modulator

IL-17 modulator 4 is a prodrug of IL-17 modulator 1 which is an efficacious modulator of IL-17.

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

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

CB2R/FAAH modulator-2 (compound 26) is a dual modulator targeting at CB2R and FAAH. CB2R/FAAH modulator-2 acts as a CB2R agonist and FAAH inhibitor, the Ki values are 10.8 and 152.9 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 6.2 μM. CB2R/FAAH modulator-2 has studies research value related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection.

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

β-catenin modulator IIa-661 is a small molecule inhibitor of the Wnt pathway with antitumour activity.

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

γ-Secretase modulator 13 is a γ-secretase modulator (GSMs) that inhibits the production of amyloid β-peptide Aβ42 and can be used to study Alzheimer's disease and tumors.

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

Calcium channel-modulator-1 is a calcium channel-modulator (IC50:0.8 μM) with specialisation to block aortic constriction.

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.

AMPA receptor modulator-2 (Example 134) is a AMPA receptor modulator, with a pIC50 of 10.1 for TARPγ2 dependent AMPA receptor[1]. pIC50 = -lgIC50. [1]. BERRY CYNTHIA G B (US), et al. AZABENZIMIDAZOLES AND THEIR USE AS AMPA RECEPTOR MODULATORS. Patent. WO2016176460.

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

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

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

Compound G-5b, an estrogen receptor modulator 10, functions as an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). It has the capability to induce apoptosis and block cells at the G1/G0 phase, making it applicable in cancer research [1].

IL-17 modulator 3 (US20200247785A1) is a chemical compound that acts as an IL-17 modulator. It has potential applications in researching inflammation, cancer, and autoimmune diseases.

5-HT1A modulator 2 hydrochloride, a derivative of 8-OH-DPAT , is a modulator of 5-HT1A with a Ki of 53 nM for 5-HT1A binding[1]. [1]. Naiman, N.,et al. 2-(Alkylamino)tetralin derivatives: interaction with 5-HT1A serotonin binding sites. Journal of Medicinal Chemistry, 1989;32(1), 253-256.

Estrogen receptor modulator 6 (compound 3a) is a highly specific and potent agonist of the estrogen receptor (ER) β with a remarkable affinity (K i = 0.44 nM). This compound exhibits an impressive 19-fold selectivity for ERβ over ERα, as evidenced by its affinity (K i = 8.4 nM).

Sirtuin modulator 2 (N-(3-(imidazo[2,1-b]thiazol-6-yl)phenyl)-2-methoxybenzamide) exhibits antidiabetic, anti-inflammatory and antitumor activities.

Compound 5TJX (ASGPR modulator-1) is a macrocyclic compound utilized in the study of protein-protein interactions [1].

CB2R/FAAH modulator-3 (compound 27) is a modulator targeting at CB2R and FAAH. CB2R/FAAH modulator-3 acts as a CB2R agonist and FAAH inhibitor, the Ki values are 20.1 and 67.6 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 3.4 μM. CB2R/FAAH modulator-3 has research value related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection.

Sirtuin Modulator 5, a sirtuin modulating agent, activates SIRT1 with an efficacy marked by a DC50 value of less than 50 μM. It is applicable in enhancing cell longevity and is researched for its therapeutic potential in a wide range of diseases such as those associated with aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular diseases, blood clotting disorders, inflammation, cancer, and flushing. Furthermore, it holds promise for conditions that could benefit from boosted mitochondrial activity [1].

GCase Modulator-1 (Compound 9g), a quinazoline derivative, functions as a glucosidase modulator with an AC50 value of 2.23 µM [1].

CD33 Splicing Modulator 1 Hydrochloride (Compound 1) is a myeloid lineage cell surface receptor CD33/Siglec 3 modulator involved in regulating microglia activity. This compound promotes exon 2 skipping in cellular mRNA pools and has research potential in addressing neurodegenerative diseases, including Alzheimer's disease [1].

A1AT Modulator 1 potently inhibits Z α1-antitrypsin (A1AT) polymerization, exhibiting a pIC50 of 8.3 [1].

mGluR5 modulator 1 is a compound that acts as a positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5). Its primary application lies in the field of schizophrenia and cognitive impairment research.

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.

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

β-Catenin modulator-1 (IIa-650) is a useful agent in cancer research for modulating β-Catenin [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. Additionally, this compound exhibits a 20% inhibitory effect on the hERG potassium channel at a concentration of 3 μM [1].

Estrogen Receptor Modulator 8 (compound 4) is an orally active inhibitor targeting Estrogen Receptor/ERR α with potent efficacy (IC50 = 0.437 nM in MCF-7 cells) and effectively hampers MCF-7 cell proliferation (IC50 = 0.1 nM) [1].

β-Catenin Modulator-5 (Compound IIa-84), an oxazole and thiazole-based compound, serves as a potent and selective modulator of β-Catenin [1].

DPP-4/GPR119 modulator 2 is an inhibitor of dipeptidyl peptidase IV (DPP-IV) (IC50: 0.22 μM) and an agonist of GPR119 (EC50: 0.95 μM).

ROR Modulator I is the first potent inverse agonist of the retinoid-related orphan receptor. It also has dual selectivity for RORβ and RORγt.

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.

IL-17A Modulator-3, an inhibitor of IL-17A/A, exhibits an IC 50 value of less than 10 μM. It is utilized in research related to inflammation, cancer, and autoimmune diseases.

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.

PCSK9 modulator-3 (Compound 13) is a potent PCSK9 modulator with an EC 50 value of 2.46 nM that has the potential in the hyperlipidemia research. PCSK9 is a recently proved target for lowering low-density lipoprotein cholesterol (LDL-C) [1].

Ras modulator-1 is a modulator of Ras.

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

NMDA receptor regulator 6 (Compound 183) is an effective NMDA receptor regulator and has research value in neurological disorders.

Nrf2-ARE/hMAO-B/QR2 modulator 1 is a new resveratrol-based multitarget-directed ligands (MTDLs) that showed a well-balanced MTDL profile: cellular activation of the NRF2-ARE pathway (CD = 9.83 μM), selective inhibition of both hMAO-B and QR2 (IC50s = 8.05 and 0.57 μM), and the best ability to promote hippocampal neurogenesis. Nrf2-ARE/hMAO-B/QR2 modulator 1 exerts neuroprotective and antioxidant actions in both acute and chronic Alzheimer models using hippocampal tissues.

Insulin level regulators can be used to treat diabetes.

TFIIH Modulator-19 induces the dimerization of trichothiodystrophy group A protein to modulate TFIIH transcriptional activity.

γ-Secretase modulator 4 is a potent γ-secretase modulator, reduces the Aβ42 level with IC50s of 0.017 μM and 0.014 μM in mouse and human, respectively.

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. It is utilized for the investigation of MRGPR X4 dependent diseases including itch, pain, and autoimmune disorders [1].

CD33 splicing modulator 1 (Compound 1) is a CD33 splicing modulator. CD33/Siglec 3 is a myeloid cell surface receptor known to regulate microglial cell activity. CD33 splicing modulator 1 has potential for the study of neurodegenerative diseases, including Alzheimer's disease.

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.

CXCR7 modulator 2 is a 7-type C-X-C chemokine receptor (CXCR7) modulator with a Ki of 13 nM.