Assay Detail
Binding
CHEMBL4223423
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to CA-SP1 P373S mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells assessed as inhibition of viral maturation by measuring virus yields after 4 to 5 days in presence of 10% FBS/15 mg/ml HSA by luciferase reporter gene assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Human immunodeficiency virus 1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Gag-Pol polyprotein (CHEMBL3638360) ↗| Type | SINGLE PROTEIN |
| Organism | Human immunodeficiency virus type 1 group M subtype B (isolate HXB2)(HIV-1) |
Publication
The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 7.76 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3828596 | — | — | 1 | 8.70 |
| CHEMBL3827026 | — | — | 1 | 8.70 |
| CHEMBL4227119 | — | — | 1 | 8.49 |
| CHEMBL4226018 | — | — | 1 | 8.42 |
| CHEMBL4225279 | — | — | 1 | 8.38 |
| CHEMBL4227326 | — | — | 1 | 8.10 |
| CHEMBL4225614 | — | — | 1 | 8.09 |
| CHEMBL3827839 | — | — | 1 | 8.06 |
| CHEMBL3787468 | — | — | 1 | 7.96 |
| CHEMBL4225865 | — | — | 1 | 7.68 |
| CHEMBL4229111 | — | — | 1 | 7.64 |
| CHEMBL4225093 | — | — | 1 | 7.58 |
| CHEMBL3775172 | — | — | 1 | 6.82 |
| CHEMBL4228038 | — | — | 1 | 6.80 |
| CHEMBL4224822 | — | — | 1 | 6.68 |
| CHEMBL404519 | BEVIRIMAT | 2.0 | 1 | 6.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3828596 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3827026 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4227119 | — | EC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4226018 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4225279 | — | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4227326 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4225614 | — | EC50 | = | 8.2 | nM | 8.09 |
| CHEMBL3827839 | — | EC50 | = | 8.7 | nM | 8.06 |
| CHEMBL3787468 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4225865 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4229111 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4225093 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3775172 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4228038 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4224822 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL404519 | BEVIRIMAT | EC50 | = | 970.0 | nM | 6.01 |