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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[4-[[5-氟-4-[2-甲基-1-(1-甲基乙基)-1H-咪唑-5-基]-2-嘧啶基]氨基]苯基][(3S)-3-(甲氨基)-1-吡咯烷]甲酮 | AZD5597 | 924641-59-8 | C23H28FN7O |
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[4-[[1-[(3-氟苯基)甲基]-1H-吲唑-5-基]氨基]-5-甲基吡咯并[2,1-F][1,2,4]三嗪-6-基]氨基甲酸(3S)-3-吗啉基甲基酯盐酸盐 | BMS-599626 | 873837-23-1 | C27H27FN8O3*ClH |
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[4-[(羟基氨基)羰基]苯基]氨基甲酸 [6-[(二乙基氨基)甲基]-2-萘基]甲酯 | Givinostat | 497833-27-9 | C24H27N3O4 |
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[4-(2-氯-4-硝基苯基)-1-哌嗪基](5-甲基-3-苯基-4-异恶唑基)甲酮 | (4-(2-chloro-4-nitrophenyl)piperazin-1-yl)(5-methyl-3-phenylisoxazol-4-yl)methanone | 341001-38-5 | C21H19ClN4O4 |
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[3,4-二氟-2-[(2-氟-4-碘苯基)氨基]苯基][3-羟基-3-[(2R)-2-哌啶基]-1-氮杂环丁基]甲酮 | cobimetinib | 934660-94-3 | C21H21F3IN3O2 |
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[2H3]-盐酸阿洛司琼 | Alosetron-d3 Hydrochloride | 1189919-71-8 | C17H19ClN4O |
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[2-[4-(2-甲氧基苯基)哌嗪-1-基]乙基](丙基)(4,5,6,7-四氢苯并噻唑-6-基)胺 | N-[2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl]-N-propyl-4,5,6,7-tetrahydro-1,3-benzothiazol-6-amine | 1148156-63-1 | C23H34N4OS |
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[2-[(3-甲基丁基)氨基]-3-吡啶基][4-(苯基甲基)-1-哌嗪基]甲酮 | (4-benzylpiperazin-1-yl)(2-(isopentylamino)pyridin-3-yl)methanone | 1270138-40-3 | C22H30N4O |
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[2-(4-氯苯基)喹啉-4-基]-(2-哌啶基)甲醇 | NSC13316 | 5428-80-8 | C21H21ClN2O |
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[1-(乙基磺酰基)-3-[4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基]氮杂环丁烷-3-基]乙腈磷酸盐 | baricitinib phosphate | 1187595-84-1 | C16H17N7O2S*H3O4P |
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[(S)-1-[[(S)-1-[[4-(羟甲基)苯基]氨基]-1-氧代-5-脲基戊烷-2-基]氨基]-3-甲基-1-氧代丁-2-基]氨基甲酸(9H-芴-9-基)甲酯 | (9H-fluoren-9-yl)methyl ((S)-1-(((S)-1-((4-(hydroxymethyl)phenyl)amino)-1-oxo-5-ureidopentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)carbamate | 159858-22-7 | C33H39N5O6 |
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[(4R,5S)-4,5-双(4-氯苯基)-2-[4-(1,1-二甲基乙基)-2-乙氧基苯基]-4,5-二氢-4,5-二甲基-1H-咪唑-1-基][4-[3-(甲磺酰基)丙基]-1-哌嗪基]甲酮 | RG-7112 | 939981-39-2 | C38H48Cl2N4O4S |
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[(1S,6S,7S,8R,8aR)-1,7,8-三羟基-1,2,3,5,6,7,8,8a-八氢吲嗪-6-基] 丁酸酯 | celgosivir | 121104-96-9 | C12H21NO5 |
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Z-因多昔芬盐酸盐 | Endoxifen hydrochloride | 1032008-74-4 | C25H27NO2*ClH |
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Y-39983二盐酸盐 | (R)-4-(1-Aminoethyl)-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzamide dihydrochloride | 173897-44-4 | C16H18Cl2N4O |
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Walrycin B; 1,6-二甲基-3-[4-(三氟甲基)苯基]嘧啶并[5,4-e]-1,2,4-三嗪-5,7(1H,6H)-二酮 | 1,6-dimethyl-3-[4-(trifluoromethyl)phenyl]pyrimido[5,4-e][1,2,4]triazine-5,7-dione | 878419-78-4 | C14H10F3N5O2 |
