Assay Detail
Binding
CHEMBL923921
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Inhibition of human recombinant EGFR by fluorescence polarization assay
24
Total Activities
24
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.12 | 8.52 |
| Activity | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL248393 | — | — | 1 | 8.52 |
| CHEMBL248392 | — | — | 1 | 8.08 |
| CHEMBL248044 | — | — | 1 | 7.62 |
| CHEMBL246419 | — | — | 1 | 7.44 |
| CHEMBL245800 | — | — | 1 | 7.40 |
| CHEMBL247196 | — | — | 1 | 7.36 |
| CHEMBL248425 | — | — | 1 | 7.28 |
| CHEMBL248221 | — | — | 1 | 7.28 |
| CHEMBL401251 | — | — | 1 | 7.22 |
| CHEMBL401054 | — | — | 1 | 7.19 |
| CHEMBL248222 | — | — | 1 | 7.17 |
| CHEMBL399438 | — | — | 1 | 7.10 |
| CHEMBL245996 | — | — | 1 | 7.10 |
| CHEMBL248220 | — | — | 1 | 6.92 |
| CHEMBL248045 | — | — | 1 | 6.75 |
| CHEMBL248391 | — | — | 1 | 6.66 |
| CHEMBL400742 | — | — | 1 | 6.66 |
| CHEMBL245799 | — | — | 1 | 6.47 |
| CHEMBL245798 | — | — | 1 | 6.44 |
| CHEMBL401644 | — | — | 1 | 6.44 |
| CHEMBL247024 | — | — | 1 | 6.40 |
| CHEMBL247197 | — | — | 1 | - |
| CHEMBL399137 | — | — | 1 | - |
| CHEMBL400194 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL248393 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL248392 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL248044 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL246419 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL245800 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL247196 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL248425 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL248221 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL401251 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL401054 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL248222 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL399438 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL245996 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL248220 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL248045 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL248391 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL400742 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL245799 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL245798 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL401644 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL247024 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL247197 | — | Activity | - | — | - | |
| CHEMBL399137 | — | Activity | - | — | - | |
| CHEMBL400194 | — | Activity | - | — | - |