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.

NED-3238 is highly potent third generation inhibitors of human arginase I and II with IC50 of 1.3 nM and 8.1 nM respectively.

PQR514 is a potent selective pan-PI3K inhibitor with binding Ki of 2.2 and 33 nM for p110α and mTOR, repectively.PQR514 inhibits phosphorylated S6 ribosomal protein (pS6, Ser235/236) and phosphorylation PKB Ser473 in A2058 cells with IC50 of 17 and 68 nM, respectively.PQR514 displays negligible interference with protein kinase activities at 10 uM in a KINOMEScan panel.PQR514 exhibits growth inhibition in vitro across a panel of 66 tumor cells with GI50 of 0.25 uM.PQR514 demonstrates significant antitumor activity aginst OVCAR-3 human ovarian cancer xenograft model in BALB/c nude mice.

SS-208 (SS208) is a novel potent, selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 12 nM, >100-fold selectivity over HDAC1/4/5/7/8/9/11.SS-208 has minimal effects on the viability of murine SM1 melanoma cells in vitro, significantly reduced in vivo tumor growth in a murine SM1 syngeneic melanoma mouse model.

GSK3527497 (GSK-3527497) is a potent, selective TRPV4 inhibitor with IC50 of 12 nM (hTRPV4).GSK3527497 is a pre-clinical candidate for treatment of diseases resulting from TRPV4 activation.

XPC-6444 is an CNS-penetrant, isoform-selective NaV1.6 inhibitors with IC50 of 41 nM, which also displayed potent block of NaV1.2 with IC50 of 125 nM.

AT-001 is a nociceptin opioid receptor (NOP) partial agonist with Ki of 10.3 nM, which may be useful to develop nondopaminergic treatments for Parkinson's Disease.

AT-004 is a nociceptin opioid receptor (NOP) partial agonist with Ki of 9.8 nM, which may be useful to develop nondopaminergic treatments for Parkinson's Disease.