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KdELECT® Kinase Assay Panel

Quantitate compound binding affinity against any kinase assay.  Inhibitor binding constants (Kd values) are calculated from duplicate 11-point dose-response curves.  Measurements are made under optimized conditions that generate true thermodynamic Kd values which facilitate direct comparison of inhibitor affinity across kinases. 

KdELECT may be used as a follow-up study tool to quantify binding affinity of compound-kinase interactions identified in primary screens, to supplement existing data, or support lead optimization and SAR activity.
 

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Panel Features & Benefits

  • 11-point dose response curve in duplicate
  • Broad dynamic range: can detect compounds with Kds <100 pM to >10 uM
  • Rapid turnaround time: 5 business days*
  • Flexible
  • Quantify binding to inactive or low activity kinases

*Eligible projects are activated every day. Data report is delivered on or before the fifth day after project begins. Premium services of 72-hour complete data delivery are available, please inquire with your account manager.
How it Works

Assay Sensitivity

Assay Sensitivity and Range
Binding constant (Kd) determinations for the indicated compounds against LOK demonstrate the broad range (> 5 logs) of interaction affinities quantitatively measured using the KINOMEscan assay platform. Assays are performed at low kinase concentrations (<0.1 nM), which enables the measurement of accurate Kd values in the pM range [click graph to enlarge].

 KdELECT Assay Panel

Listed below are the assays currently available for screening and profiling.

