Pizuglanstat is a potent, selective prostaglandin D synthase inhibitor..

PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.

PKC-412 is a broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms (α, β, γ), PDFRβ, VEGFR2, Syk, PKCη, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR. Displays potent antitumor activity.

PKG drug G1 has been shown to induce the oxidative activation of protein kinase G Iα, which in vivo results in dilation of blood vessel and blood pressure lowering; an antihypertensive.

PKI-587 is a highly potent dual PI3K/mTOR kinase inhibitor with IC50 of 0.4 nM and <0.1 μM for PI3K-α and mTOR, respectively.

Bozitinib (PLB-1001) is a highly selective c-MET kinase inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) is a ATP-competitive small-molecule inhibitor, binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily[1].

Plecanatide acetate is a guanylate cyclase-C (GC-C) receptor agonist, binds and activates GC-C receptor, with an EC50 of 190 nM in T84 cells. Plecanatide acetate shows an-inflammatory activity in models of murine colitis.

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.

Plerixafor octahydrochloride(AMD3100 8HCL) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.

Plinabulin (NPI-2358) is a vascular disrupting agents (VDA) against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells.

PluriSln 1(NSC 14613) is an inhibitor of stearoyl-coA desaturase (SCD1), the key enzyme in oleic acid biosynthesis, revealing a unique role for lipid metabolism in hPSCs.

PLX3397 is a tyrosine kinase inhibitor that potently inhibits the colony stimulating factor 1 (CSF1) receptor kinase, a driving force in the development and growth of PVNS.

PLX4032 (Vemurafenib, RG7204, Zelboraf, RO5185426) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM.

PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.

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.

PLX5622 is a a potent, selective, orally active inhibitor of CSF1R tyrosine kinase (c-Fms) activity with Ki of 5.9 nM, 60-fold less potency against KIT.

PLX647 is a highly specific dual FMS/KIT kinase inhibitor with IC50 of 28/16 nM respectively.

PLX7904(PB04) is a potent and selective paradox-breaker RAF inhibitor.

PMX53 (Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg)) is a potent C5a receptor (CD88) antagonist with IC50 of 20 nM, also is an agonist for Mas-related gene 2 (MrgX2) in human mast cells; PMX-53 (10 nM) inhibited C5a-induced Ca(2+) mobilization in HMC-1 cells, but at higher concentrations (>30 nM) it caused degranulation in LAD2 mast cells, CD34(+) cell-derived mast cells, and RBL-2H3 cells stably expressing MrgX2; inhibits zymosan-, carrageenan-, LPS- and antigen-induced hypernociception in rats.

PND-1186 is a potent FAK inhibitor with IC50 of 1.5 nM.

Pneumocandin B0 is the major analogue of a family of lipopeptides isolated from several species of several different genera, notably Cryptosporiopsis, Glarea and Pezicula. Pneumocandin B0 is a potent antifungal and acts by inhibition of the synthesis of β

PNU-112455A is an ATP-competitive CDK2/5 inhibitor with Ki of 2 uM and 2 uM for cdk2·GST-cyclin E and cdk5·GST-p25 respectively, shows no activity against c-c-Met, IGR-1R, and ERK2..

PNU-120596 is a positive allosteric modulator of α7 nAChR with EC50 of 216 nM.

PNU-159682 is a major bioactive metabolite of Nemorubicin in human liver microsomes; > 3,000-fold cytotoxic than its parent compound(MMDX and doxorubicin).

Pocapavir is an investigational enterovirus (EV) capsid inhibitor.

Pogostemon (patchouli) leaves and their extracted oils are used in perfumes and in traditional medicine to relieve sunstroke, stop vomiting, and increase appetite.

Poloppin is a cell-active, small molecule inhibitor of protein-protein interaction via the Polo-box domain (PBD) of the mitotic Polo-like kinase (PLK) with IC50 of 26.9 uM (PLK1) in FP assays.

Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) inhibitor that targets the polo-box domain.

Polymyxin B is an antibiotic primarily used for resistant gram-negative infections.

Pomalidomide-PEG4-Ph-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 4-unit PEG linker used in PROTAC technology.

Ponesimod(ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM.

Porcupine-IN-1 is potent porcupine inhibitor with an IC50 of 0.5±0.2 nM.

