RTA-408 is a synthetic triterpenoid that potently activates the antioxidative transcription factor Nrf2 and inhibits the proinflammatory transcription factor NF-κB.

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.

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.

RU 24969 hemisuccinate is a potent SR-1A/SR-1B and moderate SR-2C agonist that may also release serotonin.

RU1968 is a potent, cross-species sperm-specific Ca2+ channel CatSper inhibitor that is selective for CatSper over Slo3.

RU-521 (RU.521, RU-320521) is a potent, selective cyclic GMP-AMP synthase (cGAS) inhibitor with Kd of 36.2 nM.

RU58841 is a nonsteroidal anti-androgen with potency (IC50 = 100 nM, Ka = 1.1 nM) comparable to hydroxyflutamide.

Rubusoside is a natural sweetener and a solubilizing agent with antiangiogenic and antiallergic properties.Rubusoside can improve the survival rate of palmitic acid- induced INS- 1 cells and inhibit the occurrence of apoptosis.

Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM with binding affinity to nine PARP domains. Phase 1/2.

Rucaparib inactivates PARP activity in cells with homologous recombination DNA repair pathway mutations at LC50 values ranging from 1.3-5.5 μM.

Rufinamide(E 2080; CGP 33101; RUF 331) is a new antiepileptic agent that differs structurally from other antiepileptic drugs and is approved as adjunctive therapy for Lennox-Gastaut syndrome (LGS).

Runcaciguat is a potent soluble guanylyl cyclase (sGC) stimulator/activator..

Rupatadine is a dual histamine H1 and PAF antagonist

Rupintrivir (AG-7088, AG7088) is a potent, irreversible inhibitor of human rhinovirus 3C protease, inhibits the replication of all HRV serotypes with EC50 of 23 nM and EC90 of 82 nM.

Ruxolitinib is a potent ATP mimetic that inhibits both JAK1 and JAK2 with IC50 values of 2.7 and 4.5 nM, respectively and is relatively less selective for JAK3 (IC50 = 322 nM).

Ruxolitinib Phosphate is a potent and selective Janus kinase (JAK1, IC50 = 5.9 nM and JAK2, IC50 = 5.7 nM) inhibitor.

RVX-208(RVX 000222) is a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo; is a BET bromodomain antagonist.

RX-3117 is an orally available and potent DNA synthesis inhibitor with potential antineoplastic activity.

RX518(CK-101) is an orally available third-generation and selective inhibitor of certain epidermal growth factor receptor (EGFR) activating mutations.

Ryuvidine is a potent, selective CDK4 inhibitor with IC50 of 6.0 uM, displays >30-fold selectivity over CDK2 (IC50>100 uM).

S 38093 is a brain-penetrant antagonist of H3 receptor, with Ki of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively.

S 38093 is a novel brain-penetrant antagonist/inverse agonist of H3 receptors.