Assay Detail
Binding
CHEMBL5048418
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-3C fused human RET (705 to 1013 residues) expressed in sf9 baculovirus expression system using 5-FAM- peptide as substrate preincubated for 1 hr followed by substrate addition in presence of ATP by microfluidics assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Proto-oncogene tyrosine-protein kinase receptor Ret (CHEMBL2041) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of N-Trisubstituted Pyrimidine Derivatives as Type I RET and RET Gatekeeper Mutant Inhibitors with a Novel Kinase Binding Pose.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 7.47 | 8.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4559134 | SELPERCATINIB | 4.0 | 1 | 8.91 |
| CHEMBL5087283 | — | — | 1 | 8.29 |
| CHEMBL5074882 | — | — | 1 | 8.26 |
| CHEMBL5080296 | — | — | 1 | 8.23 |
| CHEMBL5073804 | — | — | 1 | 8.22 |
| CHEMBL5070593 | — | — | 1 | 8.21 |
| CHEMBL5078090 | — | — | 1 | 8.19 |
| CHEMBL5094848 | — | — | 1 | 8.14 |
| CHEMBL5089911 | — | — | 1 | 8.12 |
| CHEMBL5093057 | — | — | 1 | 8.08 |
| CHEMBL5085579 | — | — | 1 | 7.98 |
| CHEMBL5094196 | — | — | 1 | 7.91 |
| CHEMBL5089027 | — | — | 1 | 7.88 |
| CHEMBL5086966 | — | — | 1 | 7.87 |
| CHEMBL5079216 | — | — | 1 | 7.80 |
| CHEMBL5092920 | — | — | 1 | 7.73 |
| CHEMBL5075257 | — | — | 1 | 7.66 |
| CHEMBL5087974 | — | — | 1 | 7.61 |
| CHEMBL5081199 | — | — | 1 | 7.55 |
| CHEMBL5084023 | — | — | 1 | 7.38 |
| CHEMBL5078263 | — | — | 1 | 7.18 |
| CHEMBL5078934 | — | — | 1 | 7.03 |
| CHEMBL5075735 | — | — | 1 | 6.99 |
| CHEMBL5081142 | — | — | 1 | 6.99 |
| CHEMBL5093178 | — | — | 1 | 6.93 |
| CHEMBL5073056 | — | — | 1 | 6.86 |
| CHEMBL5083534 | — | — | 1 | 6.85 |
| CHEMBL5071633 | — | — | 1 | 6.83 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 6.82 |
| CHEMBL5083224 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4559134 | SELPERCATINIB | IC50 | = | 1.24 | nM | 8.91 |
| CHEMBL5087283 | — | IC50 | = | 5.07 | nM | 8.29 |
| CHEMBL5074882 | — | IC50 | = | 5.45 | nM | 8.26 |
| CHEMBL5080296 | — | IC50 | = | 5.82 | nM | 8.23 |
| CHEMBL5073804 | — | IC50 | = | 6.01 | nM | 8.22 |
| CHEMBL5070593 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL5078090 | — | IC50 | = | 6.43 | nM | 8.19 |
| CHEMBL5094848 | — | IC50 | = | 7.27 | nM | 8.14 |
| CHEMBL5089911 | — | IC50 | = | 7.53 | nM | 8.12 |
| CHEMBL5093057 | — | IC50 | = | 8.31 | nM | 8.08 |
| CHEMBL5085579 | — | IC50 | = | 10.52 | nM | 7.98 |
| CHEMBL5094196 | — | IC50 | = | 12.41 | nM | 7.91 |
| CHEMBL5089027 | — | IC50 | = | 13.09 | nM | 7.88 |
| CHEMBL5086966 | — | IC50 | = | 13.45 | nM | 7.87 |
| CHEMBL5079216 | — | IC50 | = | 15.87 | nM | 7.80 |
| CHEMBL5092920 | — | IC50 | = | 18.77 | nM | 7.73 |
| CHEMBL5075257 | — | IC50 | = | 22.1 | nM | 7.66 |
| CHEMBL5087974 | — | IC50 | = | 24.7 | nM | 7.61 |
| CHEMBL5081199 | — | IC50 | = | 28.11 | nM | 7.55 |
| CHEMBL5084023 | — | IC50 | = | 41.29 | nM | 7.38 |
| CHEMBL5078263 | — | IC50 | = | 66.58 | nM | 7.18 |
| CHEMBL5078934 | — | IC50 | = | 92.97 | nM | 7.03 |
| CHEMBL5075735 | — | IC50 | = | 102.51 | nM | 6.99 |
| CHEMBL5081142 | — | IC50 | = | 102.14 | nM | 6.99 |
| CHEMBL5093178 | — | IC50 | = | 116.1 | nM | 6.93 |
| CHEMBL5073056 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL5083534 | — | IC50 | = | 140.65 | nM | 6.85 |
| CHEMBL5071633 | — | IC50 | = | 146.6 | nM | 6.83 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 152.3 | nM | 6.82 |
| CHEMBL5083224 | — | IC50 | = | 160.13 | nM | 6.80 |
| CHEMBL5078777 | — | IC50 | = | 189.57 | nM | 6.72 |
| CHEMBL5074502 | — | IC50 | = | 212.3 | nM | 6.67 |
| CHEMBL5088213 | — | IC50 | = | 245.95 | nM | 6.61 |
| CHEMBL5080275 | — | IC50 | = | 252.25 | nM | 6.60 |
| CHEMBL5078648 | — | IC50 | = | 260.15 | nM | 6.58 |
| CHEMBL5083904 | — | IC50 | = | 322.4 | nM | 6.49 |