Assay Detail
Functional
CHEMBL5049323
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiviral activity against recombinant HIV1 NLRep-Rluc harbouring polymorphic T124/T125 integrase infected in human MT-2 cells assessed as inhibition of virus growth in presence of fetal bovine serum by measuring luciferase activity after 5 days
35
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Human immunodeficiency virus 1 |
| Cell Type | MT2 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Target
Human immunodeficiency virus 1 (CHEMBL378) ↗| Type | ORGANISM |
| Organism | Human immunodeficiency virus 1 |
Publication
Design, Synthesis, and Preclinical Profiling of GSK3739936 (BMS-986180), an Allosteric Inhibitor of HIV-1 Integrase with Broad-Spectrum Activity toward 124/125 Polymorphs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 35 | 8.29 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5089130 | — | — | 2 | 9.22 |
| CHEMBL5080445 | — | — | 1 | 9.22 |
| CHEMBL5074148 | — | — | 1 | 9.10 |
| CHEMBL5087287 | — | — | 1 | 9.05 |
| CHEMBL5089101 | — | — | 1 | 8.96 |
| CHEMBL5094894 | — | — | 1 | 8.89 |
| CHEMBL5078859 | — | — | 1 | 8.82 |
| CHEMBL5077187 | — | — | 1 | 8.82 |
| CHEMBL5084420 | — | — | 1 | 8.77 |
| CHEMBL5093378 | — | — | 1 | 8.77 |
| CHEMBL5091879 | — | — | 1 | 8.64 |
| CHEMBL5084138 | — | — | 1 | 8.57 |
| CHEMBL5093292 | — | — | 1 | 8.55 |
| CHEMBL5088057 | — | — | 1 | 8.48 |
| CHEMBL5077625 | — | — | 1 | 8.44 |
| CHEMBL5076276 | — | — | 1 | 8.41 |
| CHEMBL5087982 | — | — | 1 | 8.36 |
| CHEMBL5087777 | — | — | 1 | 8.32 |
| CHEMBL5079235 | — | — | 2 | 8.30 |
| CHEMBL5087827 | — | — | 1 | 8.30 |
| CHEMBL5077943 | — | — | 1 | 8.27 |
| CHEMBL5092389 | — | — | 1 | 7.95 |
| CHEMBL5085847 | — | — | 1 | 7.92 |
| CHEMBL5080580 | — | — | 1 | 7.92 |
| CHEMBL5070004 | — | — | 1 | 7.91 |
| CHEMBL5077638 | — | — | 1 | 7.83 |
| CHEMBL5080087 | — | — | 1 | 7.81 |
| CHEMBL5092167 | — | — | 1 | 7.65 |
| CHEMBL5090529 | — | — | 1 | 7.51 |
| CHEMBL5080240 | — | — | 1 | 7.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5080445 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5089130 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5074148 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5087287 | — | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5089101 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5094894 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5078859 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5077187 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5084420 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5093378 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5089130 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5091879 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5084138 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5093292 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5088057 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5077625 | — | EC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5076276 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5087982 | — | EC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5087777 | — | EC50 | = | 4.8 | nM | 8.32 |
| CHEMBL5087827 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5079235 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5077943 | — | EC50 | = | 5.4 | nM | 8.27 |
| CHEMBL5092389 | — | EC50 | = | 11.3 | nM | 7.95 |
| CHEMBL5085847 | — | EC50 | = | 11.9 | nM | 7.92 |
| CHEMBL5079235 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5080580 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5070004 | — | EC50 | = | 12.2 | nM | 7.91 |
| CHEMBL5077638 | — | EC50 | = | 14.7 | nM | 7.83 |
| CHEMBL5080087 | — | EC50 | = | 15.6 | nM | 7.81 |
| CHEMBL5092167 | — | EC50 | = | 22.6 | nM | 7.65 |
| CHEMBL5090529 | — | EC50 | = | 31.2 | nM | 7.51 |
| CHEMBL5080240 | — | EC50 | = | 37.5 | nM | 7.43 |
| CHEMBL3259907 | BI-224436 | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5080247 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5081928 | — | EC50 | = | 190.0 | nM | 6.72 |