TRP Channel
TRP channels (Transient receptor potential channels) are a group of ion channels located mostly on the plasma membrane of numerous animal cell types. There are about 28 TRP channels that share some structural similarity to each other. These are grouped into two broad groups: Group 1 includes TRPC,TRPV,TRPM,TRPN, and TRPA. In group 2, there are TRPP ,and TRPML. Many of these channels mediate a variety of sensations like the sensations of pain, hotness, warmth or coldness, different kinds of tastes, pressure, and vision. TRPs have been seen to have complex multidimensional roles in sensory signaling. Many TRPs function as intracellular calcium release channels.
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CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM.
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AVL-292是共价结合的，高选择性口服活性Btk抑制剂，IC50为0.5 nM，比对其它激酶的抑制性高1400倍以上。
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Probenecid是一种经典的有机阴离子运输竞争性抑制剂，同时也是一种瞬时感受器电位香草素受体亚家族2(TRPV2)的激动剂和人苦味觉感受器TAS2R16的抑制剂。
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CNX-774是口服活性的高效Btk抑制剂，IC50< 1 nM，能与活性位点上的Cys-481形成配体导向的共价键。
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AMG-517是一种有效的，选择性的TRPV1拮抗剂，抑制TRPV1的Capsaicin， Proton和热激活，IC50分别为0.76 nM， 0.62 nM和1.3 nM。AMG 517抑制 CAP-(500 nM), 酸 (pH 5.0),或热(45°C) 诱导的45Ca2+流入人体表达TRPV1的CHO细胞， IC50分别为0.76 nM, 0.62 nM 和 1.3 nM。AMG 517作用于表达TRPV1的细胞，抑制Capsaicin, Proton, 和热诱导的内向电流。AMG 517作用于大鼠背根神经节神经元，抑制Capsaicin诱导的天然TRPV1激活，IC50值为0.68 nM。
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