1 | 5.11 |
| CHEMBL506051 | — | — | 1 | 4.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL506605 | ISOCOMPLESTATIN | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL525803 | CHLOROPEPTIN | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL448564 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL507121 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL524665 | COMPLESTATINS A | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL524869 | COMPLESTATIN B | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL505739 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL448271 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL506051 | — | IC50 | = | 28000.0 | nM | 4.55 |