+1 650 419 9974 contact@chempartner.com

Publications

睿智医药是一家以科学为基础，以技术为导向的全球型CRO+CDMO企业。

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Rapid Discovery of CD28-specific Antibodies from Rabbits Through Single B cell Cloning on the Beacon® Platform

Antibody Engineering and Therapeutic, 2023, December, San Diego

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

38th ACS National Medicinal Chemistry Symposium, 2024, June, Seattle

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Rapid Discovery of CD28-specific Antibodies from Rabbits Through Single B cell Cloning on the Beacon® Platform

Antibody Engineering and Therapeutics, 2023, June, Amsterdam

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Amlodipine Metabolism in Human Liver Microsomes and Roles of CYP3A4/5 in the Dihydropyridine Dehydrogenation

Drug Metab Dispos 42:245–249, February 2014

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Biotransformation of Ilaprazole in Human Liver Microsomes and Human: Role of CYP3A4 in Ilaprazole Clearance and Drug-Drug Interaction

Drug Metab Dispos 46:1453–1461, October 2018

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High-Throughput Metabolic Soft-Spot Identification in Liver Microsomes by LC/UV/MS: Application of a Single Variable Incubation Time Approach

Molecules 2022,27,8058

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Characterization of 405B8H3(D‐E), a newly engineered high affinity chimeric LAG‐3 antibody with potent antitumor activity

FEBS open bio vol. 13,7 (2023): 1253-1265

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Methods to assess small molecule allosteric modulators of the STRAD pseudokinase

Methods in enzymology vol. 667 (2022): 427-453

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Molecular dynamics simulations reveal the selectivity mechanism of structurally similar agonists to TLR7 and TLR8

PLOS ONE (2022) 17(4): e0260565 

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Discovery and Optimization of the First Highly Effective and Orally Available Galectin-3 Inhibitors for Treatment of Fibrotic Disease

J. Med. Chem. 2022, 65, 19, 12626–12638

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A Novel, Orally Bioavailable, Small-Molecule Inhibitor of PCSK9 With Significant Cholesterol-Lowering Properties In Vivo

J. Lipid Res. (2022) 63(11) 100293.

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Accelerated Discovery of Unique Anti-PD-L1 Antibodies from Spleen Versus Bone Marrow of Immunized Mice by Single Plasma B Cell Cloning on the Beacon® Platform

PEGS, 2019, April, Boston

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Accelerated Discovery of Unique Anti-PD-L1 Antibodies from Spleen Versus Bone Marrow of Immunized Mice by Single Plasma B Cell Cloning on the Beacon® Platform

Antibody Engineering and Therapeutics, 2019, Amsterdam

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Accelerated Discovery of Unique Anti-PD-L1 Antibodies from Spleen Versus Bone Marrow of Immunized Mice by Single Plasma B cell Cloning on the Beacon® Platform

Antibody Engineering and Therapeutics, 2018, Dec., Amsterdam

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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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Ubiquitin-conjugating enzyme UbcH10 promotes gastric cancer growth and is a potential biomarker for gastric cancer

Oncology Reports.,2016, 36(2): 779-86

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Identification of Novel EZH2 Inhibitors through Pharmacophore-based Virtual Screening and Biological Assays

Bioorganic & Medicinal Chemistry Letters. 2016, 26, 3813–3817

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Identification of Novel Disruptor of Telomeric Silencing 1-Like (DOT1L) Inhibitors through Structure-Based Virtual Screening and Biological Assays

J. Chem. Inf. Model. 2016, 56 (3), 527–534

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Design and Discovery of new pyrimidine coupled nitrogen aromatic rings as chelating groups of JMJD3 Inhibitor

Bioorg Med Chem Lett. 2016, 26(3), 721-725

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Discovery of novel inhibitors targeting menin-mixed lineage leukemia (MLL) interface using pharmacophore- and docking-based virtual screening

Journal of Chemical Information and Modeling. ahead of print

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Chemically Diverse Group I p21-Activated Kinase (PAK) Inhibitors Impart Acute Cardiovascular Toxicity with a Narrow Therapeutic Window

J. Med. Chem., 2016, 59 (11), 5520–5541.

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Optimization of isoxazoline amide benzoxaboroles for identification of a development candidate as an oral long acting animal ectoparasiticide

Bioorganic & Medicinal Chemistry Letters 26 (2016) 3182–3186

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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

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

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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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