激动剂和抑制剂
在生物化学和药物化学领域中,激动剂和抑制剂是调节受体活性的重要分子类型。
激动剂:激动剂是指能够与特定受体结合并激活该受体,从而引起细胞内信号传递的化合物。它们通过与受体的特定位点相互作用,模拟天然配体的功能,导致生物效应的发生或增强。根据其对受体的作用机制不同,激动剂可以分为完全激动剂和部分激动剂。
完全激动剂:能够完全激活受体,达到最大生物活性。
部分激动剂:仅能部分地激活受体,即使在高浓度下也不表现出最大效应。
抑制剂:抑制剂则是相反的一类分子,它们通过与受体或其相关蛋白质结合来阻止信号传导过程。根据作用机制的不同,可以分为竞争性抑制剂和非竞争性抑制剂。
竞争性抑制剂:这些物质通过占据活性位点而减少激动剂的结合能力,通常可以通过增加激动剂浓度来克服这种抑制效应。
非竞争性抑制剂:这类抑制剂不依赖于受体结合部位,而是通过其他方式干扰信号传递,如改变受体构象或直接与G蛋白相互作用。
在药物研发过程中,激动剂和抑制剂的研究至关重要。它们不仅用于治疗疾病,还可以帮助理解生物系统的工作原理。例如,在神经科学领域,激动剂可以被用作治疗抑郁、焦虑等精神疾病的药物;而在癌症研究中,则可能使用抑制剂来阻断促进肿瘤生长的信号通路。
中文名称 | 英文名称 | CAS号 | 化学式 | 结构式图片 |
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L-缬氨酸,L-组氨酰-L-组氨酰-L-亮氨酰甘氨酰甘氨酰-L-丙氨酰-L-赖氨酰-L-谷酰 | His-his-leu-gly-gly-ala-lys-gln-ala-gly-asp-val | 89105-94-2 | C50H80N18O16 |
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L-丝氨酰-L-精氨酰-L-脯氨酰-L-苏氨酰-L-alpha-谷氨酰-L-赖氨酰-L-苏氨酰-L-异亮氨酰-L-苯丙氨酰-L-异亮氨酰-L-异亮氨酸 | H-Ser-Arg-Pro-Thr-Glu-Lys-Thr-Ile-Phe-Ile-Ile-OH | 198284-64-9 | C60H101N15O17 |
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KNK437(热激蛋白抑制剂I) | N-Formyl-3,4-methylenedioxy-benzylidine-gamma-butyrolactam | 218924-25-5 | C13H11NO4 |
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KGA和GAC抑制剂(CB-839) | CB-839 | 1439399-58-2 | C26H24F3N7O3S |
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KB-R7943甲磺酰酸盐 | 2-[2-[4-(4-Nitrobenzyloxy)phenyl]ethyl]isothiourea mesylate | 182004-65-5 | C17H21N3O6S2 |
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JNK抑制剂(BI-78D3) | 4-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)-3-((5-nitrothiazol-2-yl)thio)-1H-1,2,4-triazol-5(4H)-one | 883065-90-5 | C13H9N5O5S2 |
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JDTic;(3R)-1,2,3,4-四氢-7-羟基-N-[(1S)-1-[[(3R,4R)-4-(3-羟基苯基)-3,4-二甲基-1-哌啶基]甲基]-2-甲基丙基]-3-异喹啉甲酰胺 | (3R)-7-hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide | 361444-66-8 | C28H39N3O3 |
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JAK2抑制剂V,Z3 | NSC 42834 | 195371-52-9 | C23H24N2O |
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Ivacaftor苯磺酸盐 | N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide.besylate | 1134822-09-5 | C6H6O3S*C24H28N2O3 |
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Ipragliflozin; (1S)-1,5-脱水-1-C-[3-[(1-苯并噻吩-2-基)甲基]-4-氟苯基]-D-葡糖醇 | ipragliflozin | 761423-87-4 | C21H21FO5S |
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IRAK-1-4 抑制剂 I | IRAK-1/4 Inhibitor | 509093-47-4 | C20H21N5O4 |
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IRAK 抑制剂 6; N-[2-甲氧基-4-(4-吗啉基)苯基]-2-(3-吡啶基)-4-噻唑甲酰 | IRAK inhibitor 6 | 1042672-97-8 | C20H20N4O3S |
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Histone Acetyltransferase抑制剂 | remodelin | 949912-58-7 | C15H14N4S |
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HCV 796; 5-环丙基-2-(4-氟苯基)-6-[(2-羟基乙基)(甲基磺酰基)氨基]-N-甲基-3-苯并呋喃甲酰胺 | nesbuvir | 691852-58-1 | C22H23FN2O5S |
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Givinostat盐酸盐 | diethyl-[6-(4-hydroxycarbamoyl-phenylcarbamoyloxymethyl)-naphthalen-2-yl-methyl]-ammonium chloride | 199657-29-9 | C24H27N3O4*ClH |
