Assay Detail
Binding
CHEMBL674648
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Inhibit of phosphorylation of a tyrosine/glutamic acid copolymer by epidermal growth factor receptor prepared from human A431 carcinoma cell vesicles by immunoaffinity chromatography.
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Tyrosine kinase inhibitors. 14. Structure-activity relationships for methylamino-substituted derivatives of 4-[(3-bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyrimidine (PD 158780), a potent and specific inhibitor of the tyrosine kinase activity of receptors for the EGF family of growth factors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 8.88 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL51853 | — | — | 1 | 9.89 |
| CHEMBL166093 | — | — | 1 | 9.74 |
| CHEMBL166154 | — | — | 1 | 9.72 |
| CHEMBL165864 | — | — | 1 | 9.72 |
| CHEMBL161956 | — | — | 1 | 9.66 |
| CHEMBL355816 | — | — | 1 | 9.55 |
| CHEMBL163369 | — | — | 1 | 9.46 |
| CHEMBL351629 | — | — | 1 | 9.36 |
| CHEMBL165547 | — | — | 1 | 9.25 |
| CHEMBL162622 | — | — | 1 | 9.19 |
| CHEMBL162142 | — | — | 1 | 9.11 |
| CHEMBL165630 | — | — | 1 | 9.03 |
| CHEMBL165574 | — | — | 1 | 9.00 |
| CHEMBL165788 | — | — | 1 | 8.96 |
| CHEMBL166358 | — | — | 1 | 8.92 |
| CHEMBL162223 | — | — | 1 | 8.92 |
| CHEMBL161895 | — | — | 1 | 8.89 |
| CHEMBL165731 | — | — | 1 | 8.82 |
| CHEMBL165508 | — | — | 1 | 8.82 |
| CHEMBL162981 | — | — | 1 | 8.77 |
| CHEMBL166255 | — | — | 1 | 8.77 |
| CHEMBL349070 | — | — | 1 | 8.74 |
| CHEMBL162508 | — | — | 1 | 8.74 |
| CHEMBL163188 | — | — | 1 | 8.55 |
| CHEMBL165495 | — | — | 1 | 8.51 |
| CHEMBL166307 | — | — | 1 | 8.41 |
| CHEMBL162719 | — | — | 1 | 8.19 |
| CHEMBL162053 | — | — | 1 | 8.09 |
| CHEMBL53940 | — | — | 1 | 8.05 |
| CHEMBL163168 | — | — | 1 | 7.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL51853 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL166093 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL166154 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL165864 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL161956 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL355816 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL163369 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL351629 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL165547 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL162622 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL162142 | — | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL165630 | — | IC50 | = | 0.93 | nM | 9.03 |
| CHEMBL165574 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL165788 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL162223 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL166358 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL161895 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL165731 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL165508 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL162981 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL166255 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL349070 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL162508 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL163188 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL165495 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL166307 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL162719 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL162053 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL53940 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL163168 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL165228 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL53711 | — | IC50 | = | 0.006 | nM | - |