Publications

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

h

Mutant IDH is sufficient to initiate enchondromatosis in mice

PNAS. ( in process)

h

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

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

h

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

h

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

h

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

h

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

h

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.

h

SUBSTITUTED BENZAMIDES AND METHODS OF USE THEREOF

WO/2015/078374

h

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

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

h

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.

h

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

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

h

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

J. Med. Chem. 2015, 58, 8166−8181

h

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

J. Med. Chem. 2014, 57, 9028−9041

h

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

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

h

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

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

h

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

Plos One. 9(1): e85308

h

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

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

h

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

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

h

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

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

h

Targeted Inhibition of Mutant IDH2 in Leukemia Cells Induces Cellular Differentiation

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

h

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)

h

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

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

h

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

h

Small Molecule Activation of PKM2 in Cancer Cells Induces Serine Auxotrophy

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

h

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

h

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

FEBS J. 279(7): 1261-73

h

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

Gene. 503(2): 200-7

h

Full-length human glutaminase in complex with an allosteric inhibitor

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

h

INHIBITORS OF AKT ACTIVITY

WO/2011/130921

h

Differential Aspartate Usage Identifies a Subset of Cancer Cells Particularly

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

h

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.

h

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

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

h

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

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

h

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.

h

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

h

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.

h

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

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

h

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)”

h

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

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

h

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

h

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

h

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

h

“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

h

Patent Application Publication

US 2016/0303135 A1

h

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

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

h

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

WO2011307115

h

ANALOGS OF CELASTROL

WO2017070615A1

h

“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

h

一类黄酮衍生物及其制备方法和用途

CN1172946

h

一种6-甲氧基水杨醛的制备方法

CN101768065A

h

一类磺内酰胺类化合物及其制备方法和中间体

CN102115466B

h

一种螺环丙基甲酰衍生物的中间体化合物的制备方法

CN102557941B

h

一种米诺环素的制备方法及其中间体

CN103387512B

h

一种山环素的制备方法

CN103387511B

h

一种3-氯-5,6,7,8-四氢异喹啉的制备方法

201810781489.9

h

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

h

一种5-氨甲基-哌啶-2-酮的制备方法

201810785216.1

h

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

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

Headquarters

1F & 3F, Block A
2829 JinKe Road
Zhangjiang Hi-Tech Park
PuDong New Area
Shanghai China, 201203

w

Contact Us

China: +86 21 5132 0088
US: +1 650 419 9974
Europe: +45 4586 9000
Japan: +81 03 5403 6975

contact@chempartner.com