Assay Detail
Binding
CHEMBL3240326
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Inhibition of GST-fused human FLT3 cytoplasmic domain (amino acids 564 to 993) using Ulight-JAK1 as substrate after 1 hr by TR-FRET assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 8.27 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3237712 | — | — | 1 | 9.70 |
| CHEMBL3237706 | — | — | 1 | 9.52 |
| CHEMBL3237718 | — | — | 1 | 9.22 |
| CHEMBL3237711 | — | — | 1 | 9.22 |
| CHEMBL3237708 | — | — | 1 | 9.00 |
| CHEMBL3237719 | — | — | 1 | 9.00 |
| CHEMBL3237709 | — | — | 1 | 8.70 |
| CHEMBL3237451 | — | — | 1 | 8.70 |
| CHEMBL3237702 | — | — | 1 | 8.70 |
| CHEMBL3237703 | — | — | 1 | 8.70 |
| CHEMBL3237717 | — | — | 1 | 8.52 |
| CHEMBL3237705 | — | — | 1 | 8.52 |
| CHEMBL3237710 | — | — | 1 | 8.40 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 8.40 |
| CHEMBL3237716 | — | — | 1 | 8.30 |
| CHEMBL3237444 | — | — | 1 | 8.30 |
| CHEMBL3237450 | — | — | 1 | 8.30 |
| CHEMBL3237713 | — | — | 1 | 8.22 |
| CHEMBL3237707 | — | — | 1 | 8.22 |
| CHEMBL3237714 | — | — | 1 | 8.10 |
| CHEMBL3237715 | — | — | 1 | 8.10 |
| CHEMBL3237443 | — | — | 1 | 7.96 |
| CHEMBL3237442 | — | — | 1 | 7.85 |
| CHEMBL3237704 | — | — | 1 | 7.77 |
| CHEMBL3237446 | — | — | 1 | 7.77 |
| CHEMBL3237445 | — | — | 1 | 7.66 |
| CHEMBL3237449 | — | — | 1 | 7.37 |
| CHEMBL3237447 | — | — | 1 | 7.34 |
| CHEMBL3237448 | — | — | 1 | 7.02 |
| CHEMBL189963 | PALBOCICLIB | 4.0 | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3237712 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3237706 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3237718 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3237711 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3237708 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3237719 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3237709 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3237451 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3237702 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3237703 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3237717 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3237705 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3237710 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3237716 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3237444 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3237450 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3237713 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3237707 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3237714 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3237715 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3237443 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3237442 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3237704 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3237446 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3237445 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3237449 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3237447 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3237448 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL189963 | PALBOCICLIB | IC50 | = | 3480.0 | nM | 5.46 |