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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PITOLISANT草酸盐 | pitolisant oxalate | 362665-57-4 | (x)C2H2O4*C17H26ClNO |
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PI3K抑制剂(GDC-0032) | taselisib | 1282512-48-4 | C24H28N8O2 |
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PI3Kα抑制剂1 | N-hydroxy-2-(methyl((2-(6-(methylamino)pyridin-3-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)amino)pyrimidine-5-carboxamide | 1235449-52-1 | C23H25N9O3S |
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PI3KΔ抑制剂(ACALISIB) | (S)-2-(1-((9H-purin-6-yl)amino)ethyl)-6-fluoro-3-phenylquinazolin-4(3H)-one | 870281-34-8 | C21H16FN7O |
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PFK158游离 | PFK158 | 1462249-75-7 | C18H11F3N2O |
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PF-38414 | PF-3084014 | 1290543-63-3 | C27H41F2N5O |
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PF-3274167抑制剂 | (5-(3-(3-(2-chloro-4-fluorophenoxy)azetidin-1-yl)-5-(methoxymethyl)-4H-1,2,4-triazol-4-yl)-2-methoxypyridine) | 900510-03-4 | C19H19ClFN5O3 |
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PF 8380; 4-[3-氧代-3-(2-氧代-2,3-二氢苯并恶唑-6-基)丙基]哌嗪-1-羧酸 3,5-二氯苄酯 | 3,5-dichlorobenzyl 4-(3-oxo-3-(2-oxo-2,3-dihydrobenzo[d]oxazol-6-yl)propyl)piperazine-1-carboxylate | 1144035-53-9 | C22H21Cl2N3O5 |
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PEFICITINIB游离态 | Peficitinib | 944134-74-1 | C18H22N4O2 |
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PDK1抑制剂 | PS 48 | 1180676-32-7 | C17H15ClO2 |
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O型304 | 4-chloro-N-[2-[(4-chlorophenyl)methyl]-3-oxo-1,2,4-thiadiazol-5-yl]benzamide | 1261289-04-6 | C16H11Cl2N3O2S |
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Orteronel; 6-[(7S)-7-羟基-6,7-二氢-5H-吡咯并[1,2-c]咪唑-7-基]-N-甲基-2-萘甲酰胺 | Orteronel | 566939-85-3 | C18H17N3O2 |
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Olcegepant; N-[2-[5-氨基-1(S)-[4-(4-吡啶基)哌嗪-1-甲酰基]戊基氨基]-1(R)-(3,5-二溴-4-羟基苄基)-2-氧代乙基]-4-(2-氧代-1,2,3,4-四氢喹唑啉-3-基)哌啶-1-甲酰胺 | Olcegepant | 204697-65-4 | C38H47Br2N9O5 |
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OTSSP167盐酸盐 | OTSSP167 hydrochloride | 1431698-10-0 | C25H29Cl3N4O2 |
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OGA抑制剂(THIAMETG) | (3aR,6S)-2-ethylimino-5-(hydroxymethyl)-1,3a,5,6,7,7a-hexahydropyrano[3,2-d][1,3]thiazole-6,7-diol | 1009816-48-1 | C9H16N2O4S |
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OGA抑制剂(THIAMETG) | 2-(Ethylamino)-5-(hydroxymethyl)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d][1,3]thiazole-6,7-diol | 1009816-48-1 | C9H16N2O4S |
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OGA抑制剂(THIAMETG) | Thiamet G Discontinued | 1009816-48-1 | C9H16N2O4S |