 
KGS ▲Kinase NameEntrez Gene Symbol
AAK1AP2 associated kinase 1AAK1
ABL1(E255K)-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(F317I)-nonphosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(F317I)-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(F317L)-nonphosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(F317L)-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(H396P)-nonphosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(H396P)-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(M351T)-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(Q252H)-nonphosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(Q252H)-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(T315I)-nonphosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(T315I)-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1(Y253F)-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1-nonphosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL1-phosphorylatedc-abl oncogene 1, receptor tyrosine kinaseABL1
ABL2v-abl Abelson murine leukemia viral oncogene homolog 2 (arg, Abelson-related gene)ABL2
ACVR1activin A receptor, type IACVR1
ACVR1Bactivin A receptor, type IBACVR1B
ACVR2Aactivin A receptor, type IIAACVR2A
ACVR2Bactivin A receptor, type IIBACVR2B
ACVRL1activin A receptor type II-like 1ACVRL1
ADCK3coenzyme Q8ACABC1
ADCK4aarF domain containing kinase 4ADCK4
AKT1v-akt murine thymoma viral oncogene homolog 1AKT1
AKT2v-akt murine thymoma viral oncogene homolog 2AKT2
AKT3AKT serine/threonine kinase 3AKT3
ALKanaplastic lymphoma receptor tyrosine kinaseALK
ALK(1151Tins)anaplastic lymphoma receptor tyrosine kinaseALK
ALK(C1156Y)anaplastic lymphoma receptor tyrosine kinaseALK
ALK(F1174L)anaplastic lymphoma receptor tyrosine kinaseALK
ALK(L1196M)anaplastic lymphoma receptor tyrosine kinaseALK
AMPK-alpha1protein kinase, AMP-activated, alpha 2 catalytic subunitPRKAA1
AMPK-alpha2protein kinase, AMP-activated, alpha 2 catalytic subunitPRKAA2
ANKK1ankyrin repeat and kinase domain containing 1ANKK1
ARK5NUAK family, SNF1-like kinase, 1NUAK1
ASK1mitogen-activated protein kinase kinase kinase 5MAP3K5
ASK2mitogen-activated protein kinase kinase kinase 6MAP3K6
AURKAaurora kinase AAURKA
AURKBaurora kinase BAURKB
AURKCaurora kinase CAURKC
AXLAXL receptor tyrosine kinaseAXL
BIKEBMP2 inducible kinaseBMP2K
BLKB lymphoid tyrosine kinaseBLK
BMPR1Abone morphogenetic protein receptor, type IABMPR1A
BMPR1Bbone morphogenetic protein receptor, type IBBMPR1B
BMPR2bone morphogenetic protein receptor, type II (serine/threonine kinase)BMPR2
BMXBMX non-receptor tyrosine kinaseBMX
BRAFv-raf murine sarcoma viral oncogene homolog B1BRAF
BRAF(V600E)v-raf murine sarcoma viral oncogene homolog B1BRAF
BRKprotein tyrosine kinase 6PTK6
BRSK1BR serine/threonine kinase 1BRSK1
BRSK2BR serine/threonine kinase 2BRSK2
BTKBruton agammaglobulinemia tyrosine kinaseBTK
BUB1BUB1 mitotic checkpoint serine/threonine kinaseBUB1
CAMK1calcium/calmodulin-dependent protein kinase ICAMK1
CAMK1Bpregnancy up-regulated nonubiquitous CaM kinasePNCK
CAMK1Dcalcium/calmodulin-dependent protein kinase IDCAMK1D
CAMK1Gcalcium/calmodulin-dependent protein kinase IGCAMK1G
CAMK2Acalcium/calmodulin-dependent protein kinase II alphaCAMK2A
CAMK2Bcalcium/calmodulin-dependent protein kinase II betaCAMK2B
CAMK2Dcalcium/calmodulin-dependent protein kinase II deltaCAMK2D
CAMK2Gcalcium/calmodulin-dependent protein kinase II gammaCAMK2G
CAMK4calcium/calmodulin-dependent protein kinase IVCAMK4
CAMKK1calcium/calmodulin-dependent protein kinase kinase 1, alphaCAMKK1
CAMKK2calcium/calmodulin-dependent protein kinase kinase 2, betaCAMKK2
CASKcalcium/calmodulin-dependent serine protein kinase (MAGUK family)CASK
CDC2L1cyclin-dependent kinase 11BCDK11B
CDC2L2cyclin-dependent kinase 11ACDC2L2
CDC2L5cyclin-dependent kinase 13CDK13
CDK1cyclin-dependent kinase 1 [ Homo sapiens (human) ]CDK1
CDK10cyclin-dependent kinase 10 [ Homo sapiens (human) ]CDK10
CDK11cyclin-dependent kinase 19CDK19
CDK12cyclin-dependent kinase 12 isoform 2 [Homo sapiens]CDK12
CDK2cyclin-dependent kinase 2CDK2
CDK20 cyclin-dependent kinase 20 [ Homo sapiens (human) ]CDK20