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

Poseltinib (HM-71224, LY-3337641) is a potent and selective, covalent inhibitor of Btk with IC50 of 1.95 nM.

Potent and selective inhibitor of the TGF-β type I receptor/ALK5 (IC50 = 2.5 nM). Exhibits ~ 5000-fold selectivity over p38 MAPK. Suppresses development of renal fibrosis in a unilateral ureteral obstruction model. Also reduces proteinuria, glomeruloscler

Potent and selective non-peptide vasopressin V1A receptor antagonist; devoid of agonist activity. Displays high affinity and efficacy at both rat (KI=1.6 nM) and human (KI -1.1 - 6.3 nM) V1A receptors.

Potent inhibitor of protein kinase D (PKD); inhibits all PKD isoforms (IC50 values are 1, 2 and 2.5 nM for PKD1, PKD3 and PKD2 respectively).

Potent phosholipase D (PLD) inhibitor (IC50 values are 20 and 25 nM for PLD2 and PLD1 respectively).

Potent PKC inhibitor. Photosensitizing agent. Potent antileishmanial agent.

Potent, ATP-competitive inhibitor of Raf kinases (IC50 values are 29, 34 and 105 nM For c-Raf1, B-RafV600E and wild-type B-Raf, respectively). Displays selectivity For Raf kinases over a panel of 150 other kinases.

Potent, cell permeable inhibitor of CaM kinase II (IC50 = 0.37 μM).

Potent, cell permeable inhibitor of CaM kinase II (IC50 = 0.37 μM).

Potent, selective CB1 cannabinoid receptor antagonist/inverse agonist (Ki values are 12 and 4200 nM for CB1 and CB2 receptors respectively). Increases locomotor activity following systemic administration in vivo. Analog of SR141716A (Ki = 14 nM).

Poziotinib, is an orally bioavailable, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with potential antineoplastic activity.

PP1 is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.

PP2 analog is the analog of PP2,a Src family kinase inhibitor.

PP2 is Src family kinase inhibitor, potently inhibits Lck/Fyn with IC50 of 4 nM/5 nM, ~100-fold less potent to EGFR, inactive for ZAP-70, JAK2 and PKA.

PP242 is a selective mTOR inhibitor with IC50 of 8 nM; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively; also showed slightly weaker activity against BRD4 (Kd= 1.7 uM).

PPQ-102 is a potent CFTR inhibitor which can completely inhibited CFTR chloride current with IC 50approximately 90 nM.

PQ 401 is an IGF-1R inhibitor with IC50 of <1 μM.

PQR530 is a selective, orally bioavailable, potent dual PI3K/mTORC1/2 inhibitor.

PQR620 is a novel potent and selective brain penetrant inhibitor of mTORC1/2.

PR-619 is a broad-range DUB inhibitor with potential for further development as a chemotherapeutic agent in cancer therapy.

Pracinostat(SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6; has no activity against the class III isoenzyme SIRT I.

Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.

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

Praliciguat (IW-1973, IW1973) is a potent, orally available sGC stimulator that concentration-dependently increases the production of cGMP with EC50 of 267 nM.

Pramlintide is an analogue of amylin, a small peptide hormone that is released into the bloodstream by the β cells of the pancreas along with insulin after a meal.

Pravadoline is a cannabimimetic aminoalkylindole agonist of the cannabinoid receptors and an inhibitor of Cox-1 and Cox-2, demonstrating powerful analgesic effects through the combination of these actions.

PRE-084 hydrochloride is a high affinity, selective σ1 agonist (Ki values are 2.2 and 13091 nM for σ1 and σ2 receptors respectively).

Pregabalin

Preladenant(SCH 420814) is a potent and selective antagonist at the adenosine A2A receptor.

Presatovir (GS-5806) is a novel, orally bioavailable RSV fusion inhibitor with mean EC50 of 0.43 nM against a panel of 75 RSV A and B clinical isolates.

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.

PRIMA-1MET is methylated derivative of PRIMA-1. It can restore mutant p53 activity.

PRL-8-53|cas 51352-88-6

PRMT1 inhibitor

PRN1008 is a novel reversible, covalent and oral inhibitor of BTK with biochemical IC50 of 1.3 nM..

