Assay Detail
Binding
CHEMBL854264
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Inhibition of endogenous FLT3 in EOL1 cells
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | EOL1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 5.69 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL377193 | — | — | 1 | 7.40 |
| CHEMBL207858 | — | — | 1 | 7.22 |
| CHEMBL210989 | — | — | 1 | 6.77 |
| CHEMBL209823 | — | — | 1 | 6.47 |
| CHEMBL210355 | — | — | 1 | 6.28 |
| CHEMBL7735 | — | — | 1 | 6.24 |
| CHEMBL210486 | — | — | 1 | 6.17 |
| CHEMBL210420 | — | — | 1 | 6.16 |
| CHEMBL207895 | — | — | 1 | 6.13 |
| CHEMBL378133 | — | — | 1 | 6.06 |
| CHEMBL7602 | — | — | 1 | 6.05 |
| CHEMBL377652 | — | — | 1 | 6.04 |
| CHEMBL210477 | — | — | 1 | 6.00 |
| CHEMBL7724 | AG1295 | — | 1 | 5.96 |
| CHEMBL378558 | — | — | 1 | 5.92 |
| CHEMBL210494 | — | — | 1 | 5.89 |
| CHEMBL209084 | — | — | 1 | 5.82 |
| CHEMBL209042 | — | — | 1 | 5.64 |
| CHEMBL208640 | — | — | 1 | 5.58 |
| CHEMBL209515 | — | — | 1 | 5.58 |
| CHEMBL7296 | — | — | 1 | 5.50 |
| CHEMBL210726 | — | — | 1 | 5.47 |
| CHEMBL206894 | — | — | 1 | 5.36 |
| CHEMBL207483 | — | — | 1 | 5.34 |
| CHEMBL378930 | — | — | 1 | 5.18 |
| CHEMBL377873 | — | — | 1 | 5.17 |
| CHEMBL209774 | — | — | 1 | 5.12 |
| CHEMBL206915 | — | — | 1 | 5.03 |
| CHEMBL209233 | — | — | 1 | 5.00 |
| CHEMBL210425 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL377193 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL207858 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL210989 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL209823 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL210355 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL7735 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL210486 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL210420 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL207895 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL378133 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL7602 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL377652 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL210477 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL7724 | AG1295 | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL378558 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL210494 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL209084 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL209042 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL208640 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL209515 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL7296 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL210726 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL206894 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL207483 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL378930 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL377873 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL209774 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL206915 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL210956 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL383276 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL210368 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL380038 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL206099 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL208909 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL210425 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL209233 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL206914 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL381997 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL206469 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL207008 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL208712 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL207578 | — | IC50 | > | 30000.0 | nM | - |