Sorafenib (Bay 43-9006) is a multikinase inhibitor that inhibits Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. Sorafenib has antitumor activity and can induce autophagy and apoptosis as well as agonistic ferroptosis.

1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(7-(1-methyl-1H-pyrazol-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-3-yl)urea, a TNF-α agonistic compound, could induce cells to secrete TNF- α.

Viloxazine (Viloxazin) (Viloxazin) is a dual-action compound that functions as a norepinephrine reuptake inhibitor and exhibits potent agonistic activity towards 5-HT 2C receptors while acting as an antagonist for 5-HT 2B receptors, with respective potency values of EC 50 = 32 μM and IC 50 = 27 μM. Its primary mechanism of action involves the modulation of serotonergic and noradrenergic pathways. Viloxazine is commonly employed in depression research [1] [2].

BDC2.5 mimotope 1040-31 acetate is a effectively agonistic peptide (mimotope) for diabetogenic T cell clone BDC2.5. It can stimulate BDC2.5 cells with cells showing good response to this mimotope. 1040-31 peptide is specific for BDC2.5 TCR Tg+ (transgenic

BDC2.5 mimotope 1040-31 TFA, a specific agonistic peptide for the diabetogenic T cell clone BDC2.5, exhibits strong reactivity with BDC2.5 T-cell receptor (TCR) transgenic (Tg)+ T cells [1] [2].

This is a effectively agonistic peptide (mimotope) for diabetogenic T cell clone BDC2.5. It can stimulate BDC2.5 cells with cells showing good response to this mimotope. 1040-31 peptide is specific for BDC2.5 TCR Tg+ (transgenic) T cells. This peptide is

Fazpilodemab (BFKB8488A) is a humanized agonistic bispecific antibody that targets fibroblast growth factor receptor 1c (FGFR1c) and Klothoβ. It is utilized in research pertaining to Type 2 diabetes mellitus (T2DM) and nonalcoholic fatty liver disease (NAFLD) [1].

Vonlerolizumab(MOXR 0916) is a humanized IgG agonistic OX40-specific monoclonal antibody with potential antitumor activity for the study of tumors and immune diseases.

Tilogotamab (GEN-1029) is an enhanced hexameric mixture of two agonistic antibodies that bind to distinct epitopes on death receptor type 5 (DR5), specifically activating it. This compound is utilized in the research of multiple myeloma (MM) [1].

DPP-IV-IN-5, derived from Lycium barbarum fruits, demonstrates moderate agonistic activity towards peroxisome proliferator-activated receptor (PPARγ), showing EC50 values between 10.09 and 44.26 μM, and exhibits inhibitory activity against dipeptidyl peptidase-4 (DPPIV) with an IC50 of 47.13 μM [1].

Drozitumab (PRO 95780) is an agonistic human monoclonal antibody targeting the death receptor DR5. It demonstrates significant antitumor efficacy against rhabdomyosarcoma [1] [2] [3].

C5a Receptor Agonist (mouse, human) is a bioactive peptide derived from the C-terminus of the complement fragment 5 anaphylatoxin (C5a), functioning as an agonist for the C5a receptor. This peptide plays a role in mediating inflammatory responses by promoting chemotaxis, leukocyte degranulation, enhanced vascular permeability, and cytokine production. Its agonistic activity is critically dependent on the presence of cyclohexylalanine at position 5 and the d-isomer of Arg at the terminal position.

Giloralimab (ABBV-927), an agonistic monoclonal antibody targeting CD40, exhibits potent activity and is being investigated for potential application in cancer research [1] [2].

HBT1 is an AMPA receptor potentiator that induces production of brain-derived neurotrophic factor (BDNF) and exhibits little agonistic effect in primary neurons. HBT1 binds to ligand-binding domain of AMPA-R in glutamate dependent manner.

(+)-Cloprostenol is a analogue of prostaglandin F2α (PGF2α), and is selective prostaglandin receptor agonistic.

The substitution with Sar at position 1 of angiotensin II resulted in a partial agonistic activity.

FLTX1 is a fluorescent derivative of Tamoxifen, designed to efficiently target and label intracellular Tamoxifen-binding sites (estrogen receptors) both under permeabilized and non-permeabilized conditions. Additionally, FLTX1 demonstrates strong antiestrogenic activity in breast cancer cells, resembling the potent antiestrogenic properties of Tamoxifen. Notably, FLTX1 does not exhibit any estrogenic agonistic effect on the uterus.

