Assay Detail
Binding
CHEMBL5053344
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Inhibition of recombinant His-tagged human KIF18A (1 to 467 residues) expressed in baculovirus expression system assessed as inhibition of microtubule-stimulated ATPase activity preincubated for 15 mins followed by ATP addition and further incubated for 15 mins and measured after 40 mins by ADP-Glo reagent based assay
23
Total Activities
23
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
Heteroaryl amides useful as kif18a inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.92 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5070813 | — | — | 1 | 7.89 |
| CHEMBL5075318 | — | — | 1 | 7.82 |
| CHEMBL5075286 | — | — | 1 | 7.57 |
| CHEMBL5084317 | — | — | 1 | 7.51 |
| CHEMBL5080126 | — | — | 1 | 7.32 |
| CHEMBL5088011 | — | — | 1 | 7.26 |
| CHEMBL5086169 | — | — | 1 | 7.15 |
| CHEMBL5094470 | — | — | 1 | 7.10 |
| CHEMBL5092054 | — | — | 1 | 7.06 |
| CHEMBL5086799 | — | — | 1 | 7.04 |
| CHEMBL5081899 | — | — | 1 | 6.98 |
| CHEMBL5075334 | — | — | 1 | 6.91 |
| CHEMBL5080318 | — | — | 1 | 6.76 |
| CHEMBL5073613 | — | — | 1 | 6.69 |
| CHEMBL5079025 | — | — | 1 | 6.66 |
| CHEMBL5092540 | — | — | 1 | 6.64 |
| CHEMBL5079508 | — | — | 1 | 6.58 |
| CHEMBL5076230 | — | — | 1 | 6.57 |
| CHEMBL5087469 | — | — | 1 | 6.45 |
| CHEMBL5078599 | — | — | 1 | 6.41 |
| CHEMBL5078022 | — | — | 1 | 6.40 |
| CHEMBL5082926 | — | — | 1 | 6.34 |
| CHEMBL5074779 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5070813 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5075318 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5075286 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5084317 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5080126 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5088011 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5086169 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL5094470 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5092054 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL5086799 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL5081899 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL5075334 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL5080318 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL5073613 | — | IC50 | = | 206.0 | nM | 6.69 |
| CHEMBL5079025 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL5092540 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5079508 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL5076230 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL5087469 | — | IC50 | = | 355.0 | nM | 6.45 |
| CHEMBL5078599 | — | IC50 | = | 394.0 | nM | 6.41 |
| CHEMBL5078022 | — | IC50 | = | 402.0 | nM | 6.40 |
| CHEMBL5082926 | — | IC50 | = | 453.0 | nM | 6.34 |
| CHEMBL5074779 | — | IC50 | = | 916.0 | nM | 6.04 |