PRN1371 is an irreversible covalent FGFR1-4 kinase inhibitor, with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, 2, 3, 4 and CSF1R, respectively.

PrNMI is a peripherally restricted cannabinoid 1 receptor (CB1R) agonist, significantly alleviates spontaneous pain behaviors in the animals.

Prodigiosin is a natural red pigment produced by numerous bacterial species, has exhibited promising anticancer activity.

Proguanil is an antimalarial prodrug that is metabolized to the active metabolite cycloguanil, a dihydrofolate reductase (DHFR) inhibitor.

Proneurogenic, neuroprotective compound. Protects newborn neurons in the dentate gyrus and stimulates the growth of new neurons. Also enhances learning and memory in aged rats. Orally available and brain penetrant.

Prostaglandin E2 is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation.

PROTAC-VHL-ligand is a von Hippel–Lindau (VHL) ligand used for the proteolysis targeting chimeras (PROTACs) method, induces target protein degradation..

Protirelin is a tripeptide that stimulates the release of thyrotropin and prolactin.

Protodioscin has been shown to exhibit multiple biological actions, such as anti-hyperlipidemia, anti-cancer, sexual effects and cardiovascular properties.

PRT-060318 is a novel Syk inhibitor, prevents heparin-induced thrombocytopenia and thrombosis in a transgenic mouse model.

PRT4165 is a potent inhibitor of PRC1 (Polycomb-repressive complex 1)-mediated H2A ubiquitylation.

Prucalopride is a selective, high affinity 5-HT receptor agonistfor 5-HT4a and 5-HT4b with Ki of 2.5 nM and 8 nM, respectively.

PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.

PS 210 is a potent, specific activator of PDK1 that target the PIF-binding pocket of PDK1, does not alter the activity of any of the 121 kinases (S6K, PKB/Akt or GSK3)..

PS-1145 has been shown to be an IKK (IKB kinase) inhibitor.

PS48 is a PDK1 (phosphoinositide-dependent protein kinase 1) activator which binds to the HM/PIF binding pocket rather than the ATP-binding site.

PSI-6130(R 1656) is a Hepatitis C Virus Nucleoside Inhibitor. PSI-6130(R 1656) is useful for Antiviral agents.

PSI-6206 is a selective inhibitor of hepatitis C virus (HCV).

PSI-7977 is an investigational nucleotide analog currently in Phase 2 for treatment of chronic HCV infection.

PSMA-617 is a high potent prostate-specific membrane antigen (PSMA) inhibitor, with a Ki of 0.37 nM.

Psora-4 is a potent and selective Kv1.3 potassium channel blocker with EC50 of 3 nM.

Psoralidin possesses potent antidepressant-like, anti-inflammatory, anticancer and chemopreventive properties. Psoralidin is a dual inhibitor of COX-2 and 5-LOX

PT2385 is an orally active, small molecule inhibitor of hypoxia inducible factor (HIF)-2alpha, with potential antineoplastic activity.

PT2399(PT=2399) is a novel HIF2α Antagonist.

PTACH (NCH-51) is a SAHA-based novel inhibitor of human HDAC. PTACH exerts potent growth inhibition against various human cancer cells, with EC50 values ranging from 1 to 10 μM.

PTC-028 is an orally bioavailable compound that decreases BMI-1 levels by posttranslational modification

PTC124 (Ataluren) is a potent nonsense mutation inhibitor with EC50 of ~0.1 μM.

PTC-209 is a specific inhibitor for BMI-1 with IC50 of 0.5 uM in in both GEMS reporter and ELISA assays.

PTC-209 is a specific inhibitor for BMI-1 with IC50 of 0.5 uM in in both GEMS reporter and ELISA assays.

PTC299 (PTC-299) is a novel potent inhibitor of dihydroorotate dehydrogenase (DHODH), inhibits hypoxia-induced VEGFA protein production in HeLa cells with IC50 of 1.64 nM.

PTP1B-IN-2 is a novel protein tyrosine phosphatase-1B (PTP1B) inhibitor.

PTZ-343 is a phenothiazine derivative with chemical name: sodium 3-(10H-phenothiazin-10-yl)propane-1-sulfonate.

