SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit.

URB597 is a potent, orally bioavailable FAAH inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets.

Ibiglustat (succinate) is a selective inhibitor of glucosylceramide synthase.

VU0285655-1 is a potent, selective inhibitor of PLD2, induces autophagy in colorectal cancer cells

Upidosin (Rec 15/2739) is an α-1 adrenoceptor (α-1 AR) antagonist. Upidosin shows moderate selectivity for the α-1A AR subtype. Upidosin shows uroselectivity in urethra and prostate with a Kb value of 2-3 nM higher than in ear artery and aorta with a Kb value of 20-100 nM. Upidosin inhibits [3H]prazosin binding to cloned human α-1A adrenergic receptor. Upidosin can be used for the research of urethral obstruction.

ML390 is a human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia. ML390 bioactivity: ER-HOX-GFP (EC50 μM) = 1.8 ± 0.6; U937 (EC50 μM) = 8.8 ± 0.8; THP-1 (EC50 μM) = 6.5 ± 0.9; DHODH (IC50, μM) = 0.56 ± 0.1. ML390 may offer insight into the mechanism of overcoming differentiation arrest, and will translate into a starting point for a much-needed new and potent treatment for patients with acute myeloid leukemia. Inhibitors of dihydroorotate dehydrogenase (DHODH) showed activity to induce differentiation in multiple animal models of AML in vitro and in vivo. DHODH inhibitors demonstrated effective at prolonging survival in animal models of leukemia.

TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc.

A selective prostaglandin E receptor subtype 4 (EP4) antagonist with pKi of 8.5.

BIBF-1202 is the carboxylate metabolite of BIBF 1120, which is an oral triple angiokinase inhibitor targeting VEGFR, PDGFR, FGFR.

ML193 (CID 1261822) is a potent, selective GPR55 antagonist with IC50 of 221 nM, shows >27-, >145- and >145-fold selectivity for GPR55 over CB1, GPR35 and CB2, respectively.

AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.

I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC50=2.7 μM) and is inactive for other H2S/sulfane sulfur-producing enzymes.?I3MT-3 targets a persulfurated cysteine residue located in the active site of 3MST.

Novel potent and selective 5-HT2B receptor antagonist

PD-1/PD-L1-IN-NP19 is a PD-1/PD-L1 inhibitor, with an IC50 of 12.5 nM for human PD-1/PD-L1 interaction. PD-1/PD-L1-IN-NP19 could activate the immune microenvironment in tumor, which may contribute to its antitumor effects.

CID1231538, a benzothiazole analogue, is a potent GPR35 antagonist (IC50=0.55 μM). GPR35 is a G protein-coupled receptor (GPCR).

Lanraplenib monosuccinate (GS-9876 monosuccinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib monosuccinate (GS-9876 monosuccinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.

PFKL activator NA-11 is a small-molecule, selective PFKL activator, inhibits the NOX2-dependent oxidative burst in neutrophils by activating the glycolytic enzyme phosphofructokinase-1 liver type (PFKL).

PDD 00017273 is the first-in-class, selective inhibitor of poly(ADP-ribose) glycohydrolase (PARG) with Kd, biochemical EC50 of 1.45 nM, 26 nM.

A xanthone derivative that fuctions as an EP and DP receptor antagonist.

For the detailed information of JNJ40411813, the solubility of JNJ40411813 in water, the solubility of JNJ40411813 in DMSO, the solubility of JNJ40411813 in PBS buffer, the animal experiment (test) of JNJ40411813, the cell expriment (test) of JNJ40411813, the in vivo, in vitro and clinical trial test of JNJ40411813, the EC50, IC50,and Affinity of JNJ40411813, Please contact DC Chemicals..

BCATc Inhibitor 2 is a selective branched-chain aminotransferase (BCAT) inhibitor for research of neurodegenerative diseases. The IC50s of 0.2 μM, 0.8 μM and 3.0 μM for rat cytosolic isoenzyme rBCATc, human cytosolic isoenzyme hBCATc and rat mitochondrial isoenzyme rBCATm, respectively.

MMV390048 is a novel potent Plasmodium PI4K inhibitor with IC50 of 28 nM against intraerythrocytic life cycle stages of P. falciparum (NF54 drug-sensitive strain).

RO0711401 is a selective and orally active positive allosteric modulator of mGlu1 receptor with an EC50 of 56 nM.

NITD-2, a dengue virus (DENV) polymerase inhibitor, inhibits the DENV RdRp-mediated RNA elongation. NITD-2 penetrates cell membrane poorly.

PF-06446846 (PF-6446846) is a potent, highly selective inhibitor of PCSK9 translation with IC50 of 0.3 uM for inhibition the secretion of PCSK9 by Huh7 cells.

PKC-iota inhibitor 1 (compound 19) is a protein kinase C-iota (PKC-ι ?) inhibitor with an IC50 value of 0.34 μM.

GZD856 is a novel and orally bioavailable PDGFRα/β inhibitor with IC50s of 68.6 and 136.6 nM, respectively. Anti-lung cancer activities. Also a Bcr-AblT315I inhibitor with IC50s of 19.9 and 15.4 nM for Bcr-Abl and T315I mutant.

CGP60474 is a potent inhibitor of cyclin-dependent kinase (CDK).

Bruton tyrosine kinase inhibitor