Assay Detail
Binding
CHEMBL3266281
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Inhibition of recombinant c-MET (unknown origin) using poly-AEKY peptide as substrate after 60 mins by ADPGlo 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 | 6.42 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3263959 | — | — | 1 | 8.30 |
| CHEMBL460702 | BMS-777607 | 2.0 | 1 | 8.15 |
| CHEMBL3263958 | — | — | 1 | 8.15 |
| CHEMBL3263964 | — | — | 1 | 6.40 |
| CHEMBL3263962 | — | — | 1 | 6.25 |
| CHEMBL3263960 | — | — | 1 | 6.01 |
| CHEMBL3263963 | — | — | 1 | 5.98 |
| CHEMBL3263966 | — | — | 1 | 5.91 |
| CHEMBL3263965 | — | — | 1 | 5.78 |
| CHEMBL3263961 | — | — | 1 | 5.76 |
| CHEMBL3263967 | — | — | 1 | 5.57 |
| CHEMBL3263968 | — | — | 1 | 5.57 |
| CHEMBL3263969 | — | — | 1 | 5.57 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL1091644 | LINSITINIB | 3.0 | 1 | - |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | - |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3263959 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL460702 | BMS-777607 | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3263958 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3263964 | — | IC50 | = | 398.0 | nM | 6.40 |
| CHEMBL3263962 | — | IC50 | = | 564.0 | nM | 6.25 |
| CHEMBL3263960 | — | IC50 | = | 978.0 | nM | 6.01 |
| CHEMBL3263963 | — | IC50 | = | 1048.0 | nM | 5.98 |
| CHEMBL3263966 | — | IC50 | = | 1225.0 | nM | 5.91 |
| CHEMBL3263965 | — | IC50 | = | 1664.0 | nM | 5.78 |
| CHEMBL3263961 | — | IC50 | = | 1719.0 | nM | 5.76 |
| CHEMBL3263967 | — | IC50 | = | 2692.0 | nM | 5.57 |
| CHEMBL3263968 | — | IC50 | = | 2708.0 | nM | 5.57 |
| CHEMBL3263969 | — | IC50 | = | 2705.0 | nM | 5.57 |
| CHEMBL553 | ERLOTINIB | IC50 | > | 12500.0 | nM | - |
| CHEMBL1091644 | LINSITINIB | IC50 | > | 12500.0 | nM | - |
| CHEMBL601719 | CRIZOTINIB | IC50 | - | — | - | |
| CHEMBL1173655 | AFATINIB | IC50 | - | — | - |