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Cat. No.	Product Name	Target	Signaling Pathways
T9238	KI-7	Adenosine Receptor	GPCR/G Protein; Neuroscience
	KI-7 是一种A2B 腺苷受体阳性变构调节剂。它增强选择性 A2B 腺苷受体激动剂 BAY 60-6583 和腺苷诱导的 cAMP 积累，EC50分别为 2390 nM 和 2550 nM。它也增强非选择性 A2B 腺苷受体激动剂 NECA 诱导的 cAMP 积累，EC50为 445.8 nM。
T15812	LY2979165 mGlu2 agonist	GluR	Neuroscience
	LY2979165 (mGlu2 agonist) 是 mGluR2 的正构激动剂，可用于作为抗抑郁药的研究。
T16427	Padsevonil UCB-0942,UCB1415943-000	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Padsevonil (UCB-0942) 是一种潜在的 GABA A受体正变构调节剂，具有抗癫痫活性，可用于治疗癫痫。
T29135	VU0422288 VU-0422288,ML-396,ML396,VU 0422288,ML 396	GluR	Neuroscience
	VU0422288 (ML396) 是一种有效的 III 型 mGlu 受体 (mGlus) 正变构调节剂。VU0422288在钙动员试验中对 mGluR4、mGluR7 和 mGluR8 显示出抑制作用。VU0422288 可用于研究 Rett 综合症 (RTT)。
T29541	AC265347 AC-265347	CaSR	GPCR/G Protein
	AC265347 是一种有效的钙敏感受体 (CaSR) 激动剂和 ago-PAM 正变构调节剂，具有抗肿瘤活性，通过诱导分化抑制神经母细胞瘤肿瘤生长。AC265347 可用于研究神经母细胞瘤。
T20941	Cloransulam-methyl Cloransulam methyl	Others	Others
	Cloransulam-methyl 是一种有效的除草剂，常施用于大豆田来防治阔叶杂草。Cloransulam-methyl会在大豆植物中很快代谢掉，却会在土壤中存在。
T24827	SR 16832 SR-16832,SR16832	PPAR	DNA Damage/DNA Repair; Metabolism
	SR 16832 是一种化学合成中的砌块
T27405	GAT211 AZ4,GAT-211,AZ 4,GAT 211,AZ-4	cAMP; Cannabinoid Receptor; Arrestin	GPCR/G Protein
	GAT211 (AZ-4) 是一种具有选择性和高效性的大麻素 1 受体 (CB1R) 正变构调节剂 (PAM)，对 cAMP 和 β-arrestin2 具有较高的亲和力。GAT211 具有降眼压和抗精神病的作用，可用于研究癫痫。
T61483	GLP-1R modulator C5	Glucagon Receptor	GPCR/G Protein
	GLP-1R modulator C5 是一种小分子 GLP-1R 正变构调节剂，通过跨膜位点增强GLP-1与GLP-1R的结合，可用于研究 II 型糖尿病。。
T22638	CBiPES hydrochloride CBiPES HCl	GluR	Neuroscience
	CBiPES hydrochloride(CBiPES HCl) 是一种高效的 mGlu2 受体正变构调节剂，EC50值为 92.8 nM。CBiPES hydrochloride 可阻断 WT 和 mGlu（3）受体的作用。CBiPES hydrochloride 可用于研究像癫痫和帕金森综合征类的神经系统疾病。
T9180	LUF6096 CF-602	Adenosine Receptor	GPCR/G Protein; Neuroscience
	LUF6096 (CF-602) 是一种有效的腺苷 A3 受体 (adenosine A3 receptor) 变构增强剂。LUF6096 对任何腺苷受体显示出低正构亲和力。LUF6096 在心肌缺血/再灌注损伤中显示出保护作用。
T8963	CYM2503	Neuropeptide Y Receptor	GPCR/G Protein; Neuroscience
	CYM2503 是 GAL2 受体的正变构调节剂 (PAM)，可在体外增强甘丙肽诱导的 IP1 产生。它对受体的正构甘丙肽结合位点没有亲和力（通过其无法置换碘化甘丙肽或自行诱导 IP1 积累来衡量）。
T50048	4,4-dimethyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-2-one	Others	Others
	4,4-dimethyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-2-one 是一种苯二氮卓类衍生物，GABAA 受体的正变构调节剂，选择性地与 GABAA 受体的苯二氮卓类位点结合，具有抗焦虑、抗惊厥和镇静的活性。
T29067	Upacicalcet PLS-240,SK-1403,AJT-240	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Upacicalcet (AJT-240) 是一种静脉内拟钙剂，是一种可用于人血液透析的 SHPT，通过直接作用于甲状旁腺细胞膜钙敏感受体来抑制过量的甲状旁腺激素 (PTH) 分泌，从而降低血液中的 PTH 水平。 3 Upacicalcet 是钙敏感受体的正变构调节剂，可预防大鼠腺嘌呤诱导的继发性甲状旁腺功能亢进模型中的血管钙化和骨骼疾病。
T35841	5-Benzyloxygramine	Dopamine Receptor; 5-HT Receptor	GPCR/G Protein; Neuroscience
	5-Benzyloxygramine 是一种 N 蛋白、蛋白互作的原位稳定剂，具有抗病毒和稳定 N-NTD 蛋白的作用。它能够阻断多巴胺受体，可拮抗 5-HT 对大鼠子宫和兔耳的作用。
T12423	PF-06256142	Others	Others
