5-Azacytidine is a potent growth inhibitor and a cytotoxic agent. 5-Azacytidine acts as a demethylating agent by inhibiting DNA methyltransferase (Dnmt), forming covalent adducts with cellular DNMT1 depleting enzyme activity. 5-Azacytidine also improves t

Mizoribine(NSC 289637; HE 69; β-Bredinin) is an immunosuppressive agents (IC50=100 uM) that inhibit the proliferation of lymphocytes selectively, via inhibition of IMPDH.

Diltiazem hydrochloride is a calcium ion influx inhibitor (slow channel blocker or calcium antagonist).

Dinaciclib (SCH727965) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM, respectively.

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

Acelarin (NUC-1031) is a ProTide transformation and enhancement of the widely-used nucleoside analogue, gemcitabine.

LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.

Ticagrelor is the first reversibly binding oral P2Y12 receptor antagonist, also inhibits CYP2C9 and 4-hydroxylation with IC50 of 10.5 μM and 8.2 μM respectively.

Apremilast(CC10004) is a novel small molecule inhibitor of PDE4 with an IC50 value of 74 nM.

Ibutamoren mesylate (MK-0677) is an orally active nonpeptide growth hormone (GH) secretagogue.

Glecaprevir is a novel HCV NS3/4A protease inhibitor, with IC50 values ranging from 3.5 to 11.3 nM.

Danoprevir is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition effect for HCV genotypes 1A/1B/4/5/6 is ~10-fold higher than 2B/3A.

ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM.

MK-4827(Niraparib) tosylate is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM; with great activity in cancer cells with mutant BRCA-1 and BRCA-2; >330-fold selective against PARP3, V-PARP and Tank1.

Lumateperone Tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a SERT blocker (Ki = 61 nM).

Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium-channel complexes in the CNS.

HSD-016 (HSD016) is a potent, selective, and efficacious 11β-HSD1 inhibitor with IC50 of 149 and 530 nM for mouse and human 11β-HSD1, respectively.

Avasimibe inhibits ACAT and CYP2C9 with IC50 of 3.3 μM and 2.9 μM, respectively.

MLN4924 is a small molecule inhibitor of Nedd8 activating enzyme (NAE) with IC50 of 4 nM.

TAK-243 (MLN-7243, AOB87172) is a small-molecule, cell-permeable inhibitor of ubiquitin-activating enzyme E1 (UAE1).

AZD3965 is a selective inhibitor of monocarboxylate transporter 1 (MCT1) with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM.

Ixabepilone (Azaepothilone B; BMS 247550) is an epothilone B analog and nontaxane microtubule-stabilizing compound with clinical activity in a range of solid tumors.

Nelonicline (ABT-126) is a potent, selective α7 nicotinic receptor (nAChR) partial agonist for the treatment of cognitive impairment with schizophrenia..

Ibiglustat (Genz-682452,SAR402671), is a potent and selective Glucosylceramide synthase inhibitor and ceramide glucosyltransferase inhibitor.

Baloxavir marboxil is a prodrug of S-033447. S-033447 is a small molecule inhibitor of the cap-dependent endonuclease of influenza A and B viruses.

BLZ945 is a highly selective and brain-penetrant inhibitor of CSF1R with IC50 of 1 nM; >3200-fold higher than its affinity for other kinases.

GDC-0980 (RG7422) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM, respectively. Also a mTOR inhibitor with Ki of 17 nM, and highly selective versus others PIKK family kinases.

AST-3424 (OBI-3424, TH-3424) is a first-in-class, novel prodrug that selectively targets cancers overexpressing the enzyme AKR1C3, OBI-3424 is a highly selective prodrug that is converted by AKR1C3 to a DNA alkylating agent.

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

JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively.