Assay Detail
Binding
CHEMBL997164
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity of human N-terminal His-tagged p38alpha expressed in Escherichia coli BL21 (DE3)
9
Total Activities
9
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
Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 9 | 6.99 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL522387 | — | — | 1 | 7.92 |
| CHEMBL526560 | — | — | 1 | 7.30 |
| CHEMBL498947 | — | — | 1 | 7.26 |
| CHEMBL497615 | — | — | 1 | 7.13 |
| CHEMBL526930 | — | — | 1 | 6.90 |
| CHEMBL510516 | — | — | 1 | 6.61 |
| CHEMBL497033 | — | — | 1 | 6.47 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 6.30 |
| CHEMBL188762 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL522387 | — | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL526560 | — | Kd | = | 50.0 | nM | 7.30 |
| CHEMBL498947 | — | Kd | = | 55.0 | nM | 7.26 |
| CHEMBL497615 | — | Kd | = | 74.0 | nM | 7.13 |
| CHEMBL526930 | — | Kd | = | 127.0 | nM | 6.90 |
| CHEMBL510516 | — | Kd | = | 245.0 | nM | 6.61 |
| CHEMBL497033 | — | Kd | = | 342.0 | nM | 6.47 |
| CHEMBL5416410 | DASATINIB | Kd | = | 495.0 | nM | 6.30 |
| CHEMBL188762 | — | Kd | - | — | - |