Maraviroc is a selective CCR5 antagonist with activity against human HIV.
JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist, with pKis of 8.19, 8.20 for rat and human 5-HT7 in HEK293 cells, respectively.
MCH (human, mouse, rat) is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively. MCH (human, mouse, rat) is a highly sensitive to MCH-2R in a CHO cell line and monitoring mobilization of intracellular calcium with FLIPR, exhibits functional activation EC50 values of 3.9 nM and 0.1nM for human MCH-1R and MCH-2R, respectively[1].
Atrial Natriuretic Peptide (ANP) (1-28), human, porcine is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. ANP (1-28) inhibits endothelin-1 secretion in a dose-dependent way.
S1P5 receptor agonist-1 (example 6) is a potent and selective agonist of S1P5 receptor with an EC50 value of 20 nM[1].
RU 24969 is a selective agonist at the 5-HT1A and 5-HT1B receptors; IC50 value:Target: 5-HT1A/1B agonistRU 24969 possesses preference for the purported 5-HT1B subtype of central 5-HT1 recognition site. The reported significant linear correlation between hypotensive activity following intravenous (i.v.) administration to anesthetized rats and affinity for the central 5-HT1 binding site could only be maintained by incorporation of the affinity of RU 24969 for its low and 8-OH-DPAT for its high affinity binding site [1]. The drug RU 24969 (10 mg/kg) inhibited the rate of synthesis of 5-HT in rat brain by about 50%. Pretreatment of rats with desmethylimipramine over a longer term or clenbuterol given acutely, treatments known to enhance the behavioural responses of rats to various other 5-HT agonists, did not alter the RU 24969-induced response [2]. RU 24969 (0.03-3.0mg/kg, s.c.) dose-dependently decreased water consumption in water deprived rats [3].
Methapyrilene (Thenylpyramine) hydrochloride is an orally active H1-receptor antihistamine and an anticholinergic agent of the pyridine chemical class. Methapyrilene hydrochloride has hepatotoxicity and can be used as a hepatotoxin that cause periportal hepatic necrosis in vivo[2]
BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects[1][2][3].
TUG-424 is a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 of 32 nM. TUG-424 significantly increases glucose-stimulated insulin secretion at 100 nM. TUG-424 may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity[1].
ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM.
Alaproclate (GEA 654) hydrochloride is a selective and orally active serotonin re-uptake inhibitor (SSRI). Alaproclate hydrochloride also acts as a potent, reversible and noncompetitive antagonist of the NMDA receptor coupled ion flow[1][2].
Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.
ZD-1611 is a potent, orally active, selective ETA receptor antagonist, used for the research of ischemic stroke.
Nifeviroc is an orally active CCR5 antagonist. Nifeviroc is used for the study of HIV type-1 infection[1].
Thonzylamine is an orally active H1 histamine receptor antagonist, exhibits good antihistaminic and antianaphylactic properties. Thonzylamine can be used for the research of hypersensitivity diseases, nasal congestion, allergic conjunctivitis and other allergic diseases[1][2].
Clemastine Fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM.Target: Histamine H1 ReceptorClemastine Fumarate inhibits histamine induced rise in [Ca2+]i in HL-60 cells with an IC50 of 3 nM as compared with that of chlorpheniramine or diphenhydramine with IC50 values of 20 nM and 100 nM, respectively [1]. Clemastine showed a first-pass reduction in the extent of absorption, with oral bioavailability calculated as 39.2 +/- 12.4%. Extravascular distribution of drug was suggested by the high volume of distribution (799 +/- 315 L) and low Cmax (0.577 +/- 0.252 ng/mL/mg) observed at 4.77 +/- 2.26 hours after administration, and by the biphasic decline in plasma concentration. The terminal elimination half-life (t1/2) of clemastine was 21.3 +/- 11.6 hours. Steady-state concentrations of clemastine were consistent with linear pharmacokinetic processes, and clearance was unaffected by age in the range studied, or by race [2].
UCM-1306 is a potent and orally active human dopamine D1 receptor allosteric modulator (PAM). UCM-1306 increases the endogenous dopamine (DA) maximal effect both in human and mouse D1 receptors. UCM-1306 not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD)[1].
DAU 5884 hydrochloride is a potent muscarinic M3 receptor antagonist. DAU 5884 hydrochloride inhibits methacholine-dependent effects on cell proliferation and muscle contractility[1].
CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand, with Ki values of 3.5 and 1.2 nM, respectively. CB1/2 agonist 2 can behave as a full CB1 agonist and CB2 competitive inverse agonist. CB1/2 agonist 2 shows antinociceptive activity[1].
IPAG is a potent sigma-1 receptor antagonist with a pKi of 4.3[1]. IPAG induces apoptosis[2].
SR-31747 is a sigma ligand with immunosuppressive and anti-inflammatory properties. SR-31747 blocks cell proliferation by inhibiting sterol isomerase[1][2].
Cimbuterol is a β-adrenergic receptor agonist[1].
PSB-0788 (compound 17), xanthine-8-yl-benzenesulfonamide derivative, is a new selective high-affinity A2B antagonist with IC50 value of 3.64 nM and Ki value of 0.393 nM, respeactively. PSB-0788 (compound 17) can be used for the research for chronic inflammatory lung diseases[1].
Salmeterol is a long-acting beta2-adrenergic receptor (beta 2AR) agonist used clinically to treat asthma.Target: beta2-Adrenergic ReceptorSalmeterol is a long-acting beta2-adrenergic receptor agonist drug that is prescribed for the treatment of asthma and chronic obstructive pulmonary disease (COPD). salmeterol also binds with very high affinity at a second site, termed the "exosite", and that this exosite contributes to the long duration of action of salmeterol [1].
Hemorphin-7 is a hemorphin peptide, an endogenous opioid peptide derived from the β-chain of hemoglobin. Hemorphin peptides exhibits antinociceptive and antihypertensive activities, activating opioid receptors and inhibiting angiotensin-converting enzyme (ACE).
Carbazochrome(AC-17) is an antihemorrhagic agent.Target: OthersCarbazochrome is an antihemorrhagic agent that will cease blood flow by causing the aggregation and adhesion of platelets in the blood to form a platelet plug, ceasing blood flow from an open wound. It is hoped that this drug can be used in the future for preventing excessive blood flow during surgical operations and the treatment of hemorrhoids. Carbazochrome interacts with α-adrenoreceptors on surface of platelets, which are coupled to Gq protein and initiate PLC IP3/DAG pathway to increase intracellular free calcium concentration with these subsequent actions. Activates PLA2 and induce arachidonic acid pathway to synthese endoperoxides (TxA2, thromboxane A2). Calcium binds to calmodulin which then binds and activates myosin light-chain kinase, that will enable the myosin crossbridge to bind to the actin filament and allow contraction to begin. This will change platelet's shape and induce release of serotonin, ADP, vWF (Von Willebrand factor), PAF (Platelet-activating factor) to promote further aggregation and adhesion. From Wikipedia.
Bevenopran is a peripheral μ-opioid receptor antagonist.
KRAS G12C inhibitor 26 is a KRAS G12C inhibitor with antitumor effects (WO2021109737)[1].
BRS-3 receptor agonist-2 (compound 2) is a potent BRS-3 receptor agonist, with an EC50 of 2.5 nM for mouse BRS-3 receptor[1].