Assay Detail
Binding
CHEMBL887757
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Inhibition of human IGF1R expressed in recombinant insect cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Insulin-like growth factor 1 receptor (CHEMBL1957) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Imidazole moiety replacements in the 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like growth factor receptor-1 (IGF-1R) to improve cytochrome P450 profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.39 | 7.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL230042 | — | — | 1 | 7.34 |
| CHEMBL390002 | — | — | 1 | 7.27 |
| CHEMBL230043 | — | — | 1 | 7.17 |
| CHEMBL387611 | — | — | 1 | 7.03 |
| CHEMBL231620 | — | — | 1 | 6.85 |
| CHEMBL425819 | — | — | 1 | 6.77 |
| CHEMBL231306 | — | — | 1 | 6.75 |
| CHEMBL230412 | — | — | 1 | 6.75 |
| CHEMBL231409 | — | — | 1 | 6.75 |
| CHEMBL231510 | — | — | 1 | 6.57 |
| CHEMBL397666 | — | — | 1 | 6.41 |
| CHEMBL230204 | — | — | 1 | 6.28 |
| CHEMBL231509 | — | — | 1 | 6.26 |
| CHEMBL230309 | — | — | 1 | 6.11 |
| CHEMBL231609 | — | — | 1 | 5.89 |
| CHEMBL397667 | — | — | 1 | 5.85 |
| CHEMBL231610 | — | — | 1 | 5.60 |
| CHEMBL230205 | — | — | 1 | 5.51 |
| CHEMBL440964 | — | — | 1 | 5.40 |
| CHEMBL230308 | — | — | 1 | 5.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL230042 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL390002 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL230043 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL387611 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL231620 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL425819 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL231306 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL230412 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL231409 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL231510 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL397666 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL230204 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL231509 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL230309 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL231609 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL397667 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL231610 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL230205 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL440964 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL230308 | — | IC50 | = | 5100.0 | nM | 5.29 |