target/Trk_receptor/1

Y1 receptor antagonist 1 (H 409-22 isomer) is the active isomer of H-409/22, a neuropeptide Y (NPY) Y1 receptor antagonist that dose-dependently antagonizes the vascular response to exogenous and endogenous NPY in pigs. lagodeoxycholic acid (H 409-22 isomer) is the active isomer of H-409/22, an antagonist of neuropeptide Y (NPY) Y1 receptor.

Edg-2 receptor inhibitor 1 (SAR-100842) is an Edg-2 receptor inhibitor extracted (IC50: <0.1 μM).

DDR-TRK-1 is a selective discoid domain receptor 1 (DDR1) inhibitor with IC50 value of 9.4 nM. DDR-TRK-1 also inhibits the TRK family.

AMPA receptor modulator-1 can be activated by glutamate, thereby modulating ion channels.

LPA1 receptor antagonist 1(LPA1 R antagonist 1) is a selective and potent lysophosphatidic acid (LPA1) receptor antagonist (IC50 : 25 nM) for the study of idiopathic pulmonary fibrosis.

A2B receptor antagonist 1 (EXAMPLE 9B) is a potent A2B adenosine receptor antagonist.

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

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].

A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively.

Dopamine D2 Receptor Antagonist-1 functions as a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R), demonstrating sub-millimolar affinity.

Sigma-1 receptor antagonist 2 is a potent and selective antagonist of sigma 1 receptor (σ1 R) (σ1 and σ2 receptor with Kis of 3.88 and 1288 nM , respectively).

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

Androgen receptor antagonist 1 is an orally available full androgen receptor antagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.

Target 1 has a wide range of applications in life science related research.

(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM. GABAB receptor antagonist 1 is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.

H3 receptor antagonist 1 is used in the study of neurological diseases, histamine H3 receptor antagonist.

Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.

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

GABA receptor Antagonist 1 (compound 7w) effectively inhibits the Px RDL1 GABAR at an IC50 of 7.08 nmol/L and demonstrates insecticidal efficacy against P. xylostella, S. frugiperda, S. exigua, and S. litura with respective LC50 values of 0.09, 0.84, 0.87, and 0.68 mg/L. Moreover, this compound exhibits moderate toxicity to honeybees (48 h, ID50 = 2.22 μg/adult) and low toxicity to zebrafish (LC50: 42.4 mg/L) [1].

Interferon receptor inducer-1 Used in the treatment of a disorder in which the induction of interferon is involved. is an interferon (IFN) receptor inducer.

Histamine H4 receptor antagonist-1 is a potent antagonist of the histamine H4 receptor.

Androgen Receptor Degrader-1 (Compound 18) is a potent agent for androgen receptor degradation, applicable in cancer research [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].

Succinate/succinate receptor antagonist 1 is a potent succinate receptor antagonist. Succinate/succinate receptor antagonist 1 interrupts succinate signals in gingival tissue and inhibits the activation of SucnRl Antagonist 1. Its IC50 value is 20 μsouth of the coast. Succinate/succinate receptor antagonist 1 can be used to treat periodontal disease.

GLP-1 receptor agonist 4 is a glucagon-like peptide-1 receptor (GLP-1R) agonist , has an EC50 of 64.5 nM. GLP-1 receptor agonist 4 can be used in the research for treatment of diabetes.

Glucocorticoid Receptor Agonist-1 Phosphate Gly-Glu (TFA) serves as a cleavable linker for the synthesis of Antibody-Drug Conjugates (ADCs).

β2AR/M-receptor agonist-1 (example 131), a muscarinic antagonist and β2 adrenoceptor agonist (MABA), exhibits dual potency towards β2 adrenoceptor and muscarinic receptor. It demonstrates a significant affinity for the β2 adrenoceptor, indicated by an EC50 value of 9.2 nM, and for the muscarinic receptor with a Ki value of 30.2 nM. Furthermore, its MABA activity is highlighted by an EC50 value of 4.0 nM [1].

σ1 Receptor antagonist-1 is a selective sigma 1 receptor antagonist.

Vanilloid receptor antagonist 1 (4-(7-Hydroxy-2-isopropyl-4-oxoquinazolin-3(4H)-yl)benzonitrile) is a potent vanilloid receptor TRPV1 antagonist.

Type II TRK Inhibitor 1 is a potent inhibitor targeting multiple tropomyosin receptor kinase (TRK) fusion protein variants as well as the wild type. It demonstrates notable antiproliferative effects on Ba/F3 cells expressing CD74-TRKA G667C and ETV6-TRKC G696C, with half-maximal inhibitory concentrations (IC50s) of 6 nM and 1.7 nM, respectively [1].

Glucocorticoid receptor modulator 1 is a potent, orally active, non-steroidal selective glucocorticoid receptor modulator, exhibiting IC50 values of 9 nM and 130 nM against NF-κB and AP-1, respectively. It effectively reduces the expression of inflammatory factors such as IL-6, IL-1β, and TNF-α, and alleviates dermatitis in mice.

