Assay Detail
Binding
CHEMBL4819715
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to wild-type human partial length TTK (N505 to V798 residues) expressed in bacterial expression system by active site-directed competition binding based Kinomescan method
30
Total Activities
30
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
Pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable Threonine Tyrosine Kinase (TTK) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 30 | 8.60 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4877547 | — | — | 1 | 10.15 |
| CHEMBL4845775 | — | — | 1 | 9.92 |
| CHEMBL4875028 | — | — | 1 | 9.82 |
| CHEMBL4858486 | — | — | 1 | 9.77 |
| CHEMBL4870223 | — | — | 1 | 9.77 |
| CHEMBL4846040 | — | — | 1 | 9.70 |
| CHEMBL4869527 | — | — | 1 | 9.54 |
| CHEMBL4868353 | — | — | 1 | 9.52 |
| CHEMBL4860430 | — | — | 1 | 9.39 |
| CHEMBL4866294 | — | — | 1 | 9.39 |
| CHEMBL4867504 | — | — | 1 | 9.30 |
| CHEMBL4873395 | — | — | 1 | 9.25 |
| CHEMBL4869142 | — | — | 1 | 9.20 |
| CHEMBL4857210 | — | — | 1 | 9.15 |
| CHEMBL4861308 | — | — | 1 | 9.14 |
| CHEMBL4859914 | — | — | 1 | 8.96 |
| CHEMBL4874692 | — | — | 1 | 8.82 |
| CHEMBL4850608 | — | — | 1 | 8.55 |
| CHEMBL4863607 | — | — | 1 | 8.41 |
| CHEMBL4853778 | — | — | 1 | 8.38 |
| CHEMBL4870731 | — | — | 1 | 8.21 |
| CHEMBL4853433 | — | — | 1 | 8.10 |
| CHEMBL4859127 | — | — | 1 | 8.03 |
| CHEMBL4853927 | — | — | 1 | 6.84 |
| CHEMBL4093766 | — | — | 1 | 6.72 |
| CHEMBL4849289 | — | — | 1 | 6.70 |
| CHEMBL4855669 | — | — | 1 | 6.60 |
| CHEMBL4862196 | — | — | 1 | 6.08 |
| CHEMBL4856340 | — | — | 1 | 6.00 |
| CHEMBL4860644 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4877547 | — | Kd | = | 0.071 | nM | 10.15 |
| CHEMBL4845775 | — | Kd | = | 0.12 | nM | 9.92 |
| CHEMBL4875028 | — | Kd | = | 0.15 | nM | 9.82 |
| CHEMBL4858486 | — | Kd | = | 0.17 | nM | 9.77 |
| CHEMBL4870223 | — | Kd | = | 0.17 | nM | 9.77 |
| CHEMBL4846040 | — | Kd | = | 0.2 | nM | 9.70 |
| CHEMBL4869527 | — | Kd | = | 0.29 | nM | 9.54 |
| CHEMBL4868353 | — | Kd | = | 0.3 | nM | 9.52 |
| CHEMBL4860430 | — | Kd | = | 0.41 | nM | 9.39 |
| CHEMBL4866294 | — | Kd | = | 0.41 | nM | 9.39 |
| CHEMBL4867504 | — | Kd | = | 0.5 | nM | 9.30 |
| CHEMBL4873395 | — | Kd | = | 0.56 | nM | 9.25 |
| CHEMBL4869142 | — | Kd | = | 0.63 | nM | 9.20 |
| CHEMBL4857210 | — | Kd | = | 0.71 | nM | 9.15 |
| CHEMBL4861308 | — | Kd | = | 0.72 | nM | 9.14 |
| CHEMBL4859914 | — | Kd | = | 1.1 | nM | 8.96 |
| CHEMBL4874692 | — | Kd | = | 1.5 | nM | 8.82 |
| CHEMBL4850608 | — | Kd | = | 2.8 | nM | 8.55 |
| CHEMBL4863607 | — | Kd | = | 3.9 | nM | 8.41 |
| CHEMBL4853778 | — | Kd | = | 4.2 | nM | 8.38 |
| CHEMBL4870731 | — | Kd | = | 6.1 | nM | 8.21 |
| CHEMBL4853433 | — | Kd | = | 7.9 | nM | 8.10 |
| CHEMBL4859127 | — | Kd | = | 9.3 | nM | 8.03 |
| CHEMBL4853927 | — | Kd | = | 145.0 | nM | 6.84 |
| CHEMBL4093766 | — | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL4849289 | — | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL4855669 | — | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL4862196 | — | Kd | = | 825.0 | nM | 6.08 |
| CHEMBL4856340 | — | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL4860644 | — | Kd | > | 310.0 | nM | - |