Assay Detail
Binding
CHEMBL4177855
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Inhibition of hepatitis B virus capsid assembly infected in human HepG2.215 cells assessed as reduction in viral DNA replication measured on day 7 by real time PCR analysis
55
Total Activities
52
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Hepatitis B virus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Discovery of hepatitis B virus capsid assembly inhibitors leading to a heteroaryldihydropyrimidine based clinical candidate (GLS4).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 52 | 7.02 | 9.62 |
| EC90 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5314362 | ENTECAVIR | 4.0 | 1 | 9.62 |
| CHEMBL3742114 | — | — | 2 | 9.00 |
| CHEMBL4078766 | — | — | 1 | 8.52 |
| CHEMBL4076401 | — | — | 1 | 8.30 |
| CHEMBL4211812 | — | — | 1 | 8.22 |
| CHEMBL4210470 | — | — | 1 | 8.00 |
| CHEMBL4062770 | — | — | 1 | 7.80 |
| CHEMBL4079561 | — | — | 1 | 7.70 |
| CHEMBL4205737 | — | — | 1 | 7.58 |
| CHEMBL4075908 | — | — | 1 | 7.46 |
| CHEMBL4070728 | — | — | 1 | 7.38 |
| CHEMBL605300 | — | — | 2 | 7.32 |
| CHEMBL4077161 | — | — | 1 | 7.16 |
| CHEMBL4206627 | — | — | 1 | 7.13 |
| CHEMBL4216331 | — | — | 1 | 7.10 |
| CHEMBL484 | ADEFOVIR | 3.0 | 1 | 7.08 |
| CHEMBL4103602 | — | — | 1 | 7.00 |
| CHEMBL4209011 | — | — | 1 | 7.00 |
| CHEMBL3121560 | — | — | 2 | 7.00 |
| CHEMBL4214974 | — | — | 1 | 6.82 |
| CHEMBL4217281 | — | — | 1 | 6.70 |
| CHEMBL483 | TENOFOVIR ANHYDROUS | 3.0 | 1 | 6.62 |
| CHEMBL4208714 | — | — | 1 | 6.60 |
| CHEMBL4204130 | — | — | 1 | 6.60 |
| CHEMBL4064808 | — | — | 1 | 6.30 |
| CHEMBL4203418 | — | — | 1 | 6.10 |
| CHEMBL374731 | TELBIVUDINE | 4.0 | 1 | 6.09 |
| CHEMBL4212848 | — | — | 1 | 6.05 |
| CHEMBL4215086 | — | — | 1 | 5.92 |
| CHEMBL4092509 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5314362 | ENTECAVIR | EC50 | = | 0.24 | nM | 9.62 |
| CHEMBL3742114 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4078766 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4076401 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4211812 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4210470 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4062770 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4079561 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4205737 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4075908 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4070728 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL605300 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4077161 | — | EC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4206627 | — | EC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4216331 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL484 | ADEFOVIR | EC50 | = | 82.7 | nM | 7.08 |
| CHEMBL4103602 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4209011 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3121560 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4214974 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4217281 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL483 | TENOFOVIR ANHYDROUS | EC50 | = | 241.5 | nM | 6.62 |
| CHEMBL4208714 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4204130 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4064808 | — | EC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4203418 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL374731 | TELBIVUDINE | EC50 | = | 819.4 | nM | 6.09 |
| CHEMBL4212848 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4215086 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4092509 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4208472 | — | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4205239 | — | EC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4205574 | — | EC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL3742114 | — | EC90 | = | 6.0 | nM | - |
| CHEMBL4214335 | — | EC50 | > | 16400.0 | nM | - |
| CHEMBL4202676 | — | EC50 | > | 16400.0 | nM | - |
| CHEMBL605300 | — | EC90 | = | 102.0 | nM | - |
| CHEMBL4218589 | — | EC50 | > | 16400.0 | nM | - |
| CHEMBL4205837 | — | EC50 | > | 16400.0 | nM | - |
| CHEMBL4099050 | — | EC50 | > | 16400.0 | nM | - |
| CHEMBL4208895 | — | EC50 | > | 16400.0 | nM | - |
| CHEMBL4211206 | — | EC50 | > | 16400.0 | nM | - |
| CHEMBL4202690 | — | EC50 | > | 16400.0 | nM | - |
| CHEMBL4087266 | — | EC50 | > | 16400.0 | nM | - |
| CHEMBL4212364 | — | EC50 | > | 16400.0 | nM | - |
| CHEMBL3121560 | — | EC90 | = | 300.0 | nM | - |
| CHEMBL4205500 | — | EC50 | > | 16400.0 | nM | - |
| CHEMBL4205160 | — | EC50 | > | 16400.0 | nM | - |
| CHEMBL4210656 | — | EC50 | > | 16400.0 | nM | - |
| CHEMBL4216143 | — | EC50 | > | 16400.0 | nM | - |