TRK II-IN-1 is a potent type II inhibitor of tropomyosin receptor kinases (TRK), demonstrating inhibitory half-maximal inhibitory concentrations (IC50s) of 3.3, 6.4, 4.3, and 9.4 nM against TRKA, TRKB, TRKC, and the mutant TRKA G667C, respectively. Additionally, this compound exhibits IC50 values of 1.3 nM against FLT3, 9.9 nM against RET, and 71.1 nM against VEGFR2. TRK II-IN-1 primarily serves as a research tool for studying TRK-driven cancers [1].

Protease-Activated Receptor-1 Antagonist 2 is an orally active antagonist of protease-activated receptor-1 (PAR-1), demonstrating significant potency with an IC 50 of 7 nM. It exhibits favorable pharmacokinetic characteristics, making it valuable in cardiovascular disease (CVD) research, including studies on atherosclerosis and restenosis [1].

Glucocorticoid receptor agonist-1 Ala-Ala-Mal (compound 88), a glucocorticosteroid and glucocorticoid receptor agonist, can be conjugated with Adalimumab to formulate an ADC [1].

Protease-Activated Receptor-1 (PAR-1) Agonist TFA is a selective peptide that acts as an agonist for the proteinase-activated receptor-1 (PAR-1). Corresponding to the tethered ligand of PAR-1, this compound mimics the actions of thrombin through the PAR-1 receptor[1][2].

mGlu4 receptor agonist 1 (compound 62) is a highly effective positive allosteric modulator of mGlu4 receptors, displaying an EC 50 of 308 nM. Additionally, it exhibits noteworthy anxiolytic and antipsychotic properties [1].

Glucocorticoid receptor-IN-1 is a selective regulator of the glucocorticoid receptor (GR) and exhibits anti-inflammatory activity. glucocorticoid receptor-IN-1 has good transcriptional repression, acting on hMMP1 ( IC50: 2.11 nM) and also has a transcriptional activating effect on MMTV (EC50: 5.59 nM).

5-HT6/5-HT2A receptor ligand-1 (compound 33) is a dual antagonist for the 5-HT6 and 5-HT2A receptors. It exhibits a K i value of 2 nM and 11 nM for the respective receptors. This compound holds promise for research in neurological and psychiatric disorders [1].

CCK-B Receptor Antagonist 1 is a cholecystokinin B (CCK-B) receptor agonist and has the potential of reducing the secretion of gastric acid.

Adenosine receptor inhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR). It exhibits exceptional affinity for A1 AR, A2A AR, A2B AR, and A3 AR, with respective Ki values of >1000, 68.5, >1000, >1000 nM. This compound demonstrates notable antinociceptive, anti-inflammatory, and peripheral analgesic properties. Therefore, Adenosine receptor inhibitor 1 holds great promise for investigating cancer and neurodegenerative diseases [1].

Substance P Receptor Antagonist 1 has the potential function in gastrointestinal disorders, inflammatory diseases, respiratory, and central nervous system disorders.

Glucagon receptor antagonist -1 is a highly effective glucagon receptor antagonist.

GLP-1 receptor agonist 3 is a GLP-1 receptor agonist,Example 4A-1, has EC50s of 1.1 nM and 13 nM in Clone H6 and Clone C6 cell lines assay, respectively.

NOT Receptor Modulator 1 (2-(3-(2-(4-chlorophenyl)imidazo[1,2-a]pyridin-6-yl)phenyl)propan-2-ol) is a modulator of nuclear receptor NOT.

Glucocorticoid Receptor Agonist-1 Phosphate (Gly-Glu-Br) is an antibody-drug conjugate (ADC) linker utilized in the synthesis of ABBV-154, ABBV-927, ABBV-368, and related analogs [1].

Compound (S)-9, a GLP-1 receptor agonist, exhibits an EC50 of 76 nM for the glucagon GLP-1 receptor [1].

CCK-A receptor inhibitor 1 is a potent inhibitor of the cholecystokinin A (CCK-A) receptor (IC50: 340 nM).CCK-A receptor inhibitor 1 can be used for the study of diseases related to the digestive system.

Dopamine D3 receptor antagonist-1 is a dopamine D3 receptor selective or multi-targeting ligand with a Ki value of 1.58 nM that has demonstrated therapeutic potential for central nervous system disorders.

Dopamine D4 receptor antagonist-1 can be used in schizophrenia study. Dopamine D4 receptor antagonist-1 is a selective antagonist of Dopamine D4 receptor (DRD4). The Ki value of Dopamine D4 receptor antagonist-1 for Hd4.2 is 9.0 nM [1].

GIP/GLP-1 dual receptor agonist-1 (compound 4), a receptor agonist for both GIP and GLP-1, shows potential for the research of metabolic disorders and fatty liver diseases, such as nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD) [1].