Assay Detail
Binding
CHEMBL4354364
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His-tagged TrkC cytoplasmic domain (510 to 825 residues) expressed in baculovirus using tyr 01 as substrate incubated for 1 hr by Z'-Lyte assay
19
Total Activities
19
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
Design, synthesis and biological evaluation of 3-(imidazo[1,2-a]pyrazin-3-ylethynyl)-2-methylbenzamides as potent and selective pan-tropomyosin receptor kinase (TRK) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.74 | 8.53 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4447582 | — | — | 1 | 8.53 |
| CHEMBL3889654 | LAROTRECTINIB | 4.0 | 1 | 8.46 |
| CHEMBL4579323 | — | — | 1 | 8.39 |
| CHEMBL4161036 | — | — | 1 | 8.36 |
| CHEMBL4461048 | — | — | 1 | 8.24 |
| CHEMBL4569549 | — | — | 1 | 8.21 |
| CHEMBL4438527 | — | — | 1 | 8.19 |
| CHEMBL4454061 | — | — | 1 | 8.05 |
| CHEMBL4587651 | — | — | 1 | 7.94 |
| CHEMBL4467462 | — | — | 1 | 7.94 |
| CHEMBL4446455 | — | — | 1 | 7.84 |
| CHEMBL4469795 | — | — | 1 | 7.78 |
| CHEMBL4531144 | — | — | 1 | 7.35 |
| CHEMBL4467427 | — | — | 1 | 7.17 |
| CHEMBL4473502 | — | — | 1 | 6.89 |
| CHEMBL4438225 | — | — | 1 | 6.16 |
| CHEMBL4440122 | — | — | 1 | 6.03 |
| CHEMBL4464655 | — | — | 1 | - |
| CHEMBL4464426 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4447582 | — | IC50 | = | 2.95 | nM | 8.53 |
| CHEMBL3889654 | LAROTRECTINIB | IC50 | = | 3.49 | nM | 8.46 |
| CHEMBL4579323 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4161036 | — | IC50 | = | 4.35 | nM | 8.36 |
| CHEMBL4461048 | — | IC50 | = | 5.71 | nM | 8.24 |
| CHEMBL4569549 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4438527 | — | IC50 | = | 6.52 | nM | 8.19 |
| CHEMBL4454061 | — | IC50 | = | 8.84 | nM | 8.05 |
| CHEMBL4587651 | — | IC50 | = | 11.48 | nM | 7.94 |
| CHEMBL4467462 | — | IC50 | = | 11.46 | nM | 7.94 |
| CHEMBL4446455 | — | IC50 | = | 14.55 | nM | 7.84 |
| CHEMBL4469795 | — | IC50 | = | 16.8 | nM | 7.78 |
| CHEMBL4531144 | — | IC50 | = | 44.58 | nM | 7.35 |
| CHEMBL4467427 | — | IC50 | = | 66.98 | nM | 7.17 |
| CHEMBL4473502 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL4438225 | — | IC50 | = | 692.5 | nM | 6.16 |
| CHEMBL4440122 | — | IC50 | = | 934.9 | nM | 6.03 |
| CHEMBL4464655 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4464426 | — | IC50 | > | 1000.0 | nM | - |