RORγt inverse agonist 22 is a potent, subtype selective RORγt inverse agonist with binding IC50 of 18 nM, displays >192-fold selectivity over RORα and RORβ.

RORγt inverse agonist 32 is a potent, orally bioavailable inverse agonist of RORγt with IC50 of 9 nM in SPA binding assays.

Roseoflavin is a chemical analog of FMN and riboflavin that has antimicrobial activity.

Rotigotine is dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively. Rotigotine also has significant affinity for 5-HT1A and adrenergic α2B receptors. Rotigotine exhibits antiparkinsonian acitivity.

Rottlerin (Mallotoxin.

Roxyl-WL is a highly potent and selective inhibitor of IDO1 with IC50 of 1 nM.

Roy-Bz is the first small-molecule PKCδ-selective activator with EC50 of 58.5 nM, binds to the PKCδ-C1-domain.

RP-1859 is a selective stimulator of S1P1 and S1P5 (S1P1 IC50 = 0.20 nM; S1P5 IC50 = 170 nM) used for the treatment of autoimmunity disease.

RP-1865 is a selective stimulator of S1P1 and S1P5 used for the treatment of autoimmunity disease.

RP-5063 (Brilaroxazine) is a multimodal dopamine and serotonin modulator with partial agonist activity at DA D2, D3, D4, 5-HT1A, and 5-HT2ARs, and antagonist activity at 5-HT2B, 5-HT6 and 5-HT7Rs.

RPL-554 (LS-193855, RPL554) is a potent, orally available, dual PDE3/PDE4 inhibitor with IC50 of 0.4 nM and 1479 nM, respectively.

Rpn11 inhibitor 35 is a potent, small molecule inhibitor of the proteasome subunit Rpn11 with IC50 of 400 nM,100-fold selectivity over Csn5 and 10-fold selectivity over AMSH.

RPR260243 was the first reported hERG channel activator.

RRD-251 hydrochloride is a small molecule disruptor of Rb/Raf-1 interaction, potently and selectively disrupts the Rb/Raf-1 (IC50=77 nM) but not Rb/E2F, Rb/prohibitin, Rb/cyclin E, and Rb/HDAC binding.

RRD-251 hydrochloride is a small molecule disruptor of Rb/Raf-1 interaction, potently and selectively disrupts the Rb/Raf-1 (IC50=77 nM) but not Rb/E2F, Rb/prohibitin, Rb/cyclin E, and Rb/HDAC binding.

RS 17053 hydrochloride is a potent and selective α1A adrenoceptor antagonist, with a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays.

RSK2-IN-20 is a potent, selective, and durable inhibitpr of RSK2 with IC50 of 47 nM.

RSV inhibitor compound 1 is a novel potent, orally bioavailable RSV fusion inhibitor with EC50 of 2 nM (RSV Long strain infected HEp-2 cells) without significant cytotoxicity (CC50>100 uM).

RSV604 R enantiomer is the R-enantiomer of RSV604, which is a potent respiratory syncytial virus (RSV) inhibitor targeting the nucleocapsid protein, is less active against RSV..

RSV604 racemate is a racemic mixture, shows less potency against strains of respiratory syncytial virus (RSV) than the S-isomer.

RSV-IN-1 is a human respiratory syncytical virus (hRSV) inhibitor, with an IC50 of 0.11 μM.

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