Archive

Safety, tolerability, pharmacokinetics and pharmacodynamics of AUR101, An RORγt inhibitor, in normal healthy volunteers

Discovery and clinical development of the first small molecule checkpoint inhibitor for cancer therapy

Antitumor activity of ODM-207, a novel BET bromodomain inhibitor, in nonclinical models of ER+ breast cancer as single agent and as a combination treatment

ODM-203, a Selective Inhibitor of FGFR and VEGFR, Shows Strong Antitumor Activity, and Induces Antitumor Immunity

Highly selective peroxisome proliferator-activated receptor δ (PPARδ) modulator demonstrates improved safety profile compared to GW501516

Preclinical evaluation of PD and efficacy of novel potent selective and orally bioavailable CDK12 covalent inhibitors in TNBC model (Covalent selective, CDK12i)

Combination efficacy and safety profile of an orally bioavailable small molecule agent targeting CD47/SIRPα axis (CD47 antagonists)

Preclinical In vivo evaluation of efficacy, pharmacokinetics and pharmacodynamics of novel PRMT5 inhibitors in multiple tumor models (PRMT5i)

Identification of SMARCA2/4 degraders for the treatment of SMARCA4-mutant and other cancers (SMARCA2/4 degraders)

Potent anti-tumor activity correlated with inhibition of DNA damage response genes with highly selective and orally bioavailable CDK12 covalent inhibitors

Phase 2 trial of CA-170, a novel oral small molecule dual inhibitor of immune checkpoints VISTA and PD-1, in patients (pts) with advanced solid tumor and Hodgkin lymphoma

Oral Immune Checkpoint Antagonists Dually Targeting TIGIT and PD-1 pathways for Cancer Therapy

In vivo anti-tumor efficacy with a dual degrader of SMARCA2 and SMARCA4

Phase 2 trial of CA-170, a novel oral small molecule dual inhibitor of immune checkpoints VISTA and PD-1, in patients (pts) with advanced solid tumor and Hodgkin lymphoma

Efficacy and safety profile of AU7R-104, a small molecule targeting CD47/SIRPα pathway

An orally bioavailable small molecule dual antagonist of TIGIT and PD-L1 pathways shows immune-mediated anti-tumor activity

Identification of a novel preclinical candidate for CDK7 inhibition

Potent small molecule compounds that selectively inhibit proliferation of ABC-DLBCL cell lines

Immune-mediated anti-tumor activity with a clinical stage BET bromodomain inhibitor ODM-207 in pre-clinical models

Targeting CD47- SIRPα interaction by novel peptide-based antagonists

Functional antagonism of VSIG8-mediated immune suppression by oral VISTA agents

Identification of a novel highly selective and orally bioavailable preclinical candidate for CDK7 covalent inhibition

Novel inhibitors of protein arginine methyltransferase 5 (PRMT5) for the treatment of solid tumors

Dihydroorotate dehydrogenase (DHODH) inhibitors affect ATP depletion, endogenous ROS and mediate S-phase arrest in breast cancer cells

Identification of novel covalent inhibitors of K-Ras G12C that are efficacious in a xenograft model of NSCLC

Potent and selective inhibition of CDK7 by novel covalent inhibitors

Efficacy and safety of highly selective novel IRAK4 inhibitors for treatment of ABC-DLBCL

Oral immune checkpoint antagonists targeting PD-L1/VISTA or PD-L1/Tim3 for cancer therapy

ODM-207, a novel BET-bromodomain inhibitor as a therapeutic approach for the treatment of prostate and breast cancer

ODM-207, a novel BET-bromodomain inhibitor as a therapeutic approach for the treatment of patients with castration resistant prostate cancer

Pre-clinical efficacy in multiple syngeneic models with oral immune checkpoint antagonists targeting PD-L1 and TIM-3

Potent and selective inhibition of CDK7 by novel covalent inhibitors

Novel IRAK-4 inhibitors exhibit highly potent anti-proliferative activity in DLBCL cell lines with activating MYD88 L265P mutation (IRAK-4)

Discovery of dihydro-isoxazole derivatives as novel inhibitors of NAMPT for the treatment of multiple myeloma, (NAMPT)

Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors

Benzimidazole derivatives as potential dual inhibitors for PARP-1 and DHODH

Deregulated hepsin protease activity confers oncogenicity by concomitantly augmenting HGF/MET signaling and disrupting epithelial cohesion

AFN-1252 is a potent inhibitor of enoyl-ACP reductase from Burkholderia pseudomallei - Crystal structure, mode of action, and biological activity

Dihydroorotate Dehydrogenase (DHODH) Inhibitor Suppress Breast Cancer Cells Proliferation

