Publications

ChemPartner is a science-based, technology-driven global Contract Research Organization (CRO) and Contract Development and Manufacturing Organization (CDMO).

Approach to Rational Identification of Lead Molecular Glue Degraders for Casein Kinase 1a

EFMC International Symposium on Advances in Synthetic and Medicinal Chemistry, 2023, September, Zagreb

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Identification of GNE-131: A potent and selective hNaV1.7 inhibitor for the treatment of pain

National Medicinal Chemistry Symposium, 2016, Jun. 26-29, Chicago

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From Ergolines to Indoles: Improved Inhibitors of the Human H3 Receptor for the Treatment of Narcolepsy

ChemMedChem. 2015 Feb;10(2):266-75.

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Neuroactive Steroids.1.Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21

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人源性胃癌移植瘤模型的建立及其评价

实验动物与比较医学. 34:259-65

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Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders

J. Med. Chem., 2015, 58 (23), 9154–9170

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Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series

ACS Med. Chem. Lett., 2015, 6 (6), 711–715

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Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety

ACS Med. Chem. Lett., 2015, 6 (12), 1241–1246.

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SUBSTITUTED BENZAMIDES AND METHODS OF USE THEREOF

WO/2015/078374

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Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists

Bioorganic & Medicinal Chemistry Letters 2015 (25), 2907–2912

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Mutant IDH is sufficient to initiate enchondromatosis in mice

PNAS. ( in process)

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Discovery of an orally bioavailable isoxazoline benzoxaborole (AN8030) as a long acting animal ectoparasiticide

Bioorganic & Medicinal Chemistry Letters 25 (2015) 5589–5593

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Discovery and Optimization of Novel, Selective Histone Methyltransferase SET7 Inhibitors by Pharmacophore- and Docking-Based Virtual Screening

J. Med. Chem. 2015, 58, 8166−8181

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Neuroactive Steroids.1.Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21

J. Med. Chem. 2015, 58, 3500-3511.

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Virtual screening and biological evaluation of novel small molecular inhibitors against protein arginine methyltransferase 1 (PRMT1)

Org. Biomol. Chem., 2014, 12, 9665–9673

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Ergoline-derived inverse agonists of the human h3 receptor for the treatment of narcolepsy

ChemMedChem. 2014 Aug;9(8):1683-96

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Identifying Novel Selective Non-Nucleoside DNA Methyltransferase 1 Inhibitors through Docking-Based Virtual Screening

J. Med. Chem. 2014, 57, 9028−9041

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Steric and Electronic Factors Influence Regio-isomeric Thiazole Formations Between Substituted Benzothioamides and Ethyl Bromopyruvate

J. Heterocyclic. Chem. 2014, 51, 1137−1146

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Novel synthesis of isoxazoline indolizine amides for potential application to tropical diseases

Tetrahedron Letters, Volume 55, 2014, Pages 1936–1938

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Establishment and Characterization of 7 Novel Hepatocellular Carcinoma Cell Lines from Patient-Derived Tumor Xenografts

Plos One. 9(1): e85308

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Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation

Science,2013, 340(6132),622-6

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人源性食管癌移植瘤模型的建立、评价及其应用的初步研究

实验动物与比较医学: 33(1)

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Vortioxetine disinhibits pyramidal cell function and enhances synaptic plasticity in the rat hippocampus.

J Psychopharmacol. 2014 Oct;28(10):891-902.

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食管癌动物模型的建立

上海师范大学学报(自然科学版). 42(4): 398-404

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Small Molecule Activation of PKM2 in Cancer Cells Induces Serine Auxotrophy

Chem. Biol. 2012, 19(9), 1187-98

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HZ08 reverse the aneuploidy-induced cisplatin-resistance in Gastric cancer by modulating the p53 pathway.

European Journal of Pharmacology. 720(1-3): 84-97

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Identification of NME5 as a contributor to innate resistance to gemcitabine in pancreatic cancer cells.

