Assay Detail
Binding
CHEMBL2433360
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Inhibition of c-Met autophosphorylation in human A549 cells after 1 hr by ELISA
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A549 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Lessons from (S)-6-(1-(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)ethyl)quinoline (PF-04254644), an inhibitor of receptor tyrosine kinase c-Met with high protein kinase selectivity but broad phosphodiesterase family inhibition leading to myocardial degeneration in rats.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.71 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2431835 | — | — | 1 | 9.30 |
| CHEMBL2431834 | — | — | 1 | 9.15 |
| CHEMBL2170816 | — | — | 1 | 9.00 |
| CHEMBL2431826 | — | — | 1 | 8.40 |
| CHEMBL2431828 | — | — | 1 | 8.30 |
| CHEMBL2431819 | — | — | 1 | 8.22 |
| CHEMBL2431829 | — | — | 1 | 8.22 |
| CHEMBL2431823 | — | — | 1 | 8.10 |
| CHEMBL2431824 | — | — | 1 | 8.05 |
| CHEMBL2431825 | — | — | 1 | 7.96 |
| CHEMBL2431822 | — | — | 1 | 7.92 |
| CHEMBL2431827 | — | — | 1 | 7.92 |
| CHEMBL2431830 | — | — | 1 | 7.82 |
| CHEMBL2431838 | — | — | 1 | 7.75 |
| CHEMBL2429888 | — | — | 1 | 7.72 |
| CHEMBL2431816 | — | — | 1 | 7.72 |
| CHEMBL2431836 | — | — | 1 | 7.64 |
| CHEMBL2431815 | — | — | 1 | 7.64 |
| CHEMBL2431832 | — | — | 1 | 7.62 |
| CHEMBL2431833 | — | — | 1 | 7.60 |
| CHEMBL2431817 | — | — | 1 | 7.59 |
| CHEMBL2170953 | — | — | 1 | 7.47 |
| CHEMBL2431831 | — | — | 1 | 7.44 |
| CHEMBL2431840 | — | — | 1 | 7.36 |
| CHEMBL2431841 | — | — | 1 | 7.36 |
| CHEMBL2431839 | — | — | 1 | 7.32 |
| CHEMBL2431837 | — | — | 1 | 6.68 |
| CHEMBL2431821 | — | — | 1 | 6.46 |
| CHEMBL2431818 | — | — | 1 | 5.88 |
| CHEMBL2431820 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2431835 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL2431834 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL2170816 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2431826 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2431828 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2431819 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2431829 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2431823 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2431824 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2431825 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2431822 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2431827 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2431830 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2431838 | — | IC50 | = | 17.6 | nM | 7.75 |
| CHEMBL2429888 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2431816 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2431836 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2431815 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2431832 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2431833 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2431817 | — | IC50 | = | 25.4 | nM | 7.59 |
| CHEMBL2170953 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL2431831 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL2431840 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL2431841 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL2431839 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL2431837 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL2431821 | — | IC50 | = | 349.0 | nM | 6.46 |
| CHEMBL2431818 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL2431820 | — | IC50 | = | 2500.0 | nM | 5.60 |