512177-83-2
512177-83-2 結(jié)構(gòu)式
基本信息
(5R)-4-乙?；?1-(4-氯-2-氟苯基)-5-環(huán)己基-1,5-二氫-3-羥基-2H-吡咯-2-酮
(R)-4-Acetyl-1-(4-chloro-2-fluorophenyl)-5-cyclohexyl-3-hydroxy-1H-pyrrol-2(5H)-one
(R)-4-acetyl-1-(4-chloro-2-fluorophenyl)-5-cyclohexyl-3-hydroxy-1,5-dihydro-2H-pyrrol-2-one
(5R)-4-Acetyl-1-(4-chloro-2-fluorophenyl)-5-cyclohexyl-1,5-dihydro-3-hydroxy-2H-pyrrol-2-one
2H-Pyrrol-2-one, 4-acetyl-1-(4-chloro-2-fluorophenyl)-5-cyclohexyl-1,5-dihydro-3-hydroxy-, (5R)-
物理化學(xué)性質(zhì)
常見問題列表
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CCR2 103 nM (IC 50 , in U2OS-CCR2 cells) |
The chemokine receptor CCR2 is a G protein-coupled receptor that is involved in many diseases characterized by chronic inflammation, and therefore a large variety of CCR2 small molecule antagonists has been developed. CCR2-RA-[R] displaces [ 125 I]CCL2 from CCR2 with an pIC 50 value of 6.1. The pK D of CCR2-RA-[R] for CCR2 and CCR5 is 8.8±0.1 and 7.0±0.1, respectively. CCR2-RA-[R] inhibits CCR2 non-competitively by blocking activation-associated conformational changes and formation of the G protein-binding interface. The binding pocket of CCR2-RA-[R] is highly enclosed and possesses a balanced combination of hydrophobic and polar features, all of which favors pocket “druggability”.