NSC-5844 (RE-640) (RE640) is a bisquinoline compound with C-C chemokine receptor type 1 (CCR1)-agonistic activities.

Inactive analog of m-3M3FBS (PLC activator)

Barpisoflavone A possesses moderate estrogen partial agonistic activities and moderate antioxidant activities.

Naratriptan Hydrochloride is the hydrochloride salt form of naratriptan, a sulfonamide with selective serotonin (5-HT) 1 receptor agonistic activity and anti-migraine property. Naratriptan hydrochloride (GR-85548A hydrochloride) binds selectively and with high affinity to the 5-HT1D and 5-HT1B receptor subtypes. Activation of these 5-HT1D/B receptors located on intracranial blood vessels leads to vasoconstriction and provides relief of migraine headaches. Naratriptan hydrochloride may also exerts its effect by stimulation of 5-HT1D/1B receptors on sensory nerve endings in the trigeminal system thereby decreasing the release of pro-inflammatory neuropeptides.

TAK-653, a selective positive allosteric modulator (PAM) of AMPA receptors exhibiting minimal agonistic activity, elicits an antidepressant-like response while maintaining a favorable safety profile in rat models.

TAK-137 is a novel AMPA receptor potentiator with little agonistic effect, producing antidepressant-like effect without causing psychotomimetic effects.

TLR7/8 agonist 1 is a toll-like receptor ( TLR7 )/ TLR8 dual-agonistic imidazoquinoline.

ELA-11(human) TFA, a bioactive fragment of ELA-32, acts as a high-affinity apelin receptor agonist (K i =14 nM). It effectively inhibits forskolin-induced cAMP production and promotes β-arrestin recruitment in vitro, highlighting its significant agonistic activity.

ZK159222 is an effective 1α,25-(OH)2D3 receptor (VDR) agonist. ZK159222 has a partial agonistic character.

BDC2.5 mimotope 1040-51 is a mimotope peptide for diabetogenic T cell clone BDC2.5. isolated from non-obese diabetic mice.This is a effectively agonistic peptide (mimotope) for diabetogenic T cell clone BDC2.5. from non-obese diabetic (NOD) mice. T cells

Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).

Etofylline clofibrate has a hypolipidemic and antithrombotic effect and it also has an agonistic interaction with intimal PGI2.

TAK-683 is an effective full KISS1 receptor agonist (IC50=170 pM). TAK-683 is a nonapeptide metastin analog, shows agonistic activities to KISS1R (EC50: 0.96 nM and 1.6 nM for human and rat, respectively).

Domitroban, also known as S-145, is a thromboxane (Tx) A2-receptor antagonist with partial agonistic activity in vascular smooth muscle.

[MePhe7]-Neurokinin B is a neurokinin NK-3 receptor (NK3R) agonist, exhibiting a potent agonistic activity with an IC50 value of 3 nM. It acts as a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion through the activation of NK3R [1].

Neihulizumab (ALTB-168), an immune checkpoint agonistic antibody, targets and binds to human CD162 (PSGL-1), resulting in the downregulation of activated T-cells. It is utilized in research aimed at treating steroid-refractory acute graft-versus-host disease (SR-aGVHD), psoriasis, psoriatic arthritis, and ulcerative colitis [1].

CB1/2 agonist 3 (compound 52), a potent non-selective cannabinoid ligand, is a competitive agonist for the CB1/CB2 receptors. It exhibits CB1/CB2 agonistic activity by binding to the human CB1 and CB2 receptors, with Ki values of 5.9 nM and 3.5 nM, respectively [1].

SDP116, a synthetic peptide derivative of the GPR116 Stachel sequence, exhibits ADGRF5 agonistic activity [1].

This is a strongly agonistic peptide (mimotope) for diabetogenic T cell clone BDC2.5.

