Repotrectinib(TPX-005) is a multi-target macrocycle inhibitor of anaplastic lymphoma kinase (ALK), c-ros proto-oncogene 1 receptor tyrosine kinase (ROS1), and neurotrophic tyrosine kinase receptor (TRK)

RepSox(E-616452; SJN 2511) is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation, respectively.

Resiquimod (R-848; S28463) is a potent synthetic agonist of TLR7/TLR8 that possesses antiviral and antitumoral activities.

Retigabine 2Hcl (Ezogabine; D23129) is a Kv7.2-7.5 (KCNQ2-5) neuronal potassium channel opener witrh anticonvulsant activity.

Retigabine is a novel anti-convulsant, enhances activation of KCNQ2/Q3 potassium channels.

Reversine, a small synthetic purine analogue (2,6-disubstituted purine), is a potent inhibitior of Aurora A/B/C with IC50s of 150-500 nM.

RG108 is an inhibitor of DNA methyltransferase with IC50 of 115 nM, does not cause trapping of covalent enzymes.

RG-13022 is an inhibitor of epidermal growth factor (EGF) receptor kinase with an IC50 value of 1 µM in HT-22 cells.

RG14620 is an epidermal growth factor receptor (EGFR) inhibitor, with IC50 values of 3 μM for HER 14 colony formation and 1 pM for HER 14 DNA synthesis.

RG2833 is a brain-penetrant inhibitor of HDAC with IC50 values of 60 nM and 50 nM for HDAC1 and HDAC3, respectively.

RG7090(CTEP Derivative,Basimglurant, RO4917523) is a negative modulator of metabotropic glutamate receptor subtype 5 (mGluR5; GRM5).

RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor.

RG7388 is an oral, selective, small molecule MDM2 antagonist that inhibits binding of MDM2 to p53.

RG7834 (RO 7020322) is a highly selective and orally bioavailable HBV inhibitor, potently inhibits HBV antigens (both HBsAg and HBeAg) and HBV DNA, with IC50s of 2.8, 2.6, and 3.2 nM, respectively, in dHepaRG Cells.

RGB-286638 is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclin E-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6.

RGFP966 is specific inhibitor of HDAC3, with an IC50 of 0.08 μM and no effective inhibition of any other HDAC at concentrations up to 15 μM.

RGX-104 is an orally bioavailable agonist of the nuclear receptor liver X receptor beta (LXRbeta; NR1H2; LXR-b), with potential immunomodulating and antineoplastic activities.

RH01687 is a small molecule that protect pancreatic β cells against endoplasmic reticulum stress-induced cell death.

Rheb inhibitor NR1 is a small molecule that binds Rheb in the switch II domain (IC50=2.1 uM, Kd=1.5 uM) and selectively blocks mTORC1 signaling, potently inhibits mTORC1 driven phosphorylation of S6K1 but does not inhibit phosphorylation of AKT or ERK.

Rhosin (G04) is a potent, specific RhoA subfamily Rho GTPases inhibitor that specifically binds to RhoA to inhibit GEF reaction of RhoA with Kd of 0.4 uM, does not interact with Cdc42 or Rac1, nor the LARG.

RHPS4 is a potent inhibitor of Telomerase at submicromolar.

RI-1 is a RAD51 inhibitor with IC50 ranging from 5 to 30 μM.