Assay Detail
Binding
CHEMBL1003980
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Inhibition of human TrkA expressed in Sf9 cells by amplified luminescent proximity assay
18
Total Activities
18
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 |
Target
High affinity nerve growth factor receptor (CHEMBL2815) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of 4-aminopyrazolylpyrimidines as potent inhibitors of Trk kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.11 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL254895 | — | — | 1 | 9.22 |
| CHEMBL176544 | — | — | 1 | 8.70 |
| CHEMBL456976 | — | — | 1 | 8.22 |
| CHEMBL514257 | — | — | 1 | 8.00 |
| CHEMBL516142 | — | — | 1 | 7.89 |
| CHEMBL456985 | — | — | 1 | 7.82 |
| CHEMBL517943 | — | — | 1 | 7.00 |
| CHEMBL464801 | — | — | 1 | 7.00 |
| CHEMBL505965 | — | — | 1 | 6.92 |
| CHEMBL515822 | — | — | 1 | 6.92 |
| CHEMBL497854 | — | — | 1 | 6.57 |
| CHEMBL464800 | — | — | 1 | 6.44 |
| CHEMBL456549 | — | — | 1 | 6.19 |
| CHEMBL521895 | — | — | 1 | 6.14 |
| CHEMBL496483 | — | — | 1 | 6.12 |
| CHEMBL464179 | — | — | 1 | 5.93 |
| CHEMBL507748 | — | — | 1 | 5.72 |
| CHEMBL211095 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL254895 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL176544 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL456976 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL514257 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL516142 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL456985 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL517943 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL464801 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL505965 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL515822 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL497854 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL464800 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL456549 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL521895 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL496483 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL464179 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL507748 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL211095 | — | IC50 | < | 1.0 | nM | - |