Assay Detail
Binding
CHEMBL1033175
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Inhibition of phospho IGFR1 by cellular assay
34
Total Activities
34
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 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.66 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL467136 | — | — | 1 | 7.96 |
| CHEMBL516870 | — | — | 1 | 7.80 |
| CHEMBL464344 | — | — | 1 | 7.72 |
| CHEMBL517947 | — | — | 1 | 7.62 |
| CHEMBL468619 | — | — | 1 | 7.55 |
| CHEMBL511765 | GSK-2213727A | — | 1 | 7.42 |
| CHEMBL461876 | — | — | 1 | 7.25 |
| CHEMBL501964 | — | — | 1 | 7.14 |
| CHEMBL461018 | — | — | 1 | 7.10 |
| CHEMBL459753 | — | — | 1 | 7.09 |
| CHEMBL464552 | — | — | 1 | 7.07 |
| CHEMBL464757 | — | — | 1 | 7.07 |
| CHEMBL507625 | — | — | 1 | 6.93 |
| CHEMBL465168 | — | — | 1 | 6.89 |
| CHEMBL517340 | — | — | 1 | 6.72 |
| CHEMBL516816 | — | — | 1 | 6.70 |
| CHEMBL465789 | — | — | 1 | 6.68 |
| CHEMBL461875 | — | — | 1 | 6.67 |
| CHEMBL465374 | — | — | 1 | 6.57 |
| CHEMBL460815 | — | — | 1 | 6.56 |
| CHEMBL507810 | — | — | 1 | 6.53 |
| CHEMBL505915 | GSK-1751853A | — | 1 | 6.42 |
| CHEMBL467580 | — | — | 1 | 6.42 |
| CHEMBL450919 | — | — | 1 | 6.19 |
| CHEMBL517729 | — | — | 1 | 6.12 |
| CHEMBL463116 | — | — | 1 | 6.10 |
| CHEMBL515036 | — | — | 1 | 6.08 |
| CHEMBL464551 | — | — | 1 | 6.06 |
| CHEMBL518354 | — | — | 1 | 6.05 |
| CHEMBL464347 | — | — | 1 | 6.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL467136 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL516870 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL464344 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL517947 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL468619 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL511765 | GSK-2213727A | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL461876 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL501964 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL461018 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL459753 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL464552 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL464757 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL507625 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL465168 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL517340 | — | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL516816 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL465789 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL461875 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL465374 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL460815 | — | IC50 | = | 278.0 | nM | 6.56 |
| CHEMBL507810 | — | IC50 | = | 298.0 | nM | 6.53 |
| CHEMBL505915 | GSK-1751853A | IC50 | = | 376.0 | nM | 6.42 |
| CHEMBL467580 | — | IC50 | = | 377.0 | nM | 6.42 |
| CHEMBL450919 | — | IC50 | = | 651.0 | nM | 6.19 |
| CHEMBL517729 | — | IC50 | = | 765.0 | nM | 6.12 |
| CHEMBL463116 | — | IC50 | = | 794.0 | nM | 6.10 |
| CHEMBL515036 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL464551 | — | IC50 | = | 877.0 | nM | 6.06 |
| CHEMBL518354 | — | IC50 | = | 895.0 | nM | 6.05 |
| CHEMBL464347 | — | IC50 | = | 929.0 | nM | 6.03 |
| CHEMBL467581 | GSK-2219385A | IC50 | = | 1728.0 | nM | 5.76 |
| CHEMBL459538 | — | IC50 | = | 1984.0 | nM | 5.70 |
| CHEMBL517171 | GSK-1713088A | IC50 | = | 5366.0 | nM | 5.27 |
| CHEMBL465577 | — | IC50 | = | 7762.0 | nM | 5.11 |