Assay Detail
Binding
CHEMBL941657
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Inhibition of human IGF1R expressed in Sf21 cells by time-resolved fluorescence assay
31
Total Activities
31
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 | Intermediate |
Target
Insulin-like growth factor 1 receptor (CHEMBL1957) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.75 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL248877 | — | — | 1 | 7.64 |
| CHEMBL249082 | — | — | 1 | 7.50 |
| CHEMBL400657 | — | — | 1 | 7.46 |
| CHEMBL249295 | — | — | 1 | 7.43 |
| CHEMBL251732 | — | — | 1 | 7.43 |
| CHEMBL248698 | — | — | 1 | 7.42 |
| CHEMBL399225 | — | — | 1 | 7.29 |
| CHEMBL251326 | — | — | 1 | 7.24 |
| CHEMBL249496 | — | — | 1 | 7.19 |
| CHEMBL251534 | — | — | 1 | 7.16 |
| CHEMBL429299 | — | — | 1 | 7.15 |
| CHEMBL399021 | — | — | 1 | 7.11 |
| CHEMBL249325 | — | — | 1 | 7.10 |
| CHEMBL437584 | — | — | 1 | 7.09 |
| CHEMBL250085 | — | — | 1 | 7.05 |
| CHEMBL249711 | — | — | 1 | 6.91 |
| CHEMBL400457 | — | — | 1 | 6.90 |
| CHEMBL438344 | — | — | 1 | 6.82 |
| CHEMBL428414 | — | — | 1 | 6.76 |
| CHEMBL249296 | — | — | 1 | 6.75 |
| CHEMBL398916 | — | — | 1 | 6.73 |
| CHEMBL429832 | — | — | 1 | 6.48 |
| CHEMBL429664 | — | — | 1 | 6.31 |
| CHEMBL400727 | — | — | 1 | 6.19 |
| CHEMBL251292 | — | — | 1 | 6.17 |
| CHEMBL437198 | — | — | 1 | 6.03 |
| CHEMBL249699 | — | — | 1 | 5.88 |
| CHEMBL398957 | — | — | 1 | 5.63 |
| CHEMBL400277 | — | — | 1 | 5.63 |
| CHEMBL446197 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL248877 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL249082 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL400657 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL249295 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL251732 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL248698 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL399225 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL251326 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL249496 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL251534 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL429299 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL399021 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL249325 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL437584 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL250085 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL249711 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL400457 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL438344 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL428414 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL249296 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL398916 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL429832 | — | IC50 | = | 328.0 | nM | 6.48 |
| CHEMBL429664 | — | IC50 | = | 488.0 | nM | 6.31 |
| CHEMBL400727 | — | IC50 | = | 642.0 | nM | 6.19 |
| CHEMBL251292 | — | IC50 | = | 674.0 | nM | 6.17 |
| CHEMBL437198 | — | IC50 | = | 924.0 | nM | 6.03 |
| CHEMBL249699 | — | IC50 | = | 1309.0 | nM | 5.88 |
| CHEMBL398957 | — | IC50 | = | 2322.0 | nM | 5.63 |
| CHEMBL400277 | — | IC50 | = | 2337.0 | nM | 5.63 |
| CHEMBL446197 | — | IC50 | = | 3310.0 | nM | 5.48 |
| CHEMBL399224 | — | IC50 | = | 4334.0 | nM | 5.36 |