ep3

CBP/EP300-IN-1是一种 CBP/EP300 溴结构域抑制剂。

Anisotropine Methylbromide 是一种抗胆碱能药物，已用于缓解胃肠道痉挛和抑制胃酸分泌。

PF-04418948 是一种可口服的，选择性的前列腺素EP2受体拮抗剂，IC50为16 nM。

Prostaglandin E1 (Alprostadil) 是一种前列腺素受体配体，对小鼠 EP1、EP2、EP3、EP4和 IP 的 Ki 值分别为 36、10、1.1、2.1 和 33 nM。它诱导血管舒张并抑制血小板聚集，可作为血管扩张剂用于外周血管疾病的研究。

AH 6809 是 EP 和 DP 受体的拮抗剂，对小鼠 EP2受体的 Ki 值为 350 nM，对克隆的人类 EP1，EP2，EP3-III 和 DP 受体的 Ki 值分别为 1217、1150、1597 和 1415 nM。

ONO-AE3-208 (AE 3-208) 是一种 EP4 拮抗剂，可抑制前列腺癌的细胞迁移、侵袭和转移。

TG4-155 是一种脑渗透性 EP2 拮抗剂，对 EP2 和 DP1 具有低纳摩尔的拮抗活性。它作用于 EP2 的 KB 为 2.4 nM，比对 DP1 受体的选择性高 14 倍，比对 EP1、EP3、EP4 和 IP 的选择性比高 550-4750 倍。

EP4 receptor antagonist 1 是一种有效的特异性前列腺素 EP4受体拮抗剂，对人和小鼠 EP4受体的 IC50分别为6.1 nM 和16.2 nM。 EP4 receptor antagonist 1 可用于癌症免疫治疗的研究。

CJ-42794 (CJ-042794)是前列腺素受体 EP4的选择性拮抗剂, 抑制[3H]-PGE2与 EP4受体结合的平均 pKi 为8.5, 对 EP4选择性比 EP1, EP2和 EP3高200多倍。

Treprostinil diethanolamine (UT-15C) 是EP2、DP1和IP 的有效激动剂，对EP2、DP1、IP、EP1、EP4、EP3 和 FPKi 的值分别为 3.6、4.4、32.1、212、826、2505 和 4680 nM。Treprostinil diethanolamine 能够促使 cAMP 的上调，进而维持血管系统内的稳态，并造成人肺动脉的血管扩张。

Travoprost (Fluprostenol isopropyl ester) 是一种异丙基酯前药，是一种高亲和力的，选择性的 FP 前列腺素全受体激动剂。它能够降低眼压，有潜力应用于青光眼和眼高压。

Treprostinil (Orenitram) 是有效的 DP1、IP 和 EP2 激动剂，EC50分别为0.6、1.9 和 6.2 nM。

DG-041 是高亲和力，选择性的，有效的 EP3受体拮抗剂，在结合和 FLIPR 试验中，IC50分别为 4.6 nM 和 8.1 nM。DG-041通过抑制 PGE2促进血小板聚集。DG-041具有血脑屏障渗透性。

EP3是一种具有抗细菌和抗真菌活性的抗菌肽。该化合物对E. gallinarum、P. pyocyanea、A. baumanii、K. terrigena展示出MIC值为11.4 μg/mL的抑制效果。EP3也显示了对癌细胞的抗肿瘤作用，并能诱导细胞凋亡(apoptosis)。

EP3 antagonist 3 (compound 2) is a highly effective and specific antagonist of the EP3 receptor. It displays significant oral bioavailability and exhibits a strong pKi value of 8.3. Furthermore, EP3 antagonist 3 possesses excellent pharmacokinetic characteristics, making it a suitable candidate for experimental investigations involving overactive bladder (OAB) research [1].

EP3 antagonist 4 是一种 EP3 拮抗剂，对 hEP 有抑制作用， Ki 值为 2 nM。EP3 antagonist 4 在大鼠完整 PK 研究中显示出较低的体内清除率、高口服 AUC 和良好的生物利用度。EP3 antagonist 4 可用于研究糖尿病和细胞功能障碍。

EP3 antagonist 6 (compound 5)作为一种选择性的EP3 receptor拮抗剂，显示出口服有效性，其IC50值达到1.9 nM。它能有效抑制PGE2诱导的妊娠大鼠子宫收缩。

EP3 antagonist 7 (Compound II) 为EP3受体拮抗剂，主要应用于瘙痒、疼痛、排尿困难及应激性疾病的研究。

Compound 22 (EP3 antagonist 5) 是一种针对EP3受体的拮抗剂，其IC50为67 nM。

AtPep3 TFA is a hormone-like peptide that plays a role in the salinity stress tolerance of plants.