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O-[(5-氨基-2-苯基-7-苯并恶唑基)甲基]-3,5-二氯-L-酪氨酸 | L-Tyrosine, O-((5-amino-2-phenyl-7-benzoxazolyl)methyl)-3,5-dichloro- | 1037592-40-7 | C23H19Cl2N3O4 |
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N,N'-[硫代双(2,1-乙二基-1,3,4-噻二唑-5,2-二基)]双苯乙酰胺 | 2-phenyl-N-[5-[2-[2-[5-[(2-phenylacetyl)amino]-1,3,4-thiadiazol-2-yl]ethylsulfanyl]ethyl]-1,3,4-thiadiazol-2-yl]acetamide | 314045-39-1 | C24H24N6O2S3 |
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N,N'-(1,4-亚苯基二-2,1-乙二基)双-2-丙烷磺酰胺 | [(methylethyl)sulfonyl]{2-[4-(2-{[(methylethyl)sulfonyl]amino}ethyl)phenyl]ethyl}amine | 380607-77-2 | C16H28N2O4S2 |
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N’-(1H-苯并咪唑-2-甲基)-N’-((S)-5,6,7,8-四氢喹啉-8-基)丁烷-1,4-二胺 | AMD070 | 558447-26-0 | C21H27N5 |
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Naquotinib甲磺酸盐 | 5-{[(3R)-1-acryloylpyrrolidin-3-yl]oxy}-6-ethyl-3-({4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}amino)pyrazine-2-carboxamide monomethansulfonate | 1448237-05-5 | CH4O3S*C30H42N8O3 |
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NVPBGJ398磷酸盐 | BGJ398 | 1310746-10-1 | C26H31Cl2N7O3*H3O4P |
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NSC 348884; N1,N1,N2,N2-四[(6-甲基-1H-苯并咪唑-2-基)甲基]-1,2-乙二胺 | N,N,N',N'-tetrakis[(6-methyl-1H-benzimidazol-2-yl)methyl]ethane-1,2-diamine | 81624-55-7 | C38H40N10 |
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NBD-556; N-(4-氯苯基)-N'-(2,2,6,6-四甲基哌啶-4-基)草酰胺 | NBD-556 | 333353-44-9 | C17H24ClN3O2 |
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NBC抑制剂(S0859) | 2-Chloro-N-((2'-(N-cyanosulfamoyl)-[1,1'-biphenyl]-4-yl)methyl)-N-(4-methylbenzyl)benzamide | 1019331-10-2 | C29H24ClN3O3S |
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NAMPT抑制剂(CB30865) | CB 30865 | 206275-15-2 | C26H22BrN5O2 |
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N6022抑制剂 | N6022 | 1208315-24-5 | C24H22N4O3 |
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N6-羟苄腺苷 | T1-11 | 110505-75-4 | C17H19N5O5 |
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N6-[2-[[4-(二乙基氨基)-1-甲基丁基]氨基]-6-甲基-4-嘧啶基]-2-甲基-4,6-喹啉二胺 | N<sup>6</sup>-[2-(4-diethylamino-1-methylbutylamino)-6-methyl-pyrimidin-4-yl]-2-methyl-quinoline-4,6-diamine | 733767-34-5 | C24H35N7 |
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N6-[2-[[4-(2,4-二氯苯基)-5-(1H-咪唑-2-基)-2-嘧啶基]氨基]乙基]-3-硝基-2,6-吡啶二胺 | CHIR 98014 | 556813-39-9 | C20H17Cl2N9O2 |
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N6-(3-碘苄基)腺苷-5'-N-甲基糖酰胺 | N<sup>6</sup>-(3-iodobenzyl)adenosine-5'-N-methyluronamide | 152918-18-8 | C18H19IN6O4 |
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N5-(6-氨基己基)-N7-苄基-3-异丙基吡唑并[1,5-a]嘧啶-5,7-二胺 | BS-181 | 1092443-52-1 | C22H32N6 |
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N3-(7-环丁基-3-苯基-1,2,4-三唑并[4,3-b]哒嗪-6-基)-N1,N1,2,2-四甲基-1,3-丙二胺 | Akt-l-1 | 473382-39-7 | C22H30N6 |
