Assay Detail
Binding
CHEMBL677877
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration needed to inhibit the autophosphorylation of the cytoplasmic domain of Epidermal growth factor receptor using DELFIA/time-resolved fluorimetry.
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Expert |
Target
Epidermal growth factor receptor and ErbB2 (HER1 and HER2) (CHEMBL2111431) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
4-Anilino-6,7-dialkoxyquinoline-3-carbonitrile inhibitors of epidermal growth factor receptor kinase and their bioisosteric relationship to the 4-anilino-6,7-dialkoxyquinazoline inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 51 | 5.51 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL29197 | — | — | 1 | 7.16 |
| CHEMBL1203088 | — | — | 1 | 6.80 |
| CHEMBL109428 | — | — | 1 | 6.75 |
| CHEMBL111038 | — | — | 1 | 6.72 |
| CHEMBL323424 | — | — | 1 | 6.64 |
| CHEMBL111586 | — | — | 1 | 6.46 |
| CHEMBL112096 | — | — | 1 | 6.44 |
| CHEMBL109212 | — | — | 1 | 6.38 |
| CHEMBL109372 | — | — | 1 | 6.27 |
| CHEMBL110055 | — | — | 1 | 6.21 |
| CHEMBL320479 | — | — | 1 | 6.13 |
| CHEMBL1203026 | — | — | 1 | 6.12 |
| CHEMBL110036 | — | — | 1 | 6.09 |
| CHEMBL112225 | — | — | 1 | 6.08 |
| CHEMBL1203037 | — | — | 1 | 6.07 |
| CHEMBL111520 | — | — | 1 | 6.06 |
| CHEMBL324045 | — | — | 1 | 6.01 |
| CHEMBL109515 | — | — | 1 | 5.96 |
| CHEMBL109503 | — | — | 1 | 5.84 |
| CHEMBL109355 | — | — | 1 | 5.83 |
| CHEMBL111307 | — | — | 1 | 5.75 |
| CHEMBL113535 | — | — | 1 | 5.66 |
| CHEMBL109476 | — | — | 1 | 5.56 |
| CHEMBL419185 | — | — | 1 | 5.50 |
| CHEMBL109332 | — | — | 1 | 5.47 |
| CHEMBL109575 | — | — | 1 | 5.38 |
| CHEMBL325981 | — | — | 1 | 5.29 |
| CHEMBL110577 | — | — | 1 | 5.20 |
| CHEMBL323900 | — | — | 1 | 5.18 |
| CHEMBL111222 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL29197 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1203088 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL109428 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL111038 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL323424 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL111586 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL112096 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL109212 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL109372 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL110055 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL320479 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL1203026 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL110036 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL112225 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL1203037 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL111520 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL324045 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL109515 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL109503 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL109355 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL111307 | — | IC50 | = | 1790.0 | nM | 5.75 |
| CHEMBL113535 | — | IC50 | = | 2210.0 | nM | 5.66 |
| CHEMBL109476 | — | IC50 | = | 2730.0 | nM | 5.56 |
| CHEMBL419185 | — | IC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL109332 | — | IC50 | = | 3370.0 | nM | 5.47 |
| CHEMBL109575 | — | IC50 | = | 4180.0 | nM | 5.38 |
| CHEMBL325981 | — | IC50 | = | 5150.0 | nM | 5.29 |
| CHEMBL110577 | — | IC50 | = | 6360.0 | nM | 5.20 |
| CHEMBL323900 | — | IC50 | = | 6650.0 | nM | 5.18 |
| CHEMBL111222 | — | IC50 | = | 6750.0 | nM | 5.17 |
| CHEMBL110062 | — | IC50 | = | 6790.0 | nM | 5.17 |
| CHEMBL325760 | — | IC50 | = | 7380.0 | nM | 5.13 |
| CHEMBL323970 | — | IC50 | = | 7690.0 | nM | 5.11 |
| CHEMBL110945 | — | IC50 | = | 9040.0 | nM | 5.04 |
| CHEMBL111664 | — | IC50 | = | 13850.0 | nM | 4.86 |
| CHEMBL111033 | — | IC50 | = | 14180.0 | nM | 4.85 |
| CHEMBL114446 | — | IC50 | = | 15170.0 | nM | 4.82 |
| CHEMBL326445 | — | IC50 | = | 17020.0 | nM | 4.77 |
| CHEMBL110065 | — | IC50 | = | 21190.0 | nM | 4.67 |
| CHEMBL111443 | — | IC50 | = | 33020.0 | nM | 4.48 |
| CHEMBL541988 | — | IC50 | = | 34220.0 | nM | 4.47 |
| CHEMBL432396 | — | IC50 | = | 47940.0 | nM | 4.32 |
| CHEMBL83228 | — | IC50 | = | 50490.0 | nM | 4.30 |
| CHEMBL109625 | — | IC50 | = | 62320.0 | nM | 4.21 |
| CHEMBL324399 | — | IC50 | = | 69400.0 | nM | 4.16 |
| CHEMBL1203047 | — | IC50 | = | 70840.0 | nM | 4.15 |
| CHEMBL109259 | — | IC50 | = | 88290.0 | nM | 4.05 |
| CHEMBL439596 | — | IC50 | > | 102200.0 | nM | - |
| CHEMBL111442 | — | IC50 | > | 104700.0 | nM | - |
| CHEMBL443277 | — | IC50 | > | 81300.0 | nM | - |