Assay Detail
Binding
CHEMBL4670946
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal His6-tagged HER2-A775_G776insYVMA mutant (703 to 1029 residues) (unknown origin) expressed in Sf9 insect cells using TK as substrate preincubated for 30 mins followed by substrate addition and measured after 40 mins in presence of XL665-labeled streptavidin by HTRF assay
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 7.58 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4757592 | — | — | 1 | 10.00 |
| CHEMBL3545154 | POZIOTINIB | 3.0 | 1 | 9.52 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 8.68 |
| CHEMBL4750655 | — | — | 1 | 8.66 |
| CHEMBL4757450 | — | — | 1 | 8.64 |
| CHEMBL4800516 | — | — | 1 | 8.55 |
| CHEMBL4753389 | — | — | 1 | 8.46 |
| CHEMBL4743509 | — | — | 1 | 8.19 |
| CHEMBL4757145 | — | — | 1 | 8.13 |
| CHEMBL4786257 | — | — | 1 | 8.10 |
| CHEMBL4791900 | — | — | 1 | 8.07 |
| CHEMBL4741898 | — | — | 1 | 8.04 |
| CHEMBL4760739 | — | — | 1 | 8.00 |
| CHEMBL4776708 | — | — | 1 | 7.96 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.82 |
| CHEMBL4787483 | — | — | 1 | 7.77 |
| CHEMBL4799276 | — | — | 1 | 7.75 |
| CHEMBL4740009 | — | — | 1 | 7.70 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 7.70 |
| CHEMBL4754658 | — | — | 1 | 7.68 |
| CHEMBL4741020 | — | — | 1 | 7.48 |
| CHEMBL4785221 | — | — | 1 | 7.44 |
| CHEMBL4778909 | — | — | 1 | 7.40 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 7.35 |
| CHEMBL4751089 | — | — | 1 | 7.35 |
| CHEMBL4740834 | — | — | 1 | 7.34 |
| CHEMBL4756368 | — | — | 1 | 7.34 |
| CHEMBL4758224 | — | — | 1 | 7.28 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 7.27 |
| CHEMBL4795863 | — | — | 1 | 7.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4757592 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3545154 | POZIOTINIB | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4750655 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4757450 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4800516 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4753389 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4743509 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4757145 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4786257 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4791900 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4741898 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL4760739 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4776708 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL939 | GEFITINIB | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4787483 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4799276 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4740009 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL180022 | NERATINIB | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4754658 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4741020 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4785221 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4778909 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4751089 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4740834 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4756368 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4758224 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL554 | LAPATINIB | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4795863 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4795165 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4751894 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL4781593 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL4783667 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL1614725 | TAK-285 | IC50 | = | 311.0 | nM | 6.51 |
| CHEMBL4755170 | — | IC50 | = | 405.0 | nM | 6.39 |
| CHEMBL4759651 | — | IC50 | = | 418.0 | nM | 6.38 |
| CHEMBL4743066 | — | IC50 | = | 716.0 | nM | 6.14 |
| CHEMBL4763660 | — | IC50 | = | 1266.0 | nM | 5.90 |
| CHEMBL4763834 | — | IC50 | = | 1442.0 | nM | 5.84 |
| CHEMBL4759178 | — | IC50 | > | 2000.0 | nM | - |