LINCSapplication/xmlhttp://lincsportal.ccs.miami.edu/dcic/api/download?path=LINCS_Data/HMS_LINCS&file=LDS-1128.tar.gzprimaryOK200MultiomicsMindy Davis1U54HG006097-01KINOMEscanFluorescence intensityLifeHarmonizomeABL1-phosphorylatedMK09MK03TESK1PIK3CA(E545A)BRAF(V600E)MYLKTBK1ABL1(T315I)-phosphorylatedMP2K2MP2K3AKT2AKT3MP2K1MP2K6AKT1MP2K7MK11MP2K4MK12MP2K5KGP2KGP1KC1G1CSNK2A1KC1G2DAPK1RPS6KA5(Kin.Dom.2-C-terminal)DAPK2CSNK2A2DAPK3KPCD2KPCD3KPCD1M3K13M3K12TYRO3MK01ANKK1VGFR2VGFR1PIK4CBCDK4-cyclinD3CDK4-cyclinD1TAK1PIP5K1ANIM1PIP5K1CLYNPLK4PLK3SRMSABL1(H396P)-nonphosphorylatedDMPKMK13MK14PI42CEIF2AK1PLK2PLK1BRAFTRKCMLTKTRKBCHK2TRKAPIP5K2BCDK11EGFR(T790M)CDK14MINKCDK15CDK16RETITKRSK1(Kin.Dom.1-N-terminal)RIOK2RIOK1KIT(V559D,V654A)KPCEKPCDRIPK2RIPK5RIPK4KPCIKPCLCITKPCTPIK3CA(H1047Y)TYK2(JH2domain-pseudokinase)ABL1(H396P)-phosphorylatedEGFRRPS6KA5(Kin.Dom.1-N-terminal)RSK4(Kin.Dom.1-N-terminal)HIPK4CSNK1A1RIOK3PIK3CA(Q546K)HIPK1HIPK3HIPK2TAOK3KIT(D816H)TAOK1TAOK2PKN2PKN1FRKEGFR(L747-S752del, P753S)MYLK2MYLK4DCAMKL2RSK1(Kin.Dom.2-C-terminal)DCAMKL3SLKSTK16PIM1NEK1NEK2PIM3NEK3PIM2ROS1MAP3K4CDKL2CDKL3CSNK1G3CDKL5ABL1(Q252H)-phosphorylatedABL1(F317I)-nonphosphorylatedDYRK1ADYRK1BSgK110GCN2(Kin.Dom.2,S808G)TNNI3KVRK2M4K3RPS6KA4(Kin.Dom.2-C-terminal)FLT3(N841I)M4K1MELKMAKMAPKAPK2MAPKAPK5TNIKTSSK1KCC2DCDKL1BLKBRSK1CSF1RBRSK2JAK1(JH1domain-catalytic)STK39SNARKPKMYT1RPS6KA4(Kin.Dom.1-N-terminal)PCTK3PCTK2JAK2(JH1domain-catalytic)KIT(A829P)STK33STK35STK36ABL2NEK9NEK4NEK5NEK6TNK2NEK7TNK1EGFR(L861Q)BMXEGFR(S752-I759del)M3K2CDK9CDK8CDK7M3K6MAP3K15M3K5CDK5CDK3MRCKBCDK2MRCKAAAK1ALKPFPK5(P.falciparum)BMPR2FLT3FLT4LRRK2PIK3CDPIK3C2GPIK3CBFLT3(K663Q)PIK3CGPIK3C2BTLK2TLK1EGFR(G719C)JNK1PKAC-betaJNK3MYO3BPIK3CALCKMYO3AMETEGFR(L747-T751del,Sins)ROCK1ROCK2SRCYSK1YSK4TTKFLT3(D835H)LKB1PHKG1PHKG2ABL1(T315I)-nonphosphorylatedCSKFYNIKKAIKKBIKKETIE2TIE1MERTKPKNB(M.tuberculosis)MTORSNRKABL1(Q252H)-nonphosphorylatedCTKEPHB6FGFR3(G697C)FLT3(ITD)EGFR(E746-A750del)CHEK1EPHB2DRAK1EPHB1DRAK2EPHB4EPHB3ACVR1EPHA5EPHA4EPHA7EPHA6MUSKEPHA8CSNK1DCSNK1EKKCC1BTKSIK3ULK3ULK2SIK1ULK1SIK2EPHA1EPHA3EPHA2TXKMST1RNLKTYK2(JH1domain-catalytic)NUAK1TRPM6SRPK2SRPK3ABL1(F317I)-phosphorylatedABL1(F317L)-phosphorylatedMLCKINSRPTK6DCLK1SRPK1ICKNDR1NDR2EGFR(L747-E749del, A750P)ADCK4ADCK3ABL1(M351T)-phosphorylatedACVRL1DDR1KIT(D816V)ERK3ERK4ERK5ERK8MST2MAP4K2MST3MST4SYKINSRRMST1MET(Y1235D)GAKHCKKITSGK3RET(M918T)DDR2YESKIT(V559D,T670I)PRKXPRKRCAMKK2PAK1PIK3CA(H1047L)PAK7PAK6MAP4K5PAK3PAK2MAP4K4PAK4MAP3K3MAP3K1ABL1(E255K)-phosphorylatedS6K1AXLCAMK1NEK11MLK1MLK2MLK3YANK1YANK2YANK3KIT(L576P)IGF1RPGFRAPGFRBPFCDPK1(P.falciparum)MET(M1250T)PIK3CA(I800L)ABL1(Y253F)-phosphorylatedOSR1CASKLOKPKAC-alphaERN1ABL1(F317L)-nonphosphorylatedPIK3CA(E545K)RAF1PRP4LRRK2(G2019S)PIK3CA(M1043I)RET(V804L)EGFR(L858R)GRK1AMPK-alpha1AMPK-alpha2IRAK1GRK4GRK7RIPK1MARK4PIK3CA(C420R)MARK3MARK2MARK1FAK1FAK2RET(V804M)RSK3(Kin.Dom.2-C-terminal)CLK4CLK3CLK2CLK1FERKIT(V559D)FESBMPR1BFGFR4FGFR3FGFR2BMPR1AFGFR1GSK3BGSK3ADYRK2EGFR(L858R,T790M)MAST1KCC4DMPK2ABL1-nonphosphorylatedFLT3(R834Q)CAMK1DPDPK1HUNKIRAK3RSK3(Kin.Dom.1-N-terminal)IRAK4TGFBR1TGFBR2EGFR(G719S)FGRLATS1ZAP70LATS2JAK3(JH1domain-catalytic)RSK2(Kin.Dom.1-N-terminal)CAMK1GCAMK2BLTKRSK4(Kin.Dom.2-C-terminal)CAMK2AACVR1BAURKCAURKBAURKAERBB3ERBB4MKNK1ERBB2MKNK2CAMK2GCDC2L2LIMK2CDC2L1LIMK1CDC2L5ACVR2BACVR2AWEE1SBK1TECWEE2PIK3CA(E542K)JAK1(JH2domain-pseudokinase)BIKECSNK1A1LFLT3(D835Y)http://lincsportal.ccs.miami.edu/datasets/#/view/LDS-1128HMS