Assay Detail
Binding
CHEMBL1764613
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IGF-induced autophosphosphorylation of GST-tagged human IGF1R expressed in SF21 cells by time resolved-fluorescent assay
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Insulin-like growth factor 1 receptor (CHEMBL1957) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: advantages in comparison with competitive inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 6.07 | 7.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1762148 | — | — | 1 | 7.26 |
| CHEMBL1762179 | — | — | 1 | 7.04 |
| CHEMBL1762178 | — | — | 1 | 7.01 |
| CHEMBL1762177 | — | — | 1 | 6.81 |
| CHEMBL1762176 | — | — | 1 | 6.70 |
| CHEMBL1762155 | — | — | 1 | 6.58 |
| CHEMBL1762153 | — | — | 1 | 6.52 |
| CHEMBL1762150 | — | — | 1 | 6.39 |
| CHEMBL1762154 | — | — | 1 | 6.34 |
| CHEMBL1762175 | — | — | 1 | 6.34 |
| CHEMBL1738841 | — | — | 1 | 6.30 |
| CHEMBL1762174 | — | — | 1 | 6.24 |
| CHEMBL1762173 | — | — | 1 | 6.15 |
| CHEMBL1762172 | — | — | 1 | 6.11 |
| CHEMBL1762171 | — | — | 1 | 6.00 |
| CHEMBL1762170 | — | — | 1 | 5.98 |
| CHEMBL1762169 | — | — | 1 | 5.97 |
| CHEMBL1762168 | — | — | 1 | 5.96 |
| CHEMBL1762167 | — | — | 1 | 5.91 |
| CHEMBL1762180 | — | — | 1 | 5.80 |
| CHEMBL1762166 | — | — | 1 | 5.73 |
| CHEMBL1762149 | — | — | 1 | 5.60 |
| CHEMBL1762165 | — | — | 1 | 5.54 |
| CHEMBL1762164 | — | — | 1 | 5.53 |
| CHEMBL1762163 | — | — | 1 | 5.35 |
| CHEMBL1762162 | — | — | 1 | 5.33 |
| CHEMBL1762152 | — | — | 1 | 5.27 |
| CHEMBL1762181 | — | — | 1 | 4.10 |
| CHEMBL1762158 | — | — | 1 | - |
| CHEMBL1762157 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1762148 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL1762179 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL1762178 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL1762177 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL1762176 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL1762155 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL1762153 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1762150 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL1762154 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL1762175 | — | IC50 | = | 453.0 | nM | 6.34 |
| CHEMBL1738841 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1762174 | — | IC50 | = | 574.0 | nM | 6.24 |
| CHEMBL1762173 | — | IC50 | = | 703.0 | nM | 6.15 |
| CHEMBL1762172 | — | IC50 | = | 784.0 | nM | 6.11 |
| CHEMBL1762171 | — | IC50 | = | 995.0 | nM | 6.00 |
| CHEMBL1762170 | — | IC50 | = | 1052.0 | nM | 5.98 |
| CHEMBL1762169 | — | IC50 | = | 1061.0 | nM | 5.97 |
| CHEMBL1762168 | — | IC50 | = | 1089.0 | nM | 5.96 |
| CHEMBL1762167 | — | IC50 | = | 1241.0 | nM | 5.91 |
| CHEMBL1762180 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1762166 | — | IC50 | = | 1851.0 | nM | 5.73 |
| CHEMBL1762149 | — | IC50 | = | 2520.0 | nM | 5.60 |
| CHEMBL1762165 | — | IC50 | = | 2897.0 | nM | 5.54 |
| CHEMBL1762164 | — | IC50 | = | 2950.0 | nM | 5.53 |
| CHEMBL1762163 | — | IC50 | = | 4501.0 | nM | 5.35 |
| CHEMBL1762162 | — | IC50 | = | 4706.0 | nM | 5.33 |
| CHEMBL1762152 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL1762181 | — | IC50 | = | 79700.0 | nM | 4.10 |
| CHEMBL1762345 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1762344 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1762343 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1762342 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1762341 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1762340 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1762182 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1762161 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1762160 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1762151 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1762159 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1762156 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1762157 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1762158 | — | IC50 | > | 10000.0 | nM | - |