agonist

diABZI STING agonist-1 (Tautomerism) (diABZI STING agonist (Compound 3)) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.

Dopamine D2 receptor agonist-2 (Dopamine D2 Receptor) is a ligand targeting the dopamine D2 receptor.

5-HT7 agonist 1 (4-[4-[(2-chlorophenyl)methyl]piperazin-1-yl]-1H-indole) is a selective agonist of 5-HT7 (IC50 = 222.93 nM). 5-HT7 agonist 1 can be used in studies about CNS disorders.

CB1 inverse agonist 1 (MRL-650) is an orally active and selective CB1 agonist. The IC50s for CB1 and CB2 are 7.5 nM and 4100 nM, respectively. CB1 inverse agonist 1 shows anorexigenic effects.

D4R agonist-1 is a selective and potent D4R partial agonist (Ki:2.2 nM).D4R agonist-1 can be used to study neurological diseases.

Protease-Activated Receptor-1, PAR-1 Agonist acetate is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist acetate corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor[1][2].

GLP-1 receptor agonist 9 citrate is an agonist of GLP-1.

STING agonist-30 is a potent STING agonist that triggers STING-dependent immune activation.STING agonist-30 shows broad-spectrum inhibitory effects against a variety of viruses including HSV (Herpes Simplex Virus), rotavirus, and SARS-CoV-2 (Severe Acute Respiratory Syndrome Coronavirus 2).

TREM2 agonist-2 (I-192) is an orally active and potent myeloid triggered receptor 2 (TREM2) agonist for the study of neurodegenerative diseases.

S1R agonist 2 is a selective S1R agonist with a Ki of 88 nM for S2R and 1.1 nM for S1R and is protective against ROS and NMDA-induced neurotoxicity.

β2AR/M-receptor agonist-2 is a dual-function compound acting as a muscarinic antagonist and β2 adrenoceptor agonist (MABA). It demonstrates significant activity towards the β2 adrenoceptor with an EC50 of 3.7 nM and exhibits affinity for the human cloned M3 receptor with a Ki of 0.73 nM. This potent bronchodilator holds potential for research in chronic obstructive pulmonary disease (COPD) treatment.

HIF-2α agonist 2 is an HIF-2α agonist with an EC50 value of 1.68 μM for HIF-2α. HIF-2α agonist 2 can promote the stability of the ARNT A/B ring in the 3z structure of HIF-2a-ARNT complex without cytotoxicity to 786-o-Reha-Luc cells. HIF-2α agonist 2 can be used in the study of oxygen metabolism and is closely related to the occurrence of cancer.

GPR35 agonist 2 (TC-G 1001) is a potent GPR35 agonist.The EC50 values of GPR35 agonist 2 in the β-arrestin and Ca2+ release assays were 26 and 3.2 nM, respectively.

Glucocorticoid receptor agonist-1 is a potent glucocorticoid receptor agonist with an IC50 of 2.8 nM[1].

TREM2 agonist-1 (I-246) is a triggering receptor expressed on myeloid cells-2 (TREM2) agonist (EC50: 3.0 μM-100 μM).This compound is unstable in powder form and other related salt forms are recommended.

CB2 receptor agonist 2 (ZINC72105556) is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor, Ki = 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2.

A2AR-agonist-1 (N-(2-(1H-Indol-3-yl)ethyl)adenosine) is a potent A2AR and ENT1 agonist (Ki: 4.39 and 3.47 for A2AR and ENT1. It targets the Adenosine A2A Receptor and Adenosine Transporter for Neuroprotection.

Nurr1 agonist 8 is a low-affinity Nurr1 agonist that can be used to study neurological diseases such as Parkinson's.

GPR35 agonist 3 is a synthetic GPR35 agonist with an EC50 value of 1.4 μg in the β-arrestin recruitment assay.GPR35 agonist 3 is used in the study of cancer, type 2 diabetes, and cardiovascular disease.

TLR7 agonist 2 (TLR7-IN-1) is a specific and effective Toll-like Receptor 7 (TLR7) agonist (LEC=0.4 μM).

diABZI STING agonist-1 (trihydrochloride) is stimulator of interferon genes (STING) receptor agonist.

STING agonist-1 (G10) is a human-specific STING agonist,elicits antiviral activity against emerging Alphaviruses.

BMP signaling agonist sb4 (SB 4) is an agonist of benzoxazole bone morphogenetic protein (BMP) signaling (EC50 :74 nM)

GP130 receptor agonist-1 (N-(4-Fluorophenyl)-4-phenyl-2-thiazolami) is a potent, brain-penetrant and orally active GP130 receptor agonist.

Y4R Agonist-1 is a potent agonist of the Y4 receptor, exhibiting a K_i (inhibition constant) value of 0.048 nM.

TLR4 agonist-1 (TEA, compound 17a) is a potent activator of Toll-like Receptor 4 (TLR4) and prompts the production of MIP-1β in RAW 264.7 and MM6 cells [1].

TLR4 agonist-1 (compound 17a) serves as a potent activator of Toll-like Receptor 4 (TLR4) and stimulates the production of MIP-1β in RAW 264.7 and MM6 cells [1].

