Assay Detail
Binding
CHEMBL4200739
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Inhibition of ABL1 (64 to 515 residues)(unknown origin) expressed in Escherichia coli using FITC-Ahx-EAIYAAPFAKKK-NH2 peptide as substrate after 60 mins by caliper assay
20
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.34 | 9.40 |
| Inhibition | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4106732 | — | — | 1 | 9.40 |
| CHEMBL4208229 | ASCIMINIB | 4.0 | 1 | 9.30 |
| CHEMBL3898258 | — | — | 1 | 9.30 |
| CHEMBL4213152 | — | — | 1 | 9.15 |
| CHEMBL4217559 | — | — | 1 | 8.96 |
| CHEMBL4114922 | — | — | 1 | 8.80 |
| CHEMBL3954214 | — | — | 1 | 8.64 |
| CHEMBL4115154 | — | — | 1 | 8.40 |
| CHEMBL3910823 | — | — | 1 | 8.15 |
| CHEMBL3915183 | — | — | 1 | 7.96 |
| CHEMBL3956542 | — | — | 1 | 7.75 |
| CHEMBL3892952 | — | — | 1 | 7.75 |
| CHEMBL3908521 | — | — | 1 | 7.72 |
| CHEMBL3913939 | — | — | 1 | 7.62 |
| CHEMBL4217428 | — | — | 1 | 6.26 |
| CHEMBL4210089 | — | — | 1 | - |
| CHEMBL1234477 | — | — | 1 | - |
| CHEMBL4110570 | — | — | 1 | - |
| CHEMBL4205194 | — | — | 1 | - |
| CHEMBL4206566 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4106732 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4208229 | ASCIMINIB | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3898258 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4213152 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4217559 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4114922 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3954214 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4115154 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3910823 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3915183 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3956542 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3892952 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3908521 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3913939 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4217428 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4210089 | — | Inhibition | - | % | - | |
| CHEMBL1234477 | — | Inhibition | - | % | - | |
| CHEMBL4110570 | — | IC50 | < | 0.3 | nM | - |
| CHEMBL4205194 | — | Inhibition | - | % | - | |
| CHEMBL4206566 | — | Inhibition | - | % | - |