Plitidepsin is a cyclic depsipeptide isolated from the marine tunicate Aplidium albicans. Plitidepsin displays a broad spectrum of antitumor activities, inducing apoptosis by triggering mitochondrial cytochrome c release, initiating the Fas/DC95, JNK pathway and activating caspase 3 activation. This agent also inhibits elongation factor 1-a, thereby interfering with protein synthesis, and induces G1 arrest and G2 blockade, thereby inhibiting tumor cell growth. 了解更多

LP-261 is a novel tubulin targeting anticancer agent that binds at the colchicine site on tubulin, inducing G2/M arrest. Screening in the NCI60 cancer cell lines resulted in a mean GI50 of approximately 100 nM. 了解更多

AP1189 is a biased agonist at receptors MC1 and MC3. AP1189 reduced cytokine release, an effect reliant on both MC1 and MC3 as evident from the use of Mc1r(-/-) and Mc3r(-/-) macrophages. 了解更多

PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor agonist (GLP-1R) 了解更多

Caroverine hydrochloride is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. Caroverine hydrochloride is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action. Caroverine hydrochloride can be used for the research of inner ear tinnitus. 了解更多

PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E (Kis = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay).1 It increases cAMP levels in HEK293 cells expressing 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E receptors (EC50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg. 了解更多

AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors. It is a milti-target drug candidate for the treatment of CNS disorders. 了解更多

Vodobatinib, also known as K-0706, is a novel 3rd generation (3G) TKI effective against wild-type and mutated BCR-ABL1 with limited off-target activity. 了解更多

Tenofovir exalidex, also known as HDP-Tenofovir and CMX-157, is a novel lipid acyclic nucleoside phosphonate that delivers high intracellular concentrations of the active antiviral agent tenofovir. 了解更多

Ro0711401 is a mGlu1 receptor agonist. 了解更多

PNU 282987 is a highly selective α7 nAChR agonist (Ki = 26 nM) displaying negligible blockade of α1β1γδ and α3β4 nAChRs (IC50 ?? 60 μM). Found to be inactive against a panel of 32 receptors at 1 μM, except 5-HT3 receptors (Ki = 930 nM). 了解更多

Varenicline is a nicotinic receptor partial agonist. 了解更多

SB203186 is potent 5-HT4 receptor antagonist. 了解更多

ACH-000143 is a potent and peripherally preferred melatonin receptor agonist. 了解更多

Riamilovir, also known as Triazavirin, is a nucleoside analogue of nucleic acid and an antiviral agent, works by inhibiting the synthesis of viral RNA and DNA and replication of genomic fragments. Triazavirin is shown active in inhibition of the tick-borne encephalitis virus reproduction (strain Sofiin) by accumulation in the SKEV cell culture. 了解更多

TRC253, also known as JNJ63576253, is a potent and orally active androgen receptor antagonist. 了解更多

MK 212 hydrochloride is a 5-HT receptor agonist; displays selectivity for 5-HT2C over 5-HT2A (IC50 values are 0.028 and 0.42 μM for human 5-HT2C and 5-HT2A receptors expressed in HEK293 cells respectively). 了解更多

TMP778 is a novel, potent, and selective ROR?t inverse agonist. 了解更多

Osajin is a bioactive isoflavone present in the fruit of Maclura pomifera, commonly referred to as the Osage orange. 了解更多

ML-095 is an inhibitor of PLAP (IC50 = 3.7 μM) that demonstrates high selectivity against the related alkaline phosphatases, TNAP and IAP (IC50s > 100 μM). 了解更多

ATPO is a potent and Selective Ampa Receptor Antagonist. 了解更多

ML 193 is a selective GPR55 antagonist (IC50 = 221 nM). Exhibits >27-, >145- and >145-fold selectivity for GPR55 over CB1, GPR35 and CB2, respectively. Inhibits ERK signaling in vitro. 了解更多

SEP-363856, also known as SEP-856, is an orally active and CNS active psychotropic agent. 了解更多

Luzindole, also known as N-0774, and N-acetyl-2-benzyltryptamine, is a melatonin receptor antagonist that preferentially targets MT1B over MT1A (Ki values are = 10-27 and 158-513 nM, respectively). 了解更多

LM11A-31 is a small-molecule p75NTR modulator and proNGF antagonist. 了解更多

Pizuglanstat is a hematopoietic prostaglandin synthase inhibitor. 了解更多

ZINC30303842 is a NSD2-PWWP1 antagonist. 了解更多

Xanthurenic acid is a putative endogenous Group II metabotropic glutamate receptor agonist, on sensory transmission in the thalamus. 了解更多

Methyl dihydrojasmonate is a fragrance ingredient with a jasmine-like odor, used in many fragrance mixtures. 了解更多

Tetrahydropalmatine, an active component isolated from corydalis, possesses analgesic effects. Tetrahydropalmatine acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats. 了解更多

Flavokawain A is found in Piper methysticum (kava plant). It suppresses expression of iNOS and COX-2 in macrophages, decreases expression of Ki67, XIAP and survivin in urothelial cell carcinoma cells, and inhibits degradation of NF-??B. 了解更多

Ethyl pyruvate is a simple derivative of the endogenous metabolite, pyruvic acid. Ethyl pyruvate is an anti-inflammatory agent. 了解更多

JTE-013 is a potent and specific S1P2 (Sphingosine-1-Phosphate 2; EDG-5) antagonist. JTE-013 inhibits the specific binding of radiolabeled S1P to human and rat S1P2 with IC50s of 17 nM and 22 nM, respectively. 了解更多

EAD1 is a potent autophagy inhibitor with antiproliferative activity in lung and pancreatic cancer cells. EAD1 also induces apoptosis. 了解更多

Benzetimide hydrochloride is a muscarinic acetylcholine receptor antagonist. 了解更多

SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. 了解更多

Carbutamide (BZ-55) is an orally active and first-generation sulfonylurea with hypoglycemic activity. 了解更多

Carazolol is a non-specific β-adrenergic receptor blocking agent and binds to β receptors irreversibly. 了解更多

Quipazine maleate is a selective 5-HT receptor agonist that promotes the proliferation and apoptosis of human hepatocyte strain of L-02 strain and could also exert an excitatory effect on raphe neurons via stimulation of 5-HT2A receptors. 了解更多

ACT-389949 is a first-in-class, potent and selective and agonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX), with an EC50 of 3 nM for FPR2/ALX internalization into monocytes. 了解更多

M8-B is an antagonist of transient receptor potential melastatin 8 (TRPM8) that blocks activation by cold, icilin (Item No. 10137), or menthol in vitro (IC50s = 7.8, 26.9, and 64.3 nM, respectively). 了解更多

LASSBio-1135 is a dual TRPV1 antagonist and TNF-alpha production inhibitor. 了解更多

EMD-66684 is a non-peptide angiotensin II receptor antagonist. 了解更多

Cgs 20625 is a benzodiazepine receptor agonist. 了解更多

Leteprinim, also known as AIT-082 and SPI-205, is a neurotrophic agent potentially for the treatment of Alzheimer's disease, and spinal cord injury. 了解更多

Ro 19-4603 is a benzodiazepine receptor inverse agonist. 了解更多

Lidocaine N-ethyl bromide is a non-membrane-permeable blocker of fast Na+-dependent action potentials and voltage-dependent, non-inactivating Na+ conductance. 了解更多

NMP-7 is a non-selective agonist of the CB1 and CB2 cannabinoid receptors that acts by blocking T-type calcium channels. 了解更多

Flutonidine is an alpha2-Adrenergic receptor agonist. 了解更多