Assay Detail
Binding
CHEMBL4670944
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HER2-A775_G776insYVMA mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in HER2 induced cell viability after 96 hrs by CellTiter-Glo assay
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BaF3 |
| 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 | 6.27 | 7.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4760739 | — | — | 1 | 7.39 |
| CHEMBL4778909 | — | — | 1 | 7.28 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 7.24 |
| CHEMBL4787483 | — | — | 1 | 7.08 |
| CHEMBL4786257 | — | — | 1 | 7.08 |
| CHEMBL4757145 | — | — | 1 | 6.92 |
| CHEMBL4740834 | — | — | 1 | 6.87 |
| CHEMBL4756368 | — | — | 1 | 6.80 |
| CHEMBL4751089 | — | — | 1 | 6.59 |
| CHEMBL4757450 | — | — | 1 | 6.54 |
| CHEMBL4758224 | — | — | 1 | 6.52 |
| CHEMBL4741898 | — | — | 1 | 6.49 |
| CHEMBL4755170 | — | — | 1 | 6.46 |
| CHEMBL4795165 | — | — | 1 | 6.42 |
| CHEMBL4750655 | — | — | 1 | 6.41 |
| CHEMBL4800516 | — | — | 1 | 6.39 |
| CHEMBL4757592 | — | — | 1 | 6.37 |
| CHEMBL4743066 | — | — | 1 | 6.30 |
| CHEMBL4781593 | — | — | 1 | 6.25 |
| CHEMBL4751894 | — | — | 1 | 6.21 |
| CHEMBL4740009 | — | — | 1 | 6.20 |
| CHEMBL4783667 | — | — | 1 | 6.17 |
| CHEMBL4763834 | — | — | 1 | 6.12 |
| CHEMBL4776708 | — | — | 1 | 6.04 |
| CHEMBL4753389 | — | — | 1 | 5.95 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 5.86 |
| CHEMBL4799276 | — | — | 1 | 5.84 |
| CHEMBL4791900 | — | — | 1 | 5.65 |
| CHEMBL4741020 | — | — | 1 | 5.62 |
| CHEMBL4754658 | — | — | 1 | 5.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4760739 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4778909 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4787483 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4786257 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4757145 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4740834 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL4756368 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL4751089 | — | IC50 | = | 259.0 | nM | 6.59 |
| CHEMBL4757450 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL4758224 | — | IC50 | = | 304.0 | nM | 6.52 |
| CHEMBL4741898 | — | IC50 | = | 327.0 | nM | 6.49 |
| CHEMBL4755170 | — | IC50 | = | 349.0 | nM | 6.46 |
| CHEMBL4795165 | — | IC50 | = | 381.0 | nM | 6.42 |
| CHEMBL4750655 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4800516 | — | IC50 | = | 411.0 | nM | 6.39 |
| CHEMBL4757592 | — | IC50 | = | 431.0 | nM | 6.37 |
| CHEMBL4743066 | — | IC50 | = | 497.0 | nM | 6.30 |
| CHEMBL4781593 | — | IC50 | = | 562.0 | nM | 6.25 |
| CHEMBL4751894 | — | IC50 | = | 621.0 | nM | 6.21 |
| CHEMBL4740009 | — | IC50 | = | 638.0 | nM | 6.20 |
| CHEMBL4783667 | — | IC50 | = | 675.0 | nM | 6.17 |
| CHEMBL4763834 | — | IC50 | = | 754.0 | nM | 6.12 |
| CHEMBL4776708 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4753389 | — | IC50 | = | 1117.0 | nM | 5.95 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 1389.0 | nM | 5.86 |
| CHEMBL4799276 | — | IC50 | = | 1445.0 | nM | 5.84 |
| CHEMBL4791900 | — | IC50 | = | 2216.0 | nM | 5.65 |
| CHEMBL4741020 | — | IC50 | = | 2416.0 | nM | 5.62 |
| CHEMBL4754658 | — | IC50 | = | 2683.0 | nM | 5.57 |
| CHEMBL554 | LAPATINIB | IC50 | = | 2761.0 | nM | 5.56 |
| CHEMBL4795863 | — | IC50 | = | 2813.0 | nM | 5.55 |
| CHEMBL939 | GEFITINIB | IC50 | = | 2882.0 | nM | 5.54 |
| CHEMBL1614725 | TAK-285 | IC50 | = | 3218.0 | nM | 5.49 |
| CHEMBL4785221 | — | IC50 | = | 3302.0 | nM | 5.48 |
| CHEMBL4759651 | — | IC50 | = | 3602.0 | nM | 5.44 |
| CHEMBL4759178 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4743509 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL3545154 | POZIOTINIB | IC50 | < | 14.0 | nM | - |
| CHEMBL180022 | NERATINIB | IC50 | < | 14.0 | nM | - |
| CHEMBL4763660 | — | IC50 | > | 3000.0 | nM | - |