Assay Detail
Functional
CHEMBL620834
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration required to inhibit growth of human carcinoma epidermoid (A431) cell line
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | A-431 |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.45 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL114490 | — | — | 1 | 7.22 |
| CHEMBL424252 | — | — | 1 | 7.16 |
| CHEMBL607707 | PELITINIB | 2.0 | 1 | 7.10 |
| CHEMBL327023 | — | — | 1 | 7.00 |
| CHEMBL116853 | — | — | 1 | 6.96 |
| CHEMBL113996 | — | — | 1 | 6.92 |
| CHEMBL114728 | — | — | 1 | 6.89 |
| CHEMBL263788 | — | — | 1 | 6.85 |
| CHEMBL113900 | — | — | 1 | 6.85 |
| CHEMBL116012 | — | — | 1 | 6.85 |
| CHEMBL323630 | — | — | 1 | 6.82 |
| CHEMBL332497 | — | — | 1 | 6.80 |
| CHEMBL414631 | — | — | 1 | 6.77 |
| CHEMBL117326 | — | — | 1 | 6.75 |
| CHEMBL115187 | — | — | 1 | 6.62 |
| CHEMBL114392 | — | — | 1 | 6.58 |
| CHEMBL115440 | — | — | 1 | 6.57 |
| CHEMBL114593 | — | — | 1 | 6.55 |
| CHEMBL324718 | — | — | 1 | 6.51 |
| CHEMBL281300 | — | — | 1 | 6.44 |
| CHEMBL325156 | — | — | 1 | 6.42 |
| CHEMBL118000 | — | — | 1 | 6.39 |
| CHEMBL113901 | — | — | 1 | 6.37 |
| CHEMBL30973 | — | — | 1 | 6.35 |
| CHEMBL421047 | — | — | 1 | 6.33 |
| CHEMBL114073 | — | — | 1 | 6.23 |
| CHEMBL326280 | — | — | 1 | 6.14 |
| CHEMBL157128 | — | — | 1 | 5.92 |
| CHEMBL113902 | — | — | 1 | 5.90 |
| CHEMBL113985 | — | — | 1 | 5.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL114490 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL424252 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL607707 | PELITINIB | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL327023 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL116853 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL113996 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL114728 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL263788 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL113900 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL116012 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL323630 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL332497 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL414631 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL117326 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL115187 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL114392 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL115440 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL114593 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL324718 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL281300 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL325156 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL118000 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL113901 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL30973 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL421047 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL114073 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL326280 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL157128 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL113902 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL113985 | — | IC50 | = | 2220.0 | nM | 5.65 |
| CHEMBL116857 | — | IC50 | = | 2520.0 | nM | 5.60 |
| CHEMBL326811 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL283682 | — | IC50 | = | 5030.0 | nM | 5.30 |
| CHEMBL116525 | — | IC50 | = | 5120.0 | nM | 5.29 |