| Description | CCR2 antagonist 1 is a high-affinity and long-residence-time antagonist of CCR2 (Ki: 2.4 nM). |
| In vitro | The combination of SAR and SKR in the hit-to-lead process results in the discovery of a new high-affinity and long residence time CCR2 antagonist 1 (compound 15a, Ki=2.4 nM; RT=714 min). |
| Target activity | CCR2:2.4 nM (ki) |
| molecular weight | 549.47 |
| Molecular formula | C28H32BrF3N2O |
| CAS | 1683534-96-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Vilums M, et al. When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists. Eur J Med Chem. 2015 Mar 26;93:121-34. |