Assay Detail
Binding
CHEMBL4772612
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TrkA (unknown origin) using Tyr1 peptide as substrate in presence of ATP measured after 2 hrs by FRET-based Z-Lyte kinase assay
29
Total Activities
29
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
Design, synthesis, and Structure-Activity Relationships (SAR) of 3-vinylindazole derivatives as new selective tropomyosin receptor kinases (Trk) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.88 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4785469 | — | — | 1 | 8.82 |
| CHEMBL4792981 | — | — | 1 | 8.80 |
| CHEMBL4780049 | — | — | 1 | 8.70 |
| CHEMBL3889654 | LAROTRECTINIB | 4.0 | 1 | 8.54 |
| CHEMBL4800232 | — | — | 1 | 8.51 |
| CHEMBL4783132 | — | — | 1 | 8.46 |
| CHEMBL4800162 | — | — | 1 | 8.43 |
| CHEMBL4795019 | — | — | 1 | 8.24 |
| CHEMBL4787950 | — | — | 1 | 8.12 |
| CHEMBL4783102 | — | — | 1 | 8.06 |
| CHEMBL4796220 | — | — | 1 | 7.98 |
| CHEMBL4786112 | — | — | 1 | 7.98 |
| CHEMBL4787602 | — | — | 1 | 7.98 |
| CHEMBL4795806 | — | — | 1 | 7.97 |
| CHEMBL4777347 | — | — | 1 | 7.92 |
| CHEMBL4782515 | — | — | 1 | 7.88 |
| CHEMBL4780099 | — | — | 1 | 7.75 |
| CHEMBL4777099 | — | — | 1 | 7.68 |
| CHEMBL4778721 | — | — | 1 | 7.63 |
| CHEMBL4797186 | — | — | 1 | 7.62 |
| CHEMBL4779607 | — | — | 1 | 7.54 |
| CHEMBL4776591 | — | — | 1 | 7.39 |
| CHEMBL4778234 | — | — | 1 | 7.31 |
| CHEMBL4794286 | — | — | 1 | 7.12 |
| CHEMBL4799340 | — | — | 1 | 6.96 |
| CHEMBL4792043 | — | — | 1 | 6.72 |
| CHEMBL4799455 | — | — | 1 | 6.60 |
| CHEMBL4796985 | — | — | 1 | - |
| CHEMBL4779366 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4785469 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4792981 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4780049 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3889654 | LAROTRECTINIB | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4800232 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4783132 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4800162 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4795019 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4787950 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL4783102 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL4796220 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL4786112 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL4787602 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL4795806 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL4777347 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4782515 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL4780099 | — | IC50 | = | 17.8 | nM | 7.75 |
| CHEMBL4777099 | — | IC50 | = | 20.9 | nM | 7.68 |
| CHEMBL4778721 | — | IC50 | = | 23.3 | nM | 7.63 |
| CHEMBL4797186 | — | IC50 | = | 23.9 | nM | 7.62 |
| CHEMBL4779607 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4776591 | — | IC50 | = | 40.6 | nM | 7.39 |
| CHEMBL4778234 | — | IC50 | = | 49.3 | nM | 7.31 |
| CHEMBL4794286 | — | IC50 | = | 76.3 | nM | 7.12 |
| CHEMBL4799340 | — | IC50 | = | 110.6 | nM | 6.96 |
| CHEMBL4792043 | — | IC50 | = | 188.6 | nM | 6.72 |
| CHEMBL4799455 | — | IC50 | = | 253.6 | nM | 6.60 |
| CHEMBL4796985 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4779366 | — | IC50 | > | 1000.0 | nM | - |