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
Emavusertib, also known as CA-4948 is a potent IRAK4/FLT3 inhibitor with anti-tumor activity. CA-4948 demonstrated good cellular activity in ABC DLBCL and AML cell lines. CA-4948 demonstrated moderate to high selectivity in a panel of 329 kinases as well as exhibited desirable ADME and PK profiles including good oral bioavailability in mice, rat, and dog and showed >90% tumor growth inhibition in relevant tumor models with excellent correlation with in vivo PD modulation. 了解更多
Eleclazine, also known as GS-6615, is a selective late sodium current inhibitor. Eleclazine is potentially useful for treatment of coronary vasodilators, antiarrhythmics and vasodilators. 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
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
CRT0066101 is a PRKDs inhibitor. CRT0066101 suppressed the proliferation and migration of four bladder cancer cell lines in vitro. CRT0066101 blocked tumor growth in a mouse flank xenograft model of bladder cancer. 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
EMAC10101d is a potent and selective inhibitor of Carbonic Anhydrase Isoform toward hCA II with an inhibitory activity in the low nanomolar range. Ki of 8.1 nM 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
ZK824190 is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively. 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
KCNJ1 (Kir1.1, or renal outer medullary potassium channel) and KCNJ13 (Kir7.1) are inwardly rectifying two-transmembrane K+ channels. KCNJ1 has critical roles in kidney function, while KCNJ13 is important in the eye, kidney, and small intestine. VU590 is a small molecule inhibitor of KCNJ1 (IC50 = 294 nM) which also causes 70% inhibition of KCNJ13 at 10 ?M. It has no effect on the related channels KCNJ2 (Kir2.1) and KCNJ10 (Kir4.1) at a concentration of 10 ?M. 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
blocker of fast Na+-dependent action potentials and voltage-dependent
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
Distigmine Bromide, also known as Ubretid and BC-51, is an acetylcholinesterase inhibitor used for the treatment of underactive neurogenic bladder and myasthenia gravis. 了解更多
NPS2390 is a group I mGlu antagonist. It displays noncompetitive antagonist activity at both mGlu1 and mGlu5 receptors. NPS2390 is thought to act on a site separate from the glutamate binding pocket. 了解更多
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