The discovery and optimization of aminooxadiazoles as potent Pim kinase inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 25, Issue 4, 2015, Pages 847-855

  Wurz, Ryan P ^a   Pettus, Liping H ^a   Jackson, Claire ^a   Wu, Bin ^a   Wang, Hui Ling ^a   Herberich, Brad ^a   Cee, Victor ^a   Lanman, Brian A ^a   Reed, Anthony B ^a   Chavez, Frank ^a   Nixey, Thomas ^a   Laszlo, Jimmy ^a   Wang, Paul ^a   Nguyen, Yen ^a   Sastri, Christine ^a   Guerrero, Nadia ^a   Winston, Jeff ^a   Lipford, J Russell ^a   Lee, Matthew R ^a   Andrews, Kristin L ^a   Mohr, Christopher ^a   Xu, Yang ^a   Zhou, Yihong ^a   Reid, Darren L ^a   Tasker, Andrew S ^a   more..

^a AMGEN INC   (United States)

Author keywords

BAD phosphorylation; KMS 12; Multiple myeloma; Oxadiazole; Pim kinase inhibitor

Indexed keywords

AMINOOXADIAZOLE DERIVATIVE; CYCLOPROPANE; OXADIAZOLE DERIVATIVE; PROTEIN BAD; PROTEIN KINASE PIM 1; PROTEIN KINASE PIM 2; PROTEIN SERINE THREONINE KINASE; PROTEIN SERINE THREONINE KINASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CONFORMATIONAL TRANSITION; CONTROLLED STUDY; CRYSTAL STRUCTURE; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG POTENCY; EC50; FEMALE; GENE OVEREXPRESSION; HIGH THROUGHPUT SCREENING; HYDROGEN BOND; IC50; MOUSE; MULTIPLE MYELOMA; MULTIPLE MYELOMA CELL LINE; NONHUMAN; PROCESS OPTIMIZATION; PROTEIN PHOSPHORYLATION; RAT; SUZUKI REACTION;

MUS; RATTUS;

EID: 84964293366     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2014.12.067     Document Type: Article

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53. For more information see: http://www.discoverx.com/technology/technology-kinomescan.php. The Ambit kinase panel included: Abl, Akt1, Akt2, ALK, AMPK, Aur2, BMPR1A, BRAF, BRK, BTK, CAMK2, CAMK4, CDC7, CDK2, CDK4, CDK8, CDK18, c-KIT, CHK1, CK1δ, CKIIα CHK2, CLK1, CLK2, CLK4, DAPK1, DDR1, DMPK, DYRK1α, DYRK1β, EGFR, EPHA2, EPHA4, EPHB3, Erk1, Erk2, FGFR1, FLT3, FYN, GAK, GRK1, GSK3β, HGK, IGF1R, INSR, IRAK4, IRE1, JAK2, JNK3, KDR, LCK, LIMK1, LYN, MAPK1, MAP2K3, MAP3K1, MAP3K9, MAPK4K1, MAPKAPK2, MARK1, MARK3, MEK5, MET, MNK1b, MSK1, MST2, mTOR, NEK4, NEK6, OXSR1, p38α, p38γ p70S6K, PAK2, PDGFRβ, PI3Kα, PI3Kδ, PIM1, PIM2, PKAα, PKAC2, PKBα, PKBβ, PKC, PKR, PKCβ2, PKD2, PKGα, PLK1, PLK4, PRAKAA1, PRKG1, RAF, RIPK2, ROCK2, RPS6KB1, RSK1, SGK1, SRC, STK33, STK32B, SYK, TAK1, TAO2 TBK1, TIE2, TGFBR1, TRKA, TSSK1β, TYK2, WEE1, YSK4.