Purfalcamine is a potent, specific inhibitor of Plaasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) with IC50 of 17 nM.

Purmorphamine, which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM and also is an inducer of osteoblast differentiation with EC50 of 1 μM.

Puromycin Aminonucleoside (3'-Amino-3'-deoxy-N6,N6-dimethyladenosine) is the aminonucleoside portion of the antibiotic puromycin.

Puromycin is an aminoglycoside antibiotic isolated from the bacterium Streptomyces alboniger. It is a protein synthesis inhibitor.

Purvalanol A is a potent, cell-permeable cyclin-dependent protein kinase (cdk) inhibitor.

Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitor with IC50 values of 6, 6, 9, > 10,000, and 6 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively.

PWT143 (ME-401), is an orally bioavailable inhibitor of the delta isoform of phosphatidylinositide 3-kinase (PI3K), with potential antineoplastic activity.

PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1(Trx-1) currently in clinical development as an antitumor agent; IC50=7 uM in Hela, MTT assay, 72 h.

PX-478 is an inhibitor of HIF-1a with an IC50 of 20-30μM enhances radiosensitivity of prostate carcinoma cells.

PYR-41 is a specific and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 uM, with no or little activity at E2.

Pyridoclax(MR-29072) is a potent Mcl-1 inhibitor with Kd value of 25 nM.

Pyridostatin stabilizes G-quadruplexes, targeting the proto-oncogene SRC and telomeric G-quadruplexes, inducing DNA damage and cell-cycle arrest.

Pyridoxal isonicotinoyl hydrazine is a lipophilic, nontoxic, iron-chelating agent that shows high iron chelation efficacy both in vitro in cell culture models and in vivo in rats and mice.

Pyridoxine hydrochloride (Pyridoxol; Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.

Pyronaridine tetraphosphate is a Mannich base anti-malarial with demonstrated efficacy against drug resistant Plasmodium falciparum, P. vivax, P. ovale and P. malariae.

Pyronaridine, also known as Malaridine, is an antimalarial drug.

Pyrotinib maleate (SHR-1258 maleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50 of 13/38 nM, respectively.

Pyrroloquinoline quinone (PQQ) is used as a cofactor (prosthetic group) for enzyme-catalyzed redox reactions of glucose and methanol dehydrogenase(s).

PZ09 (PKC-zeta inhibitor 9, PKC-ζ inhibitor PZ9) is a potent, isoform selective PKC-zeta (PKC-ζ) inhibitor with IC50 of 5.18 nM, displays excellent selectivity (>200-fold) over other PKC isoforms with exception of PKC-i (10-fold). PZ09 also shows high selectivity for CDK-2 (>200-fold), as well as a broader range of other kinases (<50% inhibition at 10 uM). PZ09 is a small-molecule inhibitor, the first tool to successfully interrogate aPKC signaling in cells.

PZ-2891 is a specific, allosteric, BBB-permeable, orally active Pantothenate kinase (PANK) modulator, acting as both an orthosteric inhibitor (IC50=1.3 nM, hPANK3) and an allosteric activator of PANK3 activity in the presence of acetyl-CoA in biochemical

PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.

QC-3611 is a selective inhibitor of JARID1A/1B, which is a target existing in various tumors (JARID1A IC50 = 13 nM ;JARID1B IC50 = 2 nM). QC-3611 is promisingly to be used as an antineoplastic drug.

QCC-374 is prostanoid agonist potentially for the treatment of pulmonary arterial hypertension.

QcrB inhibitor TB47 (TB47) is a novel antimycobacterial agent that fuctions as a putative respiratory complex III (QcrB) inhibitor with MIC of 0.016-0.5 ug/mL against a panel of 56 M. tuberculosis clinical isolates.

QNZ is a NR2C/NR2D-selective NMDA receptor non-competitive antagonist (IC50 values are 3, 6, 229, and >300, >300 μM for NR2D, NR2C, NR2A, NR2B, and GluR1, respectively).

QStatin is a novel, potent, and selective Vibrio quorum sensing (QS) inhibitor, shows pan-QS inhibitor activity in diverse Vibrio species.

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

Questiomycin A is a phenoxazine and a chromophore that has been found in Streptomyces and has antibacterial and anticancer activities.

