Related Experiment Video

Updated: May 9, 2026

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
10:49

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia

Published on: September 18, 2013

Lead identification of novel and selective TYK2 inhibitors

Jun Liang1, Vickie Tsui, Anne Van Abbema

  • 1Department of Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, CA 94080, United States.

European Journal of Medicinal Chemistry
|July 23, 2013
PubMed

Keywords:
1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride2-(7-aza-1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate4-(N,N-dimethylamino)pyridineADMEAcOHBocCDCl(3)Crystal structureDCEDCMDMAPDMFDMSODMSO-d(6)DTTEDCIESIHATUHOBtHit to leadIVImmunologyJanus family kinaseKinase inhibitorLCMSLogD(7.4)MCTMDCKMadin–Darby canine kidney cellsP(app)POPhSCX-2SFCStructure–activity relationshipTCEPTFATHFTLCTYK2BMETfabsorption, distribution, metabolism, and excretionacetic acidapparent permeabilityaq.aqueousby mouthdeuterated DMSOdeuterated chloroformdichloroethanedichloromethanedimethylformamidedimethylsulfoxidedithiothreitolelectrospray ionizationhhourhydroxybenzotriazoleintravenousliquid chromatography–mass spectrometrylog of partition coefficient between octanol and pH(7.4) aqueous buffermethyl cellulose/tweenp-TsOHpara-toluenesulfonic acidphenylpre-packed Isolute(®) silica-based sorbent with a chemically bonded propylsulfonic acid functional groupsupercritical fluid chromatographytert-butyl carbamatetetrahydrofuranthin layer chromatographytrifluoroacetic acidtrifluorosulfonatetris(2-carboxyethyl)phosphineβ-mercaptoethanol

More Related Videos

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays07:42

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays

Published on: September 19, 2018

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays13:22

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

Related Concept Videos

Receptor Tyrosine Kinases01:26

Receptor Tyrosine Kinases

Receptor tyrosine kinases or RTKs are membrane-bound receptors that phosphorylate specific tyrosine on protein substrates. RTKs regulate cellular growth, differentiation, survival, and migration. They contain an extracellular ligand binding domain, a transmembrane domain, and a cytosolic tail with intrinsic kinase activity. Several extracellular signaling molecules activate RTKs in one or more ways and relay the signal downstream. Ligands such as platelet-derived growth factor (PDGF) or...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...