Assay Detail
Functional
CHEMBL4404616
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiviral activity against HIV1 NL4-3 infected in human MT2 cells measured after 3 to 4 days by luciferase reporter gene assay
35
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Human immunodeficiency virus 1 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Target
Human immunodeficiency virus 1 (CHEMBL378) ↗| Type | ORGANISM |
| Organism | Human immunodeficiency virus 1 |
Publication
Discovery and Optimization of Novel Pyrazolopyrimidines as Potent and Orally Bioavailable Allosteric HIV-1 Integrase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 35 | 6.87 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL254316 | RALTEGRAVIR | 4.0 | 1 | 8.70 |
| CHEMBL4465908 | — | — | 1 | 8.52 |
| CHEMBL4560621 | — | — | 1 | 8.52 |
| CHEMBL4468197 | — | — | 1 | 8.30 |
| CHEMBL4471769 | — | — | 1 | 8.22 |
| CHEMBL4515083 | — | — | 1 | 8.22 |
| CHEMBL4449609 | — | — | 1 | 8.22 |
| CHEMBL4561867 | — | — | 1 | 7.82 |
| CHEMBL4513683 | — | — | 1 | 7.70 |
| CHEMBL3259907 | BI-224436 | 1.0 | 1 | 7.30 |
| CHEMBL4547406 | — | — | 1 | 7.22 |
| CHEMBL4450457 | — | — | 1 | 7.22 |
| CHEMBL4457298 | — | — | 1 | 7.22 |
| CHEMBL4454900 | — | — | 1 | 7.00 |
| CHEMBL4454255 | — | — | 1 | 6.96 |
| CHEMBL4448904 | — | — | 1 | 6.89 |
| CHEMBL4573064 | — | — | 2 | 6.68 |
| CHEMBL4476366 | — | — | 1 | 6.31 |
| CHEMBL4460705 | — | — | 1 | 6.26 |
| CHEMBL4461955 | — | — | 1 | 6.21 |
| CHEMBL4565963 | — | — | 1 | 5.77 |
| CHEMBL4538853 | — | — | 1 | 5.64 |
| CHEMBL4469948 | — | — | 1 | 5.35 |
| CHEMBL4439901 | — | — | 1 | 4.89 |
| CHEMBL4560817 | — | — | 1 | 4.80 |
| CHEMBL4592862 | — | — | 1 | 4.75 |
| CHEMBL4541973 | — | — | 1 | 4.68 |
| CHEMBL4440179 | — | — | 1 | - |
| CHEMBL4592796 | — | — | 1 | - |
| CHEMBL4551451 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL254316 | RALTEGRAVIR | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4465908 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4560621 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4468197 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4471769 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4515083 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4449609 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4561867 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4513683 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3259907 | BI-224436 | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4547406 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4450457 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4457298 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4454900 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4454255 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4448904 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4573064 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4476366 | — | EC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4460705 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4461955 | — | EC50 | = | 620.0 | nM | 6.21 |
| CHEMBL4565963 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4538853 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4469948 | — | EC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4439901 | — | EC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4560817 | — | EC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL4592862 | — | EC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL4541973 | — | EC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL4440179 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4573064 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4551451 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4592796 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4587557 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4532093 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4452801 | — | EC50 | > | 40000.0 | nM | - |
| CHEMBL4475105 | — | EC50 | > | 40000.0 | nM | - |