Assay Detail
Binding
CHEMBL4338928
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse derived homozygous Tg0N4R P301S mutant tau-induced human ON4R tau aggregation harboring P301S mutant transfected in HEK293 cells preincubated for 2 hrs followed by compound addition and measured after 3 hrs by YFP-based fluorescence assay
33
Total Activities
29
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of 4-Piperazine Isoquinoline Derivatives as Potent and Brain-Permeable Tau Prion Inhibitors with CDK8 Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 29 | 6.72 | 8.30 |
| fEC50 | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4455382 | — | — | 2 | 8.30 |
| CHEMBL3828637 | — | — | 1 | 8.05 |
| CHEMBL4584784 | — | — | 2 | 7.82 |
| CHEMBL4468770 | — | — | 1 | 7.66 |
| CHEMBL4464358 | — | — | 1 | 7.46 |
| CHEMBL4473725 | — | — | 1 | 7.01 |
| CHEMBL4461214 | — | — | 1 | 6.92 |
| CHEMBL4476483 | — | — | 1 | 6.92 |
| CHEMBL4456001 | — | — | 2 | 6.92 |
| CHEMBL4444098 | — | — | 1 | 6.77 |
| CHEMBL4447689 | — | — | 2 | 6.55 |
| CHEMBL4516717 | — | — | 1 | 6.48 |
| CHEMBL4469418 | — | — | 1 | 6.41 |
| CHEMBL4442184 | — | — | 1 | 6.40 |
| CHEMBL4457953 | — | — | 1 | 6.28 |
| CHEMBL4585943 | — | — | 1 | 6.23 |
| CHEMBL4522858 | — | — | 1 | 6.17 |
| CHEMBL4593541 | — | — | 1 | 6.04 |
| CHEMBL4524428 | — | — | 1 | 5.96 |
| CHEMBL4540965 | — | — | 1 | 5.85 |
| CHEMBL4529149 | — | — | 1 | 5.00 |
| CHEMBL4573130 | — | — | 1 | - |
| CHEMBL4559139 | — | — | 1 | - |
| CHEMBL4462872 | — | — | 1 | - |
| CHEMBL4459909 | — | — | 1 | - |
| CHEMBL4557204 | — | — | 1 | - |
| CHEMBL4584145 | — | — | 1 | - |
| CHEMBL4453515 | — | — | 1 | - |
| CHEMBL4444596 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4455382 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3828637 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4584784 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4468770 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4464358 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4473725 | — | EC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4461214 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4456001 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4476483 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4444098 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4447689 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4516717 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4469418 | — | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4442184 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4457953 | — | EC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4585943 | — | EC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4522858 | — | EC50 | = | 680.0 | nM | 6.17 |
| CHEMBL4593541 | — | EC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4524428 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4540965 | — | EC50 | = | 1420.0 | nM | 5.85 |
| CHEMBL4529149 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4573130 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4559139 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4462872 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4459909 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4456001 | — | fEC50 | = | 30.0 | nM | - |
| CHEMBL4447689 | — | fEC50 | = | 210.0 | nM | - |
| CHEMBL4557204 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4584784 | — | fEC50 | = | 5.0 | nM | - |
| CHEMBL4584145 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4453515 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4455382 | — | fEC50 | = | 2.0 | nM | - |
| CHEMBL4444596 | — | EC50 | > | 10000.0 | nM | - |