Assay Detail
Binding
CHEMBL3778237
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human RET cytoplasmic domain (658 to 1114 residues) expressed in baculovirus system preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay
44
Total Activities
44
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 |
Target
Proto-oncogene tyrosine-protein kinase receptor Ret (CHEMBL2041) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 7.54 | 9.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3775169 | — | — | 1 | 9.39 |
| CHEMBL440727 | — | — | 1 | 9.12 |
| CHEMBL3774904 | — | — | 1 | 8.96 |
| CHEMBL3775557 | — | — | 1 | 8.77 |
| CHEMBL3775336 | — | — | 1 | 8.70 |
| CHEMBL3774489 | — | — | 1 | 8.59 |
| CHEMBL3775934 | — | — | 1 | 8.59 |
| CHEMBL3775879 | — | — | 1 | 8.49 |
| CHEMBL3774580 | — | — | 1 | 8.41 |
| CHEMBL3774953 | — | — | 1 | 8.41 |
| CHEMBL127907 | — | — | 1 | 8.35 |
| CHEMBL478442 | — | — | 1 | 8.34 |
| CHEMBL3775511 | — | — | 1 | 8.32 |
| CHEMBL3775190 | — | — | 1 | 8.30 |
| CHEMBL3774951 | — | — | 1 | 8.08 |
| CHEMBL3775560 | — | — | 1 | 8.03 |
| CHEMBL3775585 | — | — | 1 | 8.01 |
| CHEMBL235851 | — | — | 1 | 8.00 |
| CHEMBL3775903 | — | — | 1 | 8.00 |
| CHEMBL3774563 | — | — | 1 | 7.96 |
| CHEMBL3775415 | — | — | 1 | 7.89 |
| CHEMBL3775672 | — | — | 1 | 7.80 |
| CHEMBL3775840 | — | — | 1 | 7.72 |
| CHEMBL3774913 | — | — | 1 | 7.68 |
| CHEMBL3775164 | — | — | 1 | 7.64 |
| CHEMBL3775376 | — | — | 1 | 7.64 |
| CHEMBL3775086 | — | — | 1 | 7.54 |
| CHEMBL3775940 | — | — | 1 | 7.36 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 7.31 |
| CHEMBL3774430 | — | — | 1 | 7.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3775169 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL440727 | — | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL3774904 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3775557 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3775336 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3774489 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3775934 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3775879 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL3774580 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3774953 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL127907 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL478442 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3775511 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3775190 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3774951 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL3775560 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL3775585 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL235851 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3775903 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3774563 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3775415 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3775672 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3775840 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3774913 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3775164 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3775376 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3775086 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3775940 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL24828 | VANDETANIB | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3774430 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1277620 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3774697 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3775569 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3774935 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3220401 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL2105717 | CABOZANTINIB | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL405130 | WHI-P131 | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL3775660 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL169473 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3774450 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3775240 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL3774623 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL3774720 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL3774643 | — | IC50 | > | 10000.0 | nM | - |