	PF-06256142 is a potent and selective orthosteric D1 receptor agonist(D1 EC50=30 nM ).
T27961	LY593093 LY 593093,LY-593093
	LY593093 is a selective partial orthosteric agonist of M1 muscarinic acetylcholine receptor.
T28070	ML381 VU 0488130,ML-381,ML 381,VU-0488130,VU0488130
	ML381 is a M5-orthosteric antagonist with a high selectivity of muscarinic subtype.
T29206	ZCZ011 ZCZ 011,ZCZ-011
	ZCZ011 is a positive allosteric modulator of the cannabinoid CB1 receptor. ZCZ011 is brain penetrant, increased the potency of orthosteric agonists in mouse behavioral assays indicative of cannabimimetic activity, including antinociception, hypothermia, c
T61276	CB1R Allosteric modulator 2
	CB1R Allosteric modulator 2 (compound 18) is a potent allosteric modulator of the CB1R receptor. It exhibits negative modulation of the functional activity of orthosteric ligands (NAM) at CB1Rs, as demonstrated in previous studies [1].
T11906	LY 541850	GluR	Neuroscience
	LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC50 values of 0.161 μM and 0.038 μM, respectively.LY 541850 is claimed from human ionotropic and metabotropic glutamate (mGlu) receptors expressed in non-neuronal cells.
T70301	GAT100
	GAT100 is a potent and covalent negative allosteric modulator (NAM). GAT-100 behaved as a robust positive allosteric modulator of binding of orthosteric agonist CP55,940. This novel covalent probe can serve as a useful tool for characterizing CB1R allosteric ligand-binding motifs.
T74396	nAChR modulator-1
	nAChRmodulator-1 是一种杀虫剂，是一种昆虫 nAChR 正构调节剂。
T74397	nAChR modulator-2
	nAChRmodulator-2 是一种杀虫剂，是一种昆虫nAChR 正构调节剂。
T38111	Dimethyl-W84 (dibromide) Dimethyl-W84 (dibromide)
	Dimethyl-W84 is a selective allosteric modulator of the M2 muscarinic acetylcholine receptor. It hinders the dissociation of the orthosteric antagonist N-methylscopolamine from the M2 receptor with an EC50 value of 3 nM.
T28838	SPM-242 SPM 242
	SPM-242 is an orthosteric agonist of Sphingosine 1-phosphate (S1P) and a bitopic antagonist. S1P is a lysophospholipid signaling molecule that regulates important biological functions, including vascular development and lymphocyte trafficking, by activat
T69523	BMS-681
	BMS-681 is an orthosteric antagonist of chemokine receptor 2 (CCR2) that forms a ternary complex with CCR2 and its allosteric antagonist, CCR2-RA-[R]. Together, the complex inhibits chemokine binding with BVMS-681 in the orthosteric pocket and CCR2-RA-[R] in the intracellular allosteric G-protein binding site. When chemokine binding is inhibited, modulation responses implicated in several inflammatory and neurodegenerative diseases, including atherosclerosis, multiple sclerosis, asthma, neuropat...
T62376	GNE-9278
	GNE-9278 是一种高度选择性的 NMDAR 正变构调节剂，能够作用于 GluN1 跨膜结构域 (TMD)。GNE-9278 可以作用于活化的 NMDAR，能够提高峰值电流和激动剂亲和力。
