Assay Detail
Binding
CHEMBL5737241
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Verification on Inhibitory Activities of TAM Receptor Inhibiting Compounds on Tyro 3, Axl, and Mer: For evaluation of inhibitory activities of the compounds according to the present invention on Tyro 3, Axl, and Mer, the following test was carried out.The specific test method followed the method provided by Cisbio. The compounds of the examples were prepared at various concentrations, followed by addition of Tyro 3, Axl, or Mer and substrate peptides, and then ATP was added to initiate a reaction. After 1 hour, the reaction was stopped by addition of a solution containing EDTA. Thereafter, the amount of phosphorylated peptides was measured. Here, the phosphorylated peptides were treated with an europium (Eu)-labeled antibody recognizing phosphorylated peptides, and then after 1 hour, excited by irradiation of the light of a wavelength of 320 or 340 nm using an Envision Reader. The amount of light emitted at 665 nm was measured to investigate the degrees of inhibition of TAM receptors. The TAM receptor inhibitory activities (IC50 values) of the respective compounds were analyzed using the GraphPad Prism program, and tabulated in Tables 1 to 3 below. LDC1267 (CAS no. 1361030-48-9, Calbiochem), which is a TAM receptor inhibitor compound, was used as a positive control.
426
Total Activities
138
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 |
Publication
Pyrimidine derivative compound, optical isomer thereof, or pharmaceutically acceptable salt thereof, and composition for preventing or treating Tyro 3 related disease comprising same as active ingredient
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 142 | 6.80 | 9.92 |
| kon | 142 | - | - |
| k_off | 142 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5774701 | — | — | 3 | 9.92 |
| CHEMBL5825584 | — | — | 3 | 9.44 |
| CHEMBL5745182 | — | — | 3 | 9.11 |
| CHEMBL6034792 | — | — | 3 | 9.09 |
| CHEMBL5821741 | — | — | 3 | 9.05 |
| CHEMBL5814386 | — | — | 3 | 9.04 |
| CHEMBL5839005 | — | — | 3 | 9.00 |
| CHEMBL5981096 | — | — | 6 | 8.89 |
| CHEMBL5839331 | — | — | 3 | 8.85 |
| CHEMBL6049233 | — | — | 3 | 8.72 |
| CHEMBL5752800 | — | — | 3 | 8.48 |
| CHEMBL6012801 | — | — | 3 | 8.37 |
| CHEMBL5740011 | — | — | 3 | 8.36 |
| CHEMBL5967645 | — | — | 3 | 8.31 |
| CHEMBL5908464 | — | — | 3 | 8.16 |
| CHEMBL5903211 | — | — | 3 | 8.00 |
| CHEMBL5993520 | — | — | 3 | 7.92 |
| CHEMBL5926926 | — | — | 3 | 7.92 |
| CHEMBL5926568 | — | — | 3 | 7.82 |
| CHEMBL5957299 | — | — | 3 | 7.80 |
| CHEMBL6060115 | — | — | 3 | 7.80 |
| CHEMBL5965106 | — | — | 3 | 7.64 |
| CHEMBL5846250 | — | — | 3 | 7.60 |
| CHEMBL5873205 | — | — | 6 | 7.58 |
| CHEMBL5919842 | — | — | 3 | 7.55 |
| CHEMBL5997590 | — | — | 3 | 7.52 |
| CHEMBL5833192 | — | — | 3 | 7.50 |
| CHEMBL6022455 | — | — | 3 | 7.50 |
| CHEMBL5919001 | — | — | 3 | 7.48 |
| CHEMBL5741898 | — | — | 3 | 7.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5774701 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL5825584 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL5745182 | — | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL6034792 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL5821741 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5814386 | — | IC50 | = | 0.91 | nM | 9.04 |
| CHEMBL5839005 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5981096 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5839331 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL6049233 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5752800 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL6012801 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5740011 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5967645 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL5908464 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL5903211 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5993520 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5926926 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5926568 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5957299 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL6060115 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5965106 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5846250 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5873205 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5919842 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5997590 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL6022455 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5833192 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5919001 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5741898 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL6035885 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5873205 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5965254 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5981096 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3808844 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL3808844 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL3808844 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5779005 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL5803120 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL6042369 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL5793825 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL5916277 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5874363 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5741930 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5825621 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL6019126 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5895995 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5781552 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5935947 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL6005928 | — | IC50 | = | 180.0 | nM | 6.75 |