Assay Detail
Binding
CHEMBL3873676
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Inhibition of full length recombinant human N-terminal His6-tagged PYK2 expressed in baculovirus infected sf21 cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 8.04 | 9.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3949755 | — | — | 1 | 9.17 |
| CHEMBL3958414 | — | — | 1 | 9.08 |
| CHEMBL3956954 | — | — | 1 | 9.05 |
| CHEMBL3987106 | — | — | 1 | 8.88 |
| CHEMBL3899046 | — | — | 1 | 8.82 |
| CHEMBL3969464 | — | — | 1 | 8.81 |
| CHEMBL3908093 | — | — | 1 | 8.72 |
| CHEMBL3961368 | — | — | 1 | 8.59 |
| CHEMBL3977870 | — | — | 1 | 8.57 |
| CHEMBL3889951 | — | — | 1 | 8.51 |
| CHEMBL3912281 | — | — | 1 | 8.46 |
| CHEMBL1084546 | PF-00562271 | 1.0 | 1 | 7.89 |
| CHEMBL3965256 | — | — | 1 | 7.71 |
| CHEMBL3939286 | — | — | 1 | 7.58 |
| CHEMBL3914036 | — | — | 1 | 7.52 |
| CHEMBL3892377 | — | — | 1 | 6.91 |
| CHEMBL3927099 | — | — | 1 | 6.70 |
| CHEMBL3936048 | — | — | 1 | 6.59 |
| CHEMBL3898282 | — | — | 1 | 5.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3949755 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL3958414 | — | IC50 | = | 0.84 | nM | 9.08 |
| CHEMBL3956954 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3987106 | — | IC50 | = | 1.31 | nM | 8.88 |
| CHEMBL3899046 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3969464 | — | IC50 | = | 1.55 | nM | 8.81 |
| CHEMBL3908093 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3961368 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3977870 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3889951 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3912281 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL1084546 | PF-00562271 | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3965256 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL3939286 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3914036 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3892377 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL3927099 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL3936048 | — | IC50 | = | 256.0 | nM | 6.59 |
| CHEMBL3898282 | — | IC50 | = | 6625.0 | nM | 5.18 |