OSI-906 (Linsitinib) is a selective inhibitor of IGF-1R and IR with IC50 of 35 nM and 75 nM, respectively.

OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl.

Otenabant (CP945598) is a recently discovered selective, high affinity, competitive CB1 receptor antagonist with Ki of 0.7 nM.

OTSSP167 is a highly potent MELK inhibitor (IC50 = 0.41 nM) and inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like).

PAK4-IN-1 is an inhibitor of p21-activated kinases (PAKs), with IC50 of ≤100 nM in MTT assay.

Palosuran (ACT-058362) is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM.

Pamapimod（R-1503）is a novel p38 MAP kinase inhibitor.

Parimifasor is an immunomodulator, with anti-inflammatory activity.

Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR-α/β, and c-Kit.

PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist (IC50 = 16 nM).

PF-06840003 is an orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1),with potential immunomodulating and antineoplastic activities.

PIM447 is novel pan-PIM kinase inhibitor, including Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase.

Pimodivir(VX-787) is a novel inhibitor of influenza virus replication that blocks the PB2 cap-snatching activity of the influenza viral polymerase complex. 

Pleconarilis is a picornavirus replication inhibitor.

Plerixafor is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.

PLX51107 is a novel BET inhibitor with a unique binding mode in the acetylated lysine binding pocket of BRD4 that differentiates it from other compounds under investigation.

Posaconazole (Noxafil) is a sterol C14ɑ demethylase inhibitor with an IC50 of 0.25 nM.

Pralatrexate(Folotyn) is an antifolate, and structurally a folate analog.

PRIMA-1 is a mutant p53 reactivator, restores the sensitivity of TP53 mutant-type thyroid cancer cells to the histone methylation inhibitor 3-Deazaneplanocin A.

Quarfloxin (CX-3543) is a fluoroquinolone derivative with antineoplastic activity.

Ranolazine(RS-43285) is an antianginal agent with antiarrhythmic properties that achieves its effects via a novel mechanism of action (inhibition of the late phase of the inward sodium current), without affecting heart rate or blood pressure (BP).

Rapastinel(GLYX-13) is a NMDA receptor partial agonist that acts at the glycine site.

Refametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.

Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM.

Ro 48-8071 fumarate is an inhibitor of OSC(Oxidosqualene cyclase; IC50=6.5 nM) that has low-density lipoprotein (LDL) cholesterol lowering activity.

RO4929097 is a γ secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively.

RO5028442 is a highly potent and selective Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a).

Roscovitine (Seliciclib, CYC202, R-roscovitine) is a potent and selective CDK inhibitor for Cdc2/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p53 with IC50 of 0.65 μM, 0.7 μM, 0.7 μM and 0.16 μM, respectively.

Rostafuroxin: an ouabain-inhibitor counteracting specific forms of hypertension.

RRx-001 is a novel epigenetic modulator with potential radiosensitizing activity. It inhibits glucose 6-phosphate dehydrogenase(G6PD) in human tumor cells, binds hemoglobin and drives RBC-mediated redox reactions under hypoxia.