Assay Detail
Binding
CHEMBL679944
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration needed to inhibit the phosphorylation of a 14-residue fragment of phospholipase C-gamma1 by Epidermal growth factor receptor (prepared from human A431 carcinoma cell vesicles by immunoaffinity chromatography)
56
Total Activities
56
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. 16. 6,5,6-tricyclic benzothieno[3, 2-d]pyrimidines and pyrimido[5,4-b-] and -[4,5-b]ĭndoles as potent inhibitors of the epidermal growth factor receptor tyrosine kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 56 | 7.56 | 10.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL29197 | — | — | 1 | 10.60 |
| CHEMBL152905 | — | — | 1 | 9.57 |
| CHEMBL40734 | — | — | 1 | 9.41 |
| CHEMBL39337 | — | — | 1 | 9.36 |
| CHEMBL539822 | — | — | 1 | 9.33 |
| CHEMBL415738 | — | — | 1 | 9.00 |
| CHEMBL153573 | — | — | 1 | 9.00 |
| CHEMBL358934 | — | — | 1 | 8.96 |
| CHEMBL153206 | — | — | 1 | 8.92 |
| CHEMBL153525 | — | — | 1 | 8.91 |
| CHEMBL356850 | — | — | 1 | 8.74 |
| CHEMBL155278 | — | — | 1 | 8.68 |
| CHEMBL151593 | — | — | 1 | 8.57 |
| CHEMBL357570 | — | — | 1 | 8.10 |
| CHEMBL357367 | — | — | 1 | 8.03 |
| CHEMBL544867 | — | — | 1 | 7.96 |
| CHEMBL345294 | — | — | 1 | 7.96 |
| CHEMBL553351 | — | — | 1 | 7.91 |
| CHEMBL555921 | — | — | 1 | 7.90 |
| CHEMBL153739 | — | — | 1 | 7.70 |
| CHEMBL542755 | — | — | 1 | 7.70 |
| CHEMBL329672 | — | — | 1 | 7.64 |
| CHEMBL153170 | — | — | 1 | 7.54 |
| CHEMBL423224 | — | — | 1 | 7.51 |
| CHEMBL355982 | — | — | 1 | 7.46 |
| CHEMBL346863 | — | — | 1 | 7.40 |
| CHEMBL347282 | — | — | 1 | 7.33 |
| CHEMBL540590 | — | — | 1 | 7.32 |
| CHEMBL544868 | — | — | 1 | 7.24 |
| CHEMBL554983 | — | — | 1 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL29197 | — | IC50 | = | 0.025 | nM | 10.60 |
| CHEMBL152905 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL40734 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL39337 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL539822 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL415738 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL153573 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL358934 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL153206 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL153525 | — | IC50 | = | 1.24 | nM | 8.91 |
| CHEMBL356850 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL155278 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL151593 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL357570 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL357367 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL544867 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL345294 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL553351 | — | IC50 | = | 12.3 | nM | 7.91 |
| CHEMBL555921 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL153739 | — | IC50 | = | 19.8 | nM | 7.70 |
| CHEMBL542755 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL329672 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL153170 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL423224 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL355982 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL346863 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL347282 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL540590 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL544868 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL554983 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL346846 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL553137 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL345988 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL540082 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL153419 | — | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL150280 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL155100 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL2093928 | — | IC50 | = | 419.0 | nM | 6.38 |
| CHEMBL544865 | — | IC50 | = | 444.0 | nM | 6.35 |
| CHEMBL357097 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL538814 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL3085277 | — | IC50 | = | 538.0 | nM | 6.27 |
| CHEMBL153409 | — | IC50 | = | 732.0 | nM | 6.13 |
| CHEMBL149512 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL152984 | — | IC50 | = | 742.0 | nM | 6.13 |
| CHEMBL544640 | — | IC50 | = | 2110.0 | nM | 5.68 |
| CHEMBL448730 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL153518 | — | IC50 | = | 4270.0 | nM | 5.37 |
| CHEMBL348003 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL53753 | — | IC50 | = | 0.008 | nM | - |