A guide to picking the most selective kinase inhibitor tool compounds for pharmacological validation of drug targets

British Journal of Pharmacology

Volumn 166, Issue 3, 2012, Pages 858-876

  Uitdehaag, Joost C M ^a   Verkaar, Folkert ^b   Alwan, Husam ^c   De Man, Jos ^a   Buijsman, Rogier C ^a   Zaman, Guido J R ^a  

^a Netherlands Translational Research Center BV   (Netherlands)

^b VU UNIVERSITY AMSTERDAM   (Netherlands)

^c UNIVERSITY MEDICAL CENTER UTRECHT   (Netherlands)

Author keywords

cross screen; drug target; entropy; inhibitor; kinase; profiling; promiscuity; quantitative; selectivity; tool

Indexed keywords

2 [4 (1 HYDROXYIMINO 5 INDANYL) 3 (4 PYRIDINYL) 1H PYRAZOL 1 YL]ETHANOL; 4 (8 CYCLOPENTYL 7 ETHYL 5,6,7,8 TETRAHYDRO 5 METHYL 6 OXO 2 PTERIDINYLAMINO) 3 METHOXY N (1 METHYL 4 PIPERIDINYL)BENZAMIDE; 4 AMINO 7 TERT BUTYL 5 (4 METHYLPHENYL)PYRAZOLO[3,4 D]PYRIMIDINE; 5 (2,6 DICHLOROPHENYL) 2 (2,4 DIFLUOROPHENYLTHIO)PYRIMIDO[1,6 B]PYRIDAZIN 6 ONE; 8 [4 (1 AMINOCYCLOBUTYL)PHENYL] 9 PHENYL 1,2,4 TRIAZOLO[3,4 F][1,6]NAPHTHYRIDIN 3(2H) ONE; AMG 900; BAFETINIB; CH 5424802; CRIZOTINIB; DASATINIB; ERLOTINIB; EVEROLIMUS; GEFITINIB; GSK 1070916; IMATINIB; LAPATINIB; MUBRITINIB; NILOTINIB; PAZOPANIB; PROTEIN KINASE INHIBITOR; QUIZARTINIB; ROSCOVITINE; RUXOLITINIB; SELUMETINIB; SORAFENIB; SUNITINIB; TEMSIROLIMUS; TOFACITINIB; UNCLASSIFIED DRUG; UNINDEXED DRUG; VANDETANIB; VATALANIB; VEMURAFENIB;

BREAST CANCER; CHRONIC MYELOID LEUKEMIA; DOSE RESPONSE; DRUG APPROVAL; DRUG SCREENING; DRUG SELECTIVITY; DRUG TARGETING; ENTROPY; ENZYME INHIBITION; FILTER; GASTROINTESTINAL STROMAL TUMOR; KIDNEY CANCER; KIDNEY CARCINOMA; LIVER CANCER; LUNG NON SMALL CELL CANCER; METASTATIC MELANOMA; MYELOFIBROSIS; PANCREAS CANCER; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN TARGETING; REVIEW; SIGNAL TRANSDUCTION; THYROID MEDULLARY CARCINOMA; TRIPLE NEGATIVE BREAST CANCER; VALIDATION PROCESS;

ANIMALS; DRUG DISCOVERY; ENTROPY; ENZYME INHIBITORS; HUMANS; INHIBITORY CONCENTRATION 50; MOLECULAR STRUCTURE; PHOSPHOTRANSFERASES; PROTEIN BINDING; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY;

EID: 84860851057     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2012.01859.x     Document Type: Review

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