Assay Detail
Binding
CHEMBL677210
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In vitro inhibitory activity against Epidermal growth factor receptor (EGFR-TK) from A431 vulval squamous carcinoma cells using TKI assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | A-431 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Studies leading to the identification of ZD1839 (IRESSA): an orally active, selective epidermal growth factor receptor tyrosine kinase inhibitor targeted to the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.59 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL56936 | — | — | 1 | 8.70 |
| CHEMBL56802 | — | — | 1 | 8.30 |
| CHEMBL299893 | — | — | 1 | 8.30 |
| CHEMBL56266 | — | — | 1 | 8.30 |
| CHEMBL56502 | — | — | 1 | 8.22 |
| CHEMBL57759 | — | — | 1 | 8.15 |
| CHEMBL293090 | — | — | 1 | 8.10 |
| CHEMBL56912 | — | — | 1 | 8.10 |
| CHEMBL60826 | — | — | 1 | 8.10 |
| CHEMBL301018 | — | — | 1 | 8.05 |
| CHEMBL300791 | — | — | 1 | 8.00 |
| CHEMBL14699 | — | — | 1 | 8.00 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.64 |
| CHEMBL56505 | — | — | 1 | 7.46 |
| CHEMBL57990 | — | — | 1 | 7.31 |
| CHEMBL55425 | — | — | 1 | 7.24 |
| CHEMBL294395 | — | — | 1 | 7.21 |
| CHEMBL294034 | — | — | 1 | 7.18 |
| CHEMBL1788321 | — | — | 1 | 7.17 |
| CHEMBL56027 | — | — | 1 | 7.16 |
| CHEMBL299672 | — | — | 1 | 7.15 |
| CHEMBL291514 | — | — | 1 | 7.10 |
| CHEMBL57758 | — | — | 1 | 7.06 |
| CHEMBL293064 | — | — | 1 | 7.03 |
| CHEMBL1744086 | — | — | 1 | 7.02 |
| CHEMBL56142 | — | — | 1 | 7.01 |
| CHEMBL57892 | — | — | 1 | 7.00 |
| CHEMBL55794 | — | — | 1 | 6.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL56936 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL56802 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL299893 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL56266 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL56502 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL57759 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL293090 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL56912 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL60826 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL301018 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL300791 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL14699 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL939 | GEFITINIB | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL56505 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL57990 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL55425 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL294395 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL294034 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL1788321 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL56027 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL299672 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL291514 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL57758 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL293064 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL1744086 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL56142 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL57892 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL55794 | — | IC50 | = | 310.0 | nM | 6.51 |