death associated protein kinase 1 (Death-associated kinase (DAPK) family)

DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 1-2
Key to terms and symbols Click column headers to sort
Target used in screen: DAPK1
Ligand Sp. Type Action Value (-log10) Parameter Value (nM) Parameter
staurosporine Hs Inhibitor Inhibition 8.9 pKd 1.4 Kd
fedratinib Hs Inhibitor Inhibition 7.8 pKd 16.0 Kd
tamatinib Hs Inhibitor Inhibition 7.3 pKd 55.0 Kd
ruxolitinib Hs Inhibitor Inhibition 7.1 pKd 72.0 Kd
lestaurtinib Hs Inhibitor Inhibition 7.1 pKd 80.0 Kd
PP-242 Hs Inhibitor Inhibition 7.0 pKd 97.0 Kd
sunitinib Hs Inhibitor Inhibition 6.9 pKd 120.0 Kd
SU-14813 Hs Inhibitor Inhibition 6.6 pKd 270.0 Kd
KW-2449 Hs Inhibitor Inhibition 6.4 pKd 360.0 Kd
BI-2536 Hs Inhibitor Inhibition 6.3 pKd 540.0 Kd
GSK-1838705A Hs Inhibitor Inhibition 6.2 pKd 620.0 Kd
ruboxistaurin Hs Inhibitor Inhibition 6.0 pKd 970.0 Kd
GSK-461364A Hs Inhibitor Inhibition 5.8 pKd 1400.0 Kd
A-674563 Hs Inhibitor Inhibition 5.8 pKd 1600.0 Kd
NVP-TAE684 Hs Inhibitor Inhibition 5.7 pKd 1800.0 Kd
PI-103 Hs Inhibitor Inhibition 5.6 pKd 2400.0 Kd
afatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
doramapimod Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
BMS-345541 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
BMS-387032 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
brivanib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
CHIR-265 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
canertinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
CI-1040 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
tofacitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
dasatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
foretinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
alvocidib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
GDC-0879 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
GW-2580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
neratinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
imatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
Ki-20227 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
lapatinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
enzastaurin Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
MLN-120B Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
tandutinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
MLN-8054 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
nilotinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
pazopanib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
PD-173955 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
PHA-665752 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
PLX-4720 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
vatalanib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
R547 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
SGX-523 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
bosutinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
sorafenib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
dovitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
crizotinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
erlotinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
gefitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
GSK690693 Hs Inhibitor Inhibition 5.5 pKd 3000.0 Kd
SB203580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
masitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
linifanib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
quizartinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
axitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
motesanib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
AST-487 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
AT-7519 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
barasertib-hQPA Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
cediranib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
selumetinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
vandetanib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
tozasertib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
neflamapimod Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
TG-100-115 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
pictilisib Hs Inhibitor Inhibition 5.4 pKd 4000.0 Kd
midostaurin Hs Inhibitor Inhibition 5.3 pKd 4700.0 Kd
JNJ-28312141 Hs Inhibitor Inhibition 5.3 pKd 5000.0 Kd

References

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1. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378]

2. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem Biol, 17 (11): 1241-9. [PMID:21095574]