Sotrastaurin(AEB-071) is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM; inactive to PKCζ.

SKLB1002 is a novel and potent VEGFR-2 inhibitor with an IC50 value of 32 nM.

Sitravatinib (MGCD516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.

SGX-523 is a selective Met inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α.

Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.

S55746 (BLC201) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 (BLC201) has antitumor activity with low toxicity[1].

Rupatadine is a dual histamine H1 and PAF antagonist

RU 24969 hemisuccinate is a potent SR-1A/SR-1B and moderate SR-2C agonist that may also release serotonin.

Romidepsin strongly inhibits HDAC1 and HDAC2 with IC50 of 1.6 nM and 3.9 nM, respectively, but is relatively weak in inhibiting HDAC4 and HDAC6 with IC50 25 nM and 790 nM, respectively.

RN-1734 is a transient receptor potential vanilloid 4 (TRPV4) antagonist, blocking calcium influx induced by the TRPV4 agonist 4α-phorbol 12,13-didecanoate with IC50 values of 2.3, 5.9, and 3.2 µM for human, mouse, and rat TRPV4, respectively.

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).

Rimonabant(SR141716) is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.

Rimonabant Hcl(SR141716A) is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.

SEC inhibitor KL-2 is a peptidomimetic inhibitor of super elongation complex (SEC) and transcription elongation by Pol II, disrupts cyclin T1-AFF4 interaction (Ki=1.50 uM) within SEC; disrupts the interaction between the SEC scaffolding protein AFF4 and P

Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively[1].

p-Cresol glucuronide is a metabolite of p-cresol, a uremic toxin formed by bacterial fermentation of proteins in the large intestine. It is formed from p-cresol primarily by the UDP-glucuronosyltransferase (UGT) isoform UGT1A6, but also by UGT1A9, in huma

PF-05221304 is an orally bioavailable, liver-directed and dual ACC1 (and ACC2) inhibitor with IC50s of 7.5 nM for rat ACC1, 8.2 nM for rat ACC2, 12.4 nM for human ACC1 and 8.7 nM for human ACC2. PF-05221304 is a substrate for organic anion transport polyp

Pyrintegrin is a cell-permeable promoter of the adhesion of individually dissociated hESCs on matrigel- or laminin-, but not gelatin-coated surfaces, substantially reducing trypsinization-induced apoptosis.

PK150, an analogue of Sorafenib, shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations. PK150 inhibits Gram-positive Methicillin-sensitive S. aureus (MSSA), Methicillin-resistant S. aureus

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

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.

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

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.

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

Pirfenidone(AMR69) is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Phase 3.

Pioglitazone Hydrochloride is the hydrochloride salt preparation of Pioglitazone, a specific ligand of PPAR-γ (peroxisome proliferator-activated receptor-γ). Pioglitazone is a thiazolidinedione compound described to produce antiinflammatory and antiarteri

Pifithrin-μ is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.

Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes.

PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2/3.