Assay Detail
Binding
CHEMBL4384180
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human TOPK using MBP as substrate after 2 hrs in presence of [gamma-33P]-ATP by filter-binding method
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Lymphokine-activated killer T-cell-originated protein kinase (CHEMBL4896) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis and biological evaluation of novel 1-phenyl phenanthridin-6(5H)-one derivatives as anti-tumor agents targeting TOPK.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 6.90 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4445123 | — | — | 1 | 9.30 |
| CHEMBL4452726 | — | — | 1 | 8.81 |
| CHEMBL4440222 | — | — | 1 | 8.57 |
| CHEMBL4527920 | — | — | 1 | 8.53 |
| CHEMBL4564624 | — | — | 1 | 8.34 |
| CHEMBL4536593 | — | — | 1 | 8.26 |
| CHEMBL4452595 | — | — | 1 | 8.19 |
| CHEMBL4537262 | — | — | 1 | 7.97 |
| CHEMBL4469640 | — | — | 1 | 7.72 |
| CHEMBL4455498 | — | — | 1 | 7.68 |
| CHEMBL3672271 | — | — | 1 | 7.64 |
| CHEMBL4458265 | — | — | 1 | 7.60 |
| CHEMBL4438486 | — | — | 1 | 7.58 |
| CHEMBL4451419 | — | — | 1 | 7.35 |
| CHEMBL4473141 | — | — | 1 | 7.21 |
| CHEMBL4444190 | — | — | 1 | 7.20 |
| CHEMBL4534841 | — | — | 1 | 7.19 |
| CHEMBL4534499 | — | — | 1 | 7.19 |
| CHEMBL4552688 | — | — | 1 | 6.85 |
| CHEMBL4455728 | — | — | 1 | 6.84 |
| CHEMBL4591205 | — | — | 1 | 6.65 |
| CHEMBL4579248 | — | — | 1 | 6.49 |
| CHEMBL4436998 | — | — | 1 | 6.47 |
| CHEMBL3672369 | — | — | 1 | 6.45 |
| CHEMBL4458873 | — | — | 1 | 6.23 |
| CHEMBL4535216 | — | — | 1 | 6.19 |
| CHEMBL4535960 | — | — | 1 | 6.14 |
| CHEMBL4467180 | — | — | 1 | 6.05 |
| CHEMBL4474776 | — | — | 1 | 6.01 |
| CHEMBL4439067 | — | — | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4445123 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4452726 | — | IC50 | = | 1.56 | nM | 8.81 |
| CHEMBL4440222 | — | IC50 | = | 2.71 | nM | 8.57 |
| CHEMBL4527920 | — | IC50 | = | 2.94 | nM | 8.53 |
| CHEMBL4564624 | — | IC50 | = | 4.59 | nM | 8.34 |
| CHEMBL4536593 | — | IC50 | = | 5.44 | nM | 8.26 |
| CHEMBL4452595 | — | IC50 | = | 6.44 | nM | 8.19 |
| CHEMBL4537262 | — | IC50 | = | 10.69 | nM | 7.97 |
| CHEMBL4469640 | — | IC50 | = | 19.06 | nM | 7.72 |
| CHEMBL4455498 | — | IC50 | = | 20.88 | nM | 7.68 |
| CHEMBL3672271 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4458265 | — | IC50 | = | 25.1 | nM | 7.60 |
| CHEMBL4438486 | — | IC50 | = | 26.13 | nM | 7.58 |
| CHEMBL4451419 | — | IC50 | = | 44.89 | nM | 7.35 |
| CHEMBL4473141 | — | IC50 | = | 61.41 | nM | 7.21 |
| CHEMBL4444190 | — | IC50 | = | 63.83 | nM | 7.20 |
| CHEMBL4534841 | — | IC50 | = | 64.46 | nM | 7.19 |
| CHEMBL4534499 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4552688 | — | IC50 | = | 142.5 | nM | 6.85 |
| CHEMBL4455728 | — | IC50 | = | 143.9 | nM | 6.84 |
| CHEMBL4591205 | — | IC50 | = | 223.7 | nM | 6.65 |
| CHEMBL4579248 | — | IC50 | = | 321.3 | nM | 6.49 |
| CHEMBL4436998 | — | IC50 | = | 335.7 | nM | 6.47 |
| CHEMBL3672369 | — | IC50 | = | 353.7 | nM | 6.45 |
| CHEMBL4458873 | — | IC50 | = | 586.1 | nM | 6.23 |
| CHEMBL4535216 | — | IC50 | = | 642.9 | nM | 6.19 |
| CHEMBL4535960 | — | IC50 | = | 721.4 | nM | 6.14 |
| CHEMBL4467180 | — | IC50 | = | 894.3 | nM | 6.05 |
| CHEMBL4474776 | — | IC50 | = | 977.5 | nM | 6.01 |
| CHEMBL4439067 | — | IC50 | = | 1266.0 | nM | 5.90 |
| CHEMBL4537653 | — | IC50 | = | 1505.0 | nM | 5.82 |
| CHEMBL4588267 | — | IC50 | = | 2440.0 | nM | 5.61 |
| CHEMBL4555026 | — | IC50 | = | 2663.0 | nM | 5.58 |
| CHEMBL4442377 | — | IC50 | = | 3013.0 | nM | 5.52 |
| CHEMBL4562809 | — | IC50 | = | 4790.0 | nM | 5.32 |
| CHEMBL4528387 | — | IC50 | = | 5238.0 | nM | 5.28 |
| CHEMBL4573944 | — | IC50 | = | 6415.0 | nM | 5.19 |
| CHEMBL4585042 | — | IC50 | = | 7055.0 | nM | 5.15 |
| CHEMBL4519328 | — | IC50 | - | — | - | |
| CHEMBL4458314 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4469535 | — | IC50 | - | — | - | |
| CHEMBL4517435 | — | IC50 | - | — | - | |
| CHEMBL4551832 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4439624 | — | IC50 | - | — | - |