MS4-8107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS 48107 can readily cross the blood-brain barrier (BBB) in mice[1].

Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is an orally active and competitive heme oxygenase-1 (HO-1) inhibitor and markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2[1]. Zinc Protoporphyrin is used as a screening marker of iron deficiency in individual pregnant women and children, but also to assess population iron status in combination with haemoglobin concentration[2]. Zinc Protoporphyrin has anti-cancer activity[3].

RO-5963 is an inhibitor of the interaction of both MDM2 and MDMX with p53.

BAY 6035 is a potent and selective SMYD3 inhibitor.

NCI-006 is a potent new inhibitor of lactate dehydrogenase (LDH) that disrupts tumor growth in mice. LDH inhibition slows tumor growth but rapidly redirects pyruvate to support mitochondrial metabolism. Inhibiting both mitochondrial complex 1 and LDH suppresses metabolic plasticity of glycolytic tumors in vivo, significantly prolonging tumor growth inhibition.

BI-4924 (BI 4924) is a potent, selective NADH/NAD+-competitive PHGDH inhibitor with IC50 of 2 nM.BI-4924 splays high selectivity against the majority of other dehydrogenase targets.

TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC50 of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC50 of 95 nM). TAS-119 has potent antitumor activites.

KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1/2

ACT-541468 is a dual orexin receptor antagonist.

Sodium channel blocker. Suppresses tetrodotoxin (TTX)-resistant Na+ currents approximately twice as selectively as TTX-sensitive currents. Antinociceptive; displays analgesic effects in animal models of inflammatory and neuropathic pain.

EB-42486 is a novel, potent, and highly selective G2019S-LRRK2 inhibitor (IC50 < 0.2 nM).

ISO-1 is a macrophage migration inhibitory factor (MIF) antagonist with an IC50 of 7 μM.

PF-06821497 (compound 23a) is a potent, selective and orally active Enhancer of Zeste Homolog 2 (EZH2) inhibitor, with a Ki value <0.1 nM against mutant Y641N EZH2. Exhibits robust tumor growth inhibition.

Branaplam (LMI070; NVS-SM1) hydrochloride is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam hydrochloride inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam hydrochloride elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model.

FMK 9a is an autophagin-1 inhibitor with IC50 values of 80 and 73 μM in FRET and LRA assay.

SSR-240612 is a bradykinin B1 receptor antagonist potentially for the treatment of chronic pain.

GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect.

VU0360172 is a positive allosteric modulator of mGlu5 receptors (EC50 = 16 nM; Ki = 195 nM). VU0360172 is selective for mGlu5 and it displays no significant activity at mGlu1, mGlu2 or mGlu4 receptors.

Cadralazine is a peripheral arteriolar vasodilator and an antihypertensive drug.