Assay Detail
Binding
CHEMBL5729947
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: A partial protein of only a kinase domain of FLT3 protein was purchased from Carna Biosciences Inc., Japan, and tests were conducted as in Test Example 5. Test Example 5: A partial protein of only a kinase domain of RET protein was purchased from Carna Biosciences Inc., Japan. The phosphorylation activity toward a peptide substrate was investigated using an EZ reader (Caliper). Test compounds were each mixed with a protein solution to give 8 final concentrations from 100 nM to 0.03 nM, followed by addition of a mixed liquid of ATP and substrate peptide (Caliper) and reaction for 30 minutes. The ATP concentration used was 100 µM. A reaction liquid which contained protein but no test compound (in which the solvent DMSO alone was added at 0.8% in place of the test compound) was prepared, followed by reaction in the same manner with or without ATP addition.
54
Total Activities
18
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Diamino heterocyclic carboxamide compound
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 9.35 | 9.47 |
| kon | 18 | - | - |
| k_off | 18 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3687210 | — | — | 3 | 9.47 |
| CHEMBL3687202 | — | — | 3 | 9.46 |
| CHEMBL3687222 | — | — | 3 | 9.44 |
| CHEMBL3687215 | — | — | 3 | 9.44 |
| CHEMBL3687225 | — | — | 3 | 9.43 |
| CHEMBL3687212 | — | — | 3 | 9.43 |
| CHEMBL3687207 | — | — | 3 | 9.41 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 3 | 9.39 |
| CHEMBL3687191 | — | — | 3 | 9.36 |
| CHEMBL3687195 | — | — | 3 | 9.34 |
| CHEMBL3687223 | — | — | 3 | 9.31 |
| CHEMBL3687200 | — | — | 3 | 9.30 |
| CHEMBL3687220 | — | — | 3 | 9.29 |
| CHEMBL3687194 | — | — | 3 | 9.29 |
| CHEMBL3687224 | — | — | 3 | 9.28 |
| CHEMBL3687221 | — | — | 3 | 9.25 |
| CHEMBL3687205 | — | — | 3 | 9.18 |
| CHEMBL3687217 | — | — | 3 | 9.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3687210 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL3687202 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL3687215 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL3687222 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL3687225 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL3687212 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL3687207 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL3301622 | GILTERITINIB | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL3687191 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL3687195 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL3687223 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL3687200 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3687220 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL3687194 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL3687224 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL3687221 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL3687205 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL3687217 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL3687212 | — | kon | = | - | — | - |
| CHEMBL3687210 | — | k_off | = | - | s-1 | - |
| CHEMBL3687210 | — | kon | = | - | — | - |
| CHEMBL3687207 | — | k_off | = | - | s-1 | - |
| CHEMBL3687207 | — | kon | = | - | — | - |
| CHEMBL3687205 | — | k_off | = | - | s-1 | - |
| CHEMBL3687217 | — | k_off | = | - | s-1 | - |
| CHEMBL3687202 | — | k_off | = | - | s-1 | - |
| CHEMBL3687202 | — | kon | = | - | — | - |
| CHEMBL3687200 | — | k_off | = | - | s-1 | - |
| CHEMBL3687200 | — | kon | = | - | — | - |
| CHEMBL3687195 | — | k_off | = | - | s-1 | - |
| CHEMBL3687195 | — | kon | = | - | — | - |
| CHEMBL3687194 | — | k_off | = | - | s-1 | - |
| CHEMBL3687194 | — | kon | = | - | — | - |
| CHEMBL3687191 | — | k_off | = | - | s-1 | - |
| CHEMBL3687191 | — | kon | = | - | — | - |
| CHEMBL3687205 | — | kon | = | - | — | - |
| CHEMBL3687222 | — | k_off | = | - | s-1 | - |
| CHEMBL3687222 | — | kon | = | - | — | - |
| CHEMBL3687223 | — | k_off | = | - | s-1 | - |
| CHEMBL3687221 | — | k_off | = | - | s-1 | - |
| CHEMBL3687221 | — | kon | = | - | — | - |
| CHEMBL3687224 | — | kon | = | - | — | - |
| CHEMBL3301622 | GILTERITINIB | k_off | = | - | s-1 | - |
| CHEMBL3687224 | — | k_off | = | - | s-1 | - |
| CHEMBL3301622 | GILTERITINIB | kon | = | - | — | - |
| CHEMBL3687225 | — | kon | = | - | — | - |
| CHEMBL3687220 | — | k_off | = | - | s-1 | - |
| CHEMBL3687220 | — | kon | = | - | — | - |
| CHEMBL3687223 | — | kon | = | - | — | - |
| CHEMBL3687225 | — | k_off | = | - | s-1 | - |