Nepicastat hydrochloride is a potent and selective inhibitor of both bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors.

Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor with IC50 of 59 nM and 92 nM for HER2 and EGFR, respectively.

Netazepide (YF476, Sograzepide) is a potent, selective and orally active gastrin/CCK-2 antagonist with IC50 of 0.1 nM.

Nevirapine is a potent, non-nucleoside reverse transcriptase inhibitor (NNRTI) used in combination with nucleoside analogues for treatment of HIV-1 infection and AIDS.

Nicainoprolhe is an antiarrhythmic agent,a fast-sodiumchannel blocking drug (class Ib), also protected isolated rat hearts against reperfusion arrhythmias.

Nicardipine Hcl(YC-93) is a calcium channel blocker that has been widely used to control blood pressure in severe hypertension following events such as ischemic stroke, traumatic brain injury, and intracerebral hemorrhage.

Nilotinib (AMN-107, Tasigna) is a Bcr-Abl inhibitor with IC50 less than 30 nM.

Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM.

Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM.

Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM.

NITD 609 is a novel and potent drug candidate for the treatment of uncomplicated malaria

NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo.

NLG-8189 is an inhibitor of IDO and INDOL1 (IDO2)

NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor with excellent ADME and pharmacokinetic profiles and high efficacy in vivo.

non-nucleoside inhibitor of the NS5B

Novel psychopharmacologic agent. Displays antagonist activity at 5-HT, dopamine, noradrenalin and histamine receptor subtypes (pKi values are 8.60, 8.40, 10.15, 9.75, 10.46, 8.84, 9.60, 9.94, 8.85, 8.90, 8.84, 9.38, 8.95, 8.93, 8.9, 9.49, 8.91, 9.00 and 8

NPS 2143 hydrochloride is a selective CaSR (Ca2+-sensing receptor) inhibitor and antagonist, shown to block increases in cytoplasmic Ca2+ concentrations elicited by human Ca2+ receptors expressed in HEK293 cells with an IC50 of 43 nM. NPS 2143 hydrochlori

NPS-2143(SB 262470A ) is a selective potent calcium ion-sensing receptor antagonist with IC50 of 43 and 41 nM for cytoplasmic Ca2+ concentrations and parathyroid hormone secretion, respectively.

NS3/4A protease inhibitor

Nucleozin targets influenza A nucleoprotein (NP), a multifunctional, RNA-binding protein necessary for virus replication.

NVP-AEW541 is a potent inhibitor of IGF-1R with IC50 of 86 nM.

NVP-BEP800 is a novel, fully synthetic HSP90β inhibitor with IC50 of 58 nM.

NVP-BGT226 is a novel dual PI3K/mTOR inhibitor with IC50 of 1 nM.

NVP-TAE684(TAE684) is a highly potent and selective small-molecule ALK inhibitor, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM.

NXY-059 (Cerovive) is an EGFR and HER2 autophosphorylation inhibitor, against purified EGFR and HER2 of 10.2 and 9.8 nM, respectively.

O304 is a novel AMPK activator.

Obicetrapib is a CETP inhibitor, on the elevation of high-density lipoprotein cholesterol (HDL-C) and reduction of low-density lipoprotein cholesterol (LDL-C), alone and in combination with statin therapy.

Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.

Odanacatib (MK 0822) is a potent, selective, and neutral inhibitor of human and rabbit cathepsin K with IC50 of 0.2 nM and 1 nM , respectively.

ODM-201 is a potent and full antagonists for human AR (hAR) with IC50 values of 26 nM by transactivation assays in AR-HEK293 cells.

Oglemilast(GRC3886) is a potent PDE4 inhibitor, under clinical studies in the treatment of allergen-induced asthma.

Olacaftor (VX-440, VX440) is a next-generation CFTR corrector, showsthe potential to enhance the amount of CFTR protein at the cell’s surface and for treatment of cystic fibrosis..

Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1 and PARP2 with IC50 of 5 nM and 1 nM, respectively.

Olmesartan Acid is an angiotensin II receptor antagonist that prevents the binding of angiotensin II, thus preventing vasoconstriction.

Olmesartan medoxomil(Olmetec; Benicar; CS 866) is an angiotensin II receptor antagonist which is used as an anti-hypertensive.

Olodaterol (BI1744) is a long acting β2-adrenoceptor agonist with an EC50 of 1.4±0.08 nM.

Olodaterol is a novel, long-acting beta2-adrenergic agonist (LABA) that exerts its pharmacological effect by binding and activating beta2-adrenergic receptors located primarily in the lungs.

Oltipraz is a potent Nrf2 activator and a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST). Phase 3.

