Janus kinase 1 (Janus kinase (JakA) 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: JAK1(JH1domain-catalytic)
Ligand Sp. Type Action Value (-log10) Parameter Value (nM) Parameter
tofacitinib Hs Inhibitor Inhibition 8.8 pKd 1.6 Kd
ruxolitinib Hs Inhibitor Inhibition 8.5 pKd 3.4 Kd
staurosporine Hs Inhibitor Inhibition 8.2 pKd 6.1 Kd
lestaurtinib Hs Inhibitor Inhibition 8.1 pKd 8.8 Kd
fedratinib Hs Inhibitor Inhibition 7.7 pKd 18.0 Kd
tamatinib Hs Inhibitor Inhibition 7.7 pKd 21.0 Kd
AST-487 Hs Inhibitor Inhibition 7.1 pKd 74.0 Kd
JNJ-28312141 Hs Inhibitor Inhibition 6.7 pKd 200.0 Kd
PP-242 Hs Inhibitor Inhibition 6.5 pKd 300.0 Kd
crizotinib Hs Inhibitor Inhibition 6.5 pKd 330.0 Kd
PD-173955 Hs Inhibitor Inhibition 6.5 pKd 330.0 Kd
NVP-TAE684 Hs Inhibitor Inhibition 6.4 pKd 410.0 Kd
midostaurin Hs Inhibitor Inhibition 6.2 pKd 670.0 Kd
KW-2449 Hs Inhibitor Inhibition 5.9 pKd 1200.0 Kd
selumetinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
BI-2536 Hs Inhibitor Inhibition <5.5 pKd >3000.0 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
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
pictilisib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
GSK-1838705A Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
GSK-461364A 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
PHA-665752 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
PI-103 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
PLX-4720 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
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
SB203580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
A-674563 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
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
TG-100-115 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
vandetanib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
neflamapimod Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
dovitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
motesanib Hs Inhibitor Inhibition 5.3 pKd 5200.0 Kd
SU-14813 Hs Inhibitor Inhibition 5.2 pKd 5900.0 Kd
tozasertib Hs Inhibitor Inhibition 5.2 pKd 5900.0 Kd
sunitinib Hs Inhibitor Inhibition 5.2 pKd 6000.0 Kd
Target used in screen: JAK1(JH2domain-pseudokinase)
Ligand Sp. Type Action Value (-log10) Parameter Value (nM) Parameter
sunitinib Hs Inhibitor Inhibition 7.3 pKd 49.0 Kd
SU-14813 Hs Inhibitor Inhibition 7.0 pKd 97.0 Kd
JNJ-28312141 Hs Inhibitor Inhibition 6.8 pKd 140.0 Kd
KW-2449 Hs Inhibitor Inhibition 6.7 pKd 190.0 Kd
NVP-TAE684 Hs Inhibitor Inhibition 6.5 pKd 300.0 Kd
dovitinib Hs Inhibitor Inhibition 6.4 pKd 380.0 Kd
pictilisib Hs Inhibitor Inhibition 6.4 pKd 430.0 Kd
TG-100-115 Hs Inhibitor Inhibition 6.2 pKd 690.0 Kd
PI-103 Hs Inhibitor Inhibition 5.7 pKd 2000.0 Kd
fedratinib Hs Inhibitor Inhibition 5.7 pKd 2000.0 Kd
PHA-665752 Hs Inhibitor Inhibition 5.6 pKd 2700.0 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
BI-2536 Hs Inhibitor Inhibition <5.5 pKd >3000.0 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
lestaurtinib 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
GSK-1838705A Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
GSK-461364A 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
ruxolitinib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
Ki-20227 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
staurosporine 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
midostaurin 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
tamatinib 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
lapatinib 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
ruboxistaurin Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
SB203580 Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
A-674563 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
tozasertib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
neflamapimod Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
vandetanib Hs Inhibitor Inhibition <5.5 pKd >3000.0 Kd
PP-242 Hs Inhibitor Inhibition 5.4 pKd 3700.0 Kd
GDC-0879 Hs Inhibitor Inhibition 5.1 pKd 7800.0 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]