CDK3cyclin-dependent kinase 3CDK3
CDK4cyclin-dependent kinase 4CDK4
CDK4-cyclinD1cyclin-dependent kinase 4CDK4
CDK4-cyclinD1(F93L)cyclin-dependent kinase 4CDK4
CDK4-cyclinD3cyclin-dependent kinase 4CDK4
CDK5cyclin-dependent kinase 5CDK5
CDK6cyclin-dependent kinase 6 [ Homo sapiens (human) ]CDK6
CDK7cyclin-dependent kinase 7CDK7
CDK8cyclin-dependent kinase 8CDK8
CDK9cyclin-dependent kinase 9CDK9
CDKL1cyclin-dependent kinase-like 1 (CDC2-related kinase)CDKL1
CDKL2cyclin-dependent kinase-like 2 (CDC2-related kinase)CDKL2
CDKL3cyclin-dependent kinase-like 3CDKL3
CDKL5cyclin-dependent kinase-like 5CDKL5
CHEK1checkpoint kinase 1CHEK1
CHEK2checkpoint kinase 2CHEK2
CITcitron (rho-interacting, serine/threonine kinase 21)CIT
CLK1CDC-like kinase 1CLK1
CLK2CDC-like kinase 2CLK2
CLK3CDC-like kinase 3CLK3
CLK4CDC-like kinase 4CLK4
CSF1Rcolony stimulating factor 1 receptorCSF1R
CSF1R-autoinhibitedcolony stimulating factor 1 receptorCSF1R
CSKc-src tyrosine kinaseCSK
CSNK1A1casein kinase 1, alpha 1CSNK1A1
CSNK1A1Lcasein kinase 1, alpha 1-likeCSNK1A1L
CSNK1Dcasein kinase 1, deltaCSNK1D
CSNK1Ecasein kinase 1, epsilonCSNK1E
CSNK1G1casein kinase 1, gamma 1CSNK1G1
CSNK1G2casein kinase 1, gamma 2CSNK1G2
CSNK1G3casein kinase 1, gamma 3CSNK1G3
CSNK2A1casein kinase 2, alpha 1 polypeptideCSNK2A1
CSNK2A2casein kinase 2, alpha prime polypeptideCSNK2A2
CTKmegakaryocyte-associated tyrosine kinaseMATK
DAPK1death-associated protein kinase 1DAPK1
DAPK2death-associated protein kinase 2DAPK2
DAPK3death-associated protein kinase 3DAPK3
DCAMKL1doublecortin-like kinase 1DCLK1
DCAMKL2doublecortin-like kinase 2DCLK2
DCAMKL3doublecortin-like kinase 3DCLK3
DDR1discoidin domain receptor tyrosine kinase 1DDR1
DDR2discoidin domain receptor tyrosine kinase 2DDR2
DDR2(T654M)discoidin domain receptor tyrosine kinase 2DDR2
DLKmitogen-activated protein kinase kinase kinase 12MAP3K12
DMPKdystrophia myotonica-protein kinaseDMPK
DMPK2CDC42 binding protein kinase gamma (DMPK-like)CDC42BPG
DRAK1serine/threonine kinase 17aSTK17A
DRAK2serine/threonine kinase 17bSTK17B
DYRK1Adual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1ADYRK1A
DYRK1Bdual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1BDYRK1B
DYRK2dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 2DYRK2
EGFRepidermal growth factor receptorEGFR
EGFR(E746-A750del)epidermal growth factor receptorEGFR
EGFR(G719C)epidermal growth factor receptorEGFR
EGFR(G719S)epidermal growth factor receptorEGFR
EGFR(L747-E749del, A750P)epidermal growth factor receptorEGFR
EGFR(L747-S752del, P753S)epidermal growth factor receptorEGFR
EGFR(L747-T751del,Sins)epidermal growth factor receptorEGFR
EGFR(L858R)epidermal growth factor receptorEGFR
EGFR(L858R,T790M)epidermal growth factor receptorEGFR
EGFR(L861Q)epidermal growth factor receptorEGFR
EGFR(S752-I759del)epidermal growth factor receptorEGFR
EGFR(T790M)epidermal growth factor receptorEGFR
EIF2AK1eukaryotic translation initiation factor 2-alpha kinase 1EIF2AK1
EPHA1EPH receptor A1EPHA1
EPHA2EPH receptor A2EPHA2
EPHA3EPH receptor A3EPHA3
EPHA4EPH receptor A4EPHA4
EPHA5EPH receptor A5EPHA5
EPHA6EPH receptor A6EPHA6
EPHA7EPH receptor A7EPHA7
EPHA8EPH receptor A8EPHA8
EPHB1EPH receptor B1EPHB1
EPHB2EPH receptor B2EPHB2
EPHB3EPH receptor B3EPHB3
EPHB4EPH receptor B4EPHB4
EPHB6EPH receptor B6EPHB6
ERBB2erb-b2 receptor tyrosine kinase 2ERBB2
ERBB3erb-b2 receptor tyrosine kinase 3ERBB3
ERBB4erb-b2 receptor tyrosine kinase 4ERBB4
ERK1mitogen-activated protein kinase 3MAPK3
ERK1(Q122L)mitogen-activated protein kinase 3MAPK3
ERK2mitogen-activated protein kinase 1MAPK1
ERK3mitogen-activated protein kinase 6MAPK6
ERK4mitogen-activated protein kinase 4MAPK4
ERK5mitogen-activated protein kinase 7MAPK7
ERK8mitogen-activated protein kinase 15MAPK15
ERN1endoplasmic reticulum to nucleus signaling 1ERN1
FAKPTK2 protein tyrosine kinase 2PTK2
FERfer (fps/fes related) tyrosine kinaseFER
FESfeline sarcoma oncogeneFES
FGFR1fibroblast growth factor receptor 1FGFR1
FGFR2fibroblast growth factor receptor 2FGFR2
FGFR2(N550K)fibroblast growth factor receptor 2FGFR2
FGFR3fibroblast growth factor receptor 3FGFR3
