Assay Detail
Binding
CHEMBL5734096
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: Inhibition constants of MerTK, Flt3, Tyro3 and Axl kinase activity by an active compound as described herein is determined at the Km for ATP using a microfluidic capillary electrophoresis (MCE) assay in which phosphorylated and unphosphorylated substrate peptides were separated and analyzed using a LabChip EZ Reader.Briefly, activity assays were performed in a 384 well, polypropylene microplate in a final volume of 50 μl, of 50 mM Hepes, Ph 7.4 containing 10 mM MgCl2, 1.0 mM DTT, 0.01% Triton X-100, 0.1% Bovine Serum Albumin (BSA), containing 1.0 μM fluorescent substrate and ATP at the Km for each enzyme. All reactions were terminated by addition of 20 μL of 70 mM EDTA. After a 180 mM incubation, phosphorylated and unphosphorylated substrate peptides were separated in buffer supplemented with 1×CR-8 on a LabChip EZ Reader equipped with a 12-sipper chip. Data were analyzed using EZ Reader software. Assay conditions for MCE assays
120
Total Activities
40
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Tyrosine-protein kinase receptor UFO (CHEMBL4895) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Therapeutic uses of selected pyrrolopyrimidine compounds with anti-mer tyrosine kinase activity
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 7.09 | 8.00 |
| kon | 40 | - | - |
| k_off | 40 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5859186 | — | — | 3 | 8.00 |
| CHEMBL5987550 | — | — | 3 | 7.85 |
| CHEMBL5954941 | — | — | 3 | 7.80 |
| CHEMBL5756274 | — | — | 3 | 7.80 |
| CHEMBL5946790 | — | — | 3 | 7.72 |
| CHEMBL5833137 | — | — | 3 | 7.68 |
| CHEMBL3326004 | — | — | 3 | 7.66 |
| CHEMBL5855696 | — | — | 3 | 7.64 |
| CHEMBL5783827 | — | — | 3 | 7.64 |
| CHEMBL5999759 | — | — | 3 | 7.62 |
| CHEMBL5786246 | — | — | 3 | 7.58 |
| CHEMBL5741347 | — | — | 3 | 7.54 |
| CHEMBL5811066 | — | — | 3 | 7.50 |
| CHEMBL5926635 | — | — | 3 | 7.50 |
| CHEMBL5909081 | — | — | 3 | 7.42 |
| CHEMBL5841713 | — | — | 3 | 7.42 |
| CHEMBL3326003 | — | — | 3 | 7.36 |
| CHEMBL5781955 | — | — | 3 | 7.31 |
| CHEMBL5884595 | — | — | 3 | 7.29 |
| CHEMBL5939104 | — | — | 3 | 7.22 |
| CHEMBL6042505 | — | — | 3 | 7.17 |
| CHEMBL5775786 | — | — | 3 | 7.17 |
| CHEMBL5751372 | — | — | 3 | 7.15 |
| CHEMBL5903745 | — | — | 3 | 7.11 |
| CHEMBL5779208 | — | — | 3 | 7.04 |
| CHEMBL5763958 | — | — | 3 | 7.03 |
| CHEMBL5945173 | — | — | 3 | 7.03 |
| CHEMBL6051061 | — | — | 3 | 6.87 |
| CHEMBL5740093 | — | — | 3 | 6.86 |
| CHEMBL6059816 | — | — | 3 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5859186 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5987550 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5954941 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5756274 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5946790 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5833137 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3326004 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5855696 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5783827 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5999759 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5786246 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5741347 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5811066 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5926635 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5909081 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5841713 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3326003 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5781955 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5884595 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL5939104 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5775786 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL6042505 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5751372 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL5903745 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5779208 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL5763958 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL5945173 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL6051061 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL5740093 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL6059816 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL5836590 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL5911874 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL5787997 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL5954972 | — | IC50 | = | 421.0 | nM | 6.38 |
| CHEMBL5829651 | — | IC50 | = | 533.0 | nM | 6.27 |
| CHEMBL5977105 | — | IC50 | = | 609.0 | nM | 6.21 |
| CHEMBL6027781 | — | IC50 | = | 1073.0 | nM | 5.97 |
| CHEMBL5818859 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL6041800 | — | IC50 | = | 1613.0 | nM | 5.79 |
| CHEMBL3326008 | — | IC50 | = | 3948.0 | nM | 5.40 |
| CHEMBL3326004 | — | k_off | = | - | s-1 | - |
| CHEMBL6042505 | — | kon | = | - | — | - |
| CHEMBL3326004 | — | kon | = | - | — | - |
| CHEMBL6041800 | — | kon | = | - | — | - |
| CHEMBL6041800 | — | k_off | = | - | s-1 | - |
| CHEMBL5740093 | — | k_off | = | - | s-1 | - |
| CHEMBL3326003 | — | kon | = | - | — | - |
| CHEMBL3326003 | — | k_off | = | - | s-1 | - |
| CHEMBL5818859 | — | kon | = | - | — | - |
| CHEMBL6027781 | — | kon | = | - | — | - |