T63717	CAM833
	CAM833 是有效的抑制 BRCA2 和 RAD51 之间相互作用的正位抑制剂，也能够抑制 RAD51 的寡聚，能够作用于 ChimRAD51 蛋白 (Kd: 366 nM)。
T62610	LY3154885
	LY3154885 是一种口服具有活力的多巴胺 D1 受体正变构调节剂 (PAM)。LY3154885 对药物-药物相互作用 (DDI) 的风险具有改善作用。
T62016	CB1R Allosteric modulator 1
	CB1R Allosteric modulator 1 (compound 11) 是有效的 CB1R 变构调节剂。CB1R Allosteric modulator 1 显示出对 CB1Rs 正构配体 (NAM) 功能活性的负面影响。
T61180	GAT564
	GAT564 (Compound 15d) is a highly effective allosteric modulator of cannabinoid 1 receptor (CB1R), having EC50 values of 87 nM and 320 nM for cAMP and β-arrestin2, respectively. It significantly enhances the binding of orthosteric ligands to hCB1R. Moreover, GAT564 exhibits remarkable efficacy as a topical agent, resulting in a significant reduction of intraocular pressure (IOP) in an ocular normotensive murine model of glaucoma [1].
T71179	LON63114
	LON63114, also known as FFA2-Agonist-1 is a selective orthosteric agonist of human FFA2. FFA2-Agonist-1 is potentially useful in the treatment of gastrointestinal disorders and inflammatory bowel diseases. LON63114 was reported in WO2011076732. This product has no formal name at the moment. For the convenience of communication, a temporal code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming).
T72744	(R)-PF-06256142
	(R)-PF-06256142 是 PF-06256142 的 R 型活性较差的对映异构体。PF-06256142 是一种有效的、选择性的正构D1 receptor 激动剂，可以减少相对于多巴胺和其他含儿茶酚激动剂的受体脱敏。
T37725	Tetrahydrodeoxycorticosterone 21-Hydroxypregnanolone,Tetrahydro-11-deoxycorticosterone	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Tetrahydrodeoxycorticosterone(Tetrahydro-11-deoxycorticosterone) 是一种有效的 GABAA 受体正变构调节剂 (PAM)，具有神经保护活性，选择性抑制神经类固醇介导的 GABA 诱发电流在 GABAA 受体上的增强，可用于研究神经疾病。
T70326	Mevidalen HBA
	Mevidalen, also known as LY3154207, is a novel, potent, and subtype selective human D1 positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50 = 3 nM). In contrast to orthosteric agonists, LY3154207 showed a distinct pharmacological profile without a bell-shaped dose-response relationship or tachyphylaxis in preclinical models. Identification of a crystalline form of free LY3154207 from the discovery lots was not successful. Instead, a novel cocrystal form with superi...
T82233	HCAR2 agonist 1
	HCAR2 agonist 1 (Compound 9n) 是一种偏向Gi蛋白的变构调节剂，能够激活Gi蛋白相关的信号传导通路。该化合物展现了明显的抗炎效果，能够显著降低促炎细胞因子（TNF-α、IL-1β、IL-6 和 MCP-1）的mRNA表达水平，并在结肠炎小鼠模型中增强正位激动剂的抗炎作用。
T73272	VU6019650
	VU6019650 是一种强效、选择性的M5mAChR 正向拮抗剂 (IC50=36 nM)，能够用于减轻阿片类药物使用障碍 (OUD) 的研究。VU6019650 具有血脑透过性，可能调节中边缘多巴胺能奖赏回路。VU6019650 能够阻断Oxotremorine M iodide 诱导引起的腹侧被盖区中脑 (VTA) 多巴胺神经元的放电速率的增加。
T83955	MOMBA
	MOMBA是一种针对人类自由脂肪酸2(hFFA2)工程化受体和设计药物激活的设计受体(DREADD)的选择性正交激动剂，对野生型hFFA2、hFFA3和小鼠FFA2无活性。MOMBA能够在表达hFFA2-DREADD受体的细胞中抑制forskolin刺激的cAMP水平，其功效改善且与山梨酸的效力相当。在hFFA2-DREADD转基因小鼠中，MOMBA治疗显著降低肠道传输速度，并促进依赖浓度的结肠隐窝GLP-1释放。该化合物具有口服生物利用度。

