Assay Detail
Binding
CHEMBL3887112
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: Reagents and consumables were purchased from Sigma Aldrich, Carna Biosciences, or Caliper Life Sciences. All assay reaction conditions for IC50 determinations were within the linear range with respect to time and enzyme concentration. In a 384 well polypropylene plate, TrkA (0.4 nM, Carna 08-186) was pre-incubated in a 100 mM Hepes-NaOH pH 7.5 buffer containing 0.01% Triton X-100, 10 mM MgCl2, 0.1% BSA, 1 mM DTT, 10 uM sodium orthovanadate and 10 uM beta-glycerophosphate and compound with a concentration of 2.5% DMSO for 15 minutes at room temperature. The reaction was initiated with an equal volume of peptide substrate (Caliper Life Sciences catalog no. 760430) and ATP in the aforementioned buffer. The final concentrations in the reaction were 200 pM TrkA, 1.5 uM peptide substrate and 55 uM ATP (ATP Km). The reaction was incubated at room temperature for 180 minutes and terminated with a buffer containing excess EDTA (100 mM Hepes-NaOH pH 7.5, 0.02% Brij.
80
Total Activities
79
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
High affinity nerve growth factor receptor (CHEMBL2815) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Tropomyosin-related kinase (TRK) inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 80 | 7.63 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3678283 | — | — | 1 | 9.70 |
| CHEMBL3678287 | — | — | 1 | 9.70 |
| CHEMBL3678284 | — | — | 1 | 9.70 |
| CHEMBL3678285 | — | — | 1 | 9.70 |
| CHEMBL3673477 | — | — | 1 | 9.70 |
| CHEMBL3673478 | — | — | 1 | 9.70 |
| CHEMBL3673479 | — | — | 1 | 9.70 |
| CHEMBL3678286 | — | — | 1 | 9.70 |
| CHEMBL3673452 | GZ-389988 | 2.0 | 1 | 9.52 |
| CHEMBL3673489 | — | — | 1 | 9.52 |
| CHEMBL3678297 | — | — | 1 | 9.52 |
| CHEMBL3678300 | — | — | 1 | 9.40 |
| CHEMBL3673480 | — | — | 1 | 9.30 |
| CHEMBL3673453 | — | — | 1 | 9.30 |
| CHEMBL3673476 | — | — | 1 | 9.22 |
| CHEMBL3673463 | — | — | 1 | 9.05 |
| CHEMBL3673436 | — | — | 1 | 9.00 |
| CHEMBL3678301 | — | — | 1 | 9.00 |
| CHEMBL3673462 | — | — | 1 | 9.00 |
| CHEMBL3673486 | — | — | 1 | 8.70 |
| CHEMBL3673439 | — | — | 1 | 8.52 |
| CHEMBL3673483 | — | — | 1 | 8.52 |
| CHEMBL3678292 | — | — | 1 | 8.52 |
| CHEMBL3673488 | — | — | 1 | 8.40 |
| CHEMBL3673487 | — | — | 1 | 8.30 |
| CHEMBL3678298 | — | — | 1 | 8.30 |
| CHEMBL3673481 | — | — | 1 | 8.22 |
| CHEMBL3673442 | — | — | 1 | 8.22 |
| CHEMBL3678299 | — | — | 1 | 8.15 |
| CHEMBL3673440 | — | — | 1 | 8.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3678287 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3678285 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3678286 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3673477 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3678283 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3673478 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3673479 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3678284 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3678297 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3673452 | GZ-389988 | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3673489 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3678300 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3673453 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3673480 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3673476 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3673463 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3678301 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3673436 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3673462 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3673486 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3673439 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3678292 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3673483 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3673488 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3673487 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3678298 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3673481 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3673442 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3673440 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3678299 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3678289 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3673461 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3673438 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3673482 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3673485 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3678302 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3673459 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3673464 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3673475 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3673468 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3678303 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3678291 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3673466 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3673484 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3673455 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3678290 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3678288 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3678293 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3673437 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL3673467 | — | IC50 | = | 88.0 | nM | 7.06 |