FGFR3(G697C)fibroblast growth factor receptor 3FGFR3
FGFR3(K650E)fibroblast growth factor receptor 3FGFR3
FGFR3(V555M)fibroblast growth factor receptor 3FGFR3
FGFR4fibroblast growth factor receptor 4FGFR4
FGRFGR proto-oncogene, Src family tyrosine kinaseFGR
FLT1fms-related tyrosine kinase 1 (vascular endothelial growth factor/vascular permeability factor receptor)FLT1
FLT3fms-related tyrosine kinase 3FLT3
FLT3(D835H)fms-related tyrosine kinase 3FLT3
FLT3(D835V)fms-related tyrosine kinase 3FLT3
FLT3(D835Y)fms-related tyrosine kinase 3FLT3
FLT3(ITD)fms-related tyrosine kinase 3FLT3
FLT3(ITD,D835V)fms-related tyrosine kinase 3FLT3
FLT3(ITD,F691L)fms-related tyrosine kinase 3FLT3
FLT3(K663Q)fms-related tyrosine kinase 3FLT3
FLT3(N841I)fms-related tyrosine kinase 3FLT3
FLT3(R834Q)fms-related tyrosine kinase 3FLT3
FLT3-autoinhibitedfms-related tyrosine kinase 3FLT3
FLT4fms-related tyrosine kinase 4FLT4
FRKfyn-related kinaseFRK
FYNFYN oncogene related to SRC, FGR, YESFYN
GAKcyclin G associated kinaseGAK
GCN2(Kin.Dom.2,S808G)eukaryotic translation initiation factor 2 alpha kinase 4EIF2AK4
GRK1G protein-coupled receptor kinase 1GRK1
GRK2adrenergic, beta, receptor kinase 1 [ Homo sapiens (human) ] ADRBK1
GRK3adrenergic, beta, receptor kinase 2 [ Homo sapiens (human) ] ADRBK2
GRK4G protein-coupled receptor kinase 4GRK4
GRK7G protein-coupled receptor kinase 7GRK7
GSK3Aglycogen synthase kinase 3 alphaGSK3A
GSK3Bglycogen synthase kinase 3 betaGSK3B
HASPINgerm cell associated 2 (haspin)GSG2
HCKhemopoietic cell kinaseHCK
HIPK1homeodomain interacting protein kinase 1HIPK1
HIPK2homeodomain interacting protein kinase 2HIPK2
HIPK3homeodomain interacting protein kinase 3HIPK3
HIPK4homeodomain interacting protein kinase 4HIPK4
HPK1mitogen-activated protein kinase kinase kinase kinase 1MAP4K1
HUNKhormonally up-regulated Neu-associated kinaseHUNK
ICKintestinal cell (MAK-like) kinaseICK
IGF1Rinsulin-like growth factor 1 receptorIGF1R
IKK-alphaconserved helix-loop-helix ubiquitous kinaseCHUK
IKK-betainhibitor of kappa light polypeptide gene enhancer in B-cells, kinase betaIKBKB
IKK-epsiloninhibitor of kappa light polypeptide gene enhancer in B-cells, kinase epsilonIKBKE
INSRinsulin receptorINSR
INSRRinsulin receptor-related receptorINSRR
IRAK1interleukin-1 receptor-associated kinase 1IRAK1
IRAK2interleukin-1 receptor-associated kinase 2 [ Homo sapiens (human) ]IRAK2
IRAK3interleukin-1 receptor-associated kinase 3IRAK3
IRAK4interleukin-1 receptor-associated kinase 4IRAK4
ITKIL2-inducible T-cell kinaseITK
JAK1(JH1domain-catalytic)Janus kinase 1JAK1
JAK1(JH2domain-pseudokinase)Janus kinase 1JAK1
JAK2(JH1domain-catalytic)Janus kinase 2JAK2
JAK3(JH1domain-catalytic)Janus kinase 3JAK3
JNK1mitogen-activated protein kinase 8MAPK8
JNK2mitogen-activated protein kinase 9MAPK9
JNK3mitogen-activated protein kinase 10MAPK10
KITv-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
KIT(A829P)v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
KIT(D816H)v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
KIT(D816V)v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
KIT(L576P)v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
KIT(V559D)v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
KIT(V559D,T670I)v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
KIT(V559D,V654A)v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
KIT-autoinhibitedv-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homologKIT
LATS1large tumor suppressor kinase 1LATS1
LATS2large tumor suppressor kinase 2LATS2
LCKlymphocyte-specific protein tyrosine kinaseLCK
LIMK1LIM domain kinase 1LIMK1
LIMK2LIM domain kinase 2LIMK2
LKB1serine/threonine kinase 11STK11
LOKserine/threonine kinase 10STK10
LRRK2leucine-rich repeat kinase 2LRRK2
LRRK2(G2019S)leucine-rich repeat kinase 2LRRK2
LTKleukocyte receptor tyrosine kinaseLTK
LYNv-yes-1 Yamaguchi sarcoma viral related oncogene homologLYN
LZKmitogen-activated protein kinase kinase kinase 13MAP3K13
MAKmale germ cell-associated kinaseMAK
MAP3K1mitogen-activated protein kinase kinase kinase 1MAP3K1