LINCS (Harvard Medical School)The KINOMEscan assay platform is based on a competition binding assay that is run for a compound of interest against each of a panel of 442 kinases. The assay has three components: a kinase-tagged phage, a test compound, and an immobilized ligand that the compound competes with to displace the kinase. The amount of kinase bound to the immobilized ligand is determined using quantitative PCR of the DNA tag. Kd values (nM) reported for each compound were determined using 11 serial threefold dilutions of test compound and a DMSO control. A null result means no inhibition of kinase binding to the ligand in the presence of the compound and low Kd means strong inhibition.LINCSWe tested the interaction of 72 kinase inhibitors with 442 kinases covering >80% of the human catalytic protein kinome. Our data show that, as a class, type II inhibitors are more selective than type I inhibitors, but that there are important exceptions to this trend. The data further illustrate that selective inhibitors have been developed against the majority of kinases targeted by the compounds tested. Analysis of the interaction patterns reveals a class of 'group-selective' inhibitors broadly active against a single subfamily of kinases, but selective outside that subfamily. The data set suggests compounds to use as tools to study kinases for which no dedicated inhibitors exist. It also provides a foundation for further exploring kinase inhibitor biology and toxicity, as well as for studying the structural basis of the observed interaction patterns. Our findings will help to realize the direct enabling potential of genomics for drug development and basic research about cellular signaling.Comprehensive analysis of kinase inhibitor selectivity.Davis Mindy I MI, Hunt Jeremy P JP, Herrgard Sanna S, Ciceri Pietro P, Wodicka Lisa M LM, Pallares Gabriel G, Hocker Michael M, Treiber Daniel K DK, Zarrinkar Patrick P PPAC220., N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo [2, 1-b] [1, AC-220, 3] benzothiazol 2-yl]phenyl}urea, Quizartinib, AC010220, QUIZARTINIB, (2E)-N-(4-(3-Chloro-4-Fluoroanilino)-7-(((3S)-Oxolan-3-Yl)Oxy)Quinoxazolin-6-yl)-4-(Dimethylamino)but-2-EnamideMGC130048, human being, SGCG_HUMAN, Activity, determination, Laboratory, A4, Gene, protein, Development, Medication, protein-containing complex, Foundation, Pharmaceutical Development, TYPE, Human, DAGA4, protein polypeptide chains, Structural, Homo sapiens, polypeptide chain, 35DAG, Gene Products, symptoms, Functional, Kinase, Research Activity, protein aggregate, MAM, gamma-SG, Drug Target Prediction, SCG3, Laboratory Research, Phosphotransferase, Man, Priorities, gamma sarcoglycan, study, Man (Taxonomy), Research, Comparative Genomics, Medication Development, proteins, Transphosphorylase, set, grupos, Pharmaceutical, gamma-sarcoglycan, kinase inhibitor, toxic