2714478-83-6
2714478-83-6 structure
- Name: CCR2 Covalent-IN-14
- Chemical Name: CCR2 Covalent-IN-14
- CAS Number: 2714478-83-6
- Molecular Formula: C23H16Cl2F3N3O4S2
- Molecular Weight: 590.413
- Create Date: 2022-07-01 16:24:07
- Modify Date: 2024-01-14 15:32:07
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CCR2 covalent-IN-14 is a covalent, negative allosteric modulator (NAM) of CCR2, binds to intracellularly pocket of CCR2 with Ki of 4 nM.CCR2 covalent-IN-14 is more potent than non-covalent analogue and wash-resistant in functional assays (IC50=33 nM in GTPγS binding assay on U2OS-CCR2 cell membranes, IC50=4 nM in β-arrestin recruitment assays).CCR2 covalent-IN-14 displays little to no inhibitory potency on CCR1 and CCR5.The affinity of CCR2 covalent-IN-14 for both the C70S and C75S CCR2 mutants is significantly decreased compared to WT CCR2.
| Name | CCR2 Covalent-IN-14 |
|---|
| Description | CCR2 covalent-IN-14 is a covalent, negative allosteric modulator (NAM) of CCR2, binds to intracellularly pocket of CCR2 with Ki of 4 nM.CCR2 covalent-IN-14 is more potent than non-covalent analogue and wash-resistant in functional assays (IC50=33 nM in GTPγS binding assay on U2OS-CCR2 cell membranes, IC50=4 nM in β-arrestin recruitment assays).CCR2 covalent-IN-14 displays little to no inhibitory potency on CCR1 and CCR5.The affinity of CCR2 covalent-IN-14 for both the C70S and C75S CCR2 mutants is significantly decreased compared to WT CCR2. |
|---|---|
| References | 1. Ortiz Zacarías NV, et al. J Med Chem. 2021 Mar 11;64(5):2608-2621. |
| Molecular Formula | C23H16Cl2F3N3O4S2 |
|---|---|
| Molecular Weight | 590.413 |