autotaxin modulator 1

Autotaxin modulator 1 is a new modulator of Autotaxin.

Kv3 modulator 1 is a voltage-gated potassium channel Kv3 modulator that can be used to study neurologic-level diseases.

ALDH2 modulator 1 is a potent, orally active modulator of acetaldehyde dehydrogenase-2 (ALDH2), which reduces blood alcohol levels in mice.

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

Fluorogen binding modulator-1 (Fluorogen binding modulator-1) is a nonfluorescent inhibitors of Fluorogen–Fluorogen Activating Protein Binding Pairn.

CB2R FAAH modulator-1, a cannabinoid type 2 receptor (CB2R) agonist, is also a fatty acid amide hydrolase (FAAH) inhibitor (IC50=4 μM) that reduces the production of pro-inflammatory and anti-inflammatory cytokines and is commonly used in inflammation studies. The Kis for CB2R and CB1R are 14.8 nM and 241.3 nM, respectively.

Smurf-1 modulator CMP Example 20 (Smurf-1-IN-20) is a potent Smurf-1 modulator.

Calcium channel-modulator-1, a calcium channel-modulator (IC50: 0.8 μM), specializes in blocking aortic constriction.

CB2 modulator 1 is a potent CB2 modulator. It can be used for the research for immune disorders, osteoporosis, inflammation, renal ischemia.

S1PR1 modulator 1 is a selective inhibitor of S1PR1, with a pIC50 of 7.6.

gamma-secretase modulator 1 is a modulator of γ secretase and can be used in studies about the treatment of Alzheimer's disease.

5-HT1A modulator 1 exhibits high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM).

CRBN modulator-1 (WUN29654) is a Thalidomide analog and CRBN modulator,has an IC50 of 3.5 μM and a Ki of 0.98 μM.

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.

Estrogen receptor modulator 1 causes regression of Tamoxifen-resistant, hormone-independent xenograft tumors. Estrogen receptor modulator 1 is an orally active and selective estrogen receptor modulator (SERM) (pIC50: 0.46).

GPR40/FFAR1 modulator 1 is a Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1) agonist and allosteric modulator.

NR2F6 modulator-1 is a potent modulator of nuclear receptor subfamily 2, group F, member 6 (NR2F6), used to study immune regulation and modulation of tumour stem cell activity.

Nur77 modulator 1 is an effective Nur77 binder (KD = 3.58 μM) that up-regulates Nur77 expression, mediates its sub-cellular localization, induces Nur77-dependent ER stress and autophagy, and leads to cell apoptosis, demonstrating anti-hepatoma activity.

mGluR3 modulator-1 (1-ethyl-3-(morpholin-4-yl)-5,6,7,8-tetrahydroisoquinoline-4-carbonitrile) is a positive allosteric modulator of mGluR3 and can be used in studies about the treatment of Parkinson's disease.

Sirtuin modulator 1 (SRT3025 Hydrochloride) is a modulator of SIRT1 with EC1.5 of < 1 μM.

Nrf2-ARE hMAO-B QR2 modulator 1, a new resveratrol-based multitarget-directed ligand (MTDL), exhibits a well-balanced MTDL profile: it activates the NRF2-ARE pathway (CD = 9.83 μM), selectively inhibits both hMAO-B and QR2 (IC50s = 8.05 and 0.57 μM), and effectively promotes hippocampal neurogenesis. It exerts neuroprotective and antioxidant actions in both acute and chronic Alzheimer models using hippocampal tissues.

RNA Splicing Modulator 1 (Compound 233) is a modulator of RNA splicing, exhibiting an AC50 value of less than 100 nM [1].

CD33 splicing modulator 1 (Compound 1) is a CD33 splicing modulator that targets the CD33 Siglec 3 myeloid cell surface receptor, known for regulating microglial cell activity, and holds potential for studying neurodegenerative diseases such as Alzheimer's disease.

β-Catenin modulator-1 (IIa-650) is a valuable agent in cancer research for modulating β-Catenin [1].

KRAS G12D modulator-1 (compound 6), a potent modulator of KRAS G12D, exhibits IC50 values of 1-10 μM against NEA-G12D, PPI-G12D, and p ERK-AGS, and is utilized in cancer research [1].