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WAY 161503盐酸盐 | 8,9-dichloro-2,3,4,4a-tetrahydro-1H,6H-pyrazino[1,2-a]quinoxalin-5-one | 75704-24-4 | C11H11Cl2N3O |
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Vicriviroc苹果酸盐;1-[(4,6-二甲基-5-嘧啶基)羰基]-4-[(3S)-4-[(1R)-2-甲氧基-1-[4-(三氟甲基)苯基]乙基]-3-甲基-1-哌嗪基]-4-甲基哌啶苹果酸盐 | 1-[(4,6-Dimethyl-5-pyrimidinyl)carbonyl]-4-[(3S)-4-[(1R)-2-methoxy-1-[4-(trifluoromethyl)phenyl]ethyl]-3-methyl-1-piperazinyl]-4-methylpiperidine malate | 541503-81-5 | C32H44F3N5O7 |
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Val-cit-PAB-OH(VAL-CIT-PAB-羟基) | (S)-2-((S)-2-amino-3-methylbutanamido)-N-(4-(hydroxymethyl)phenyl)-5-ureidopentanamide | 159857-79-1 | C18H29N5O4 |
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VUF11207三氟乙酸酯盐 | VUF11207 | 1378524-41-4 | C27H35FN2O4 |
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VER155008抑制剂 | VER155008 | 1134156-31-2 | C25H23Cl2N7O4 |
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Uprosertib,GSK2141795抑制剂 | N-{(1S)-2-amino-1-[(3,4-difluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-furancarboxamide | 1047634-65-0 | C18H16Cl2F2N4O2 |
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Tirasemtiv(CK-2017357)抑制剂 | 6-ethynyl-1-(pentan-3-yl)-1H-imidazo[4,5-b]pyrazin-2(3H)-one | 1005491-05-3 | C12H14N4O |
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TRPM8离子通道激动剂(ICILIN) | 3-(2-hydroxy-phenyl)-6-(3-nitro-phenyl)-3,4-dihydro-1H-pyrimidin-2-one | 36945-98-9 | C16H13N3O4 |
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TMC353121;2-[[6-[[[2-(3-羟基丙基)-5-甲基苯基]氨基]甲基]-2-[[3-(吗啉-4-基)丙基]氨基]苯并咪唑-1-基]甲基]-6-甲基吡啶-3-醇 | TMC-353121 | 857066-90-1 | C32H42N6O3 |
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TH588抑制剂 | TH588 | 1609960-31-7 | C13H12Cl2N4 |
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TH 302; N,N'-双(2-溴乙基)二氨基膦酸 (1-甲基-2-硝基-1H-咪唑-5-基)甲酯 | evofosfamide | 918633-87-1 | C9H16Br2N5O4P |
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TARIQUIDAR二甲磺酸盐六水合物 | Tariquidar (methanesulfonate, hydrate) | 625375-83-9 | C40H52N4O15S2 |
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TAK960抑制剂 | TAK-960 | 1137868-52-0 | C27H34F3N7O3 |
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Solcitinib抑制剂 | N-[5-[4-(3,3-dimethylazetidine-1-carbonyl)phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide | 1206163-45-2 | C22H23N5O2 |
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SKQ1溴化物 | 2,3-dimethyl-1,4-benzoquinon-5-decyl-triphenylphosphonium bromide | 934826-68-3 | Br*C36H42O2P |
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SIRT1抑制剂(INAUHZIN) | 2-((5H-[1,2,4]triazino[5,6-b]indole-3yl)thio)-1-(10H-phenothiazin-10-yl)butan-1-one | 309271-94-1 | C25H19N5OS2 |
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SD-06; 3-[N-(2-羟基乙酰基)-4-哌啶基]-4-(4-嘧啶基)-5-(4-氯苯基)吡唑 | 2-{4-[3-(4-chlorophenyl)-4-pyrimidin-4-yl-1H-pyrazol-5-yl]piperidin-1-yl}-2-oxoethanol | 271576-80-8 | C20H20ClN5O2 |