Crystal structure of ATP-binding subunit of an ABC transporter from Geobacillus kaustophilus

Discovery of O-(3-carbamimidoylphenyl)-L-serine amides as matriptase inhibitors using a fragment-linking approach

Efficacy of Selective RAR-related Orphan Receptor gamma (RORγ) Inverse Agonists in Inflammatory Disease Models

Discovery and Optimization of a Novel Series of IRAK-4 Inhibitors for the Treatment of Autoimmune Disorders

Identification of a potent inhibitor of enoyl ACP reductase FabI from Burkholderia pseudomallei - crystal structure, Mode of Action and Biological Activity

3Alkoxy-pyrrolo[1,2b]pyrazolines as Selective Androgen Receptor Modulators with Ideal Physicochemical Properties for Transdermal Administration

Discovery of azetidine based ene-amides as potent bacterial enoyl ACP reductase (FabI) inhibitors

Structure-Guided Discovery of 1,3,5 Tri-Substituted Benzenes as Potent & Selective Matriptase Inhibitors Exhibiting in Vivo Antitumor Efficacy

Expression of the fatty acid receptor GPR120 in the gut of diet-induced-obese rats and its role in GLP-1 secretion

X-ray structure of PTP1B in complex with a new PTP1B inhibitor

Novel inhibitors of nicotinamide phosphoribosyltransferase and their evaluation in combination with bortezomib

Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia

Equipotent antagonism towards both ligands and excellent anti-tumor efficacy with a peptide inhibitor of PD-1 immune checkpoint pathway

Discovery of potent & selective retinoid related orphan receptor gamma (ROR-gamma) inverse agonists for the treatment of TH17 mediated diseases

Equipotent antagonism, transient immune activation and excellent antitumor efficacy with a peptide inhibitor of PD-1 immune checkpoint pathway

Identification of potent BET bromodomain inhibitors for treatment of cancer

Novel inhibitors of nicotinamide phosphoribosyltransferase (NAMPT)

Efficient throughput method for hygroscopicity classification of active and inactive pharmaceutical ingredients by water vapor sorption analysis

Discovery of PyridylBis(oxy)benzamide Derivatives as Selective Matriptase Inhibitors

Discovery of 7-azaindole based anaplastic lymphoma kinase (ALK) inhibitors: wild type and mutant (L1196M) active compounds with unique binding mode

Design and synthesis of 2-substituted benzoxazoles as novel PTP1B inhibitors

Diphenylether derivative as selective inhibitor of protein tyrosine phosphatase 1B (PTP1B) over t-cell protein tyrosine phosphatase (TCPTP) identified through virtual screening

Inhibition of matriptase results in efficacy in preclinical models of osteoarthritis

Identification of PI3K isoform selective inhibitors for treatment of inflammatory indications

Demonstration of anti-tumor efficacy in multiple preclinical cancer models using a novel peptide inhibitor (Aurigene-012) of the PD-1 signaling pathway

Preliminary safety evaluation of novel small molecule inhibitors of caspase-3

Synthesis and Biological Evaluation of 3-(4-aminophenyl)-2-(1H-indol-3-yl)Propanamide derivatives as novel PTP1B Inhibitors

Developing Selective Inhibitors Of Ptp1b Over TcCPTP.

Investigation of orally administered small molecule inhibitors of caspase-3 in murine models of apoptosis

Discovery of indole tetrafluoro phenoxymethyl ketone-based potent novel small molecule inhibitors of caspase-3

Aurigene-012 as a novel peptide inhibitor of the PD1 signaling pathway – Identification of a preclinical drug candidate for cancer therapy, Natural Peptides to Drugs

Demonstration of anti-tumor efficacy in multiple preclinical cancer models using a novel peptide inhibitor (Aurigene-012) of the PD-1 signaling pathway

Synthesis and biological evaluation of novel oxalamido derivatives as caspase-3 inhibitors

Cannabinoid 1 (CB1) receptor--pharmacology, role in pain and recent developments in emerging CB1 agonists

Evaluation of the effects of Mitragyna Speciosa alkaloid extract on cytochrome P450 enzymes using a high throughput assay

Peptide hormone isoforms: N- terminally branched PYY3–36 isoforms give improved lipid and fat-cell metabolism in diet-induced obese mice

Peptide Architecture: Adding an α-Helix to PYY lysine side chain provides nanomolar binding and body weight lowering effects

A Structure-Based Strategy for New Drug Discovery

Development of DPP IV Inhibitors

Rational selection of structurally diverse natural product scaffolds with favorable ADME properties for drug discovery

The multiple orthogonal tools approach to define molecular causation in the validation of druggable targets

The impact of structure-guided drug design on clinical agents