Assay Detail
Binding
CHEMBL2024744
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal hexa-histidine tagged human cloned Eg5 (1 to 368 amino acids) expressed in Escherichia coli BL21 (DE3) assessed as reduction of MT-stimulated ATPase activity by pyruvate kinase/lactate dehydrogenase-linked assay
19
Total Activities
19
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
Triphenylbutanamines: kinesin spindle protein inhibitors with in vivo antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.65 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL228814 | ISPINESIB | 2.0 | 1 | 8.60 |
| CHEMBL2023001 | — | — | 1 | 8.47 |
| CHEMBL261613 | — | — | 1 | 8.38 |
| CHEMBL2022994 | — | — | 1 | 8.29 |
| CHEMBL392369 | — | — | 1 | 8.04 |
| CHEMBL2022999 | — | — | 1 | 8.01 |
| CHEMBL2023002 | — | — | 1 | 8.01 |
| CHEMBL2022996 | — | — | 1 | 7.99 |
| CHEMBL2022998 | — | — | 1 | 7.97 |
| CHEMBL2022997 | — | — | 1 | 7.97 |
| CHEMBL2022995 | — | — | 1 | 7.89 |
| CHEMBL429597 | — | — | 1 | 7.87 |
| CHEMBL2023000 | — | — | 1 | 7.71 |
| CHEMBL392695 | S-TRITYL-L-CYSTEINE | — | 1 | 6.84 |
| CHEMBL408072 | — | — | 1 | 6.82 |
| CHEMBL2022591 | — | — | 1 | 6.69 |
| CHEMBL2022590 | — | — | 1 | 6.67 |
| CHEMBL2022588 | — | — | 1 | 6.63 |
| CHEMBL2022589 | — | — | 1 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL228814 | ISPINESIB | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL2023001 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL261613 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL2022994 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL392369 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL2022999 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL2023002 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL2022996 | — | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL2022998 | — | Ki | = | 10.7 | nM | 7.97 |
| CHEMBL2022997 | — | Ki | = | 10.8 | nM | 7.97 |
| CHEMBL2022995 | — | Ki | = | 12.8 | nM | 7.89 |
| CHEMBL429597 | — | Ki | = | 13.6 | nM | 7.87 |
| CHEMBL2023000 | — | Ki | = | 19.3 | nM | 7.71 |
| CHEMBL392695 | S-TRITYL-L-CYSTEINE | Ki | = | 143.8 | nM | 6.84 |
| CHEMBL408072 | — | Ki | = | 152.3 | nM | 6.82 |
| CHEMBL2022591 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL2022590 | — | Ki | = | 211.3 | nM | 6.67 |
| CHEMBL2022588 | — | Ki | = | 235.4 | nM | 6.63 |
| CHEMBL2022589 | — | Ki | = | 384.4 | nM | 6.42 |