Assay Detail
Binding
CHEMBL5731041
Review assay metadata, readout intent, target linkage, and publication context from the same page.
TrkA Binding Assay: The ability of a compound to bind to TrkA was measured by Invitrogen's LanthaScreen¿ Eu Kinase Binding Assay. In this assay, His-tagged recombinant human TrkA (cytoplasmic domain) from Invitrogen is incubated with Invitrogen's Alexa-Fluor¿ Tracer 236, biotinylated anti-His, and europium-labeled Streptavidin, compound (2% DMSO final) in buffer (25 mM MOPS, pH 7.5, 5 mM MgCl2, 0.005% Triton X-100). After a 60-minute incubation at 22° C., the reaction was measured using the EnVision via TR-FRET dual wavelength detection, and the POC was calculated from the emission ratio. The compound dose response data was fit to a 4-parameter logistic model and IC50 was defined as the concentration of compound at 50 POC.
111
Total Activities
35
Compounds Tested
3
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
Macrocyclic compounds as Trk kinase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 7.06 | 7.26 |
| kon | 37 | - | - |
| k_off | 37 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5951632 | — | — | 3 | 7.26 |
| CHEMBL5838232 | — | — | 3 | 7.26 |
| CHEMBL5911587 | — | — | 3 | 7.26 |
| CHEMBL5961180 | — | — | 3 | 7.26 |
| CHEMBL5933891 | — | — | 3 | 7.26 |
| CHEMBL5857084 | — | — | 3 | 7.26 |
| CHEMBL6042579 | — | — | 3 | 7.26 |
| CHEMBL5873607 | — | — | 3 | 7.26 |
| CHEMBL5755646 | — | — | 3 | 7.26 |
| CHEMBL5750604 | — | — | 3 | 7.26 |
| CHEMBL5948704 | — | — | 3 | 7.26 |
| CHEMBL6027001 | — | — | 6 | 7.26 |
| CHEMBL5945078 | — | — | 3 | 7.26 |
| CHEMBL5904612 | — | — | 3 | 7.26 |
| CHEMBL5917350 | — | — | 6 | 7.26 |
| CHEMBL5950386 | — | — | 3 | 7.26 |
| CHEMBL6049913 | — | — | 3 | 7.26 |
| CHEMBL5893788 | — | — | 3 | 7.26 |
| CHEMBL5884156 | — | — | 3 | 7.26 |
| CHEMBL5859966 | — | — | 3 | 7.26 |
| CHEMBL5785412 | — | — | 3 | 7.26 |
| CHEMBL5920025 | — | — | 3 | 7.26 |
| CHEMBL5755453 | — | — | 3 | 7.26 |
| CHEMBL5883373 | — | — | 3 | 7.26 |
| CHEMBL5773504 | — | — | 3 | 7.26 |
| CHEMBL5964251 | — | — | 3 | 7.26 |
| CHEMBL5954185 | — | — | 3 | 7.26 |
| CHEMBL5748453 | — | — | 3 | 7.26 |
| CHEMBL5937561 | — | — | 3 | 7.26 |
| CHEMBL6000044 | — | — | 3 | 7.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5884156 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL6027001 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5748453 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5948704 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5954185 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL6027001 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5750604 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5937561 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5945078 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL6000044 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5904612 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5755646 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5917350 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5964251 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5917350 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL6042579 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5933891 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5773504 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5857084 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5859966 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5893788 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL6049913 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5785412 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5950386 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5951632 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5873607 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5920025 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5755453 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5838232 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5883373 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5911587 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5961180 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5785570 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL5891353 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL5796897 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL5840790 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL5877251 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL5937561 | — | k_off | = | - | s-1 | - |
| CHEMBL5785570 | — | k_off | = | - | s-1 | - |
| CHEMBL5877251 | — | k_off | = | - | s-1 | - |
| CHEMBL5937561 | — | kon | = | - | — | - |
| CHEMBL5785412 | — | k_off | = | - | s-1 | - |
| CHEMBL5964251 | — | kon | = | - | — | - |
| CHEMBL5785412 | — | kon | = | - | — | - |
| CHEMBL5964251 | — | k_off | = | - | s-1 | - |
| CHEMBL6000044 | — | k_off | = | - | s-1 | - |
| CHEMBL5884156 | — | k_off | = | - | s-1 | - |
| CHEMBL6000044 | — | kon | = | - | — | - |
| CHEMBL5859966 | — | k_off | = | - | s-1 | - |
| CHEMBL5877251 | — | kon | = | - | — | - |