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GW627368X抑制剂 | N-(benzenesulfonyl)-2-[4-(4,9-diethoxy-3-oxo-1H-benzo[f]isoindol-2-yl)phenyl]acetamide | 439288-66-1 | C30H28N2O6S |
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GSK2193874游离态 | GSK2193874 | 1336960-13-4 | C37H38BrF3N4O |
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GPR109A受体激动剂(MK-0354) | MK-0354 | 851776-28-8 | C7H8N6 |
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GNE-495游离态 | 8-amino-N-(1-(cyclopropanecarbonyl)azetidin-3-yl)-2-(3-fluorophenyl)-1,7-naphthyridine-5-carboxamide | 1449277-10-4 | C22H20FN5O2 |
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GNE-477抑制剂 | GNE-477 | 1032754-81-6 | C21H28N8O3S2 |
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GLYX13抑制剂 | Glyx-13 | 117928-94-6 | C18H31N5O6 |
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GENZ-644282抑制剂 | 2,3-dimethoxy-12-(2-(methylamino)ethyl)[1,3]dioxolo[4',5':4,5]-benzo[1,2-h]benzo[c][1,6]naphthyridin-13(12H)-one | 529488-28-6 | C22H21N3O5 |
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Forxiga; 丙二醇达格列嗪水合物 | dapagliflozin (S) propylene glycol hydrate | 960404-48-2 | C3H8O2*C21H25ClO6*H2O |
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Fagomine; 桑叶生物碱; (2R,3R,4R)-2-羟甲基哌啶-3,4-二醇 | D-fagomine | 53185-12-9 | C6H13NO3 |
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FRAX1036游离态 | Frax1036 | 1432908-05-8 | C28H32ClN7O |
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EZATIOSTAT游离的 | γ-glutamyl-S-(benzyl)cysteinyl-(R)-(-)-phenylglycine diethyl ester | 168682-53-9 | C27H35N3O6S |
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ERRΒ/Γ激动剂(GSK-4716) | (E)-N'-(4-(diethylamino)benzylidene)-4-hydroxybenzohydrazide | 95167-41-2 | C18H21N3O2 |
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EMD638683 (形态 S); (alphaS)-3,5-二氟-alpha-羟基苯乙酸 2-(2-乙基-4-羟基-3-甲基苯甲酰基)肼 | N'-[(S)-2-(3,5-difluorophenyl)-2-hydroxyacetyl]-2-ethyl-4-hydroxy-3-methylbenzohydrazide | 1184940-46-2 | C18H18F2N2O4 |
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EMD638683 (形态 R); (alphaR)-3,5-二氟-alpha-羟基苯乙酸 2-(2-乙基-4-羟基-3-甲基苯甲酰基)肼 | N'-[(R)-2-(3,5-difluorophenyl)-2-hydroxyacetyl]-2-ethyl-4-hydroxy-3-methylbenzohydrazide | 1184940-47-3 | C18H18F2N2O4 |
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EMD 534085; N-[2-(二甲基氨基)乙基]-N'-[[(2R,4aS,5R,10bS)-3,4,4a,5,6,10b-六氢-5-苯基-9-(三氟甲基)-2H-吡喃并[3,2-c]喹啉-2-基]甲基]脲 | EMD 534085 | 858668-07-2 | C25H31F3N4O2 |
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Decernotinib(VX-509)抑制剂 | (R)-2-((2-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl)amino)-2-methyl-N-(2,2,2-trifluoroethyl)butanamide | 944842-54-0 | C18H19F3N6O |
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DL-青霉胺 | DL-Penicillamin | 52-66-4 | C5H11NO2S |
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DL-肉碱盐酸盐 | dl-carnitine hydrochloride | 461-05-2 | C7H16NO3*Cl |
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DL-肉碱 | L-carnitine | 406-76-8 | C7H15NO3 |
