Assay Detail
Functional
CHEMBL4479427
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cytotoxicity against human NCI-H1993 cells assessed as growth inhibition after 72 hrs by CCK-8 assay
84
Total Activities
84
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI-H1993 |
| Confidence | 1 — Organism |
| 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 |
|---|---|---|---|
| IC50 | 84 | 6.49 | 7.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4570217 | — | — | 1 | 7.93 |
| CHEMBL4589643 | — | — | 1 | 7.71 |
| CHEMBL4068255 | — | — | 1 | 7.61 |
| CHEMBL4554813 | — | — | 1 | 7.53 |
| CHEMBL4551781 | — | — | 1 | 7.50 |
| CHEMBL4554510 | — | — | 1 | 7.49 |
| CHEMBL2001019 | PF-04217903 | 1.0 | 1 | 7.47 |
| CHEMBL4542192 | — | — | 1 | 7.45 |
| CHEMBL4524262 | — | — | 1 | 7.34 |
| CHEMBL4587352 | — | — | 1 | 7.22 |
| CHEMBL4483314 | — | — | 1 | 7.08 |
| CHEMBL4566100 | — | — | 1 | 6.96 |
| CHEMBL4528350 | — | — | 1 | 6.83 |
| CHEMBL4585798 | — | — | 1 | 6.79 |
| CHEMBL4553657 | — | — | 1 | 6.77 |
| CHEMBL4579449 | — | — | 1 | 6.76 |
| CHEMBL4538345 | — | — | 1 | 6.73 |
| CHEMBL4560881 | — | — | 1 | 6.72 |
| CHEMBL4558786 | — | — | 1 | 6.71 |
| CHEMBL4531351 | — | — | 1 | 6.69 |
| CHEMBL4527506 | — | — | 1 | 6.65 |
| CHEMBL4581168 | — | — | 1 | 6.62 |
| CHEMBL4559359 | — | — | 1 | 6.62 |
| CHEMBL4519232 | — | — | 1 | 6.48 |
| CHEMBL4540942 | — | — | 1 | 6.35 |
| CHEMBL4567631 | — | — | 1 | 6.29 |
| CHEMBL4561132 | — | — | 1 | 6.29 |
| CHEMBL4590141 | — | — | 1 | 6.24 |
| CHEMBL4549233 | — | — | 1 | 6.22 |
| CHEMBL4586780 | — | — | 1 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4570217 | — | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL4589643 | — | IC50 | = | 19.5 | nM | 7.71 |
| CHEMBL4068255 | — | IC50 | = | 24.7 | nM | 7.61 |
| CHEMBL4554813 | — | IC50 | = | 29.4 | nM | 7.53 |
| CHEMBL4551781 | — | IC50 | = | 31.3 | nM | 7.50 |
| CHEMBL4554510 | — | IC50 | = | 32.7 | nM | 7.49 |
| CHEMBL2001019 | PF-04217903 | IC50 | = | 33.6 | nM | 7.47 |
| CHEMBL4542192 | — | IC50 | = | 35.5 | nM | 7.45 |
| CHEMBL4524262 | — | IC50 | = | 46.1 | nM | 7.34 |
| CHEMBL4587352 | — | IC50 | = | 60.2 | nM | 7.22 |
| CHEMBL4483314 | — | IC50 | = | 83.7 | nM | 7.08 |
| CHEMBL4566100 | — | IC50 | = | 108.8 | nM | 6.96 |
| CHEMBL4528350 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL4585798 | — | IC50 | = | 161.6 | nM | 6.79 |
| CHEMBL4553657 | — | IC50 | = | 171.2 | nM | 6.77 |
| CHEMBL4579449 | — | IC50 | = | 175.4 | nM | 6.76 |
| CHEMBL4538345 | — | IC50 | = | 186.8 | nM | 6.73 |
| CHEMBL4560881 | — | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL4558786 | — | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL4531351 | — | IC50 | = | 206.1 | nM | 6.69 |
| CHEMBL4527506 | — | IC50 | = | 225.8 | nM | 6.65 |
| CHEMBL4581168 | — | IC50 | = | 239.4 | nM | 6.62 |
| CHEMBL4559359 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL4519232 | — | IC50 | = | 329.1 | nM | 6.48 |
| CHEMBL4540942 | — | IC50 | = | 449.9 | nM | 6.35 |
| CHEMBL4567631 | — | IC50 | = | 519.0 | nM | 6.29 |
| CHEMBL4561132 | — | IC50 | = | 513.9 | nM | 6.29 |
| CHEMBL4590141 | — | IC50 | = | 570.2 | nM | 6.24 |
| CHEMBL4549233 | — | IC50 | = | 599.1 | nM | 6.22 |
| CHEMBL4586780 | — | IC50 | = | 614.0 | nM | 6.21 |
| CHEMBL3334553 | — | IC50 | = | 617.0 | nM | 6.21 |
| CHEMBL4560823 | — | IC50 | = | 664.8 | nM | 6.18 |
| CHEMBL4587451 | — | IC50 | = | 726.2 | nM | 6.14 |
| CHEMBL4521693 | — | IC50 | = | 949.8 | nM | 6.02 |
| CHEMBL4526936 | — | IC50 | = | 956.0 | nM | 6.02 |
| CHEMBL4541607 | — | IC50 | = | 1109.0 | nM | 5.96 |
| CHEMBL4581508 | — | IC50 | = | 1159.0 | nM | 5.94 |
| CHEMBL4532610 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL4541026 | — | IC50 | = | 2325.0 | nM | 5.63 |
| CHEMBL4534161 | — | IC50 | = | 2661.0 | nM | 5.58 |
| CHEMBL4556499 | — | IC50 | = | 2893.0 | nM | 5.54 |
| CHEMBL4564491 | — | IC50 | = | 3285.0 | nM | 5.48 |
| CHEMBL4529060 | — | IC50 | = | 4948.0 | nM | 5.31 |
| CHEMBL4520183 | — | IC50 | = | 6661.0 | nM | 5.18 |
| CHEMBL4522638 | — | IC50 | = | 7488.0 | nM | 5.13 |
| CHEMBL4564859 | — | IC50 | = | 7909.0 | nM | 5.10 |
| CHEMBL4563384 | — | IC50 | - | — | - | |
| CHEMBL4521417 | — | IC50 | - | — | - | |
| CHEMBL4529638 | — | IC50 | - | — | - | |
| CHEMBL4554402 | — | IC50 | > | 10000.0 | nM | - |