Assay Detail
Binding
CHEMBL2175491
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive inhibition of N-terminal His6-tagged recombinant human c-MET (974 to 1390 amino acids) by spectrophotometry
42
Total Activities
42
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 of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 42 | 7.51 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2170818 | — | — | 1 | 9.00 |
| CHEMBL2170969 | — | — | 1 | 8.89 |
| CHEMBL2170966 | — | — | 1 | 8.70 |
| CHEMBL2170968 | — | — | 1 | 8.40 |
| CHEMBL2170954 | — | — | 1 | 8.40 |
| CHEMBL2169896 | — | — | 1 | 8.32 |
| CHEMBL2001019 | PF-04217903 | 1.0 | 1 | 8.30 |
| CHEMBL2170967 | — | — | 1 | 8.22 |
| CHEMBL2170816 | — | — | 1 | 8.22 |
| CHEMBL2170819 | — | — | 1 | 8.22 |
| CHEMBL2170949 | — | — | 1 | 8.21 |
| CHEMBL2170806 | — | — | 1 | 8.15 |
| CHEMBL2170955 | — | — | 1 | 8.05 |
| CHEMBL2170957 | — | — | 1 | 7.96 |
| CHEMBL2170950 | — | — | 1 | 7.86 |
| CHEMBL2170953 | — | — | 1 | 7.82 |
| CHEMBL2170820 | — | — | 1 | 7.72 |
| CHEMBL2170810 | — | — | 1 | 7.70 |
| CHEMBL2170946 | — | — | 1 | 7.70 |
| CHEMBL2170807 | — | — | 1 | 7.68 |
| CHEMBL2170952 | — | — | 1 | 7.47 |
| CHEMBL2170815 | — | — | 1 | 7.46 |
| CHEMBL2170808 | — | — | 1 | 7.43 |
| CHEMBL2170947 | — | — | 1 | 7.37 |
| CHEMBL2170817 | — | — | 1 | 7.36 |
| CHEMBL2170961 | — | — | 1 | 7.29 |
| CHEMBL2170814 | — | — | 1 | 7.23 |
| CHEMBL2170948 | — | — | 1 | 7.21 |
| CHEMBL2170951 | — | — | 1 | 7.17 |
| CHEMBL2170959 | — | — | 1 | 7.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2170818 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2170969 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL2170966 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2170968 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2170954 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2169896 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL2001019 | PF-04217903 | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2170967 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2170816 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2170819 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2170949 | — | Ki | = | 6.14 | nM | 8.21 |
| CHEMBL2170806 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2170955 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL2170957 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2170950 | — | Ki | = | 13.7 | nM | 7.86 |
| CHEMBL2170953 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2170820 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL2170810 | — | Ki | = | 19.8 | nM | 7.70 |
| CHEMBL2170946 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2170807 | — | Ki | = | 20.9 | nM | 7.68 |
| CHEMBL2170952 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL2170815 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL2170808 | — | Ki | = | 37.3 | nM | 7.43 |
| CHEMBL2170947 | — | Ki | = | 43.2 | nM | 7.37 |
| CHEMBL2170817 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL2170961 | — | Ki | = | 51.8 | nM | 7.29 |
| CHEMBL2170814 | — | Ki | = | 58.6 | nM | 7.23 |
| CHEMBL2170948 | — | Ki | = | 61.7 | nM | 7.21 |
| CHEMBL2170951 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL2170959 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL2170811 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL2170813 | — | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL2170809 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL2170956 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL2170805 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL2170965 | — | Ki | = | 188.0 | nM | 6.73 |
| CHEMBL2170960 | — | Ki | = | 379.0 | nM | 6.42 |
| CHEMBL2170964 | — | Ki | = | 425.0 | nM | 6.37 |
| CHEMBL2170812 | — | Ki | = | 653.0 | nM | 6.18 |
| CHEMBL2170962 | — | Ki | = | 6510.0 | nM | 5.19 |
| CHEMBL2170963 | — | Ki | = | 7390.0 | nM | 5.13 |
| CHEMBL2170958 | — | Ki | > | 10000.0 | nM | - |