Quetiapine fumarate is an atypical antipsychotic used in the treatment of schizophrenia, bipolar I mania, bipolar II depression, bipolar I depression.

Quillaic acid(Quillaja sapogenin) is the major aglycone of the widely studied saponins of the Chilean indigenous tree Quillaja saponaria Mol; can elicit dose-dependent antinociceptive effects in two murine thermal models.

Quinupristin/dalfopristin, or quinupristin-dalfopristin is a combination of two antibiotics used to treat infections by staphylococci and by vancomycin-resistant Enterococcus faecium.

Quisinostat (JNJ-26481585) 2HCl is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, modest potent to HDACs 2, 4, 10, and 11.

Quizartinib (AC220) is a potent, selective, second-generation FLT3 inhibitor with Kd of 1.6 nM, inhibits Wt FLT3 and FLT3-ITD autophosphorylation in MV4-11cell with IC50 of 4.2 and 1.1 nM, respectively.

Quizartinib (AC220) is a second-generation FLT3 inhibitor for Flt3(ITD/WT) with IC50 of 1.1 nM/4.2 nM, 10-fold more selective for Flt3 than KIT, PDGFRα, PDGFRβ, RET, and CSF-1R. Phase 1/2.

Q-VD-Oph is a potent pan-caspase inhibitor with IC50 ranged from 25 to 400 nM for caspases 1,3,8, and 9.

QX77 is a chaperone-mediated autophagy (CMA) activator.

R112 is an ATP-competitive inhibitor of Syk kinase with a Ki of 96 nM. R112 inhibits Syk kinase activity with an IC50 of 226 nM.

R121919 is a potent small-molecule CRF1 receptor antagonist with a Ki of 2 to 5 nM for the CRF1 receptor and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types.

R1487 is a p38 MAP kinase inhibitor with an IC50 of 10nM. It may have potential as a treatment for inflammatory diseases such as rheumatoid arthritis.

R1487 is a p38 MAP kinase inhibitor with an IC50 of 10nM. It may have potential as a treatment for inflammatory diseases such as rheumatoid arthritis.

R1530 is the multikinase inhibitor with potential antiangiogenesis and antineoplastic activities.

R162 is an inhibitor of GDH activity and represses glioma cell growth.

R243 is a potent, small molecule CCR8 antagonist that inhibits CCR8 signaling and chemotaxis, inhibits CCL1-induced Ca2+ flux and CCL1-driven peritoneal macrophages aggregation at 0.2 uM.

R306465, also known as JNJ-16241199, is a novel hydroxamate-based histone deacetylase (HDAC) inhibitor with broad-spectrum antitumour activity against solid and haematological malignancies in preclinical models.

R406 is a potent Syk inhibitor with IC50 of 41 nM and also potently inhibits Flt3.

R406 is a potent Syk inhibitor with IC50 of 41 nM and also potently inhibits Flt3.

R428 is a potent and selective small-molecule inhibitor(IC50=14 nM), blocks the activities of Axl.

R-7050 is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.

R-7128(Mericitabine) is a selective nucleoside analog inhibitor of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, with activity across all HCV genotypes.

R788 (Fostamatinib), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM.

R935788 (Fostamatinib disodium, R788) is a Syk inhibitor with IC50 of 41 nM.

Rac BHFF is a potent and selective GABAB receptor positive allosteric modulator that increases the efficacy and potency of GABA ( > 149% and > 15-fold respectively). Orally active and exhibits anxiolytic activity in vivo.

Racecadotril (acetorphan), a potent enkephalinase inhibitor (IC50= 4.5 uM), protects endogenous enkephalins from degradation.

RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM).

RAD51-IN-17 is a quinazolinone derivative that inhibts homologous recombinase RAD51, effectively inhibits both RAD51 foci formation in response to DNA damage, and proliferation of TNBC cell lines.

Radafaxine Hcl(BW-306U; GW-353162A) is a potent metabolite of bupropion; selective for inhibiting the reuptake of norepinephrine over dopamine; DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulat

Radezolid (RX-1741) is a novel oxazolidinone antibiotic agent.

Radiprodil is an orally active and selective NMDA NR2B antagonist; a potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions.

Radotinib(IY-5511) is a novel and selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM for wild-type BCR-ABL1 kinase.