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SB269970盐酸盐 | (R)-3-((2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)phenol | 201038-74-6 | C18H28N2O3S |
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SB242235;4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 | 4-(4-fluorophenyl)-5-(2-methoxypyrimidine-4-yl)-1-(piperidine-4-yl)imidazole | 193746-75-7 | C19H20FN5O |
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SB1317(TG02)抑制剂 | TG02 | 1204918-72-8 | C23H24N4O |
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SB-408124盐酸盐 | SB-408124 Hydrochloride | 1431697-90-3 | C19H19ClF2N4O |
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SB 705498; N-(2-溴苯基)-N'-[(3R)-1-[5-(三氟甲基)-2-吡啶基]-3-吡咯烷基]脲 | N-(2-bromophenyl)-N'-[((R)-1-(5-trifluoromethyl-2-pyridyl)pyrrolidin-3-yl)]urea | 501951-42-4 | C17H16BrF3N4O |
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SB 242084双盐酸盐 水合物 | SB 242084 | 181632-25-7 | C21H19ClN4O2 |
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RO5126766(CH5126766)抑制剂 | VS-6766 | 946128-88-7 | C21H18FN5O5S |
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RGX-104游离酸 | 2-[3-[(3R)-3-[[2-chloro-3-(trifluoromethyl)phenyl]methyl-(2,2-diphenylethyl)amino]butoxy]phenyl]acetic acid | 610318-54-2 | C34H33ClF3NO3 |
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RET激酶抑制剂(AST487) | AST-487 | 630124-46-8 | C26H30F3N7O2 |
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REPERTAXINL-赖氨酸盐 | R(-)-2-(4-isobutylphenyl)propionyl methanesulfonamide L-lysine salt | 266359-93-7 | C6H14N2O2*C14H21NO3S |
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REL-N-[5-[4-[5-[[(2R,6S)-2,6-二甲基-4-吗啉基]甲基]-2-恶唑基]-1H-吲唑-6-基]-2-甲氧基-3-吡啶基]甲烷磺酰胺 | N-[5-[4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1H-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methanesulfonamide | 1254036-66-2 | C24H28N6O5S |
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RAF抑制剂(LY3009120) | LY3009120 | 1454682-72-4 | C23H29FN6O |
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R7128;(2'R)-2'-去氧-2'-氟-2'-甲基胞苷3',5'-双(2-甲基丙酸)酯 | (2R,3R,4R,5R)-5-(4-amino-2-oxopyrimidin-1(2H)-yl)-4-fluoro-2-((isobutyryloxy)methyl)-4-methyltetrahydrofuran-3-yl isobutyrate | 940908-79-2 | C18H26FN3O6 |
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R-利伐沙班 | 5-R-rivaroxaban | 865479-71-6 | C19H18ClN3O5S |
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P游离酸 | 2-[[2-[[2-[[2-[[2-[[5-Amino-2-[[5-amino-2-[[1-[6-amino-2-[[1-[2-amino-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-5-oxopentanoyl]amino]-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoic acid | 71977-09-8 | C63H97N17O14S |
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PTC-209抑制剂 | PTC-209 | 315704-66-6 | C17H13Br2N5OS |
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PKR抑制剂(MITAPIVAT) | N-(4-(4-(cyclopropylmethyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide | 1260075-17-9 | C24H26N4O3S |
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