Assay Detail
Binding
CHEMBL5109392
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human FAK (393 to 698 residues) using poly (4:1 Glu, Tyr) peptide as substrate incubated for 60 mins in presence of ATP by ADP-Glo reagent based luminescent assay
20
Total Activities
20
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, synthesis and activity evaluation of isopropylsulfonyl-substituted 2,4- diarylaminopyrimidine derivatives as FAK inhibitors for the potential treatment of pancreatic cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 9.42 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5170906 | — | — | 1 | 10.00 |
| CHEMBL5198068 | — | — | 1 | 9.97 |
| CHEMBL5196177 | — | — | 1 | 9.93 |
| CHEMBL5176233 | — | — | 1 | 9.91 |
| CHEMBL5206909 | — | — | 1 | 9.81 |
| CHEMBL5187385 | — | — | 1 | 9.79 |
| CHEMBL5190968 | — | — | 1 | 9.72 |
| CHEMBL5177776 | — | — | 1 | 9.71 |
| CHEMBL5176990 | — | — | 1 | 9.67 |
| CHEMBL5204729 | — | — | 1 | 9.56 |
| CHEMBL5186801 | — | — | 1 | 9.53 |
| CHEMBL5178369 | — | — | 1 | 9.50 |
| CHEMBL5199835 | — | — | 1 | 9.50 |
| CHEMBL5177168 | — | — | 1 | 9.29 |
| CHEMBL5192604 | — | — | 1 | 9.24 |
| CHEMBL5180558 | — | — | 1 | 9.01 |
| CHEMBL5195974 | — | — | 1 | 8.87 |
| CHEMBL5197230 | — | — | 1 | 8.85 |
| CHEMBL458997 | — | — | 1 | 8.35 |
| CHEMBL5188293 | — | — | 1 | 8.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5170906 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5198068 | — | IC50 | = | 0.1076 | nM | 9.97 |
| CHEMBL5196177 | — | IC50 | = | 0.1165 | nM | 9.93 |
| CHEMBL5176233 | — | IC50 | = | 0.1242 | nM | 9.91 |
| CHEMBL5206909 | — | IC50 | = | 0.1534 | nM | 9.81 |
| CHEMBL5187385 | — | IC50 | = | 0.161 | nM | 9.79 |
| CHEMBL5190968 | — | IC50 | = | 0.1924 | nM | 9.72 |
| CHEMBL5177776 | — | IC50 | = | 0.1941 | nM | 9.71 |
| CHEMBL5176990 | — | IC50 | = | 0.2131 | nM | 9.67 |
| CHEMBL5204729 | — | IC50 | = | 0.275 | nM | 9.56 |
| CHEMBL5186801 | — | IC50 | = | 0.2963 | nM | 9.53 |
| CHEMBL5178369 | — | IC50 | = | 0.3146 | nM | 9.50 |
| CHEMBL5199835 | — | IC50 | = | 0.3146 | nM | 9.50 |
| CHEMBL5177168 | — | IC50 | = | 0.5143 | nM | 9.29 |
| CHEMBL5192604 | — | IC50 | = | 0.5794 | nM | 9.24 |
| CHEMBL5180558 | — | IC50 | = | 0.9763 | nM | 9.01 |
| CHEMBL5195974 | — | IC50 | = | 1.336 | nM | 8.87 |
| CHEMBL5197230 | — | IC50 | = | 1.415 | nM | 8.85 |
| CHEMBL458997 | — | IC50 | = | 4.502 | nM | 8.35 |
| CHEMBL5188293 | — | IC50 | = | 7.553 | nM | 8.12 |