化合物

Cat.No: T9238

Target: Adenosine Receptor

Cat.No: T15812

Synonym: mGlu2 agonist

Target: GluR

Cat.No: T16427

Synonym: UCB-0942,UCB1415943-000

Target: GABA Receptor

Cat.No: T29135

Synonym: VU-0422288,ML-396,ML396,VU 0422288,ML 396

Target: GluR

Cat.No: T29541

Synonym: AC-265347

Target: CaSR

Cloransulam-methyl

Cat.No: T20941

Synonym: Cloransulam methyl

Target: Others

Cat.No: T24827

Synonym: SR-16832,SR16832

Target: PPAR

Cat.No: T27405

Synonym: AZ4,GAT-211,AZ 4,GAT 211,AZ-4

Target: cAMP, Cannabinoid Receptor, Arrestin

GLP-1R modulator C5

Cat.No: T61483

Target: Glucagon Receptor

CBiPES hydrochloride

Cat.No: T22638

Synonym: CBiPES HCl

Target: GluR

Cat.No: T9180

Synonym: CF-602

Target: Adenosine Receptor

Cat.No: T8963

Target: Neuropeptide Y Receptor

4,4-dimethyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-2-one

Cat.No: T50048

Target: Others

Cat.No: T29067

Synonym: PLS-240,SK-1403,AJT-240

Target: Calcium Channel

5-Benzyloxygramine

Cat.No: T35841

Target: Dopamine Receptor, 5-HT Receptor

Cat.No: T12423

Target: Others

Cat.No: T27961

Synonym: LY 593093,LY-593093

Cat.No: T28070

Synonym: VU 0488130,ML-381,ML 381,VU-0488130,VU0488130

Cat.No: T29206

Synonym: ZCZ 011,ZCZ-011

CB1R Allosteric modulator 2

Cat.No: T61276

Cat.No: T11906

Target: GluR

Cat.No: T70301

nAChR modulator-1

Cat.No: T74396

nAChR modulator-2

Cat.No: T74397

Dimethyl-W84 (dibromide)

Cat.No: T38111

Synonym: Dimethyl-W84 (dibromide)

Cat.No: T28838

Synonym: SPM 242

Cat.No: T69523

Cat.No: T62376

Cat.No: T63717

Cat.No: T62610

CB1R Allosteric modulator 1

Cat.No: T62016

Cat.No: T61180

Cat.No: T71179

(R)-PF-06256142

Cat.No: T72744

Tetrahydrodeoxycorticosterone

Cat.No: T37725

Synonym: 21-Hydroxypregnanolone,Tetrahydro-11-deoxycorticosterone

Target: GABA Receptor

Cat.No: T70326

HCAR2 agonist 1

Cat.No: T82233

Cat.No: T73272

Cat.No: T83955

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