Reference Compound Data
Reference data & interaction maps for kinase inhibitor compounds
KINOME
scan 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 for download 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 |
|
Yes |
Yes |
Yes |
FLT3, CSF1R, VEGFR2 |
| AC220 |
Yes |
|
|
Yes |
FLT3 |
| AG-013736/Axitinib |
|
|
|
Yes |
|
| AMG-706 |
|
Yes |
|
Yes |
VEGFR2, FLT1, FLT4, KIT |
| AST-487 |
|
Yes |
|
Yes |
FLT3, KIT |
| AT-7519 |
|
|
|
Yes |
|
| AZD-1152HQPA |
|
Yes |
|
Yes |
AURKB |
| AZD-2171/Cediranib |
|
|
|
Yes |
|
| AZD-6244/ARRY-886 |
|
|
|
Yes |
|
| BI-2536 |
|
|
|
Yes |
|
| BIBF-1120(derivative) |
|
|
|
Yes |
|
| BIBW-2992/Afatinib |
|
|
|
Yes |
|
| BIRB-796 |
|
Yes |
Yes |
Yes |
p38-alpha |
| BMS-345541 |
|
|
|
Yes |
|
| BMS-387032/SNS-032 |
|
Yes |
|
Yes |
CDK2 |
| BMS-540215 |
|
|
|
Yes |
|
| CEP-701/Lestaurtinib |
Yes |
|
|
Yes |
JAK2 |
| CGP-52421 |
Yes |
|
|
|
FLT3 |
| CHIR-258/TKI-258 |
|
Yes |
|
Yes |
FLT3, FGFR3 |
| CHIR-265/RAF-265 |
|
Yes |
|
Yes |
BRAF, VEGFR2 |
| CI-1033 |
|
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 |
|
|
|
Yes |
|
| Flavopiridol |
|
Yes |
Yes |
Yes |
CDK1,2,4, & CDK9 |
| GDC-0879 |
|
|
|
Yes |
BRAF |
| GDC-0941 |
|
|
|
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 |
|
|
|
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 |
|
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 |
|
|
|
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 |
|
|
|
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 |
|
|
|
Yes |
|
| TG-100-115 |
|
|
|
Yes |
|
| Vatalanib/PTK-787 |
|
Yes |
Yes |
Yes |
VEGFR2 |
| VX-680/MK-0457 |
|
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)