Assay Detail
Binding
CHEMBL5380374
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Binding affinity to ALK L1196M mutant (unknown origin) assessed as inhibition constant
7
Total Activities
7
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
Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 8.42 | 9.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3286820 | — | — | 1 | 9.54 |
| CHEMBL5438242 | — | — | 1 | 9.21 |
| CHEMBL3286830 | LORLATINIB | 4.0 | 1 | 9.15 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 8.09 |
| CHEMBL3286812 | — | — | 1 | 8.09 |
| CHEMBL3286809 | — | — | 1 | 7.46 |
| CHEMBL3286808 | — | — | 1 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3286820 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL5438242 | — | Ki | = | 0.62 | nM | 9.21 |
| CHEMBL3286830 | LORLATINIB | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL601719 | CRIZOTINIB | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL3286812 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL3286809 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL3286808 | — | Ki | = | 38.0 | nM | 7.42 |