Assay Detail
Binding
CHEMBL2328844
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of telomerase-mediated supercoiling activity in human MGC803 cells after 24 hrs by TRAP-PCR-ELISA assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MGC-803 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of novel 2-methyl-4,5-substitutedbenzo[f]-3,3a,4,5-tetrahydro-pyrazolo[1,5-d][1,4]oxazepin-8(7H)-one derivatives as telomerase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.37 | 6.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2323142 | — | — | 1 | 6.11 |
| CHEMBL2323143 | — | — | 1 | 5.77 |
| CHEMBL2323147 | — | — | 1 | 5.68 |
| CHEMBL284328 | HOMIDIUM BROMIDE | 2.0 | 1 | 5.62 |
| CHEMBL2321890 | — | — | 1 | 5.50 |
| CHEMBL2323145 | — | — | 1 | 5.18 |
| CHEMBL2323144 | — | — | 1 | 4.97 |
| CHEMBL2323141 | — | — | 1 | 4.83 |
| CHEMBL2323146 | — | — | 1 | 4.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2323142 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL2323143 | — | IC50 | = | 1710.0 | nM | 5.77 |
| CHEMBL2323147 | — | IC50 | = | 2110.0 | nM | 5.68 |
| CHEMBL284328 | HOMIDIUM BROMIDE | IC50 | = | 2390.0 | nM | 5.62 |
| CHEMBL2321890 | — | IC50 | = | 3140.0 | nM | 5.50 |
| CHEMBL2323145 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL2323144 | — | IC50 | = | 10820.0 | nM | 4.97 |
| CHEMBL2323141 | — | IC50 | = | 14800.0 | nM | 4.83 |
| CHEMBL2323146 | — | IC50 | = | 21900.0 | nM | 4.66 |