hGPR91 antagonist 3 (Compound 5g) is a potent, selective, and orally active antagonist of hGPR91 (%F: 26). hGPR91 antagonist 3 has the potential for the research of hypertension, autoimmune disease and retinal angiogenesis.

Overview. A common route of resistance to tuberculosis involves Mtb erm37 expression, which expresses an RNA methyltransferase that methylates the A2058 position of the 23S ribosome RNA, hindering macrolide antibiotic binding.

BI-3231 is a novel potent and selective HSD17B13 inhibitor with IC50 of 1 nM and Ki of 0.7 nM, respectively. BI-3231 is a valuable chemical probe to further elucidate the biological function of HSD17B13.

Evocalcet (KHK7580) is an novel oral calcimimetic agent which acts via allosteric activation of the calcium sensing receptor (CaSR). Evocalcet (0, 20 and 60 nM) dose-dependently increases cytoplasmic [Ca2+] concentrations with an EC50 value of 92.7 nM in hCaR-HEK293 cells.

UCL-TRO-1938 is a small-molecule activator of the PI3Kα isoform with EC50 of 60 μM. UCL-TRO-1938 activats PI3Kα but not PI3Kβ or PI3Kδ and effectively boosts endogenous protective and regenerative signalling.

DU011 is a noncanonical anti-infective agent and small-molecule inhibitor of capsule biogenesis, targets MprA (Kd=30 nM), a MarR family transcriptional repressor of multidrug efflux pumps, inhibits capsule expression in E. coli. DU011 does not alter Escherichia coli antibiotic resistance and has significantly enhanced inhibition of capsule expression, compared with other proposed MprA ligands, such as salicylate and 2,4-dinitrophenol (DNP).

RTI-13951-33 is a potent, selective, brain-penetrant agonist of the orphan receptor GPR88 with EC50 of 25 nM in in vitro cAMP functional assay.

DS42450411 (DS 42450411, DS-42450411) is a potent, orally active hepcidin production inhibitor with IC50 of 32 nM.

GNE-8505 is a DLK inhibitor (IC50 = 10nM).

GSK3395879 (GSK-3395879) is a novel potent, selective, orally bioavailable antagonist of TRPV4 with IC50 of 1 nM (hTRPV4); exhibits little or no activity against a broad panel of TRP channels (IC50 > 10µM for TRPA1, TRPV1, TRPM2, TRPM4, TRPM8, TRPC3, TRPC4, TRPC5, TRPC6); demonstrates the ability to inhibit TRPV4-mediated pulmonary edema in an in vivo rat model.

LSN 3213128 is a novel potent, selective and orally-bioavailable antifolate with potent and specific inhibitory activity for AICARFT.

GSK8175 is a non-nucleoside polymerase (NS5B) inhibitor of hepatitis C virus (HCV). GSK8175 is a sulfonamide- N-benzoxaborole analog with low in vivo clearance across preclinical species and broad-spectrum activity against HCV replicons.

BMS-955176 (GSK-3532795) is a second-generation HIV-1 maturation inhibitor that exhibits potent activity (EC50=3.9±3.4 nM) against a library (n=87) of gag/pr recombinant viruses.

RTS-V5 (Dual HDAC-proteasome inhibitor RTS-V5) is the first-in-class, dual HDAC-proteasome inhibitor with IC50 of 0.27 uM (HDAC6), inhibits HDAC8 (IC50=0.53 uM), and low activity against HDAC/1/2/3.

ANT431 is a novel potent metallo-β-lactamase (MBL) inhibitor with IC50 of 290 nM and 195 nM for NDM-1 and VIM-2, shows a comparatively weak inhibitor of VIM-1 and IMP-1 (Ki of 14.6 and 4.15 uM, respectively).

BMS-823778 (BMS823778) is an orally available, potent and selective inhibitor of 11βHSD-1 with IC50 of 2.3 nM, displays >10,000-fold selectivity over 11βHSD-2.

HMG499 is a potent and selective HMG-CoA reductase inhibitor.

DPM-1001 is a potent, selective, orally bioavailable inhibitor of the protein-tyrosine phosphatase PTP1B with IC50 of 100 nM, also chelates copper, which enhanced its potency as a PTP1B inhibitor.

MSC2504877 (MSC-2504877) a novel small molecule selective tankyrase inhibitor with IC50 of 0.7/0.8 nM against TNKS1/2, shows 771-fold selectivity for TNKS1 over PARP1 (IC50=0.54 uM).

BMS-962212 is a potent, highly selective and reversible small molecule coagulation Factor XIa (FXIa) inhibitor with Ki of 0.7 nM.

MLT-748 (MLT748) is a potent, selective, allosteric inhibitor of MALT1 paracaspase with IC50 of 5 nM, does not show inhibitory activity against 22 other tested human proteases (IC50>100 uM).

MLT-747 (MLT747) is a potent, selective, allosteric inhibitor of MALT1 paracaspase with IC50 of 14 nM.

SUVN-G3031 (SUVN-G 3031) is a potent, selective, orally active histamine H3 receptor (H3R) inverse agonist with Ki of 8.73 nM (hH3R).

BMS-932481 (BMS932481) is a potent, selective, orraly active γ-secretase modulator (GSM), shows selectivity for Aβ40 and Aβ42 reduction (IC50=6.6 nM) while sparing total Aβ levels both in vitro and in vivo.

JNJ4796 (JNJ 4796, JNJ-4796) is an orally active small-molecule fusion inhibitor of influenza virus hemagglutinin (HA) with EC50 of 33 nM (H1N1 neutralization).

Suramin sodium salt (BAY-205, NF-060) is an antitrypansomal drug that also possesses antitumor activity.

NRX-103095 is an enhancer of an E3 ligase-substrate interaction.

PF-06372865 is a novel potent, α2/3 functionally selective GABAA receptor positive allosteric modulator.

CCT365623 is a potent, selective and orally bioavailable LOX inhibitor with IC50 of 0.9 μM and 1.5 μM for LOX and LOXL2.

Pecavaptan is a vasopressin receptor antagonist.