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.

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.

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.

TAS-117 is a highly selective, non-ATP competitive pan-Akt inhibitor with IC50 of 4.8/1.6/44 nM for Akt1/Akt2/Akt3 respectively.

VPC 14449 is a potent and selective androgen receptor DNA-binding domain (AR-DBD) inhibitor with IC50 of 0.34 uM, without affecting AR protein expression.

VPC-18005 (VPC18005) is a novel small molecule ERG (ETS-related gene) antagonist that inhibits ERG-induced transcription and interacts directly with the ERG-ETS domain, disrupts the ERG binding to DNA (Kd=250 uM).

An STAT3 inhibitor that selectively targets the DNA-binding domain of STAT3, without affecting the activation and dimerization of STAT3.

BDCRB (GW 275175) is a potent and selective inhibitor of human CMV replication by blocking the processing and maturation of viral DNA..

PF04802367 is a potent, highly selective GSK-3 inhibitor with IC50 of 2.1 nM for human GSK-3β in enzyme assays; shows equal effectivity against GSK-3α and GSK-3β with IC50 of 10.0 and 9.0 nM respectively in mobility shift assays, inhibits phosphorylation of tau with an IC50 of 466 nM in a stable inducible CHO cell line over-expressing GSK-3β and substrate tau; modulates tau phosphorylation in vitro and in vivo.

dTRIM24 is a potent TRIM24 bromodomain inhibitor with IC50 of 217.8 nM (TRIM24 ligand displacement).

(-)-Isoproterenol hydrochloride is an agonist of beta-adrenergic receptor. (-)-Isoproterenol hydrochloride is also used in the treatment of bradycardia; bronchodilator.

Piperazine Erastin is an analog of Erastin, which can induces ferroptosis in cancer cells, an iron-dependent form of nonapoptotic cell death..

Telotristat ethyl (LX1606) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.

Parbendazole is an anthelmintic drug. Parbendazole is a potent inhibitor of microtubule assembly, destabilizes tubulin and exhibits a broad-spectrum anthelmintic activity.

SBI-993 is an analog of SBI-477 that shows improved potency and suitable pharmacokinetic properties for in vivo bioavailability