Assay Detail
Binding
CHEMBL4353545
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant N-terminal His-tagged FAK (393 to 698 residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) peptide as substrate incubated for 60 mins by ADP-Glo assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 2,4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel FAK inhibitors with antitumor and anti-angiogenesis activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.54 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4554455 | — | — | 1 | 10.15 |
| CHEMBL4469292 | — | — | 1 | 8.07 |
| CHEMBL4438250 | — | — | 1 | 7.49 |
| CHEMBL4458861 | — | — | 1 | 6.76 |
| CHEMBL4453262 | — | — | 1 | 6.50 |
| CHEMBL4590434 | — | — | 1 | 6.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4554455 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL4469292 | — | IC50 | = | 8.57 | nM | 8.07 |
| CHEMBL4438250 | — | IC50 | = | 32.7 | nM | 7.49 |
| CHEMBL4458861 | — | IC50 | = | 175.4 | nM | 6.76 |
| CHEMBL4453262 | — | IC50 | = | 316.3 | nM | 6.50 |
| CHEMBL4590434 | — | IC50 | = | 506.7 | nM | 6.29 |