Assay Detail
Binding
CHEMBL828663
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Inhibitory concentration against human tyrosine protein kinase receptor TIE-2
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Novel 4-amino-furo[2,3-d]pyrimidines as Tie-2 and VEGFR2 dual inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.67 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL194911 | — | — | 1 | 8.70 |
| CHEMBL372617 | — | — | 1 | 7.66 |
| CHEMBL194149 | — | — | 1 | 7.55 |
| CHEMBL195567 | — | — | 1 | 7.23 |
| CHEMBL196841 | — | — | 1 | 6.72 |
| CHEMBL193752 | — | — | 1 | 6.56 |
| CHEMBL194150 | — | — | 1 | 6.52 |
| CHEMBL372845 | — | — | 1 | 6.30 |
| CHEMBL363389 | — | — | 1 | 6.27 |
| CHEMBL194057 | — | — | 1 | 6.22 |
| CHEMBL365773 | — | — | 1 | 6.07 |
| CHEMBL196021 | — | — | 1 | 6.00 |
| CHEMBL383603 | — | — | 1 | 5.83 |
| CHEMBL362915 | — | — | 1 | 5.75 |
| CHEMBL195640 | — | — | 1 | - |
| CHEMBL373073 | GW642138X | — | 1 | - |
| CHEMBL196022 | GW642125X | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL194911 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL372617 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL194149 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL195567 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL196841 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL193752 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL194150 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL372845 | — | IC50 | = | 501.0 | nM | 6.30 |
| CHEMBL363389 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL194057 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL365773 | — | IC50 | = | 851.0 | nM | 6.07 |
| CHEMBL196021 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL383603 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL362915 | — | IC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL195640 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL373073 | GW642138X | IC50 | > | 20000.0 | nM | - |
| CHEMBL196022 | GW642125X | IC50 | > | 20000.0 | nM | - |