TAK-683 TFA, a potent full KISS1 receptor (KISS1R) agonist with a half-maximal inhibitory concentration (IC50) of 170 pM, exhibits enhanced metabolic stability. As a nonapeptide metastin analog, it demonstrates agonistic activities towards KISS1R, with effective concentration (EC50) values of 0.96 nM for humans and 1.6 nM for rats. In vivo, TAK-683 TFA reduces gonadotropin-releasing hormone (GnRH) levels in the hypothalamus and decreases plasma follicle-stimulating hormone (FSH), luteinizing hormone (LH), and testosterone levels. Given these effects, TAK-683 TFA holds promise for research into hormone-dependent prostate cancer.

Benufutamab (GEN1029), a death receptor 5 (DR5)-specific agonistic antibody, comprises a blend of two non-competing DR5-specific IgG1 antibodies with an E430G mutation in the Fc domain. This compound exhibits antitumor effects [1].

DSP-1053, a benzylpiperidine derivative, is a potent inhibitor of the serotonin transporter (SERT) with a dissociation constant (K i) of 1.02 nM and exhibits partial agonistic activity at the 5-HT 1A receptor with a K i of 5.05 nM, indicating its potential as an antidepressant.

Agroclavine is a clavine type of ergot alkaloid with D1 dopamine and a-adrenoceptor agonistic properties.

Gliquidone (AR-DF 26) is a potent, second-generation sulfonylurea with antihyperglycemic activity. Like other second-generation compounds, gliquidone exerts greater binding affinity to SUR1 and increased potency compared to first-generation compounds. In addition, this agent exerts peroxisome proliferator-activated receptor (PPAR) gamma agonistic activity.

TAK-683 TFA is a potent full agonist of the KISS1 receptor (KISS1R; IC50: 170 pM) with improved metabolic stability. It shows agonistic activities to KISS1R (EC50s: 0.96 nM and 1.6 nM for human and rat).

Axomadol (EN3324) is a centrally active analgesic compound. It has opioid agonistic properties and inhibitory effects on the reuptake of monoamines.

Cifurtilimab (SEA-CD40), a nonfucosylated humanized IgG1 monoclonal antibody with agonistic properties, targets the CD40 receptor and demonstrates antitumor activities [1] [2].

Sotigalimab, a CD40 agonistic monoclonal antibody, is utilized in research targeting metastatic pancreatic adenocarcinoma [1].

KISS1-305, the Metastin/Kisspeptin analog, is a prototype peptide and a chemical probe. KISS1-305 has suboptimal KISS1R agonistic activity, and resists plasma protease degradation.KISS1-305 is a proto- type peptide that resists plasma protease degradation

Onzigolide (BIM-23A760), a chimeric compound combining properties of both dopamine and somatostatin, exhibits strong agonistic activity towards the D2 subtype of dopamine receptors (D2R) as well as type 2 somatostatin receptors (SSTR2).

Gliquidone-d6 is a deuterated compound of Gliquidone. Gliquidone has a CAS number of 33342-05-1. Gliquidone is a potent, second-generation sulfonylurea with antihyperglycemic activity. Like other second-generation compounds, gliquidone exerts greater binding affinity to SUR1 and increased potency compared to first-generation compounds. In addition, this agent exerts peroxisome proliferator-activated receptor (PPAR) gamma agonistic activity.

TAK-683 acetate is a nonapeptide metastin analog and a potent full agonist of the KISS1 receptor (KISS1R), exhibiting IC 50 =170 pM and enhanced metabolic stability. This compound shows agonistic activities towards KISS1R, with EC 50 values of 0.96 nM and 1.6 nM for human and rat KISS1R, respectively. TAK-683 acetate effectively depletes GnRH in the hypothalamus and reduces plasma levels of FSH, LH, and testosterone in vivo, showcasing its potential for hormone-dependent prostate cancer research.

GR231118 TFA, a neuropeptide Y C-terminus analogue, acts as a potent, competitive, and relatively selective antagonist at the human neuropeptide YY receptor, exhibiting a pKi of 10.4. It serves as a strong agonist at the human neuropeptide YY4 receptor with a pEC50 of 8.6 and a pKi of 9.6, while demonstrating weak agonistic activity at both human and rat neuropeptide YY2 and YY5 receptors. Additionally, this compound shows high affinity for the mouse neuropeptide YY6 receptor, with a pKi value of 8.8 [1].

Gliquidone sodium is a hypoglycemic sulfonylurea which may protect the liver from injury from diabetes.