Assay Detail
Binding
CHEMBL955911
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged human IGF1R expressed in Sf9 cells by Wallac Victor fluorometer
34
Total Activities
34
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
Insulin-like growth factor 1 receptor (CHEMBL1957) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: potent inhibitors of the IGF-1R receptor tyrosine kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 8.48 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL476259 | GSK-1326255A | — | 1 | 9.52 |
| CHEMBL477069 | GSK-1173862A | — | 1 | 9.40 |
| CHEMBL475073 | — | — | 1 | 9.30 |
| CHEMBL514868 | — | — | 1 | 9.22 |
| CHEMBL476044 | — | — | 1 | 9.10 |
| CHEMBL464971 | — | — | 1 | 9.10 |
| CHEMBL459069 | — | — | 1 | 9.10 |
| CHEMBL458865 | GSK-1220512A | — | 1 | 9.10 |
| CHEMBL514828 | — | — | 1 | 9.00 |
| CHEMBL463932 | — | — | 1 | 8.89 |
| CHEMBL476451 | — | — | 1 | 8.80 |
| CHEMBL1964272 | — | — | 1 | 8.80 |
| CHEMBL476059 | — | — | 1 | 8.80 |
| CHEMBL477950 | — | — | 1 | 8.80 |
| CHEMBL514615 | — | — | 1 | 8.80 |
| CHEMBL475884 | — | — | 1 | 8.70 |
| CHEMBL507625 | — | — | 1 | 8.70 |
| CHEMBL475883 | — | — | 1 | 8.70 |
| CHEMBL475286 | — | — | 1 | 8.49 |
| CHEMBL515602 | — | — | 1 | 8.49 |
| CHEMBL473669 | — | — | 1 | 8.49 |
| CHEMBL473254 | — | — | 1 | 8.40 |
| CHEMBL516816 | — | — | 1 | 8.40 |
| CHEMBL513897 | GSK-994854A | — | 1 | 8.30 |
| CHEMBL505983 | — | — | 1 | 8.30 |
| CHEMBL475074 | — | — | 1 | 8.30 |
| CHEMBL475482 | — | — | 1 | 8.20 |
| CHEMBL515909 | — | — | 1 | 8.10 |
| CHEMBL450071 | GSK-1392956A | — | 1 | 7.80 |
| CHEMBL472846 | — | — | 1 | 7.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL476259 | GSK-1326255A | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL477069 | GSK-1173862A | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL475073 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL514868 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL476044 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL464971 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL459069 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL458865 | GSK-1220512A | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL514828 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL463932 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL476451 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL1964272 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL476059 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL477950 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL514615 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL507625 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL475884 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL475883 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL475286 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL515602 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL473669 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL473254 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL516816 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL475074 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL505983 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL513897 | GSK-994854A | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL475482 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL515909 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL450071 | GSK-1392956A | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL472846 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL465374 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL511013 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL475080 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL475285 | — | IC50 | = | 10000.0 | nM | 5.00 |