Assay Detail
Binding
CHEMBL5053357
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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
174
Total Activities
172
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
Pyridine derivatives as kif18a inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 174 | 6.76 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5085003 | — | — | 1 | 7.55 |
| CHEMBL5070081 | — | — | 1 | 7.48 |
| CHEMBL5089377 | — | — | 1 | 7.44 |
| CHEMBL5081958 | — | — | 1 | 7.42 |
| CHEMBL5081138 | — | — | 1 | 7.41 |
| CHEMBL5069662 | — | — | 1 | 7.41 |
| CHEMBL5094366 | — | — | 1 | 7.41 |
| CHEMBL5075099 | — | — | 1 | 7.40 |
| CHEMBL5070961 | — | — | 1 | 7.39 |
| CHEMBL5080025 | — | — | 1 | 7.38 |
| CHEMBL5082827 | — | — | 1 | 7.38 |
| CHEMBL5087600 | — | — | 1 | 7.38 |
| CHEMBL5082574 | — | — | 1 | 7.38 |
| CHEMBL5088847 | — | — | 1 | 7.37 |
| CHEMBL5074431 | — | — | 1 | 7.33 |
| CHEMBL5094013 | — | — | 1 | 7.33 |
| CHEMBL5077534 | — | — | 1 | 7.32 |
| CHEMBL5069883 | — | — | 1 | 7.29 |
| CHEMBL5073385 | — | — | 1 | 7.28 |
| CHEMBL5079474 | — | — | 1 | 7.28 |
| CHEMBL5083376 | — | — | 1 | 7.27 |
| CHEMBL5088406 | — | — | 1 | 7.27 |
| CHEMBL5094867 | — | — | 1 | 7.26 |
| CHEMBL5090438 | — | — | 1 | 7.26 |
| CHEMBL5087701 | — | — | 1 | 7.25 |
| CHEMBL5084958 | — | — | 1 | 7.25 |
| CHEMBL5077269 | — | — | 1 | 7.24 |
| CHEMBL5077439 | — | — | 1 | 7.24 |
| CHEMBL5087207 | — | — | 1 | 7.22 |
| CHEMBL5074801 | — | — | 1 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5085003 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5070081 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5089377 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5081958 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5094366 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5069662 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5081138 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5075099 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5070961 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5082574 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5087600 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5082827 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5080025 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5088847 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5074431 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5094013 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5077534 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5069883 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL5073385 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5079474 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5088406 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5083376 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5090438 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5094867 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5087701 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5084958 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5077439 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5077269 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5087207 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5074801 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL5084915 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL5082844 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL5082280 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5091294 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5079699 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5080641 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5076819 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL5092875 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL5075796 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL5090073 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5087537 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5089118 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5083345 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5083731 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL5075568 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL5084915 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL5079211 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5078310 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5070127 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL5090269 | — | IC50 | = | 94.0 | nM | 7.03 |