MAP3K15mitogen-activated protein kinase kinase kinase 15MAP3K15
MAP3K2mitogen-activated protein kinase kinase kinase 2MAP3K2
MAP3K3mitogen-activated protein kinase kinase kinase 3MAP3K3
MAP3K4mitogen-activated protein kinase kinase kinase 4MAP3K4
MAP4K2mitogen-activated protein kinase kinase kinase kinase 2MAP4K2
MAP4K3mitogen-activated protein kinase kinase kinase kinase 3MAP4K3
MAP4K4mitogen-activated protein kinase kinase kinase kinase 4MAP4K4
MAP4K5mitogen-activated protein kinase kinase kinase kinase 5MAP4K5
MAPKAPK2mitogen-activated protein kinase-activated protein kinase 2MAPKAPK2
MAPKAPK5mitogen-activated protein kinase-activated protein kinase 5MAPKAPK5
MARK1MAP/microtubule affinity-regulating kinase 1MARK1
MARK2MAP/microtubule affinity-regulating kinase 2MARK2
MARK3MAP/microtubule affinity-regulating kinase 3MARK3
MARK4MAP/microtubule affinity-regulating kinase 4MARK4
MAST1microtubule associated serine/threonine kinase 1MAST1
MEK1mitogen-activated protein kinase kinase 1MAP2K1
MEK2mitogen-activated protein kinase kinase 2MAP2K2
MEK3mitogen-activated protein kinase kinase 3MAP2K3
MEK4mitogen-activated protein kinase kinase 4MAP2K4
MEK5mitogen-activated protein kinase kinase 5MAP2K5
MEK6mitogen-activated protein kinase kinase 6MAP2K6
MELKmaternal embryonic leucine zipper kinaseMELK
MERTKc-mer proto-oncogene tyrosine kinaseMERTK
METmet proto-oncogene (hepatocyte growth factor receptor)MET
MET(M1250T)met proto-oncogene (hepatocyte growth factor receptor)MET
MET(Y1235D)met proto-oncogene (hepatocyte growth factor receptor)MET
MINKmisshapen like kinase 1MINK1
MKK7mitogen-activated protein kinase kinase 7MAP2K7
MKNK1MAP kinase interacting serine/threonine kinase 1MKNK1
MKNK2MAP kinase interacting serine/threonine kinase 2MKNK2
MLCKmyosin light chain kinase 3MYLK3
MLK1mitogen-activated protein kinase kinase kinase 9MAP3K9
MLK2mitogen-activated protein kinase kinase kinase 10MAP3K10
MLK3mitogen-activated protein kinase kinase kinase 11MAP3K11
MLKLmixed lineage kinase domain-like protein isoform 1 [Homo sapiens]MLKL
MLKL(full-length)mixed lineage kinase domain-like protein isoform 1 [Homo sapiens]MLKL
MRCKACDC42 binding protein kinase alpha (DMPK-like)CDC42BPA
MRCKBCDC42 binding protein kinase beta (DMPK-like)CDC42BPB
MST1serine/threonine kinase 4STK4
MST1Rmacrophage stimulating 1 receptor (c-met-related tyrosine kinase)MST1R
MST2serine/threonine kinase 3STK3
MST3serine/threonine kinase 24STK24
MST4serine/threonine protein kinase MST4MST4
MTORmechanistic target of rapamycin (serine/threonine kinase)MTOR
MUSKmuscle, skeletal, receptor tyrosine kinaseMUSK
MYLKmyosin light chain kinaseMYLK
MYLK2myosin light chain kinase 2MYLK2
MYLK4myosin light chain kinase family, member 4MYLK4
MYO3Amyosin IIIAMYO3A
MYO3Bmyosin IIIBMYO3B
NDR1serine/threonine kinase 38STK38
NDR2serine/threonine kinase 38 likeSTK38L
NEK1NIMA (never in mitosis gene a)-related kinase 1NEK1
NEK10NIMA (never in mitosis gene a)- related kinase 10NEK10
NEK11NIMA (never in mitosis gene a)-related kinase 11NEK11
NEK2NIMA (never in mitosis gene a)-related kinase 2NEK2
NEK3NIMA (never in mitosis gene a)-related kinase 3NEK3
NEK4NIMA (never in mitosis gene a)-related kinase 4NEK4
NEK5NIMA (never in mitosis gene a)-related kinase 5NEK5
NEK6NIMA (never in mitosis gene a)-related kinase 6NEK6
NEK7NIMA (never in mitosis gene a)-related kinase 7NEK7
NEK9NIMA (never in mitosis gene a)-related kinase 9NEK9
NIKmitogen-activated protein kinase kinase kinase 14MAP3K14
NIM1serine/threonine-protein kinase NIM1MGC42105
NLKnemo-like kinaseNLK
OSR1oxidative-stress responsive 1OXSR1
p38-alphamitogen-activated protein kinase 14MAPK14
p38-betamitogen-activated protein kinase 11MAPK11
p38-deltamitogen-activated protein kinase 13MAPK13
p38-gammamitogen-activated protein kinase 12MAPK12
PAK1p21 protein (Cdc42/Rac)-activated kinase 1PAK1
PAK2p21 protein (Cdc42/Rac)-activated kinase 2PAK2
PAK3p21 protein (Cdc42/Rac)-activated kinase 3PAK3
PAK4p21 protein (Cdc42/Rac)-activated kinase 4PAK4
PAK6p21 protein (Cdc42/Rac)-activated kinase 6PAK6
PAK7p21 protein (Cdc42/Rac)-activated kinase 7PAK7