Olumacostat glasaretil is a small molecule inhibitor of acetyl coenzyme A carboxylase (ACC).

Olutasidenib is a highly potent, selective inhibitor of mutant Isocitrate dehydrogenase (IDH)1 that could be used in the treatment of acute myeloid leukemia.

Omapatrilat is a dual inhibitor of the metalloproteases ACE and NEP with Ki values of 0.64 and 0.45 nM, respectively.

Ombrabulin (AVE8062) hydrochloride is a synthetic derivative of CA-4-P, which inhibits growth in a large number of drug-resistant animal tumors and carcinogen-induced tumors.

Ombrabulin (AVE8062) hydrochloride is a synthetic derivative of CA-4-P, which inhibits growth in a large number of drug-resistant animal tumors and carcinogen-induced tumors.

Omidenepag Isopropyl (DE-117, OMDI) is the prodrug of Omidenepag, which is a potent, selective agonist human EP2 receptor; demonstrates excellent IOP-lowering activities following ocular administration in ocular normotensive monkeys, Omidenepag Isopropyl (OMDI) is a clinical candidate for the treatment of glaucoma.

ONO-4059 is a highly selective, orally bioavailable BTK inhibitor with a potency (IC50) of 2.2 nM.

ONO-4059 is a novel Small Molecule Dual Inhibitor Of Bruton’s Tyrosine Kinase (Btk) and Tec Kinase.

Opiranserin (VVZ-149, VVZ-000149) is a potent, selective, mixed glycine GlyT2 transporter blocker (IC50= 0.86 uM), purine P2X3 receptor antagonist (IC50=0.87 uM) and serotonin 5-HT2A receptor antagonist (IC50=1.3 uM).

Oprozomib (ONX 0912) selectively inhibits CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.

Org 26576 is a AMPA receptor positive allosteric modulator.

ORIC-101 (ORIC101) is a highly potent, selective steroidal glucocorticoid receptor (GR) antagonist (IC50=5.6 nM) with reduced androgen receptor (AR) agonistic activity.

Oseltamivir acid (GS 4071, Ro 64-0802, Oseltamivir carboxylate) is a potent inhibitor of influenza neuraminidase (NA) with Ki of <1 nM for both A and B strains,showed potent activity against COVID-19(SARS-COV-2).

OSELTAMIVIR is an active (orally) inhibitor of the influenze virus neuraminidase and converted to the active acid metabolite in vivo.

OSI-027 is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, respectively.

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.

Ostarine(MK-2866; GTX-024)A modulator to human androgen receptor.

OSU-03012(AR-12) is a potent inhibitor of recombinant PDK-1 with IC50 of 5 μM and 2-fold increase in potency over OSU-02067.

Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.

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).

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).

Oxaliplatin is a second generation potent platinum-based anti-neoplastic agent that is believed to form inter- and intrastrand DNA adducts which activate signaling pathways culminating in apoptosis. The development of Oxaliplatin was inspired from the eff

Ozanimod (RPC1063) is a selective S1P1R modulator

PAC-14028 is a potent and selective transient receptor potential vanilloid type I (TRPV1) antagonist.

Padsevonil (UCB-0942, UCB0942) is a potential anti-seizure agent that functions as a pre- and post-synaptic inhibitor..

Pagoclone is an active (+)-enantiomer of the racemate RP 59037. Pagoclone is a partial GABA(A) receptor agonist used for the treatment of panic and anxiety disorders.

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

Palbociclib (PD-0332991) is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity.

Palbociclib is an oral, small molecule cyclin-dependent kinase 4/6 (CDK4/6) inhibitor, now in Phase 3 clinical development for advanced breast cancer.

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.

Panobinostat(LBH-589) is a broad-spectrum HDAC inhibitor; low nanomolar concentrations (IC50=5-20 nM) of LBH589 induced cell-cycle arrest, apoptosis, and histone (H3K9 and H4K8) hyperacetylation in MOLT-4 and Reh cell.

Pantoprazole is a proton pump inhibitor used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease.

Pantoprazole sodium salt(SKF96022; Protonix) is a proton pump inhibitor drug used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease.

Parecoxib is a selective COX2 inhibitor.

PARECOXIB SODIUM

Paricalcitol

Parimifasor is an immunomodulator, with anti-inflammatory activity.

Paroxetine hydrochloride hemihydrate is a antidepressant agents known as selective serotonin-reuptake inhibitors (SSRIs).

Pazopanib Hcl (GW-786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively.

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

PBI-4050 (Setogepram, PBI4050) is a synthetic analog of a medium-chain fatty acid that displays agonist and antagonist ligand affinity toward GPR40 and GPR84, respectively.

