Assay Detail
Binding
CHEMBL2015673
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant Tie2 expressed in baculovirus expression system using GST-PLCgamma as substrate after 1 hr by time-resolved fluorescence analysis
12
Total Activities
12
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 |
Publication
Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.45 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2010869 | — | — | 1 | 8.40 |
| CHEMBL2010873 | — | — | 1 | 8.00 |
| CHEMBL2010872 | CEP-11981 | 2.0 | 1 | 7.66 |
| CHEMBL2010871 | — | — | 1 | 7.57 |
| CHEMBL2010870 | — | — | 1 | 7.12 |
| CHEMBL2010877 | — | — | 1 | 6.78 |
| CHEMBL2011061 | — | — | 1 | 6.62 |
| CHEMBL2010878 | — | — | 1 | - |
| CHEMBL2010876 | — | — | 1 | - |
| CHEMBL2010874 | — | — | 1 | - |
| CHEMBL2010875 | — | — | 1 | - |
| CHEMBL150894 | CEP-5214 | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2010869 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2010873 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2010872 | CEP-11981 | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2010871 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2010870 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL2010877 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL2011061 | — | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL2010878 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL2010876 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL2010874 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL2010875 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL150894 | CEP-5214 | IC50 | > | 10000.0 | nM | - |