AtPep3 is a hormone-like peptide that plays a role in the salinity stress tolerance of plants.

CBP EP300 bromodomain receptor-IN-1 (Compound 10) 作为一种溴结构域受体抑制剂，能有效与具备溴结构域的蛋白进行结合，其结合效能达到纳摩尔级别。

EP39 是一种有效的HIV-1成熟抑制剂。EP39 与 Gag 的 SP1 结构域相互作用。EP39 通过与 SP1 结构域的 QVT 基序结合来降低 CA-SP1 连接的动力学，并通过稳定瞬态 α 螺旋结构来扰乱 SP1 结构域两侧的自然螺旋平衡。EP39 通过阻止HIV-1的成熟而起作用，从而阻断其感染性。

EP300 CBP-IN-1 (compound 172) 作为一种EP300 CBP抑制剂显示出高效性，其对CBP BRD 和 EP300 BRD 的IC50值均在纳摩尔级别，分别是2.3 nM和2.1 nM。此外，该化合物还能抑制前列腺癌CWR22RV1细胞的增殖。

Ep300 CREBBP-IN-3 (Example 61) 是一种有效的Ep300和CREBBP 抑制剂，IC50分别为 0.056 μM 和 0.095 μM。Ep300 CREBBP-IN-3 可用于癌症研究。

Ep300 CREBBP-IN-2 (Example 73) 是一种有效的和具有口服活性的Ep300和CREBBP 抑制剂，IC50分别为 0.052 μM 和 0.148 μM。Ep300 CREBBP-IN-2 可用于癌症研究。

Ep300 CREBBP-IN-8 (Example 37) 是一种有效的和具有口服活性的 Ep300和CREBBP 抑制剂，IC50分别为 0.014 μM 和 0.018 μM。Ep300 CREBBP-IN-8 可用于癌症研究。

Ep300 CREBBP-IN-4 (Example 56) 是一种有效的Ep300和CREBBP 抑制剂，IC50分别为 0.024 μM 和 0.064 μM。Ep300 CREBBP-IN-4 可用于癌症研究。

ONO-AE-248 is a selective agonist of EP3 receptor.

Butaprost is a chemical compound that functions as a selective agonist for the prostaglandin E receptor (EP2). It exhibits an EC50 of 33 nM and a Ki of 2.4 μM when interacting with the murine EP2 receptor. However, Butaprost demonstrates lower activity against murine EP1, EP3, and EP4 receptors. Furthermore, it effectively attenuates fibrosis by inhibiting the TGF-β Smad2 signaling pathway [1] [2] [3].

KAG-308 is an effective selective and orally active agonist of the EP4 receptor (Ki: 2.57 nM and EC50: 17 nM for human EP4 receptor), more selective over EP1, EP2, EP3, and IP receptor. KAG-308 suppresses colitis and promotes histological mucosal healing,

The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 . Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis. KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other prostanoid receptors). In functional assays it has been shown to stimulate secreted alkaline phosphatase gene reporter activity in EP4-transfected HEK293 cells with an EC50 value of 0.19 nM, demonstrating >5,000 and 50,000-fold selectivity against EP2 and TP, respectively. KMN-80 can induce the differentiation of bone marrow stem cells from both young and aged rats into osteoblasts in vitro (EC50s = 20 and 153 nM, respectively) and exhibits favorable tolerability up to at least 10 μM, whereas the EP4 agonist L-902,688 is highly cytotoxic at similar concentrations in these cells. KMN-80 has been used to repair calvarial defects in an in vivo rat craniomaxillofacial reconstruction model (rate of reduction in defect size equivalent to BMP-2 treated rats) and to promote bone formation in a rat incisor tooth socket model.

11-Deoxy-16,16-dimethyl Prostaglandin E2 (11-deoxy-16,16-dimethyl PGE2) is a stable synthetic analog of Prostaglandin E2 (PGE2), acting as an agonist for both EP2 and EP3 receptors. It effectively inhibits gastric acid secretion and ulcer formation in rats, with ED50 values of 1 mg kg and 0.021 mg kg, respectively. This compound is also 900 times more potent than Prostaglandin F2α (PGF2α) in inducing contraction of human respiratory tract smooth muscle in vitro.