PASKPAS domain containing serine/threonine kinase [ Homo sapiens (human) ]PASK
PCTK1cyclin-dependent kinase 16CDK16
PCTK2cyclin-dependent kinase 17CDK17
PCTK3cyclin-dependent kinase 18CDK18
PDGFRAplatelet-derived growth factor receptor, alpha polypeptidePDGFRA
PDGFRBplatelet-derived growth factor receptor, beta polypeptidePDGFRB
PDPK13-phosphoinositide dependent protein kinase-1PDPK1
PFCDPK1(P.falciparum)Calcium-dependent protein kinase 1CDPK1
PFPK5(P.falciparum)Protein Kinase 5MAL13P1.279
PFTAIRE2Cyclin-Dependent Kinase 15CDK15
PFTK1Cyclin-Dependent Kinase 14CDK14
PHKG1phosphorylase kinase, gamma 1 (muscle)PHKG1
PHKG2phosphorylase kinase, gamma 2 (testis)PHKG2
PIK3C2Bphosphoinositide-3-kinase, class 2, beta polypeptidePIK3C2B
PIK3C2Gphosphoinositide-3-kinase, class 2, gamma polypeptidePIK3C2G
PIK3CAphosphoinositide-3-kinase, catalytic, alpha polypeptidePIK3CA
PIK3CA(C420R)phosphoinositide-3-kinase, catalytic, alpha polypeptidePIK3CA
PIK3CA(E542K)phosphoinositide-3-kinase, catalytic, alpha polypeptidePIK3CA
PIK3CA(E545A)phosphoinositide-3-kinase, catalytic, alpha polypeptidePIK3CA
PIK3CA(E545K)phosphoinositide-3-kinase, catalytic, alpha polypeptidePIK3CA
PIK3CA(H1047L)phosphoinositide-3-kinase, catalytic, alpha polypeptidePIK3CA
PIK3CA(H1047Y)phosphoinositide-3-kinase, catalytic, alpha polypeptidePIK3CA
PIK3CA(I800L)phosphoinositide-3-kinase, catalytic, alpha polypeptidePIK3CA
PIK3CA(M1043I)phosphoinositide-3-kinase, catalytic, alpha polypeptidePIK3CA
PIK3CA(Q546K)phosphoinositide-3-kinase, catalytic, alpha polypeptidePIK3CA
PIK3CBphosphoinositide-3-kinase, catalytic, beta polypeptidePIK3CB
PIK3CDphosphoinositide-3-kinase, catalytic, delta polypeptidePIK3CD
PIK3CGphosphoinositide-3-kinase, catalytic, gamma polypeptidePIK3CG
PIK4CBphosphatidylinositol 4-kinase, catalytic, betaPI4KB
PIKFYVEphosphoinositide kinase, FYVE finger containing [ Homo sapiens (human) ] PIKFYVE
PIM1pim-1 oncogenePIM1
PIM2pim-2 oncogenePIM2
PIM3pim-3 oncogenePIM3
PIP5K1Aphosphatidylinositol-4-phosphate 5-kinase, type I, alphaPIP5K1A
PIP5K1Cphosphatidylinositol-4-phosphate 5-kinase, type I, gammaPIP5K1C
PIP5K2Bphosphatidylinositol-5-phosphate 4-kinase, type II, betaPIP4K2B
PIP5K2Cphosphatidylinositol-5-phosphate 4-kinase, type II, gammaPIP4K2C
PKAC-alphaprotein kinase, cAMP-dependent, catalytic, alphaPRKACA
PKAC-alpha(L206R)cAMP-dependent protein kinase catalytic subunit alpha isoform Calpha1 [Homo sapiens]PRKACA
PKAC-betaprotein kinase, cAMP-dependent, catalytic, betaPRKACB
PKMYT1protein kinase, membrane associated tyrosine/threonine 1PKMYT1
PKN1protein kinase N1PKN1
PKN2protein kinase N2PKN2
PKNB(M.tuberculosis)Transmembrane Serine/Threonine-Protein Kinase BpknB
PLK1polo-like kinase 1PLK1
PLK2polo-like kinase 2PLK2
PLK3polo-like kinase 3PLK3
PLK4polo-like kinase 4PLK4
PRKCDprotein kinase C, deltaPRKCD
PRKCEprotein kinase C, epsilonPRKCE
PRKCHprotein kinase C, etaPRKCH
PRKCIprotein kinase C, iotaPRKCI
PRKCQprotein kinase C, thetaPRKCQ
PRKD1protein kinase D1PRKD1
PRKD2protein kinase D2PRKD2
PRKD3protein kinase D3PRKD3
PRKG1protein kinase, cGMP-dependent, type IPRKG1
PRKG2protein kinase, cGMP-dependent, type IIPRKG2
PRKReukaryotic translation initiation factor 2-alpha kinase 2EIF2AK2
PRKXprotein kinase, X-linkedPRKX
PRP4pre-mRNA processing factor 4BPRPF4B
PYK2PTK2B protein tyrosine kinase 2 betaPTK2B
QSKSIK family kinase 3KIAA0999
RAF1v-raf-1 murine leukemia viral oncogene homolog 1RAF1
RETret proto-oncogeneRET
RET(A883F)ret proto-oncogeneRET
RET(M918T)ret proto-oncogeneRET
RET(V804E)ret proto-oncogeneRET
RET(V804L)ret proto-oncogeneRET
RET(V804M)ret proto-oncogeneRET
RIOK1RIO kinase 1RIOK1
RIOK2RIO kinase 2RIOK2
RIOK3RIO kinase 3RIOK3
RIPK1receptor (TNFRSF)-interacting serine-threonine kinase 1RIPK1
RIPK2receptor-interacting serine-threonine kinase 2RIPK2
RIPK3receptor-interacting serine-threonine kinase 3RIPK3
RIPK4receptor-interacting serine-threonine kinase 4RIPK4
RIPK5dual serine/threonine and tyrosine protein kinaseDSTYK
ROCK1Rho-associated, coiled-coil containing protein kinase 1ROCK1
ROCK2Rho-associated, coiled-coil containing protein kinase 2ROCK2
ROS1c-ros oncogene 1 , receptor tyrosine kinaseROS1
