Assay Detail
Binding
CHEMBL3789695
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length insulin receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 stimulation measured after 10 mins by quantitative Western blot analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.79 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1091644 | LINSITINIB | 3.0 | 1 | 7.80 |
| CHEMBL3786167 | — | — | 1 | 6.99 |
| CHEMBL3785951 | — | — | 1 | 6.78 |
| CHEMBL3785500 | — | — | 1 | 6.33 |
| CHEMBL1614712 | — | — | 1 | 6.05 |
| CHEMBL3787614 | — | — | 1 | - |
| CHEMBL3787112 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1091644 | LINSITINIB | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3786167 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL3785951 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL3785500 | — | IC50 | = | 471.0 | nM | 6.33 |
| CHEMBL1614712 | — | IC50 | = | 892.0 | nM | 6.05 |
| CHEMBL3787614 | — | IC50 | - | — | - | |
| CHEMBL3787112 | — | IC50 | - | — | - |