RAF265 (CHIR-265) is a highly selective B-Raf and VEGFR2 inhibitor with IC50 of 3-60 nM and EC50 of 30 nM, including B-Raf, C-Raf and mutant B-Raf.

RAF709 is a novel Raf kinase inhibitor extracted from patent WO2014151616A1, compound example 131, has an IC50 of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.

Ralinepag is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist, with EC50s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively.

Raltegravir Salt is a potent human immunodeficiency virus (HIV) integrase inhibitor and a novel anti-AIDS drug.

Raltitrexed(ZD1694), an inhibitor of thymidylate synthase, is an antimetabolite drug used in cancer chemotherapy.

Ramosetron Hydrochloride(YM060 Hydrochloride) is a serotonin 5-HT3 receptor antagonist for the treatment of nausea and vomiting.

Ranolazine (Ranexa)

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).

RapaLink-1 is a third-generation mTOR inhibitor that overcomes resistance to existing first- and second-generation inhibitors; blocks mTOR signaling of the F2108L mTOR and M2327I mTOR drug resistant mutants; RapaLink-1 is more potent mTOR inhibitor than rapamycin.

Rapamycin (Sirolimus, AY-22989, WY-090217) is a specific mTOR inhibitor with IC50 of ~0.1 nM. -

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

Raphin1 is an orally available selective phosphatase inhibitor improves proteostasis and diminishes deficits in a mouse model of Huntington’s disease.

RAS activator compound 1 is a small molecule RAS activator compound that increases the rate of SOS-catalyzed nucleotide exchange in vitro with EC50 of 14 uM; targets SOS1 induced biphasic modulation of RAS-GTP and ERK phosphorylation levels, through negative feedback on SOS1 that regulates the interaction between SOS1 and GRB2.

RasGRP3 ligand 96 is a potent, selective ligand of Ras guanine-releasing protein 3 (RasGRP3) with Ki of 1.75 nM, showed 73-fold and 45-fold selectivity relative to PKCα and PKCε for in vitro binding activity resepctively.

Ravidasvir (PPI-668;BI 238630) is a potent pan-genotypic HCV NS5A inhibitor with IC50 of 0.12/0.01/1.14 nM for HCV gt-1a/1b/3a in replicon luciferase assay;

Ravidasvir(PPI-668) is a NS5A Inhibitor.

Razuprotafib is a potent protein tyrosine phosphatase β (HPTPβ) inhibitor..

RBC8 is a novel small molecule inhibitor of Ral GTPase; has IC50 of 3.5 μM in H2122 cell and 3.4 μM in H358 cell.

Rbin-1 is a potent, reversible, and specific chemical inhibitor of eukaryotic ribosome biogenesis. Rbin-1 inhibits the ATPase with GI50 of 136±7 nM.

RCGD423 is a gp130 modulator, which prevents articular cartilage degeneration and promotes repair.

RD162 is a second-generation, orally available antiandrogen that binds to androgen receptor (AR) with IC50 of 30.9 nM.

ReACp53 is a cell-penetrating peptide,designed to inhibit p53 amyloid formation.

Rebaudioside C(Dulcoside B) is used as natural sweeteners to diabetics and others on carbohydrate-controlled diets.

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.

Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.

Regorafenib (BAY 73-4506, Fluoro-Sorafenib) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.

Regorafenib hydrochloride (BAY73-4506) is a potent, orally active multikinase inhibitor that potently inhibits endothelial cell kinases in biochemical and cellular kinase phosphorylation assays with nanomolar range (IC50=3-200 nM).

Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases [ESBLs] and KPC) and class C (AmpC) enzymes.

Relugolix is a novel, non-peptide, orally active gonadotropin-releasing hormone (GnRH) antagonist with IC50 of 0.33 nM in the presence of 40% fetal bovine serum, TAK-385 possesses higher affinity and potent antagonistic activity compared with TAK-013.

Remodelin is an inhibitor of acetyl-transferase NAT10.

Remodelin is an inhibitor of acetyl-transferase NAT10.

Reparixin(DF 1681Y) is an inhibitor of CXCL8 receptor, also inhibit CXCR1 and CXCR2 activation, which has been shown to attenuate inflammatory responses in various injury models.

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.