Assay Detail
Binding
CHEMBL1810165
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Inhibition of GST-tagged FLT3 expressing wild type kinase domain expressed in Sf9 insect cells after 4 hrs by Kinase-Glo assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Sf9 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.35 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1807483 | — | — | 1 | 8.22 |
| CHEMBL1807478 | — | — | 1 | 8.15 |
| CHEMBL1807469 | — | — | 1 | 8.15 |
| CHEMBL1807467 | — | — | 1 | 8.10 |
| CHEMBL1807789 | — | — | 1 | 8.00 |
| CHEMBL1807785 | — | — | 1 | 8.00 |
| CHEMBL1807392 | — | — | 1 | 7.89 |
| CHEMBL1807386 | — | — | 1 | 7.85 |
| CHEMBL1807470 | — | — | 1 | 7.82 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 7.70 |
| CHEMBL1807482 | — | — | 1 | 7.70 |
| CHEMBL1807477 | — | — | 1 | 7.54 |
| CHEMBL1807786 | — | — | 1 | 7.30 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.27 |
| CHEMBL1807788 | — | — | 1 | 7.22 |
| CHEMBL1807475 | — | — | 1 | 7.19 |
| CHEMBL1807479 | — | — | 1 | 7.16 |
| CHEMBL1807787 | — | — | 1 | 7.15 |
| CHEMBL1807471 | — | — | 1 | 7.05 |
| CHEMBL1807473 | — | — | 1 | 7.00 |
| CHEMBL1807485 | — | — | 1 | 6.96 |
| CHEMBL1807468 | — | — | 1 | 6.92 |
| CHEMBL1807484 | — | — | 1 | 6.92 |
| CHEMBL1807474 | — | — | 1 | 6.80 |
| CHEMBL1807481 | — | — | 1 | 6.57 |
| CHEMBL1807480 | — | — | 1 | 6.46 |
| CHEMBL1807472 | — | — | 1 | 6.44 |
| CHEMBL1807466 | — | — | 1 | 6.23 |
| CHEMBL1807389 | — | — | 1 | - |
| CHEMBL1807388 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1807483 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1807478 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1807469 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1807467 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1807789 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1807785 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1807392 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1807386 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1807470 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL223360 | LINIFANIB | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1807482 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1807477 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1807786 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1807788 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1807475 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL1807479 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1807787 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL1807471 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1807473 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1807485 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1807468 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1807484 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1807474 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1807481 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL1807480 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1807472 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL1807466 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL1807389 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1807388 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1807476 | — | IC50 | > | 1000.0 | nM | - |