PBI-4050 (Setogepram, PBI4050) is a synthetic analog of a medium-chain fatty acid that displays agonist and antagonist ligand affinity toward GPR40 and GPR84, respectively.

PBTZ169 is a decaprenyl-phosphoribose-epimerase (DprE1) inhibitor.

PC786 (PC-786) is a potent non-nucleoside RSV L-protein polymerase inhibitor with IC50 of 2.1 nM and 0.5 nM in cell-free enzyme assay and mini-genome assay in HEp-2 cells, respectively.

PCI-32765 (Ibrutinib) is a potent and highly selective Btk inhibitor with IC50 of 0.5 nM.

PCO371 is a novel, orally active small molecule that acts as a full agonist of PTHR1.

PD 123319 is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.

PD0325901 (PD325901) is selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM.

Peficitinib(ASP015K,JNJ-54781532) is a novel potent JAK inhibitor, which demonstrated potent efficacy in adjuvant-induced arthritis model in rats.

Pelitinib (EKB-569; WAY-EKB 569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM.

Pemafibrate is an orally bioavailable and selective agonist of peroxisome proliferator-activated receptor α (PPARα; EC50 = 1 nM for transcriptional activity), a transcription factor that is essential for regulation of lipid homeostasis.

Pemetrexed disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively.

Peramivir

Peramivir, also known as BCX1812 and RWJ 270201, is an antiviral drug for the treatment of influenza. Peramivir is a neuraminidase inhibitor, acting as a transition-state analogue inhibitor of influenza neuraminidase and thereby preventing new viruses from emerging from infected cells. Peramivir was approved to treat influenza infection in adults.

Perampanel(E2007; ER 155055-90) is a selective noncompetitive AMPA-type glutamate receptor antagonist which has demonstrated anticonvulsant activity in experimental seizure models and antiepileptic activity in clinical trials.

Perifosine (KRX-0401) is a novel Akt inhibitor with IC50 of 4.7 μM.

PF 05089771 is a Nav1.7 channel blocker extracted from patent WO/2010/079443 A1, compound example 788, has an IC50 of 8.6 nM.

PF 477736 is a CHK inhitor with Ki values of 0.49 and 47 nM for Chk1 and Chk2 respectively. A proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity

PF-00446687 hydrochloride (PF-446687) is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 nM.

PF-00446687(PF-446687) is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 nM.

PF-00562271 is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively.

PF-03758309 is an orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity.

PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM, susceptible to oncogenic mutations (no activity to Y1230C mutant).

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

PF-04447943 is a brain-permeable phosphodiesterase (PDE) inhibitor that is selective for PDE9A (IC50 = 12 nM) over other PDEs (IC50s = >940 nM) in enzymatic assays of second messenger hydrolysis.

PF-04449913 is a potent and orally bioavailable inhibitor of smoothened with IC50 of 5 nM(Gli-luciferase reporter reporter in C3H10T1/2); the hedgehog pathway inhibitor

PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.

PF-04971729 is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2, is currently in phase 2 trials for the treatment of diabetes mellitus.

PF-04995274 is a 5-HT4 receptor partial agonist. It thought to act centrally as a pro-cognitive agent that being developed for the treatment of Alzheimer's disease (AD).

PF-05175157 is a potent and selective inhibitor of both acetyl-CoA carboxylase isoform ACC1 located primarily in liver and adipose tissue and isoform ACC2 dominant in skeletal and heart muscle, with IC50 values of 27 nM and 33 nM, respectively.

PF-05180999 (PF 5180999) is a potent, selective, brain-penetrating and orally bioavailable phosphodiesterase 2A (PDE2A) inhibitor with IC50 of 1 nM.

PF-06263276 (PF06263276, PF 6263276) is a potent, selective pan JAK inhibitor with IC50 of 2.2, 23.1, 59.9 and 29.7 nM for JAK1, JAK2, JAK3, and TYK2, respectively.

PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively.

PF-06282999 is a potent and selective myeloperoxidase inhibitor which is potential useful for the treatment of cardiovascular diseases.

PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC50 of 7 nM.

PF-06459988 (PF06459988, PF 6459988) is a potent, selective, irreversible EGFR mutants with IC50 of 13, 7, 21 and 90 nM for EGFR L858R-T790M, Del-T790M, L858R, and EGFR Del, respectively.

PF06463922 is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.

PF-06651600 is a potent JAK3-selective inhibitor with an IC50 of 33.1 nM.

PF-06700841 is an inhibitor of JAK1 and TYK2 kinases. PF-06700841 has been investigated for the treatment of psoriasis and lupus.

