Assay Detail
Binding
CHEMBL4620769
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged recombinant human MPS1 expressed in baculovirus expression system using biotin-Ahx-PWDPDDADITEILG as substrate preincubated for 15 mins followed by substrate and 10 uM ATP addition and measured after 60 mins by TR-FRET assay
59
Total Activities
59
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
Treating Cancer by Spindle Assembly Checkpoint Abrogation: Discovery of Two Clinical Candidates, BAY 1161909 and BAY 1217389, Targeting MPS1 Kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 59 | 7.67 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4642174 | — | — | 1 | 9.70 |
| CHEMBL4645348 | — | — | 1 | 9.30 |
| CHEMBL4632416 | — | — | 1 | 9.30 |
| CHEMBL4634949 | — | — | 1 | 9.30 |
| CHEMBL4469414 | LUVIXASERTIB | 2.0 | 1 | 9.22 |
| CHEMBL4634997 | — | — | 1 | 9.22 |
| CHEMBL4456085 | BAY-1217389 | 1.0 | 1 | 9.15 |
| CHEMBL4640247 | — | — | 1 | 9.00 |
| CHEMBL4637496 | — | — | 1 | 8.70 |
| CHEMBL4649817 | — | — | 1 | 8.70 |
| CHEMBL4635532 | — | — | 1 | 8.52 |
| CHEMBL4649445 | — | — | 1 | 8.52 |
| CHEMBL4633081 | — | — | 1 | 8.41 |
| CHEMBL3908648 | — | — | 1 | 8.40 |
| CHEMBL4634241 | — | — | 1 | 8.34 |
| CHEMBL4647298 | — | — | 1 | 8.30 |
| CHEMBL3940165 | — | — | 1 | 8.30 |
| CHEMBL4643612 | — | — | 1 | 8.30 |
| CHEMBL4644831 | — | — | 1 | 8.20 |
| CHEMBL4646296 | — | — | 1 | 8.15 |
| CHEMBL4649409 | — | — | 1 | 8.15 |
| CHEMBL4632548 | — | — | 1 | 8.10 |
| CHEMBL4646621 | — | — | 1 | 8.00 |
| CHEMBL3410060 | — | — | 1 | 8.00 |
| CHEMBL4639541 | — | — | 1 | 7.96 |
| CHEMBL4646380 | — | — | 1 | 7.96 |
| CHEMBL4637247 | — | — | 1 | 7.89 |
| CHEMBL4643900 | — | — | 1 | 7.89 |
| CHEMBL4646785 | — | — | 1 | 7.85 |
| CHEMBL3410069 | — | — | 1 | 7.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4642174 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4645348 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4634949 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4632416 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4469414 | LUVIXASERTIB | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4634997 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4456085 | BAY-1217389 | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4640247 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4637496 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4649817 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4635532 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4649445 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4633081 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3908648 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4634241 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4647298 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4643612 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3940165 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4644831 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL4646296 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4649409 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4632548 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4646621 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3410060 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4646380 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4639541 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4637247 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4643900 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4646785 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3410069 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4635026 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4644042 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3974070 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3410066 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4643569 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4632931 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4633800 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3410065 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4649394 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4638361 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4633990 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4642796 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4634064 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4632986 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4639860 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4641956 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4639842 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4646574 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4647665 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4640897 | — | IC50 | = | 684.0 | nM | 6.17 |