Assay Detail
Binding
CHEMBL3380550
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human His-tagged full length AURKA using kemptide peptide as substrate after 60 mins
27
Total Activities
22
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 |
Publication
Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 6.42 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3263053 | — | — | 1 | 7.82 |
| CHEMBL3298373 | — | — | 1 | 7.72 |
| CHEMBL3298369 | — | — | 2 | 7.27 |
| CHEMBL3263036 | — | — | 1 | 7.14 |
| CHEMBL3298372 | — | — | 1 | 6.77 |
| CHEMBL3298291 | — | — | 1 | 6.75 |
| CHEMBL3298293 | — | — | 2 | 6.70 |
| CHEMBL3298286 | — | — | 2 | 6.68 |
| CHEMBL3298370 | — | — | 1 | 6.68 |
| CHEMBL3298376 | — | — | 1 | 6.54 |
| CHEMBL3298371 | — | — | 1 | 6.34 |
| CHEMBL3298288 | — | — | 1 | 6.32 |
| CHEMBL3298375 | — | — | 1 | 6.30 |
| CHEMBL3298287 | — | — | 2 | 6.28 |
| CHEMBL3298285 | — | — | 1 | 6.11 |
| CHEMBL3262780 | — | — | 1 | 6.06 |
| CHEMBL3298368 | — | — | 2 | 6.06 |
| CHEMBL3298290 | — | — | 1 | 6.02 |
| CHEMBL3298289 | — | — | 1 | 5.77 |
| CHEMBL3298374 | — | — | 1 | 5.68 |
| CHEMBL3298366 | — | — | 1 | 5.54 |
| CHEMBL3298367 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3263053 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3298373 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL3298369 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL3263036 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL3298372 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL3298291 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL3298293 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL3298286 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL3298370 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL3298286 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL3298376 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL3298369 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL3298371 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL3298288 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL3298375 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL3298287 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL3298285 | — | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL3262780 | — | Ki | = | 870.0 | nM | 6.06 |
| CHEMBL3298368 | — | Ki | = | 870.0 | nM | 6.06 |
| CHEMBL3298290 | — | Ki | = | 950.0 | nM | 6.02 |
| CHEMBL3298287 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL3298289 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL3298368 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL3298374 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL3298293 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL3298366 | — | Ki | = | 2900.0 | nM | 5.54 |
| CHEMBL3298367 | — | Ki | > | 5700.0 | nM | - |