Assay Detail
Binding
CHEMBL1025723
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IGF1R phosphorylation by cellular assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Insulin-like growth factor 1 receptor (CHEMBL1957) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine inhibitors of IGF-1R: elimination of an acid-mediated decomposition pathway.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.84 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL456252 | GSK-2110236A | — | 1 | 8.22 |
| CHEMBL458414 | — | — | 1 | 8.05 |
| CHEMBL514873 | — | — | 1 | 8.00 |
| CHEMBL457105 | — | — | 1 | 7.82 |
| CHEMBL517163 | — | — | 1 | 7.80 |
| CHEMBL458864 | — | — | 1 | 7.75 |
| CHEMBL457548 | — | — | 1 | 7.60 |
| CHEMBL515519 | — | — | 1 | 7.55 |
| CHEMBL514258 | — | — | 1 | 7.42 |
| CHEMBL515846 | — | — | 1 | 7.28 |
| CHEMBL461876 | — | — | 1 | 7.27 |
| CHEMBL1964269 | — | — | 1 | 7.04 |
| CHEMBL514718 | — | — | 1 | 6.97 |
| CHEMBL507625 | — | — | 1 | 6.93 |
| CHEMBL458415 | GSK-2186269A | — | 1 | 6.80 |
| CHEMBL1964270 | — | — | 1 | 6.26 |
| CHEMBL463322 | — | — | 1 | 6.18 |
| CHEMBL458437 | — | — | 1 | 6.11 |
| CHEMBL456269 | — | — | 1 | 6.01 |
| CHEMBL458660 | — | — | 1 | 5.77 |
| CHEMBL1964271 | — | — | 1 | 5.75 |
| CHEMBL458438 | GSK-1511931A | — | 1 | 5.60 |
| CHEMBL514577 | — | — | 1 | 5.56 |
| CHEMBL457322 | — | — | 1 | 4.52 |
| CHEMBL463931 | GSK-2163632A | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL456252 | GSK-2110236A | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL458414 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL514873 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL457105 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL517163 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL458864 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL457548 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL515519 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL514258 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL515846 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL461876 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1964269 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL514718 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL507625 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL458415 | GSK-2186269A | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1964270 | — | IC50 | = | 546.0 | nM | 6.26 |
| CHEMBL463322 | — | IC50 | = | 654.0 | nM | 6.18 |
| CHEMBL458437 | — | IC50 | = | 773.0 | nM | 6.11 |
| CHEMBL456269 | — | IC50 | = | 982.0 | nM | 6.01 |
| CHEMBL458660 | — | IC50 | = | 1695.0 | nM | 5.77 |
| CHEMBL1964271 | — | IC50 | = | 1770.0 | nM | 5.75 |
| CHEMBL458438 | GSK-1511931A | IC50 | = | 2534.0 | nM | 5.60 |
| CHEMBL514577 | — | IC50 | = | 2745.0 | nM | 5.56 |
| CHEMBL457322 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL463931 | GSK-2163632A | IC50 | < | 2.0 | nM | - |