Assay Detail
Binding
CHEMBL3424980
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant N-terminal His6-tagged IGF-1R using fluorescence substrate after 80 mins by caliper off-chip incubation mobility shift assay
21
Total Activities
21
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 |
Target
Insulin-like growth factor 1 receptor (CHEMBL1957) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 5.64 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3421973 | — | — | 1 | 7.52 |
| CHEMBL3421970 | — | — | 1 | 7.29 |
| CHEMBL3421969 | — | — | 1 | 7.14 |
| CHEMBL3421968 | — | — | 1 | 6.11 |
| CHEMBL3421966 | — | — | 1 | 6.01 |
| CHEMBL3421967 | — | — | 1 | 5.83 |
| CHEMBL3421636 | — | — | 1 | 5.62 |
| CHEMBL3421971 | — | — | 1 | 5.50 |
| CHEMBL3421972 | — | — | 1 | 5.48 |
| CHEMBL3421981 | — | — | 1 | 5.10 |
| CHEMBL3421963 | — | — | 1 | 4.47 |
| CHEMBL3421964 | — | — | 1 | 4.39 |
| CHEMBL3421978 | — | — | 1 | 4.33 |
| CHEMBL3421974 | — | — | 1 | 4.17 |
| CHEMBL3421975 | — | — | 1 | - |
| CHEMBL3421976 | — | — | 1 | - |
| CHEMBL3421977 | — | — | 1 | - |
| CHEMBL3421979 | — | — | 1 | - |
| CHEMBL3421965 | — | — | 1 | - |
| CHEMBL3421962 | — | — | 1 | - |
| CHEMBL3421980 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3421973 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3421970 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3421969 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL3421968 | — | IC50 | = | 779.0 | nM | 6.11 |
| CHEMBL3421966 | — | IC50 | = | 965.0 | nM | 6.01 |
| CHEMBL3421967 | — | IC50 | = | 1489.0 | nM | 5.83 |
| CHEMBL3421636 | — | IC50 | = | 2409.0 | nM | 5.62 |
| CHEMBL3421971 | — | IC50 | = | 3174.0 | nM | 5.50 |
| CHEMBL3421972 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3421981 | — | IC50 | = | 7992.0 | nM | 5.10 |
| CHEMBL3421963 | — | IC50 | = | 34125.0 | nM | 4.47 |
| CHEMBL3421964 | — | IC50 | = | 40515.0 | nM | 4.39 |
| CHEMBL3421978 | — | IC50 | = | 46942.0 | nM | 4.33 |
| CHEMBL3421974 | — | IC50 | = | 67727.0 | nM | 4.17 |
| CHEMBL3421975 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3421976 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3421977 | — | IC50 | > | 29000.0 | nM | - |
| CHEMBL3421979 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3421965 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3421962 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3421980 | — | IC50 | > | 100000.0 | nM | - |