Assay Detail
Binding
CHEMBL1025722
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Inhibition of IGF1R
29
Total Activities
29
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 | 29 | 8.56 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL463931 | GSK-2163632A | — | 1 | 9.70 |
| CHEMBL458414 | — | — | 1 | 9.52 |
| CHEMBL514873 | — | — | 1 | 9.52 |
| CHEMBL458864 | — | — | 1 | 9.30 |
| CHEMBL457105 | — | — | 1 | 9.30 |
| CHEMBL459069 | — | — | 1 | 9.15 |
| CHEMBL514258 | — | — | 1 | 9.15 |
| CHEMBL517163 | — | — | 1 | 9.10 |
| CHEMBL464971 | — | — | 1 | 9.10 |
| CHEMBL458415 | GSK-2186269A | — | 1 | 9.10 |
| CHEMBL515519 | — | — | 1 | 9.10 |
| CHEMBL458865 | GSK-1220512A | — | 1 | 9.05 |
| CHEMBL461876 | — | — | 1 | 9.00 |
| CHEMBL515846 | — | — | 1 | 8.89 |
| CHEMBL463932 | — | — | 1 | 8.89 |
| CHEMBL514718 | — | — | 1 | 8.80 |
| CHEMBL507625 | — | — | 1 | 8.70 |
| CHEMBL457548 | — | — | 1 | 8.70 |
| CHEMBL1964269 | — | — | 1 | 8.30 |
| CHEMBL1964270 | — | — | 1 | 8.22 |
| CHEMBL457322 | — | — | 1 | 8.10 |
| CHEMBL1964271 | — | — | 1 | 8.00 |
| CHEMBL458437 | — | — | 1 | 7.89 |
| CHEMBL463322 | — | — | 1 | 7.60 |
| CHEMBL456269 | — | — | 1 | 7.50 |
| CHEMBL514577 | — | — | 1 | 7.10 |
| CHEMBL458438 | GSK-1511931A | — | 1 | 6.60 |
| CHEMBL458660 | — | — | 1 | 6.40 |
| CHEMBL456252 | GSK-2110236A | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL463931 | GSK-2163632A | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL458414 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL514873 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL458864 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL457105 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL459069 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL514258 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL517163 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL464971 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL458415 | GSK-2186269A | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL515519 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL458865 | GSK-1220512A | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL461876 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL515846 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL463932 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL514718 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL507625 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL457548 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1964269 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1964270 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL457322 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL1964271 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL458437 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL463322 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL456269 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL514577 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL458438 | GSK-1511931A | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL458660 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL456252 | GSK-2110236A | IC50 | < | 0.2 | nM | - |