Assay Detail
Binding
CHEMBL950344
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Inhibition of TIE2
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
TIE-2/VEGF-R2 SAR and in vitro activity of C3-acyl dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.97 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL401881 | — | — | 1 | 8.30 |
| CHEMBL269924 | — | — | 1 | 7.89 |
| CHEMBL403158 | — | — | 1 | 7.82 |
| CHEMBL444105 | — | — | 1 | 7.70 |
| CHEMBL402182 | — | — | 1 | 7.62 |
| CHEMBL255959 | — | — | 1 | 7.58 |
| CHEMBL271861 | — | — | 1 | 7.37 |
| CHEMBL402531 | — | — | 1 | 7.37 |
| CHEMBL411520 | — | — | 1 | 7.24 |
| CHEMBL271849 | — | — | 1 | 7.20 |
| CHEMBL410100 | — | — | 1 | 7.14 |
| CHEMBL401900 | — | — | 1 | 7.08 |
| CHEMBL428876 | — | — | 1 | 6.87 |
| CHEMBL271042 | — | — | 1 | 6.87 |
| CHEMBL255405 | — | — | 1 | 6.57 |
| CHEMBL255406 | — | — | 1 | 6.52 |
| CHEMBL270827 | — | — | 1 | 6.43 |
| CHEMBL255404 | — | — | 1 | 6.14 |
| CHEMBL406909 | — | — | 1 | 6.00 |
| CHEMBL270828 | — | — | 1 | 5.96 |
| CHEMBL258437 | — | — | 1 | 5.87 |
| CHEMBL346631 | CEP-7055 | 1.0 | 1 | 5.87 |
| CHEMBL271301 | — | — | 1 | - |
| CHEMBL404497 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL401881 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL269924 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL403158 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL444105 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL402182 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL255959 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL271861 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL402531 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL411520 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL271849 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL410100 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL401900 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL428876 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL271042 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL255405 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL255406 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL270827 | — | IC50 | = | 372.0 | nM | 6.43 |
| CHEMBL255404 | — | IC50 | = | 726.0 | nM | 6.14 |
| CHEMBL406909 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL270828 | — | IC50 | = | 1101.0 | nM | 5.96 |
| CHEMBL258437 | — | IC50 | = | 1357.0 | nM | 5.87 |
| CHEMBL346631 | CEP-7055 | IC50 | = | 1357.0 | nM | 5.87 |
| CHEMBL271301 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL404497 | — | IC50 | > | 1000.0 | nM | - |