Immuno modulator-1 (compound 22) effectively suppresses the secretion of TNFα and IL-2 in human peripheral blood mononuclear cells (hPBMC), with IC50 values of 4.7 nM and 26 nM, respectively, and exhibits a 20% inhibitory effect on the hERG potassium channel at a concentration of 3 μM [1].

RIG-1 modulator 1 is useful for the treatment of viral infections including influenza virus, HBV, HCV and HIV.

Mutant p53 modulator-1 is a mutant p53 modulator that hinders the progression of cancers containing p53 mutations.

MRGPRX4 modulator-1 (compound 31-2) is a potent antagonist of the mas-related G-protein receptor X4 (MRGPR X4) with an IC50 < 100 nM against MRGPR4, utilized for investigating MRGPR X4-dependent diseases including itch, pain, and autoimmune disorders [1].

GPR120 modulator 1 is useful for modulating GPR120.

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.

Ras modulator-1 is a chemical compound that modulates the activity of Ras.

KCC2 Modulator-1 (Example 52), possessing an EC50 value of 0.146 μM, acts as a modulator of KCC2 and is utilized in the study of diseases mediated by KCC2 [1].

MRGPRX2 modulator-1 (example 17), a modulator of the mas-related G-protein receptor X2 (MRGPRX2), is employed in studies focused on inflammation, pain, and autoimmune disorders [1].

IRAK4 Modulator-1 (example 161), an IRAK4 modulator with an IC50 of 4.647 μM, is employed in the investigation of IRAK-mediated disorders [1].

ISR Modulator-1 (Compound 212) acts as a regulator for the integrated stress response pathway (ISR).

IGF-1Rmodulator 1 (Example 5) is an IGF-1R modulator featuring an EC50 of 0.29 μM (FGFR1), 0.25 μM (IGF1R), 0.34 μM (TrkA), and 0.39 μM (TrkB). This compound is useful in research on diseases characterized by impaired signaling of neurotrophic and or other trophic factors, such as Alzheimer’s disease.

CXCR7 modulator 1 is an effective and orally bioavailable peptoid hybrid CXCR7 modulator with Ki of 9 nM.

TRPC5 modulator-1 (Compound 9) is a TRPC5 modulator with an IC50 of less than 1 nM, suitable for studying neuropsychiatric disorders.

Utrophin Modulator 1 (UM1) is a highly effective agent that upregulates utrophin protein levels, displaying an EC 50 of 0.11 μM. Its application in the investigation of Duchenne Muscular Dystrophy (DMD) has been well-established [1].

DPP-4 GPR119 modulator 1 (Compound 22) is an orally active compound that acts as both a dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist, demonstrating a glucose-lowering effect in blood and moderate inhibition of the hERG channel with an IC50 value of 4.9 µM. This compound is applicable in diabetes research [1].

Opioid receptor modulator 1 is a modulator of the opioid receptor.

IL-17 Modulator 1 (disodium) is a potent, orally active compound, known for its high efficacy in modulating IL-17. This compound is extensively utilized for researching various diseases such as psoriasis, ankylosing spondylitis, and psoriatic arthritis[1].

GPR17 Modulator-1 (Compound 2-046) is a regulator of the G protein-coupled receptor 17 (GPR17), displaying an IC50 of less than 10 nM against hGPR17 in CHO cells. This compound exhibits moderate pharmacokinetic properties in mice and possesses the ability to permeate the blood-brain barrier (BBB).

Compound 38-S is an orally active CB1R/AMPK modulator with a K i of 0.81 nM and an IC50 of 3.9 nM for CB1R. This compound activates AMPK and has been shown to decrease food intake and body weight, in addition to enhancing glucose tolerance and insulin sensitivity [1].

GluN2B receptor modulator-1 is a potent and selective allosteric modulator of the GluN2B receptor, demonstrating negative modulation by inhibiting receptor activity and exhibiting high selectivity towards the GluN2B subunit, with an IC50 value of 31 nM.

A3AR modulator 1 (MRS8054), an orally active positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR) (Adenosine Receptor), significantly enhances the efficacy (E max) of Cl-IB-MECA-stimulated [35 S]GTPγS binding [1].