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

PF-2341066 (Crizotinib) is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nnM, respectivley.

PF-2545920 a highly selective and potent PDE10A inhibitor with an IC50 of 0.37 nM.

PF299804 is a potent, irreversible pan-ErbB inhibitor against ErbB1, ErbB2 and ErbB4 with IC50 of 6 nM, 45.7 nM and 73.7 nM, respectively.

PF-3274167 is a high-affinity nonpeptide oxytocin receptor (OTR) antagonist, with Ki of 9.5 nM.

PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively.

PFK-158 is a potent and selective inhibitor of PFKFB3 that is currently being investigated in a phase I study in patients with advanced solid malignancies.

PI3K-IN-2 is a PI3K inhibitor, inhibits pPKB and pS6 with "++++/+++(+)" in A2058 melanoma cell.

Pibrentasvir is a novel and pan-genotypic hepatitis C virus (HCV) NS5A inhibitor with EC50s ranging from 1.4 to 5.0 pM against HCV replicons containing NS5A from genotypes 1 to 6.

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. 

Pirmenol hydrochloride inhibits IK.ACh by blocking muscarinic receptors. The IC50 of Pirmenol for inhibition of Carbachol-induced IK.ACh is 0.1 μM.

Pitolisant Hcl(BF2.649;Ciproxidine ) is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM).

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.

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.

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.

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.

Polmacoxib is an inhibitor of cyclooxygenase 2 (COX-2) and the carbonic anhydrase subtypes I (CAI) and CAII.

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

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

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.

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

Pramipexole is a dopamine agonist of the non-ergoline class indicated for treating Parkinson's disease (PD) and restless legs syndrome (RLS).

Pramipexole is a partial/full D2S, D2L, D3, D4, receptor agonist with a Ki of 3.9, 2.2, 0.5, 5.1 nM.

Pramiracetam

Pregabalin

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.

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.

Protective effects of a squalene synthase inhibitor, lapaquistat acetate (TAK-475), on statin-induced myotoxicity in guinea pigs.

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

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

Pyrimethamine is a potent inhibitor of multi-drug and toxin extrusion transporters. This compound inhibits Mdr-1(Pgp) and thus allows for active drugs to stay within the cell for longer periods of time, increasing their effectiveness by preventing efflux

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

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.

R15A inhibitor.

R547 is a potent and selective CDK inhibitor with Ki and IC50 of 1-3 nM and 80 nM respectively.

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.

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

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.

Rafoxanide is a salicylanilide used as an antiparasitic agent.

Raltegravir potassium salt(MK0518 potassium salt) is a potent integrase (IN) inhibitor, used to treat HIV infection.

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.

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).

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.

Ravidasvir(PPI-668) is a NS5A Inhibitor.

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.

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.

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)

Resminostat(RAS2410; 4SC-201) is a potent inhibitor of HDAC1/3/6(IC50=43-72 nM); less potent to HDAC8 with IC50 of 877 nM.

Retapamulin is a topical antibiotic, which binds to both E. coli and S. aureus ribosomes with similar potencies with Kd of 3 nM.

RG7800 a small molecule SMN2 splicing modifier to enter human clinical trials to treat spinal muscular atrophy.

Rho-kinase (ROCK) inhibitor

Ribavirin is a guanosine analog with antiviral properties against DNA and RNA viruses, including respiratory syncytial virus, hepatitis C, and influenza.

Rifabutin (Mycobutin)

Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM; shows 30-fold greater selectivity against PLK2 and no activity to PLK3.

Rilpivirine(R 278474, TMC 278) is a type of anti-HIV medicine called a non-nucleoside reverse transcriptase inhibitor (NNRTI).

Risperidone(R 64 766) is a serotonin 5-HT2 receptor blocker(Ki= 0.16 nM) and a potent dopamine D2 receptor antagonist(Ki= 1.4 nM).

Ritonavir is an inhibitor of HIV protease used to treat HIV infection and AIDS,showed potent activity against COVID-19(SARS-COV-2) .

Rivaroxaban (Xarelto; BAY 59-7939) is a novel, oral, direct Factor Xa (FXa) inhibitor in late-stage development for the prevention and treatment of thromboembolic disorders.

Rivastigmine hydrogen tartrate is a parasympathomimetic or cholinergic agent for the treatment of mild to moderate dementia of the Alzheimer’s type and Parkinson's disease.

RN-486 is a Bruton's tyrosine kinase (Btk) inhibitor.

Ro 28-1675 (Ro 0281675) is a potent allosteric GK activator with a SC1.5 value of 0.24± 0.0019 uM.

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.