Assay Detail
Binding
CHEMBL4394507
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Binding affinity to wild-type human partial length GAK (G13 to Y338 residues) expressed in bacterial expression system by Kinomescan method
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 21 | 7.58 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | 9.52 |
| CHEMBL81073 | — | — | 1 | 9.38 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 8.89 |
| CHEMBL4440586 | — | — | 1 | 8.59 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 8.51 |
| CHEMBL304929 | — | — | 1 | 8.17 |
| CHEMBL1092250 | — | — | 1 | 8.12 |
| CHEMBL309682 | — | — | 1 | 8.00 |
| CHEMBL111038 | — | — | 1 | 7.92 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 7.89 |
| CHEMBL535429 | — | — | 1 | 7.51 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 7.10 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 7.07 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 7.00 |
| CHEMBL4468521 | — | — | 1 | 6.82 |
| CHEMBL4446630 | — | — | 1 | 6.72 |
| CHEMBL98248 | — | — | 1 | 6.62 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 6.60 |
| CHEMBL1089203 | — | — | 1 | 5.92 |
| CHEMBL4467033 | — | — | 1 | 5.30 |
| CHEMBL4447797 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545396 | BMS-690514 | Kd | = | 0.3 | nM | 9.52 |
| CHEMBL81073 | — | Kd | = | 0.42 | nM | 9.38 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 1.3 | nM | 8.89 |
| CHEMBL4440586 | — | Kd | = | 2.6 | nM | 8.59 |
| CHEMBL553 | ERLOTINIB | Kd | = | 3.1 | nM | 8.51 |
| CHEMBL304929 | — | Kd | = | 6.8 | nM | 8.17 |
| CHEMBL1092250 | — | Kd | = | 7.6 | nM | 8.12 |
| CHEMBL309682 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL111038 | — | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL939 | GEFITINIB | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL535429 | — | Kd | = | 31.0 | nM | 7.51 |
| CHEMBL1173655 | AFATINIB | Kd | = | 79.0 | nM | 7.10 |
| CHEMBL24828 | VANDETANIB | Kd | = | 86.0 | nM | 7.07 |
| CHEMBL31965 | CANERTINIB | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL4468521 | — | Kd | = | 150.0 | nM | 6.82 |
| CHEMBL4446630 | — | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL98248 | — | Kd | = | 240.0 | nM | 6.62 |
| CHEMBL180022 | NERATINIB | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL1089203 | — | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL4467033 | — | Kd | = | 5000.0 | nM | 5.30 |
| CHEMBL4447797 | — | Kd | > | 10000.0 | nM | - |