Assay Detail
Binding
CHEMBL4399997
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His-tagged TrkA kinase domain (441-796 residues) expressed in baculovirus expression system incubated with enzyme/ATP mixture for 20 mins by HTRF assay
31
Total Activities
31
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 |
Target
High affinity nerve growth factor receptor (CHEMBL2815) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Type 2 inhibitor leads of human tropomyosin receptor kinase (hTrkA).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.41 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL457614 | — | — | 1 | 9.52 |
| CHEMBL4555143 | — | — | 1 | 8.57 |
| CHEMBL4447685 | — | — | 1 | 8.52 |
| CHEMBL4475899 | — | — | 1 | 7.85 |
| CHEMBL4579301 | — | — | 1 | 7.27 |
| CHEMBL1707321 | — | — | 1 | 7.11 |
| CHEMBL4440941 | — | — | 1 | 7.01 |
| CHEMBL1710419 | — | — | 1 | 6.92 |
| CHEMBL4473447 | — | — | 1 | 6.86 |
| CHEMBL4535656 | — | — | 1 | 6.84 |
| CHEMBL4525857 | — | — | 1 | 6.69 |
| CHEMBL4453766 | — | — | 1 | 6.59 |
| CHEMBL4444267 | — | — | 1 | 6.58 |
| CHEMBL4573099 | — | — | 1 | 6.55 |
| CHEMBL4472006 | — | — | 1 | 6.43 |
| CHEMBL4454926 | — | — | 1 | 6.29 |
| CHEMBL4534509 | — | — | 1 | 6.17 |
| CHEMBL4476611 | — | — | 1 | 6.11 |
| CHEMBL4574596 | — | — | 1 | 6.07 |
| CHEMBL4469499 | — | — | 1 | 5.99 |
| CHEMBL4471969 | — | — | 1 | 5.61 |
| CHEMBL4584676 | — | — | 1 | 5.56 |
| CHEMBL1440955 | — | — | 1 | 5.30 |
| CHEMBL4556526 | — | — | 1 | 5.30 |
| CHEMBL4574946 | — | — | 1 | 5.30 |
| CHEMBL4462705 | — | — | 1 | 5.30 |
| CHEMBL1901362 | — | — | 1 | 5.30 |
| CHEMBL4452308 | — | — | 1 | 5.30 |
| CHEMBL4465070 | — | — | 1 | 5.30 |
| CHEMBL4519300 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL457614 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4555143 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4447685 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4475899 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL4579301 | — | IC50 | = | 53.6 | nM | 7.27 |
| CHEMBL1707321 | — | IC50 | = | 77.6 | nM | 7.11 |
| CHEMBL4440941 | — | IC50 | = | 97.4 | nM | 7.01 |
| CHEMBL1710419 | — | IC50 | = | 121.7 | nM | 6.92 |
| CHEMBL4473447 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL4535656 | — | IC50 | = | 143.7 | nM | 6.84 |
| CHEMBL4525857 | — | IC50 | = | 204.6 | nM | 6.69 |
| CHEMBL4453766 | — | IC50 | = | 259.6 | nM | 6.59 |
| CHEMBL4444267 | — | IC50 | = | 264.4 | nM | 6.58 |
| CHEMBL4573099 | — | IC50 | = | 283.5 | nM | 6.55 |
| CHEMBL4472006 | — | IC50 | = | 371.4 | nM | 6.43 |
| CHEMBL4454926 | — | IC50 | = | 517.3 | nM | 6.29 |
| CHEMBL4534509 | — | IC50 | = | 667.7 | nM | 6.17 |
| CHEMBL4476611 | — | IC50 | = | 775.2 | nM | 6.11 |
| CHEMBL4574596 | — | IC50 | = | 843.1 | nM | 6.07 |
| CHEMBL4469499 | — | IC50 | = | 1017.1 | nM | 5.99 |
| CHEMBL4471969 | — | IC50 | = | 2449.6 | nM | 5.61 |
| CHEMBL4584676 | — | IC50 | = | 2726.5 | nM | 5.56 |
| CHEMBL1440955 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4556526 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4574946 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4462705 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL1901362 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4452308 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4465070 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4519300 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4549993 | — | IC50 | = | 5000.0 | nM | 5.30 |