Assay Detail
Binding
CHEMBL5680957
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ABL1 H396P mutant (229 to 499 residues) using ABLtide as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by spectrophotometric analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.16 | 9.30 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | MONDO:0004992 |
| EFO_TERM | EFO_TERM | - | — | cancer |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1421 | DASATINIB ANHYDROUS | 4.0 | 1 | 9.30 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 8.96 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 8.85 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1421 | DASATINIB ANHYDROUS | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL255863 | NILOTINIB | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1738757 | REBASTINIB | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL941 | IMATINIB | IC50 | = | 3000.0 | nM | 5.52 |