gpcrs

Takeda103A (CMPD103A) 是 GRK2抑制剂。G 蛋白偶联受体是许多生理过程的核心。Takeda103A 对研究心力衰竭具有潜在的研究价值。

4-CMTB 是选择性的游离脂肪酸受体 2(FFA2/GPR43)的激动剂以及正变构调节剂 (pEC50=6.38)。

Orphan GPCR SP9155 agonist P550 (mouse, rat) (26RFa (mouse, rat)) is an orphan GPCR with an orexigenic effect belonging to the RFamide peptide family. It acts as the cognate ligand for the mouse orphan receptor GPR103, which is also known as SP9155 or AQ27.

MS67 is a potent and selective degrader of the WD40 repeat domain protein 5 (WDR5) with a dissociation constant (Kd) of 63 nM. It exhibits no activity against protein methyltransferases, kinases, G-protein-coupled receptors (GPCRs), ion channels, and transporters. Notably, MS67 demonstrates significant anticancer properties.

N-phenylthiophene-2-carboximidamide 是一种噻吩衍生物，可以作为蛋白酪氨酸激酶（PTKs）的抑制剂和 G 蛋白偶联受体（GPCR）的配体发挥作用。

PRX-07034 hydrochloride 是一种有效的高度选择性5-HT6受体拮抗剂，Ki 为 4-8 nM，IC50为 19 nM，可用于增强工作记忆和认知灵活性的研究。

Alimemazine (Trimeprazine) is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist. Alimemazine also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs.

VU0463271 (N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide) 是一种有效的、特异性的 KCC2 拮抗剂，其 IC50 为 61 nM，特异性是密切相关的 Na-K-2Cl 协同转运蛋白 1 (NKCC1) 的 100 倍以上，在更大的 GPCR、离子通道和转运蛋白面板中没有活性。

VU0029767 is a selective positive allosteric modulator of M1, a member of the muscarinic acetylcholine family of GPCRs (mAChRs). VU0029767 increases potency and efficacy of acetylcholine (ACh) at M1.

GRC-17536 is an orally available, potent, and selective transient receptor potential anchor protein 1 (TRPA1) inhibitor that has been shown to be highly effective in the treatment of inflammation and neuropathic pain in animal models. The selectivity of G

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。

ZK 756326 是一种选择性的非肽 CCR8 趋化因子受体激动剂（IC50：1.8 μM，在人体内；2.6 μM，在小鼠体内）。对 CCR4/5 和 CXCR3/4 没有活性，比其他 26 种 GPCR 的选择性高 28 倍（对 α2A 和 5-HT 受体的选择性较低）。诱导趋化性并抑制 Env 介导的 (HIV) 细胞-细胞融合。

C16 Lactosylceramide is an endogenous bioactive sphingolipid. It forms membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs), suggesting a role in cell signaling. Plasma levels of C16 lactosylceramide are elevated in insulin-resistant cattle. C16 Lactosylceramide is also upregulated in a mouse model of Niemann-Pick type C1 disease, a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder.

1-Palmitoyl Lysophosphatidic Acid (sodium salt)是一种LPA衍生物和内源性代谢物，可用于生命科学领域的相关研究。

Potent and selective GPR84 biased agonist (EC50 = 33 nM). Exhibits no significant activity in a panel of 168 other GPCRs. Exhibits bias for G protein signaling pathways. Induces morphological changes in primary murine bone marrow-derived macrophages (BMDMs) in a cellular impedance assay, and promotes phagocytosis by M1 polarized U937 cells. Induces migration of primary human monocytes, but has no effect on macrophage chemotaxis.

NCT 501 hydrochloride is a potent and selective ALDH1A1 inhibitor (IC50 = 40 nM). Exhibits >1000-fold selectivity for ALDH1A1 over ALDH3A1, ALDH1B1, ALDH2, HPGD and HSD17β4. Also selective over a panel of 168 GPCRs. Blood-brain barrier permeable.

AM-3189 is a potent and selective GPR40 Agonist with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837. AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. Similar to AMG 837, while highly potent on GPR40, AM-3189 was highly selective over the closely related GPCRs, GPR41 and GPR43. 13kdemonstrated low clearance, moderate volume of distribution, and good oral bioavailability. AM-3189 does not penetrate the rat CNS as indicated by a rat brain to plasma ratio of 0.04 at 3 h after an oral dose of 5 mg kg.

Angiotensin II human TFA 是肾素-血管紧张素系统中的强效血管收缩剂，通过与 AT1R 和 AT2R 受体作用调节血压，可激活交感神经、促进醛固酮合成和肾功能，诱导血管平滑肌细胞增殖及成纤维细胞中 I 型和 III 型胶原合成，导致血管和心肌增厚、纤维化，并诱导凋亡及促进毛细血管生成，可用于构建心脏肥大、高血压和腹主动脉瘤模型。

Argipressin (diacetate) (AVP (diacetate)，又称antidiuretic hormone (ADH)) 是一种由垂体后叶分泌的含9个氨基酸的神经肽。通过作用于三种G蛋白偶联受体(GPCRs)，Avpr1a (V1a)、Avpr1b (V1b) 及Avpr2 (V2)，它调控体液平衡、渗透压及心血管系统的生理功能，并可能对中枢代谢过程产生重要影响。

Oleoyl-L-alpha-lysophosphatidic acid sodium salt为必需的细胞膜生物合成代谢物，可通过与G蛋白偶联受体（GPCR）（即LPA受体）相互作用来介导信号传导，是LPA1和LPA2受体的内源性激动剂。

MS48107 是 G 蛋白偶联受体 68 (GPR68) 的选择性正变构调节剂，对GPR68的选择性高于密切相关的神经递质转运蛋白，质子 GPCR 和 hERG 离子通道。它可以穿越过小鼠的血脑屏障。

Neurokinin B TFA, a member of the tachykinin family, binds to a series of GPCRs, including neurokinin receptors 1 (NK1R), NK2R, and NK3R, to modulate their biological effects.

Selective, high affinity, non-competitive α1A adrenoceptor antagonist (Ki = 0.35 nM). Exhibits no significant activity against a range of other GPCRs, including α2A, β1 and β2 adrenoceptors. Antagonizes effects of phenylephrine on isolated rabbit prostate

Neuropeptide W-30 (human) 作为中枢神经系统的一种关键应激介质，它参与调节下丘脑-垂体-肾上腺 (HPA) 轴和交感系统的输出。作为两种孤儿G蛋白偶联受体 (GPCRs) GPR7和GPR8的内源性配体，Neuropeptide W-30 (human) 可在类似的有效浓度下激活并与GPR7和GPR8结合。