potential, Development and Research, Research Priority, ATP Phosphotransferases, ATP, single organism signaling., screening, Genomics, findings, grupo, Data Set, 35 kDa dystrophin-associated glycoprotein, protein complex, Comparative, Modern, Proteins, SG-gamma, Research Priorities, Functional Genomics, Phosphotransferases, SGCG, LGMD2C, group, Priority, Prediction, native protein, natural protein, inhibition of kinase activity, Protein, chemical analysis, Research Activities, margin of safety, sarcoglycan, Target Prediction, Drug Target Predictions, Research and Development, Transphosphorylases, DMDA1, ensemble, Kinases, Rest, signs, gamma (35kDa dystrophin-associated glycoprotein), human, Protein Gene Products, Drug, Activities, Gene Proteins, Computational Prediction of Drug-Target Interactions, DMDA, signalling process, 35kD dystrophin-associated glycoprotein, Modern Man, SCARMD2, Drug Target, Structural Genomics, assay, groupe, humans, GruppeDimethyl, Methane, DNS, determination, (Deoxyribonucleotide)n, number, dimethylsulfoxyde, Rimso 100, Polymerase Chain Reactions, Null Results, Inverse, presence, Deoxyribonucleic acids, prevention, Sulphoxide, Inverse PCR, Deoxyribonucleic Acid, resilient, Kinase, Low, Polymerase Chain, prevention and control, Phosphotransferase, Rheumabene, S(O)Me2, Null Result, sulfinylbis(methane), strong, thymus nucleic acid, me75, reference sample, ligand, dimethyl sulphoxide, Inverse Polymerase Chain Reaction, Double Stranded, Deoxyribonucleic acid, Transphosphorylase, D17Mit170, T1, Rimso-50, preventive measures, dimetil sulfoxido, Rimso, Dimethylsulphinyl, Dimethylsulfoxide, scientific observation, Reaction, Double-Stranded DNA, Anchored PCR, (Deoxyribonucleotide)m, deoxyribonucleic acids, DNAn, ATP Phosphotransferases, Dimethylsulfoxid, ATP, Controlled, measuring, sulfinylbis-, Controlling, Ligand, DMSO, Anchored Polymerase Chain Reaction, preventive therapy, cou, dimethyli sulfoxidum, dmso, DNAn+1, methylsulfinylmethane, Negative Result, tough., Double-Stranded, Tl3, Tl2, Phosphotransferases, (Deoxyribonucleotide)n+m, count in organism, (CH3)2SO, Lr, Dimexide, Dimethylsulphoxide, chemical analysis, ds-DNA, Sulfoxide, desoxyribose nucleic acid, Sulfinylbis(methane), PCR, Rimso 50, Transphosphorylases, Anchored, Reactions, Nested, Nested Polymerase Chain Reaction, Kinases, Rimso50, prophylaxis, dimethyl sulfoxide, Sclerosol, Dimethyl Sulphoxide, polymerase chain reaction, control, ds DNA, Desoxyribonukleinsaeure, Bra, Nested PCR, assay, DNA, dimethyl sulfur oxideinhibition of kinase activity., kinase inhibitor, assay, determination, chemical analysisSERIAL, Group, Panel Device, N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo [2, Measured, MEASURED, Quizartinib, (2E)-N-(4-(3-Chloro-4-Fluoroanilino)-7-(((3S)-Oxolan-3-Yl)Oxy)Quinoxazolin-6-yl)-4-(Dimethylamino)but-2-Enamide, Serial Number, Panel, AC220., 1-b] [1, Measured Tumor Identification, AC-220, 3] benzothiazol 2-yl]phenyl}urea, AC010220, QUIZARTINIB, serialNumberTextfalseAC220 KINOMEscanFor the panel of kinases, the Kd is measured using 11 serial threefold dilutions of AC220.2016-06-032016-06-03LDS-112822037378