Question: Please type the answers, avoid hand writting (answer as many as you can please). Much appreciated. Binding data Compound CXCR21C50 ID InM) MC4-1 36 MC4-2
Binding data Compound CXCR21C50 ID InM) MC4-1 36 MC4-2 3600 MC4-3 476 MC4-4 28,000 MC4-5 1000 MC4-6 20 MC4-7 3.0 MC4-8 7200 MC4.0 15 MC4-10 17 MC4-11 6.8 MC4-12 3.8 MC4-13 2.6 CXCRTIC50 InM Inactive Inactive Inactive Inactive inactive Inactive Inactive inactive 910 3058 254 26 1843 Using the information above, please answer the following 1. a) Which compound is the most potent inhibitor of CXCR2Based on the SAR of compounds MC4-1 through MC4-8 what functional groups are contributing to the potency of this compound? (Draw the compound and circle contributing functional groups) b) Considering only compounds MC4-9 through MC4-13, which compound is the most selective for CXCR2 over CXCRIP Which compound is the least selective? Draw the structural feature that is responsible for enhanced CXCRT potency c) Compounds MCA through MC4-8 were unsuitable for further development de to poor solubility. The remaining compounds had acceptable solubility and one of them entered human clinical trials. What structural feature contributed to poor solubility? What forces phenomena may account for this? Using only combinations of groups trom these molecules propose a new, closely related structure that is likely to be a potent, dual-inhibitor of CXCR2 and CXCR1. Drawit. Please answer it with clarifications. Thank you in advance
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