Assay Detail
Binding
CHEMBL3266282
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant INSR (unknown origin) using fluorescent dye-labelled KKSRGDYMTMQIG peptide peptide as substrate after 1 hr by IMAP assay
17
Total Activities
17
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
Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.11 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1091644 | LINSITINIB | 3.0 | 1 | 7.75 |
| CHEMBL3263959 | — | — | 1 | 7.41 |
| CHEMBL3263958 | — | — | 1 | 6.77 |
| CHEMBL3263964 | — | — | 1 | 5.54 |
| CHEMBL3263963 | — | — | 1 | 5.28 |
| CHEMBL3263962 | — | — | 1 | 5.10 |
| CHEMBL3263965 | — | — | 1 | 4.93 |
| CHEMBL3263960 | — | — | 1 | - |
| CHEMBL3263961 | — | — | 1 | - |
| CHEMBL3263966 | — | — | 1 | - |
| CHEMBL3263967 | — | — | 1 | - |
| CHEMBL3263968 | — | — | 1 | - |
| CHEMBL3263969 | — | — | 1 | - |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL460702 | BMS-777607 | 2.0 | 1 | - |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | - |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1091644 | LINSITINIB | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3263959 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3263958 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3263964 | — | IC50 | = | 2872.0 | nM | 5.54 |
| CHEMBL3263963 | — | IC50 | = | 5228.0 | nM | 5.28 |
| CHEMBL3263962 | — | IC50 | = | 7867.0 | nM | 5.10 |
| CHEMBL3263965 | — | IC50 | = | 11805.0 | nM | 4.93 |
| CHEMBL3263960 | — | IC50 | > | 12500.0 | nM | - |
| CHEMBL3263961 | — | IC50 | > | 12500.0 | nM | - |
| CHEMBL3263966 | — | IC50 | > | 12500.0 | nM | - |
| CHEMBL3263967 | — | IC50 | > | 12500.0 | nM | - |
| CHEMBL3263968 | — | IC50 | > | 12500.0 | nM | - |
| CHEMBL3263969 | — | IC50 | > | 12500.0 | nM | - |
| CHEMBL553 | ERLOTINIB | IC50 | > | 12500.0 | nM | - |
| CHEMBL460702 | BMS-777607 | IC50 | > | 12500.0 | nM | - |
| CHEMBL601719 | CRIZOTINIB | IC50 | - | — | - | |
| CHEMBL1173655 | AFATINIB | IC50 | - | — | - |