FEBS J. 279(7): 1261-73

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Transactivation of the human NME5 gene by Sp1 in pancreatic cancer cells.

Gene. 503(2): 200-7

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Intrinsic gemcitabine resistance in a novel pancreatic cancer cell line is associated with cancer stem cell-like phenotype.

Int J Oncol. 40 (3): 798-806

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INHIBITORS OF AKT ACTIVITY

WO/2011/130921

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Differential Aspartate Usage Identifies a Subset of Cancer Cells Particularly

Cell Reports 17, 876–890, October 11, 2016

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Full-length human glutaminase in complex with an allosteric inhibitor

Biochem. 2011, 50(50), 10764 -70

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AG-348 enhances pyruvate kinase activity in red blood cells from patients with pyruvate kinase deficiency

Blood. 2017 Sep 14;130(11):1347-1356.

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AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations

Cancer Discov. 2017 May;7(5):478-493.

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Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions

ACS Med Chem Lett. 2017 Nov 28;8(12):1224-1229.

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A small molecule activator of Nav1.1 channels increases fast-spiking interneuron excitability and GABAergic transmission in vitro and has anti-convulsive effects in vivo

European Journal of Neuroscience, Vol. 46, pp. 1887–1896, 2017

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Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers

ACS Med Chem Lett. 2018 Jan 19;9(4):300-305.

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H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma

Cancer Res. 2017 Dec 15;77(24):6999-7013.

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Precision Targeted Therapy with BLU-667 for RET -Driven Cancers

“Cancer Discovery (July 1 2018 8 (7) 836-849; DOI:10.1158/2159-8290.CD-18-0338)”

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First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway

Cancer Discov. 2015 Apr;5(4):424-37.

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EZH2 inhibition by tazemetostat results in altered dependency on B-cell activation signaling in DLBCL

AACR August 23, 2017; DOI: 10.1158/1535-7163.MCT-16-0840

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Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma

SCIEntIfIC Reports | (2017) 7:17993 | DOI:10.1038/s41598-017-18446-z

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“Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2”

PNAS | May 7, 2013 | vol. 110 | no. 19 | 7923

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“Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas”

PLOS ONE| DOI:10.1371/journal.pone.0111840 December 10, 2014

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Patent Application Publication

US 2016/0303135 A1

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Selective Killing of SMARCA2- and SMARCA4- deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models

AACR Mol Cancer Ther; 16(5) May 2017

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Pyrimidine hydroxyl amide compounds as protein deacetylase inhibitors and methods of use thereof.

WO2011307115

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Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo

ACS Med. Chem. Lett. 3, 10, 850-855

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“Discovery of A‑971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders”

J. Med. Chem. 2015, 58, 9154-9170

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一类黄酮衍生物及其制备方法和用途

CN1172946

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一种6-甲氧基水杨醛的制备方法

CN101768065A

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ANALOGS OF CELASTROL

WO2017070615A1

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一种螺环丙基甲酰衍生物的中间体化合物的制备方法

CN102557941B

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一种米诺环素的制备方法及其中间体

CN103387512B

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一类磺内酰胺类化合物及其制备方法和中间体

CN102115466B

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一种3-氯-5,6,7,8-四氢异喹啉的制备方法

201810781489.9

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一种4-溴甲基-2-三甲基硅乙炔苯基-1-磺酰氟的制备方法

201810781490.1

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一种山环素的制备方法

CN103387511B

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一种5-氨甲基-哌啶-2-酮的制备方法

201810785216.1

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Mtb PKNA/PKNB Dual Inhibition Provides Selectivity Advantages for Inhibitor Design To Minimize Host Kinase Interactions

ACS Med. Chem. Lett. 2017, 8, 1224-1229

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Fragment-Based Drug Discovery of 2‑Thiazolidinones as BRD4 Inhibitors: 2. Structure-Based Optimization

J. Med. Chem. 2015, 58, 1281−1297

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