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N3-(4-氟苯基)-1H-吡唑并[3,4-D]嘧啶-3,4-二胺 | N3-(4-fluorophenyl)-1h-pyrazolo[3,4-d]pyrimidine-3,4-diamine | 522629-08-9 | C11H9FN6 |
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N2-[[3-[(2,1,3-苯并噻二唑-4-基磺酰基)氨基]-2-噻吩基]羰基]-L-精氨酸三氟乙酸盐 | (S)-2-{[3-(benzo[1,2,5]thiadiazole-4-sulfonylamino)thiophene-2-carbonyl]amino}-5-guanidino-pentanoic acid trifluoroacetate | 1210945-69-9 | C2HF3O2*C17H19N7O5S3 |
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N2-(7-氯-4-喹啉基)-N1-[2-[(7-氯-4-喹啉基)氨基]乙基]-N1-甲基-1,2-乙二胺 | Lys-05 | 1391426-22-4 | C23H23Cl2N5 |
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N2'-(反式-4-氨基环己基)-5'-氯-N6-[(3-氟苯基)甲基]-[2,4'-联吡啶]-2',6-二胺 | N2'-(trans-4-aminocyclohexyl)-5'-chloro-N6-(3-fluorobenzyl)-2,4'-bipyridine-2',6-diamine | 1263369-28-3 | C23H25ClFN5 |
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N1-(4-氯苯基)-6-甲基-N5-[3-(9H-嘌呤-6-基)-2-吡啶]-1,5-异喹啉二胺 | N5-(3-(9H-purin-6-yl)pyridin-2-yl)-N1-(4-chlorophenyl)-6-methylisoquinoline-1,5-diamine | 1093100-40-3 | C26H19ClN8 |
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N1-(2-氨基苯基)-N8-苯基辛烷二酰胺 | BML-210 | 537034-17-6 | C20H25N3O2 |
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N1-(2-氨基苯基)-N7-(4-甲基苯基)庚二酰胺 | pimelic diphenylamide 106 | 937039-45-7 | C20H25N3O2 |
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N-(9,10-二氧杂菲基-2-基)-2,2-二甲基丙酰胺 | Protein Tyrosine Phosphatase CD45 Inhibitor | 345630-40-2 | C19H17NO3 |
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N-(5-(N-(4-(1,1,1,3,3,3-六氟-2-羟基丙烷-2-基)苯基)氨磺酰基)-4-甲基噻唑-2-基)乙酰胺 | SR1001 | 1335106-03-0 | C15H13F6N3O4S2 |
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N-(4-氯苯胺基)-N'-(4-氯苯基)-3,3-二甲基-2-氧代丁酰胺基酰胺 | (E)-N,N’-bis(4-chlorophenyl)-3,3-dimethyl-2-oxobutanehydrazonamide | 934369-14-9 | C18H19Cl2N3O |
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N-苯基-4-[[(苯基氨基)硫代甲酰基]氨基]苯磺酰胺 | N-phenyl-4-[[(phenylamino)thioxomethyl]amino]benzenesulfonamide | 245342-14-7 | C19H17N3O2S2 |
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N-脱甲基奈妥吡坦 | 2-(3,5-bistrifluoromethylphenyl)-N-methyl-N-(6-piperazin-1-yl-4-o-tolylpyridin-3-yl)isobutyramide | 290296-72-9 | C29H30F6N4O |
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N-羟基-4-[(1,2,3,4-四氢-2-甲基-5H-吡啶并[4,3-b]吲哚-5-基)甲基]苯甲酰胺 2,2,2-三氟乙酸酯 | Tubastatin A (trifluoroacetic salt) | 1239262-52-2 | C2HF3O2*C20H21N3O2 |
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N-羟基-2-[4-(2-萘磺酰基)-1-哌嗪]-5-嘧啶羧酰胺 | N-hydroxy-2-(4-(naphthalen-2-ylsulfonyl)piperazin-1-yl)pyrimidine-5-carboxamide | 604769-01-9 | C19H19N5O4S |
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N-甲基-L-丙氨酰-(2S)-2-环己基甘氨酰-N-[2-(2-恶唑基)-4-苯基-5-噻唑基]-L-脯氨酰胺 | CUDC-427 | 1446182-94-0 | C29H36N6O4S |
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N-环丙基-5-(噻吩-2-基)异恶唑-3-甲酰胺 | N-cyclopropyl-5-(thiophen-2-yl)isoxazole-3-carboxamide | 832115-62-5 | C11H10N2O2S |
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