RPS6KA4(Kin.Dom.1-N-terminal)ribosomal protein S6 kinase, 90kDa, polypeptide 4RPS6KA4
RPS6KA4(Kin.Dom.2-C-terminal)ribosomal protein S6 kinase, 90kDa, polypeptide 4RPS6KA4
RPS6KA5(Kin.Dom.1-N-terminal)ribosomal protein S6 kinase, 90kDa, polypeptide 5RPS6KA5
RPS6KA5(Kin.Dom.2-C-terminal)ribosomal protein S6 kinase, 90kDa, polypeptide 5RPS6KA5
RSK1(Kin.Dom.1-N-terminal)ribosomal protein S6 kinase, 90kDa, polypeptide 1RPS6KA1
RSK1(Kin.Dom.2-C-terminal)ribosomal protein S6 kinase, 90kDa, polypeptide 1RPS6KA1
RSK2(Kin.Dom.1-N-terminal)ribosomal protein S6 kinase, 90kDa, polypeptide 3RPS6KA3
RSK2(Kin.Dom.2-C-terminal)ribosomal protein S6 kinase alpha-3RPS6KA3
RSK3(Kin.Dom.1-N-terminal)ribosomal protein S6 kinase, 90kDa, polypeptide 2RPS6KA2
RSK3(Kin.Dom.2-C-terminal)ribosomal protein S6 kinase, 90kDa, polypeptide 2RPS6KA2
RSK4(Kin.Dom.1-N-terminal)ribosomal protein S6 kinase, 90kDa, polypeptide 6RPS6KA6
RSK4(Kin.Dom.2-C-terminal)ribosomal protein S6 kinase, 90kDa, polypeptide 6RPS6KA6
S6K1ribosomal protein S6 kinase, 70kDa, polypeptide 1RPS6KB1
SBK1SH3-binding domain kinase 1SBK1
SGKserum/glucocorticoid regulated kinase 1SGK1
SgK110Putative uncharacterized serine/threonine-protein kinase (Sugen kinase 110)SgK110
SGK2serum/glucocorticoid regulated kinase 2SGK2
SGK3serum/glucocorticoid regulated kinase family, member 3SGK3
SIKsalt-inducible kinase 1SIK1
SIK2salt-inducible kinase 2SIK2
SLK STE20 like kinaseSLK
SNARKNUAK family, SNF1-like kinase, 2NUAK2
SNRKSNF related kinaseSNRK
SRCSRC proto-oncogene, non-receptor tyrosine kinaseSRC
SRMSsrc-related kinase lacking C-terminal regulatory tyrosine and N-terminal myristylation sitesSRMS
SRPK1SFRS protein kinase 1SRPK1
SRPK2SFRS protein kinase 2SRPK2
SRPK3SFRS protein kinase 3SRPK3
STK16serine/threonine kinase 16STK16
STK33serine/threonine kinase 33STK33
STK35serine/threonine kinase 35STK35
STK36serine/threonine kinase 36STK36
STK39serine/threonine kinase 39STK39
SYKspleen tyrosine kinaseSYK
TAK1mitogen-activated protein kinase kinase kinase 7MAP3K7
TAOK1TAO kinase 1TAOK1
TAOK2TAO kinase 2TAOK2
TAOK3TAO kinase 3TAOK3
TBK1TANK-binding kinase 1TBK1
TECtec protein tyrosine kinaseTEC
TESK1testis-specific kinase 1TESK1
TGFBR1transforming growth factor, beta receptor 1TGFBR1
TGFBR2transforming growth factor, beta receptor II (70/80kDa)TGFBR2
TIE1tyrosine kinase with immunoglobulin-like and EGF-like domains 1TIE1
TIE2TEK tyrosine kinase, endothelialTEK
TLK1tousled-like kinase 1TLK1
TLK2tousled-like kinase 2TLK2
TNIKTRAF2 and NCK interacting kinaseTNIK
TNK1tyrosine kinase, non-receptor, 1TNK1
TNK2tyrosine kinase, non-receptor, 2TNK2
TNNI3KTNNI3 interacting kinaseTNNI3K
TRKAneurotrophic tyrosine kinase, receptor, type 1NTRK1
TRKBneurotrophic tyrosine kinase, receptor, type 2NTRK2
TRKCneurotrophic tyrosine kinase, receptor, type 3NTRK3
TRPM6transient receptor potential cation channel, subfamily M, member 6TRPM6
TSSK1Btestis-specific serine kinase 1BTSSK1B
TSSK3testis-specific serine/threonine-protein kinase 3TSSK3
TTKTTK protein kinaseTTK
TXKTXK tyrosine kinaseTXK
TYK2(JH1domain-catalytic)tyrosine kinase 2TYK2
TYK2(JH2domain-pseudokinase)tyrosine kinase 2TYK2
TYRO3TYRO3 protein tyrosine kinaseTYRO3
ULK1unc-51-like kinase 1ULK1
ULK2unc-51-like kinase 2ULK2
ULK3unc-51-like kinase 3ULK3
VEGFR2kinase insert domain receptor (a type III receptor tyrosine kinase)KDR
VPS34phosphatidylinositol 3-kinase, catalytic subunit type 3PIK3C3
VRK2vaccinia related kinase 2VRK2
WEE1WEE1 G2 checkpoint kinase WEE1
WEE2WEE1 homolog 2WEE2
WNK1WNK lysine deficient protein kinase 1WNK1
WNK2WNK lysine deficient protein kinase 2WNK2
WNK3WNK lysine deficient protein kinase 3WNK3
WNK4WNK lysine deficient protein kinase 4WNK4
YANK1serine/threonine kinase 32ASTK32A
YANK2serine/threonine kinase 32BSTK32B
YANK3serine/threonine kinase 32CSTK32C
YESv-yes-1 Yamaguchi sarcoma viral oncogene homolog 1YES1
YSK1serine/threonine kinase 25STK25
YSK4mitogen-activated protein kinase kinase kinase 19MAP3K19
ZAKsterile alpha motif and leucine zipper containing kinase AZK ZAK
ZAP70zeta-chain (TCR) associated protein kinase 70kDaZAP70
 

