Assay Detail
Functional
CHEMBL867241
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PAE cells overexpressing TrkA
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | PAE |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
High affinity nerve growth factor receptor (CHEMBL2815) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of novel isothiazole inhibitors of the TrkA kinase: structure-activity relationship, computer modeling, optimization, and identification of highly potent antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.64 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL211095 | — | — | 1 | 8.15 |
| CHEMBL211168 | — | — | 1 | 7.77 |
| CHEMBL211160 | — | — | 1 | 7.34 |
| CHEMBL425066 | — | — | 1 | 7.16 |
| CHEMBL209466 | — | — | 1 | 7.02 |
| CHEMBL445660 | — | — | 1 | 6.96 |
| CHEMBL211883 | — | — | 1 | 6.93 |
| CHEMBL210340 | — | — | 1 | 6.54 |
| CHEMBL378978 | — | — | 1 | 6.52 |
| CHEMBL377040 | — | — | 1 | 6.46 |
| CHEMBL208881 | — | — | 1 | 6.24 |
| CHEMBL210933 | — | — | 1 | 6.22 |
| CHEMBL211328 | — | — | 1 | 6.12 |
| CHEMBL211880 | — | — | 1 | 6.01 |
| CHEMBL211858 | — | — | 1 | 5.99 |
| CHEMBL209535 | — | — | 1 | 5.93 |
| CHEMBL210331 | — | — | 1 | 5.54 |
| CHEMBL211096 | — | — | 1 | - |
| CHEMBL210139 | — | — | 1 | - |
| CHEMBL210090 | — | — | 1 | - |
| CHEMBL212317 | — | — | 1 | - |
| CHEMBL377444 | — | — | 1 | - |
| CHEMBL384214 | — | — | 1 | - |
| CHEMBL378736 | — | — | 1 | - |
| CHEMBL209506 | — | — | 1 | - |
| CHEMBL377243 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL211095 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL211168 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL211160 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL425066 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL209466 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL445660 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL211883 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL210340 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL378978 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL377040 | — | IC50 | = | 344.0 | nM | 6.46 |
| CHEMBL208881 | — | IC50 | = | 581.0 | nM | 6.24 |
| CHEMBL210933 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL211328 | — | IC50 | = | 756.0 | nM | 6.12 |
| CHEMBL211880 | — | IC50 | = | 978.0 | nM | 6.01 |
| CHEMBL211858 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL209535 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL210331 | — | IC50 | = | 2870.0 | nM | 5.54 |
| CHEMBL211096 | — | IC50 | - | — | - | |
| CHEMBL210139 | — | IC50 | - | — | - | |
| CHEMBL210090 | — | IC50 | - | — | - | |
| CHEMBL212317 | — | IC50 | - | — | - | |
| CHEMBL377444 | — | IC50 | - | — | - | |
| CHEMBL384214 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL378736 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL209506 | — | IC50 | - | — | - | |
| CHEMBL377243 | — | IC50 | - | — | - |