Compound 28.1, also known as TAS2R14 agonist-2, is a potent and selective inhibitor of TAS2R14, exhibiting an EC50 of 72 nM [1].

RXFP1 receptor agonist-5 (Example 98) is an agonist that targets the RXFP1 receptor and demonstrates its bioactivity by inhibiting cAMP production in HEK293 cells with stable human RXFP1 expression, exhibiting an EC50 of 1.3 nM [1].

RXFP1 receptor agonist-4 (Example 268) is an agonist for the RXFP1 receptor, demonstrated to suppress cAMP production in HEK293 cells that stably express the human RXFP1 receptor, exhibiting an effective concentration (EC50) of 4.9 nM [1].

Compound 1, identified as a GPR61 inverse agonist, exhibits an IC50 of 11 nM, rendering it suitable for metabolism and body weight disorder research, including obesity and cachexia [1].

Cisd2 agonist 2 (compound 6), with an EC50 of 191 nM, is an orally active activator of Cisd2, a protein whose levels are associated with nonalcoholic fatty liver disease (NAFLD). In vivo studies have demonstrated that Cisd2 agonist 2 exhibits no significant toxicity in heterozygous hepatocyte-specific Cisd2 knockout (Cisd2hKO-het) mice [1].

GPR139 agonist-2 (compound 20a), a potent GPR139 agonist with an EC50 of 24.7 nM, has demonstrated efficacy in rescuing social interaction deficits and alleviating cognitive deficits in murine schizophrenia models, indicating its potential in antischizophrenia drug research [1].

GPR120 Agonist 2 is a potent and selective GPR120 receptor agonist.

RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist (IC50=63.8 nM), with improved drug-like properties[1].

STING agonist-23 (CF505) is a non-nucleotide, small-molecule compound that stimulates STING, enhancing the phosphorylation of STING, TBK1, and IRF3. It elevates the production of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells and demonstrates efficacy against SARS-CoV strains [1].

STING agonist-23 (CF502) is a non-nucleotide, small-molecule stimulator of the STING pathway. Upon activation, it enhances the phosphorylation of STING, TBK1, and IRF3, leading to elevated levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. Moreover, STING agonist-23 demonstrates efficacy against SARS-CoV series strains [1].

Compound 24, a 5-HT2 agonist-1, selectively activates 5-HT2A, 5-HT2B, and 5-HT2C receptors with IC50 values of 10 nM, 8.3 nM, and 1.6 nM, respectively. The free base form of this compound is utilized in research pertaining to depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headaches, PTSD, seizure disorders, and additional CNS disorders [1].

TAS2R14 agonist is a potent partial agonist of TAS2R14, displaying an EC50 value of 116.6 ± 23.6 nM [1].

TLR7/8 agonist 4 hydroxy-PEG6-acid, a Drug-Linker Conjugate for ADCs, comprises the TLR7/8 agonist 4 and a hydroxy-PEG6-acid linker, suitable for the synthesis of antibody-drug conjugates (ADCs) [1].

RXFP1 receptor agonist-1 (Example 2), an agonist of the RXFP1 receptor, suppresses cAMP production in HEK293 cells that constitutively express the human RXFP1, exhibiting an EC50 of 300 nM [1].

NLRP3 agonist 1 (compound 23) serves as a potent, orally active agent that activates Caspase-1 enzyme, leading to the cleavage of proinflammatory cytokines pro-IL-1β and pro-IL-18 into their active forms [1].

Nurr1 agonist 7 is an agonist of Nurr1 (EC50: 0.12 μM), which can be used to study neurological disorders such as Parkinson's disease.

Compound CMC23, an FPR2 agonist, mitigates lactate dehydrogenase release in LPS-stimulated cultures and reduces pro-inflammatory IL-1β and IL-6 levels. It also attenuates phosphor-STAT3 levels through the STAT3/SOCS3 signaling pathway [1].

AHR agonist 3 is an agent with therapeutic activity.

RORγ inverse agonist 1 has anti-inflammatory activity and can be used to treat rheumatism and psoriasis.

BMP Agonist 1 (compound 2 b) is a small-molecule stimulator of bone morphogenic protein (BMP) signaling, crucial for the differentiation of C2C12 cells. It acts by inhibiting GSK3β and enhancing β-catenin signaling, thereby synergistically modulating Id2 and Id3 expression. This compound is employed in skeletal disease and defect research [1].

Orexin 2 Receptor Agonist (OX2R) is an effective (EC50: 23 nM) and OX2R-selective (OX1R/OX2R EC50 ratio: 70) agonist.

Glucocorticoid receptor agonist-2 Ala-Ala-Mal (compound 79) serves as a precursor for synthesizing anti-inflammatory antibody-drug conjugate (ADC) molecules and acts as an active reference for ABBV-3373 [1].

RXFP1 receptor agonist-6 (Example 7) serves as an agonist for the RXFP1 receptor and effectively suppresses cAMP production in HEK293 cells that stably express the human RXFP1, exhibiting an EC50 of 12 nM [1].