Assay Detail
Functional
CHEMBL4394504
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human UCH1 cells measured after 72 hrs by alamar blue assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| 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 |
|---|---|---|---|
| IC50 | 34 | 5.67 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | 7.30 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 7.10 |
| CHEMBL607707 | PELITINIB | 2.0 | 1 | 7.05 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 7.00 |
| CHEMBL3545154 | POZIOTINIB | 3.0 | 1 | 6.96 |
| CHEMBL3544983 | TESEVATINIB | 3.0 | 1 | 6.82 |
| CHEMBL2408045 | SAPITINIB | 2.0 | 1 | 6.38 |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | 6.28 |
| CHEMBL29197 | — | — | 1 | 6.18 |
| CHEMBL304929 | — | — | 1 | 6.04 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 6.00 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 5.85 |
| CHEMBL1092250 | — | — | 1 | 5.68 |
| CHEMBL4447797 | — | — | 1 | 5.58 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 5.50 |
| CHEMBL98248 | — | — | 1 | 5.44 |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 5.37 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 5.29 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 5.26 |
| CHEMBL309682 | — | — | 1 | 5.14 |
| CHEMBL1089203 | — | — | 1 | 5.12 |
| CHEMBL111038 | — | — | 1 | 5.06 |
| CHEMBL81073 | — | — | 1 | 4.96 |
| CHEMBL311959 | — | — | 1 | 4.96 |
| CHEMBL4467033 | — | — | 1 | 4.89 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 4.82 |
| CHEMBL4440586 | — | — | 1 | 4.77 |
| CHEMBL4468521 | — | — | 1 | 4.60 |
| CHEMBL4518437 | — | — | 1 | 4.43 |
| CHEMBL4446630 | — | — | 1 | 4.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL31965 | CANERTINIB | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL607707 | PELITINIB | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1173655 | AFATINIB | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3545154 | POZIOTINIB | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3544983 | TESEVATINIB | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2408045 | SAPITINIB | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL3545396 | BMS-690514 | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL29197 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL304929 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL24828 | VANDETANIB | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL939 | GEFITINIB | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1092250 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4447797 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL554 | LAPATINIB | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL98248 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL217092 | SARACATINIB | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL180022 | NERATINIB | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL309682 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL1089203 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL111038 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL81073 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL311959 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4467033 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL288441 | BOSUTINIB | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4440586 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4468521 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4518437 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL4446630 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL535429 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4443342 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4514780 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4462395 | — | IC50 | > | 50000.0 | nM | - |