Assay Detail
Binding
CHEMBL5722908
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Inhibition of full-length PYK2 (unknown origin) with C-terminal NanoLuc-fusion expressed in HEK293T cells by NanoBRET assay
9
Total Activities
9
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-kinetic relationship reveals the mechanism of selectivity of FAK inhibitors over PYK2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.09 | 7.10 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | MONDO:0004992 |
| EFO_TERM | EFO_TERM | - | — | cancer |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL472212 | — | — | 1 | 7.10 |
| CHEMBL5722981 | — | — | 1 | 7.08 |
| CHEMBL5723019 | — | — | 1 | 6.92 |
| CHEMBL1084546 | PF-00562271 | 1.0 | 1 | 6.82 |
| CHEMBL3137331 | DEFACTINIB | 3.0 | 1 | 6.20 |
| CHEMBL5722989 | — | — | 1 | 6.01 |
| CHEMBL514554 | — | — | 1 | 5.44 |
| CHEMBL5722987 | — | — | 1 | 4.64 |
| CHEMBL5722946 | — | — | 1 | 4.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL472212 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL5722981 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL5723019 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL1084546 | PF-00562271 | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL3137331 | DEFACTINIB | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL5722989 | — | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL514554 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL5722987 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL5722946 | — | Ki | = | 26000.0 | nM | 4.58 |