Assay Detail
Binding
CHEMBL4479426
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of c-Met kinase (unknown origin) assessed as decrease in phosphorylation of TK substrate-biotin peptide preincubated for 5 to 10 mins followed by ATP addition measured after 30 mins by HTRF assay
84
Total Activities
84
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 optimization of a series of imidazo[4,5-b]pyrazine derivatives as highly potent and exquisitely selective inhibitors of the mesenchymal-epithelial transition factor (c-Met) protein kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 84 | 7.99 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2001019 | PF-04217903 | 1.0 | 1 | 9.52 |
| CHEMBL4483314 | — | — | 1 | 9.00 |
| CHEMBL4542192 | — | — | 1 | 9.00 |
| CHEMBL4524262 | — | — | 1 | 8.89 |
| CHEMBL4570217 | — | — | 1 | 8.88 |
| CHEMBL4068255 | — | — | 1 | 8.84 |
| CHEMBL4560823 | — | — | 1 | 8.80 |
| CHEMBL4585798 | — | — | 1 | 8.80 |
| CHEMBL4551781 | — | — | 1 | 8.80 |
| CHEMBL4589643 | — | — | 1 | 8.77 |
| CHEMBL4561132 | — | — | 1 | 8.74 |
| CHEMBL4581168 | — | — | 1 | 8.71 |
| CHEMBL4554510 | — | — | 1 | 8.64 |
| CHEMBL4527506 | — | — | 1 | 8.60 |
| CHEMBL4558786 | — | — | 1 | 8.60 |
| CHEMBL4549233 | — | — | 1 | 8.57 |
| CHEMBL4559359 | — | — | 1 | 8.56 |
| CHEMBL4519232 | — | — | 1 | 8.55 |
| CHEMBL4587352 | — | — | 1 | 8.54 |
| CHEMBL4531351 | — | — | 1 | 8.49 |
| CHEMBL4526936 | — | — | 1 | 8.48 |
| CHEMBL4566100 | — | — | 1 | 8.47 |
| CHEMBL4538345 | — | — | 1 | 8.44 |
| CHEMBL4586780 | — | — | 1 | 8.44 |
| CHEMBL4553657 | — | — | 1 | 8.42 |
| CHEMBL4560881 | — | — | 1 | 8.40 |
| CHEMBL4587451 | — | — | 1 | 8.38 |
| CHEMBL4521693 | — | — | 1 | 8.36 |
| CHEMBL4579449 | — | — | 1 | 8.35 |
| CHEMBL4590141 | — | — | 1 | 8.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2001019 | PF-04217903 | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4483314 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4542192 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4524262 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4570217 | — | EC50 | = | 1.32 | nM | 8.88 |
| CHEMBL4068255 | — | EC50 | = | 1.45 | nM | 8.84 |
| CHEMBL4560823 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4585798 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4551781 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4589643 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4561132 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4581168 | — | EC50 | = | 1.94 | nM | 8.71 |
| CHEMBL4554510 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4558786 | — | EC50 | = | 2.49 | nM | 8.60 |
| CHEMBL4527506 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4549233 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4559359 | — | EC50 | = | 2.74 | nM | 8.56 |
| CHEMBL4519232 | — | EC50 | = | 2.79 | nM | 8.55 |
| CHEMBL4587352 | — | EC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4531351 | — | EC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4526936 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4566100 | — | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4538345 | — | EC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4586780 | — | EC50 | = | 3.67 | nM | 8.44 |
| CHEMBL4553657 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4560881 | — | EC50 | = | 3.95 | nM | 8.40 |
| CHEMBL4587451 | — | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4521693 | — | EC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4579449 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4590141 | — | EC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4540942 | — | EC50 | = | 4.9 | nM | 8.31 |
| CHEMBL4554813 | — | EC50 | = | 4.9 | nM | 8.31 |
| CHEMBL4532610 | — | EC50 | = | 5.17 | nM | 8.29 |
| CHEMBL4529638 | — | EC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4541607 | — | EC50 | = | 6.41 | nM | 8.19 |
| CHEMBL4521417 | — | EC50 | = | 7.7 | nM | 8.11 |
| CHEMBL4576153 | — | EC50 | = | 8.7 | nM | 8.06 |
| CHEMBL4539073 | — | EC50 | = | 9.3 | nM | 8.03 |
| CHEMBL4563384 | — | EC50 | = | 9.4 | nM | 8.03 |
| CHEMBL3334553 | — | EC50 | = | 9.9 | nM | 8.00 |
| CHEMBL4538592 | — | EC50 | = | 10.6 | nM | 7.97 |
| CHEMBL4567631 | — | EC50 | = | 11.4 | nM | 7.94 |
| CHEMBL4568802 | — | EC50 | = | 11.7 | nM | 7.93 |
| CHEMBL4529060 | — | EC50 | = | 12.37 | nM | 7.91 |
| CHEMBL4528350 | — | EC50 | = | 12.71 | nM | 7.90 |
| CHEMBL4556499 | — | EC50 | = | 13.25 | nM | 7.88 |
| CHEMBL4548105 | — | EC50 | = | 13.5 | nM | 7.87 |
| CHEMBL4586640 | — | EC50 | = | 14.1 | nM | 7.85 |
| CHEMBL4534161 | — | EC50 | = | 15.19 | nM | 7.82 |
| CHEMBL4541026 | — | EC50 | = | 15.94 | nM | 7.80 |