KdELECT Study Data Reports (11-point dose response curves)

KdELECT Study reports are delivered as three separate data files and include:

1. Study Report - A PDF file containing a project summary, description of the assay protocol and algorithm used to fit curves, color coded data matrix which provides a Kd values for each compound against the tested kinases and curve images which display the data points, and the best fit curve for each Kd determination (view Kd sample report).

2. Data Report - A spreadsheet file containing the average Kd value reported from duplicate Kd determinations (reported in nM), which can be easily imported into most data management and visualization tools (including TREEspot Profile Visualization Tool).

3. Raw Data Report - A spreadsheet containing data values obtained for each replicate (reported as relative signal) for each compound at each tested concentration.

Sample Curve Images

sample Kd data

Binding constant (Kd) determination for the interaction between Compound F and Aurora Kinase B (AURKB).  Kd values were calculated by fitting dose-response curves to the Hill binding equation using the Levenberg–Marquardt algorithm.  Duplicate Kd values calculated for this interaction were 36.5 nM and 24.3 nM

Frequently Asked Questions About Kd Determinations (dissociation constants)

What is the difference between a Kd and an IC50?

Activity-based assays provide IC50 values, which are defined as a measure of a compound's effectiveness in inhibiting a kinase, and an indication of the inhibitor concentration required to reduce kinase activity by 50%. In other words it is the half maximal (50%) inhibitory concentration (IC) of a substance (50% IC, or IC50).  In contrast, KINOMEscan competition binding assays do not measure kinase activity.  Instead, compound affinity for a kinase is measured at a range of compound concentrations to calculate potency, expressed as a dissociation constant, and is a true thermodynamic constant used to describe binding affinity.  The formula used to describe this:

Kd = ([K][I]/[C])

[K] = molar concentration of non-inhibitor bound kinase at equilibrium
[I] = molar concentration of the free inhibitor at equilibrium
[C] = molar concentration of kinase-inhibitor complex at equilibrium

How are IC50 and KD values correlated?

IC50 is not a direct indicator of affinity, nor is Kd a direct indicator of inhibition.  However, the two can be related using the Cheng-Prusoff equation:

 Ki = (IC50)/(1+([S]/[Km]))

Ki = binding affinity of the inhibitor; an absolute value or inhibition constant
IC50 = the inhibitory strength of the compound
[S] = substrate concentration
[Km] = substrate concentration where kinase activity is at half maximal

How do the two values correlate for measured interactions?

Since 2005, KINOMEscan scientists have extensively assessed and characterized binding interactions against a panel of over 100 reference compounds, and have published on over 40 of them.  This set of compounds includes approved therapeutics, clinical candidates and tool compounds against a growing panel of kinase assays.  A list of profiled compounds, links to publications and supplementary data may be found in our Reference Compound Data page.  This body of data collectively validates the correlation and agreement between published IC50 literature values and corresponding Kd values for most compound-kinase interactions.  In general, good agreement between IC50 values of small molecule kinase inhibitors described in literature and corresponding Kd values for those interactions can be seen.  In cases of data divergence, there are often revealing explanations and may provide additional knowledge and context around compound characterization efforts.