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DL-犬尿氨酸 | Kynurenine | 343-65-7 | C10H12N2O3 |
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D-精氨酰-2,6-二甲基-L-酪氨酰-L-赖氨酰-L-苯丙氨酰胺 | D-Arg-2'6'-Dmt-Lys-Phe-NH<sub>2</sub> | 736992-21-5 | C32H49N9O5 |
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Ciproxidine; 1-[3-[3-(4-氯苯基)丙氧基]丙基]哌啶盐酸盐 | pitolisant hydrochloride | 903576-44-3 | C17H26ClNO*ClH |
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CP640186抑制剂 | (3R)-1'-(9-anthrylcarbonyl)-3-(morpholin-4-ylcarbonyl)-1,4'-bipiperidine | 591778-68-6 | C30H35N3O3 |
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CO-1686氢溴酸盐 | Rociletinib hydrobromide | 1446700-26-0 | 2BrH*C27H28F3N7O3 |
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CGP 60474; 3-[[4-[2-[(3-氯苯基)氨基]-4-嘧啶基]-2-吡啶基]氨基]-1-丙醇 | CGP-60474 | 164658-13-3 | C18H18ClN5O |
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CFI-400945游离态 | (1R,2S)-(E)-2-(3-(4-((cis-2,6-dimethylmorpholino)methyl)styryl)-1H-indazol-6-yl)-5‘-methoxyspiro[cyclopropane-1,3’-indolin]-2-one | 1338806-73-7 | C33H34N4O3 |
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CEP-32496(盐酸盐) | 1-[3-(6,7-dimethoxy-quinazolin-4-yloxy)-phenyl]-3-[5-(2,2,2-trifluoro-1,1-dimethylethyl)isoxazol-3-yl]urea hydrochloride | 1227678-26-3 | C24H22F3N5O5*ClH |
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CCT 241533; (3R,4S)-4-[[2-(5-氟-2-羟基苯基)-6,7-二甲氧基-4-喹唑啉基]氨基]-alpha,alpha-二甲基-3-吡咯烷甲醇 | CCT241533 | 1262849-73-9 | C23H27FN4O4 |
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CB 300919; 4-[[[7-氯-3,4-二氢-3-甲基-2-[(4-甲基-1-哌嗪基)甲基]-4-氧代-6-喹唑啉基]甲基]-2-丙炔-1-基氨基]-N-(3-吡啶基甲基)苯甲酰胺 | CB 300919 | 289715-28-2 | C32H34ClN7O2 |
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Buparlisib盐酸盐 | 5-(2,6-dimorpholin-4-ylpyrimidin-4-yl)-4-trifluoromethylpyridin-2-ylamine hydrochloride | 1312445-63-8 | C18H21F3N6O2*ClH |
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BTZ 043;2-[(2S)-2-甲基-1,4-二氧杂-8-氮杂螺[4.5]癸烷-8-基]-8-硝基-6-三氟甲基-4H-1,3-苯并噻嗪-4-酮 | 2-[(2S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]dec-8-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one | 1161233-85-7 | C17H16F3N3O5S |
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BMS-687453抑制剂 | BMS-687453 | 1000998-59-3 | C22H21ClN2O6 |
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BIIB-024; 6-氨基-5-氯-N-[(1R)-1-[5-[[[5-氯-4-(三氟甲基)-2-吡啶基]氨基]羰基]-2-噻唑基]乙基]-4-嘧啶甲酰胺 | (R)-2-(1-(6-amino-5-chloropyrimidine-4-carboxamido)ethyl)-N-(5-chloro-4-(trifluoromethyl)pyridin-2-yl)thiazole-5-carboxamide | 1096708-71-2 | C17H12Cl2F3N7O2S |
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BI-847325,MEK和极光激酶(AK)的ATP竞争性双重抑制剂 | (Z)-3-(3-(((4-((dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide | 1207293-36-4 | C29H28N4O2 |
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BEZ235 对甲苯磺酸盐 | 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile monotosylate salt | 1028385-32-1 | C7H8O3S*C30H23N5O |
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