Assay Detail
Binding
CHEMBL686676
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Concentration required to achieve 50% inhibition of tyrosine phosphorylation on human Her-2 receptor tyrosine kinase (HER-2 RTK)
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 54 | 4.57 | 5.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL85021 | — | — | 1 | 5.16 |
| CHEMBL89723 | — | — | 1 | 5.09 |
| CHEMBL86945 | — | — | 1 | 4.88 |
| CHEMBL86944 | — | — | 1 | 4.82 |
| CHEMBL86326 | — | — | 1 | 4.79 |
| CHEMBL48760 | — | — | 1 | 4.77 |
| CHEMBL87746 | — | — | 1 | 4.72 |
| CHEMBL314021 | — | — | 1 | 4.65 |
| CHEMBL89505 | — | — | 1 | 4.19 |
| CHEMBL90277 | — | — | 1 | 4.18 |
| CHEMBL315546 | — | — | 1 | 4.04 |
| CHEMBL86432 | — | — | 1 | 4.04 |
| CHEMBL315701 | — | — | 1 | 4.03 |
| CHEMBL316020 | — | — | 1 | - |
| CHEMBL431025 | — | — | 1 | - |
| CHEMBL313259 | — | — | 1 | - |
| CHEMBL329367 | — | — | 1 | - |
| CHEMBL86631 | — | — | 1 | - |
| CHEMBL420411 | — | — | 1 | - |
| CHEMBL316009 | — | — | 1 | - |
| CHEMBL87325 | — | — | 1 | - |
| CHEMBL89809 | — | — | 1 | - |
| CHEMBL421548 | — | — | 1 | - |
| CHEMBL314146 | — | — | 1 | - |
| CHEMBL89483 | — | — | 1 | - |
| CHEMBL89721 | — | — | 1 | - |
| CHEMBL328710 | — | — | 1 | - |
| CHEMBL330321 | — | — | 1 | - |
| CHEMBL86921 | — | — | 1 | - |
| CHEMBL88405 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL85021 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL89723 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL86945 | — | IC50 | = | 13200.0 | nM | 4.88 |
| CHEMBL86944 | — | IC50 | = | 15200.0 | nM | 4.82 |
| CHEMBL86326 | — | IC50 | = | 16200.0 | nM | 4.79 |
| CHEMBL48760 | — | IC50 | = | 16900.0 | nM | 4.77 |
| CHEMBL87746 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL314021 | — | IC50 | = | 22500.0 | nM | 4.65 |
| CHEMBL89505 | — | IC50 | = | 64800.0 | nM | 4.19 |
| CHEMBL90277 | — | IC50 | = | 66600.0 | nM | 4.18 |
| CHEMBL86432 | — | IC50 | = | 91400.0 | nM | 4.04 |
| CHEMBL315546 | — | IC50 | = | 90200.0 | nM | 4.04 |
| CHEMBL315701 | — | IC50 | = | 92600.0 | nM | 4.03 |
| CHEMBL86480 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL316268 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL85403 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL86755 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL86943 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL87080 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL89363 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL87208 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL87402 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL86837 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL328452 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL89040 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL276711 | SEMAXANIB | IC50 | > | 100000.0 | nM | - |
| CHEMBL314217 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL313578 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL314798 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL316008 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL87783 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL87325 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL88405 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL86921 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL330321 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL328710 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL89721 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL89483 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL314146 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL421548 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL89809 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL89697 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL316009 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL420411 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL86631 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL329367 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL313259 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL431025 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL316020 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL87324 | — | IC50 | > | 100000.0 | nM | - |