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Reference Data & Interaction Maps for Kinase Inhibitor Compounds

KINOMEscan® data has been widely published and referenced in leading publications and support many landmark kinase inhibitors papers.  These data represent among the most extensive collection of compound selectivity and interaction data available and is a powerful resource for investigators desiring to benchmark novel compounds against known drugs, gain valuable insights into the tractability of the kinome or identify important compound/kinase clusters.  This complimentary resource is available below. 

All compounds were profiled in two steps:  Each compound screened against a panel of assays at a single concentration of 10 μM to identify candidate kinase targets.  For each interaction observed in the primary screen (Percent of Control <35%), quantitative dissociation constant (Kd) was determined. Data reported are Kd values.

Profiled Compounds

Inhibitor Blood. (2009) Nat. Biotech. (2008) Nat. Biotech. (2005) Nat. Biotech. (2011) Primary Targets
A-674563       Yes  
AB-1010/Masitinib       Yes  
ABT-869/Linifanib   Yes Yes Yes FLT3, CSF1R, VEGFR2
AC220/Quizartinib Yes     Yes FLT3
AG-013736/Axitinib       Yes  
AMG-706/Motesanib   Yes   Yes VEGFR2, FLT1, FLT4, KIT
AST-487   Yes   Yes FLT3, KIT
AT-7519   Yes   Yes  
AZD-1152HQPA/Barasertib   Yes   Yes AURKB
AZD-2171/Cediranib       Yes  
AZD-6244/ARRY-886/Selumetinib       Yes  
BI-2536       Yes  
BIBF-1120(derivative)/Nintedanib       Yes  
BIBW-2992/Afatinib       Yes  
BIRB-796/Doramapimod   Yes Yes Yes p38-alpha
BMS-345541       Yes  
BMS-387032/SNS-032   Yes   Yes CDK2
BMS-540215/Brivanib       Yes  
CEP-701/Lestaurtinib Yes     Yes JAK2
CGP-52421 Yes       FLT3
CHIR-258/TKI-258/Dovitinib   Yes   Yes FLT3, FGFR3
CHIR-265/RAF-265   Yes   Yes BRAF, VEGFR2
CI-1033/Canertinib   Yes Yes Yes EGFR, ERBB2
CI-1040       Yes  
CP-690550/tofacitinib   Yes   Yes JAK3
CP-724714   Yes     ERBB2
Crizotinib       Yes  
Dasatinib   Yes   Yes ABL1, SRC
EKB-569   Yes Yes   EGFR
Erlotinib   Yes Yes Yes EGFR
EXEL-2880/GSK1363089/Foretinib       Yes  
Flavopiridol/Alvocidib   Yes Yes Yes CDK1,2,4, & CDK9
GDC-0879       Yes BRAF
GDC-0941/Pictilisib       Yes pan-PI3K
Gefitinib   Yes Yes Yes EGFR
GSK-1838705A       Yes  
GSK-461364A       Yes  
GSK-690693       Yes  
GW-2580   Yes   Yes CSF1R
HKI-272/Neratinib       Yes EGFR
Imatinib   Yes Yes Yes ABL1, KIT, PDGFRB
INCB018424/Ruxolitinib       Yes JAK1, JAK2
JNJ-28312141       Yes  
JNJ-7706621   Yes     CDK2, CDK1, AURKB
Ki-20227       Yes  
KW-2449       Yes  
Lapatinib/GW-2016   Yes Yes Yes EGFR, ERBB2
LY-317615/Enzastaurin       Yes  
LY-333531/Ruboxistaurin   Yes Yes Yes PRKCB1
MLN-120B       Yes  
MLN-518/Tandutinib Yes Yes Yes Yes FLT3, KIT
MLN-8054   Yes   Yes AURKA
Nilotinib/AMN107       Yes  
Pazopanib/GW-786034   Yes   Yes FLT1, FLT4, PDGFRA, PDGFRB, VEGFR1, VEGFR2, VEGFR3
PD-173955       Yes  
PHA-665752       Yes  
PI-103   Yes   Yes PIK3CA
Midostaurin/PKC-412 Yes Yes Yes Yes FLT3, KIT
PP-242       Yes  
PLX-4720       Yes  
R406/Tamatinib       Yes  
R547       Yes  
Roscovitine/CYC202   Yes Yes   CDK1, CDK2, CDK5
SB-202190   Yes Yes   p38-alpha
SB-203580   Yes Yes Yes p38-alpha
SB-431542   Yes     TGFBR1/ALK5, ACVR1B/ALK4
SGX-523       Yes  
SKI-606/Bosutinib       Yes  
Sorafenib/BAY-43-9006 Yes Yes Yes Yes VEGFR2, BRAF
SP600125     Yes   JNK
Staurosporine   Yes Yes Yes PRKCH, Pan-inhibitor
SU-14813   Yes   Yes FLT1, FLT3, KIT, PDGFRB, VEGFR2
Sunitinib/SU-11248 Yes Yes Yes Yes KIT, FLT3, VEGFR2
TAE-684       Yes  
TG-101348/Fedratinib       Yes  
TG-100-115       Yes  
Vatalanib/PTK-787   Yes Yes Yes VEGFR2
VX-680/MK-0457/Tozasertib   Yes   Yes AURKA, AURKB, AURKC
VX-745   Yes Yes Yes p38-alpha
ZD-6474/Vandetanib   Yes Yes Yes VEGFR2, EGFR, RET

Source References

Davis, M.I. el al. Comprehensive analysis of kinase inhibitor selectivity.  Nature Biotechnol. 29, 1046–1051 (2011)

Zarrinkar, P.P. et al. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood. First Edition Paper, prepublished online August 4, 2009; DOI 10.1182/blood-2009-05-222034

Karaman, M.W. et al. A quantitative analysis of kinase inhibitor selectivity. Nat. Biotechnol. 26, 127-132 (2008)

Fabian, M.A. et al. A small molecule-kinase interaction map for clinical kinase inhibitors. Nat. Biotechnol. 23, 329-336 (2005)