EP4 receptor agonist 2（compound 31）是一种有效的EP4 receptor激动剂，其EC50值为0.8 nM；而对EP2、EP3、EP4的Ki值分别为>100000、38000、3.1 nM。

CAY10580 is a potent and selective prostaglandin EP 4 receptor agonist ( K i =35 nM).

PF-06748962 is a potent and selective lactam-based prostaglandin EP3 receptor antagonist.

Tafluprost acid is a selective agonist at the prostaglandin F receptor.

SC 51089 是一种选择性的前列腺素受体 PGE2 拮抗剂，对前列腺素受体亚型具有选择性，具有抗伤害活性，可改善亨廷顿病 R6/1 小鼠模型中的运动缺陷并挽救记忆力下降。

Prostaglandin E2 activates four distinct G protein-coupled receptors, EP1-4. Rivenprost is a potent and selective agonist for the EP4 receptor (Ki = 0.7, 56, 620, and >10,000 nM for EP4, EP3, EP2, and EP1, respectively). It has been used to promote EP4-mediated bone formation, prevent bone loss related to osteoporosis, drive osteoblast differentiation, and stabilize bone implants.[1][2][3][4][5] Rivenprost has also been used to support wound healing.[6]

L-798106 (CM9) 是一种具有选择性和高效性的前列腺素类 EP3 受体拮抗剂 ，抑制 EP4，EP1 和 EP2 受体，抑制动脉粥样硬化中促炎细胞因子的水平，可减弱 PGE2 诱导的咳嗽。

ONO-AE3-208 is an EP4 receptor antagonist with a Ki of 1.3 nM, exhibiting less potent activity against EP3, FP, and TP receptors (Ki values of 30, 790, and 2,400 nM, respectively), while showing no effect on other prostanoid receptors. In wild type mice, treatment with ONO-AE3-208, in conjunction with 3% dextran sodium sulfate, results in severe colitis characterized by epithelial loss, crypt damage, and inflammation, thereby mimicking the effects of EP4 deletion. Further, this compound has been utilized to investigate the role of EP4 signaling in various biological contexts, including immune and autoimmune responses, inflammation, and cancer.

L 888607 is an effective and selective CRTH2 agonist (Ki: 0.8 nM).

SC 51089 free base 是一种选择性的前列腺素受体EP1拮抗剂，对EP1，TP，EP3和FP 受体的Ki 值分别为 1.3，11.2，17.5 和 61.1 μM。SC 51089 free base 具有神经保护活性。

Alprostadil sodium 是一种前列腺素受体配体，对小鼠 EP1、EP2、EP3、EP4和 IP 的 Ki 值分别为 36、10、1.1、2.1 和 33 nM。它诱导血管舒张并抑制血小板聚集，可作为血管扩张剂用于外周血管疾病的研究。

19(R)-hydroxy Prostaglandin E1 是 EP1 和 EP3 受体亚型的激动剂，并对平滑肌表现出收缩活性，也是灵长类动物精液中的主要前列腺素。

EP3 and EP1 receptor agonist

17-Phenyl trinor Prostaglandin E2 (17-phenyl trinor PGE2) is a synthetic analog of PGE2, functioning as an agonist at the EP1 and EP3 receptors. It induces contraction of the guinea pig ileum at a 11 µM concentration and displays slightly less potency than PGE2 in stimulating the gerbil colon and rat uterus. Notably, with an ED50 value of 350 µg kg, 17-phenyl trinor PGE2 exhibits 4.4 times greater antifertility efficacy in hamsters compared to PGE2.

17-phenyl trinor PGE2 ethyl amide is derived from 17-phenyl trinor PGE2, a synthetic analog of PGE2 that acts as an agonist of EP1 and EP3 receptors in mice (Ki = 14 and 3.7 nM, respectively) and EP1, EP3, and EP4 in rats (Ki = 25, 4.3, and 54 nM, respectively). 17-phenyl trinor PGE2 causes contraction of guinea pig ileum at a concentration of 11 μM and is 4.4 times more potent than PGE2 as an antifertility agent in hamsters. Modification of the C-1 carboxyl group to an ethyl amide serves to increase lipid solubility, thereby improving uptake into tissues and further lowering the effective concentration. Ethyl amide groups are then removed by amidases, regenerating the active free acid.

8-iso Prostaglandin E1 能引起犬肺静脉中的痉挛，还能够起到血管舒张作用。