Assay Detail
Binding
CHEMBL5100223
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His/SUMO tagged wild type human c-Met (1038 to 1346 residues) transfected in Escherichia coli using Tyr06 peptide as substrate incubated for 1 hr in presence of ATP by FRET-based Z'-Lyte assay
51
Total Activities
51
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 D6808, a Highly Selective and Potent Macrocyclic c-Met Inhibitor for Gastric Cancer Harboring <i>MET</i> Gene Alteration Treatment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 51 | 7.81 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5170338 | — | — | 1 | 8.55 |
| CHEMBL5181396 | — | — | 1 | 8.54 |
| CHEMBL3402762 | TEPOTINIB | 4.0 | 1 | 8.51 |
| CHEMBL5190062 | — | — | 1 | 8.48 |
| CHEMBL5179451 | — | — | 1 | 8.40 |
| CHEMBL5190727 | — | — | 1 | 8.40 |
| CHEMBL5177753 | — | — | 1 | 8.38 |
| CHEMBL5172104 | — | — | 1 | 8.32 |
| CHEMBL5203866 | — | — | 1 | 8.31 |
| CHEMBL5170241 | — | — | 1 | 8.30 |
| CHEMBL5191797 | — | — | 1 | 8.27 |
| CHEMBL5202957 | — | — | 1 | 8.27 |
| CHEMBL5187748 | — | — | 1 | 8.24 |
| CHEMBL5203752 | — | — | 1 | 8.17 |
| CHEMBL5172458 | — | — | 1 | 8.17 |
| CHEMBL5179628 | — | — | 1 | 8.13 |
| CHEMBL5179900 | — | — | 1 | 8.12 |
| CHEMBL5192592 | — | — | 1 | 8.12 |
| CHEMBL5208989 | — | — | 1 | 8.09 |
| CHEMBL5171999 | — | — | 1 | 8.06 |
| CHEMBL5171761 | — | — | 1 | 8.05 |
| CHEMBL5175023 | — | — | 1 | 8.00 |
| CHEMBL5178026 | — | — | 1 | 8.00 |
| CHEMBL5209284 | — | — | 1 | 7.98 |
| CHEMBL5180246 | — | — | 1 | 7.97 |
| CHEMBL5208253 | — | — | 1 | 7.97 |
| CHEMBL5185647 | — | — | 1 | 7.94 |
| CHEMBL5208277 | — | — | 1 | 7.88 |
| CHEMBL5195890 | — | — | 1 | 7.88 |
| CHEMBL5178545 | — | — | 1 | 7.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5170338 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5181396 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3402762 | TEPOTINIB | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5190062 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5179451 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5190727 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5177753 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5172104 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL5203866 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL5170241 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5191797 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL5202957 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL5187748 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL5203752 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL5172458 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL5179628 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL5179900 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL5192592 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL5208989 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL5171999 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL5171761 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL5175023 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL5178026 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL5209284 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL5208253 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL5180246 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL5185647 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL5208277 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL5195890 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL5178545 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL5180060 | — | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL5169752 | — | IC50 | = | 14.7 | nM | 7.83 |
| CHEMBL5185798 | — | IC50 | = | 14.9 | nM | 7.83 |
| CHEMBL5175646 | — | IC50 | = | 15.1 | nM | 7.82 |
| CHEMBL5188088 | — | IC50 | = | 18.3 | nM | 7.74 |
| CHEMBL5169499 | — | IC50 | = | 18.4 | nM | 7.74 |
| CHEMBL5184921 | — | IC50 | = | 20.4 | nM | 7.69 |
| CHEMBL5184513 | — | IC50 | = | 25.9 | nM | 7.59 |
| CHEMBL5204053 | — | IC50 | = | 26.4 | nM | 7.58 |
| CHEMBL5195042 | — | IC50 | = | 35.6 | nM | 7.45 |
| CHEMBL5209084 | — | IC50 | = | 41.6 | nM | 7.38 |
| CHEMBL5205446 | — | IC50 | = | 78.6 | nM | 7.11 |
| CHEMBL5179035 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL5175412 | — | IC50 | = | 171.2 | nM | 6.77 |
| CHEMBL5208042 | — | IC50 | = | 207.7 | nM | 6.68 |
| CHEMBL5193518 | — | IC50 | = | 662.6 | nM | 6.18 |
| CHEMBL5180657 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5176316 | — | IC50 | = | 2275.0 | nM | 5.64 |
| CHEMBL5183806 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5182585 | — | IC50 | > | 10000.0 | nM | - |