Assay Detail
Binding
CHEMBL1064922
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Inhibition of HER2
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.36 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL598799 | — | — | 1 | 8.00 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 7.99 |
| CHEMBL597551 | — | — | 1 | 7.97 |
| CHEMBL597752 | — | — | 1 | 7.91 |
| CHEMBL596736 | — | — | 1 | 7.82 |
| CHEMBL598797 | CUDC-101 | 1.0 | 1 | 7.80 |
| CHEMBL598377 | — | — | 1 | 7.72 |
| CHEMBL598163 | — | — | 1 | 7.70 |
| CHEMBL597773 | — | — | 1 | 7.70 |
| CHEMBL597569 | — | — | 1 | 7.62 |
| CHEMBL596754 | — | — | 1 | 7.62 |
| CHEMBL605976 | — | — | 1 | 7.56 |
| CHEMBL599398 | — | — | 1 | 7.42 |
| CHEMBL598164 | — | — | 1 | 7.42 |
| CHEMBL604094 | — | — | 1 | 7.36 |
| CHEMBL598611 | — | — | 1 | 7.29 |
| CHEMBL598610 | — | — | 1 | 7.15 |
| CHEMBL598798 | — | — | 1 | 7.12 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 6.87 |
| CHEMBL598406 | — | — | 1 | 6.76 |
| CHEMBL596761 | — | — | 1 | 6.65 |
| CHEMBL596964 | — | — | 1 | 6.53 |
| CHEMBL596957 | — | — | 1 | 6.32 |
| CHEMBL598407 | — | — | 1 | 6.25 |
| CHEMBL596755 | — | — | 1 | - |
| CHEMBL599218 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL598799 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL554 | LAPATINIB | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL597551 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL597752 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL596736 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL598797 | CUDC-101 | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL598377 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL598163 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL597773 | — | IC50 | = | 20.1 | nM | 7.70 |
| CHEMBL597569 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL596754 | — | IC50 | = | 24.2 | nM | 7.62 |
| CHEMBL605976 | — | IC50 | = | 27.8 | nM | 7.56 |
| CHEMBL599398 | — | IC50 | = | 38.4 | nM | 7.42 |
| CHEMBL598164 | — | IC50 | = | 38.2 | nM | 7.42 |
| CHEMBL604094 | — | IC50 | = | 43.5 | nM | 7.36 |
| CHEMBL598611 | — | IC50 | = | 51.6 | nM | 7.29 |
| CHEMBL598610 | — | IC50 | = | 71.2 | nM | 7.15 |
| CHEMBL598798 | — | IC50 | = | 76.5 | nM | 7.12 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 134.5 | nM | 6.87 |
| CHEMBL598406 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL596761 | — | IC50 | = | 225.2 | nM | 6.65 |
| CHEMBL596964 | — | IC50 | = | 295.4 | nM | 6.53 |
| CHEMBL596957 | — | IC50 | = | 478.2 | nM | 6.32 |
| CHEMBL598407 | — | IC50 | = | 556.9 | nM | 6.25 |
| CHEMBL596755 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL599218 | — | IC50 | > | 2000.0 | nM | - |