Assay Detail
Binding
CHEMBL4669540
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of tracer 236 binding to recombinant human GST-tagged full length FAK expressed in baculovirus expression system incubated for 1 hr by Lanthascreen TR-FRET assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 9.10 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4781502 | — | — | 1 | 10.05 |
| CHEMBL4786602 | — | — | 1 | 9.96 |
| CHEMBL4776318 | — | — | 1 | 9.55 |
| CHEMBL3040440 | VS-4718 | 1.0 | 1 | 9.52 |
| CHEMBL4792928 | — | — | 1 | 9.47 |
| CHEMBL4742859 | — | — | 1 | 9.38 |
| CHEMBL4748255 | — | — | 1 | 9.36 |
| CHEMBL4761718 | — | — | 1 | 9.36 |
| CHEMBL4800129 | — | — | 1 | 9.24 |
| CHEMBL4742157 | GSK-2256098 | 2.0 | 1 | 9.17 |
| CHEMBL4743129 | — | — | 1 | 8.89 |
| CHEMBL4759226 | — | — | 1 | 8.74 |
| CHEMBL4757328 | — | — | 1 | 8.60 |
| CHEMBL4780583 | — | — | 1 | 8.49 |
| CHEMBL4755900 | — | — | 1 | 8.29 |
| CHEMBL4758042 | — | — | 1 | 7.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4781502 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL4786602 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL4776318 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL3040440 | VS-4718 | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4792928 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL4742859 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL4748255 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL4761718 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL4800129 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL4742157 | GSK-2256098 | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL4743129 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4759226 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4757328 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4780583 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4755900 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4758042 | — | IC50 | = | 29.0 | nM | 7.54 |