Assay Detail
Binding
CHEMBL862513
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Inhibition of erbB2 fusion protein expressed in baculovirus by ELISA
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 8.01 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL437890 | — | — | 1 | 9.30 |
| CHEMBL203599 | — | — | 1 | 9.15 |
| CHEMBL204638 | — | — | 1 | 9.15 |
| CHEMBL203661 | — | — | 1 | 9.10 |
| CHEMBL203644 | — | — | 1 | 8.96 |
| CHEMBL202360 | — | — | 1 | 8.72 |
| CHEMBL205059 | — | — | 1 | 8.68 |
| CHEMBL202411 | — | — | 1 | 8.68 |
| CHEMBL204085 | — | — | 1 | 8.64 |
| CHEMBL378144 | — | — | 1 | 8.62 |
| CHEMBL382073 | — | — | 1 | 8.59 |
| CHEMBL380669 | — | — | 1 | 8.55 |
| CHEMBL203645 | — | — | 1 | 8.42 |
| CHEMBL202424 | — | — | 1 | 8.27 |
| CHEMBL91867 | — | — | 1 | 7.77 |
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | 3.0 | 1 | 7.70 |
| CHEMBL202556 | — | — | 1 | 7.58 |
| CHEMBL373207 | — | — | 1 | 7.34 |
| CHEMBL202421 | — | — | 1 | 7.17 |
| CHEMBL202621 | — | — | 1 | 6.52 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 6.46 |
| CHEMBL202398 | — | — | 1 | 6.33 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 6.29 |
| CHEMBL202425 | — | — | 1 | 6.22 |
| CHEMBL383499 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL437890 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL203599 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL204638 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL203661 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL203644 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL202360 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL205059 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL202411 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL204085 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL378144 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL382073 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL380669 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL203645 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL202424 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL91867 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL545315 | CANERTINIB DIHYDROCHLORIDE | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL202556 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL373207 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL202421 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL202621 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL939 | GEFITINIB | IC50 | = | 343.0 | nM | 6.46 |
| CHEMBL202398 | — | IC50 | = | 464.0 | nM | 6.33 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 511.0 | nM | 6.29 |
| CHEMBL202425 | — | IC50 | = | 597.0 | nM | 6.22 |
| CHEMBL383499 | — | IC50 | > | 1000.0 | nM | - |