AC710
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
9.3
|
pKd |
40 |
|
⤷ |
pKd
9.3
(Kd 5x10-10 M)
[40]
|
linifanib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
9.2
|
pKd |
13 |
|
⤷ |
pKd
9.2
(Kd 6.3x10-10 M)
[13]
|
dovitinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
9.2
|
pKd |
13 |
|
⤷ |
pKd
9.2
(Kd 6.4x10-10 M)
[13]
|
crenolanib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
9.1
|
pKd |
27 |
|
⤷ |
pKd
9.1
(Kd 7.4x10-10 M)
[27]
|
AST-487
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
9.1
|
pKd |
13 |
|
⤷ |
pKd
9.1
(Kd 7.9x10-10 M)
[13]
|
quizartinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.8 – 8.9
|
pKd |
10,13 |
|
⤷ |
pKd
8.8 – 8.9
(Kd 1.6x10-9 – 1.3x10-9 M)
[10,13]
|
compound 6li [Chan et al., 2022]
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.6
|
pKd |
9 |
|
⤷ |
pKd
8.6
(Kd 2.5x10-9 M)
[9]
|
tandutinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.5
|
pKd |
13 |
|
⤷ |
pKd
8.5
(Kd 3x10-9 M)
[13]
|
compound 5e [PMID: 28580438]
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.4
|
pKd |
28 |
|
⤷ |
pKd
8.4
(Kd 3.6x10-9 M)
[28]
Description: Measured using the Z′-LYTE Kinase Assay Kit and wild type FLT3.
|
lestaurtinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.1
|
pKd |
13 |
|
⤷ |
pKd
8.1
(Kd 8.5x10-9 M)
[13]
|
midostaurin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.0
|
pKd |
13 |
|
⤷ |
pKd
8.0
(Kd 1.1x10-8 M)
[13]
|
RG-1530
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.0
|
pKd |
62 |
|
⤷ |
pKd
8.0
(Kd 1.1x10-8 M)
[62]
|
KW-2449
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.8
|
pKd |
13 |
|
⤷ |
pKd
7.8
(Kd 1.5x10-8 M)
[13]
|
mobinitinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.5 – 7.6
|
pKd |
74 |
|
⤷ |
pKd
7.6
(Kd 2.6x10-8 M)
[74]
Description: Affinity for WT FLT3
pKd
7.5
(Kd 3.4x10-8 M)
[74]
Description: Affinity for FLT3-ITD mutant
|
belizatinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.4
|
pKd |
39 |
|
⤷ |
pKd
7.4
(Kd 4.2x10-8 M)
[39]
Description: Binding affinity in vitro.
|
UNC4203
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.8
|
pKi |
83 |
|
⤷ |
pKi
7.8
(Ki 1.614x10-8 M)
[83]
|
AST-487
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
6.9
|
pKi |
69 |
|
⤷ |
pKi
6.9
(Ki 1.2x10-7 M)
[69]
Description: Inhibition of wild type FLT3
|
nefextinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
9.5 – 9.7
|
pIC50 |
75 |
|
⤷ |
pIC50
9.7
(IC50 2x10-10 M)
[75]
Description: Inhibitor potency for FLT3 D835Y mutant
pIC50
9.6
(IC50 2.8x10-10 M)
[75]
Description: Inhibition potency for WT FLT3
pIC50
9.5
(IC50 3.4x10-10 M)
[75]
Description: Inhibitor potency for FLT3-ITD fusion
|
gilteritinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
~9.5
|
pIC50 |
37 |
|
⤷ |
pIC50
~9.5
(IC50 ~3x10-10 M)
[37]
|
denfivontinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
9.4
|
pIC50 |
36 |
|
⤷ |
pIC50
9.4
(IC50 4x10-10 M)
[36]
|
Gö 6976
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
9.1
|
pIC50 |
79 |
|
⤷ |
pIC50
9.1
(IC50 7x10-10 M)
[79]
Description: Inhibitory activity against recombinant FLT3 in an in vitro kinase assay.
|
TTT-3002
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
9.1
|
pIC50 |
42 |
|
⤷ |
pIC50
9.1
(IC50 7.2x10-10 M)
[42]
Description: Inhibition of FLT3 phosphorylation in Molm14 human leukemia cells that carry the FLT3/ITD activation mutation
|
compound 8i [PMID: 22765894]
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
9.1
|
pIC50 |
80 |
|
⤷ |
pIC50
9.1
(IC50 8x10-10 M)
[80]
|
compound 8h [PMID: 22765894]
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
9.1
|
pIC50 |
32 |
|
⤷ |
pIC50
9.1
(IC50 8.5x10-10 M)
[32]
|
dorsomorphin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
>9.0
|
pIC50 |
43 |
|
⤷ |
pIC50
>9.0
(IC50 <1x10-9 M)
[43]
Description: Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits
|
RGB-286638
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
9.0
|
pIC50 |
11 |
|
⤷ |
pIC50
9.0
(IC50 1x10-9 M)
[11]
|
ilorasertib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
9.0
|
pIC50 |
21 |
|
⤷ |
pIC50
9.0
(IC50 1x10-9 M)
[21]
Description: Measuring inhibition of kinase activity in a biochemical assay.
|
tuspetinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
9.0
|
pIC50 |
5 |
|
⤷ |
pIC50
9.0
(IC50 1.1x10-9 M)
[5]
|
dovitinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.5 – 9.0
|
pIC50 |
57,63 |
|
⤷ |
pIC50
8.5 – 9.0
(IC50 3x10-9 – 1x10-9 M)
[57,63]
|
compound 34f [PMID: 37535845]
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.4 – 9.0
|
pIC50 |
4 |
|
⤷ |
pIC50
9.0
(IC50 1x10-9 M)
[4]
Description: Inhibition of FLT3-D835Y catalytic activity
pIC50
8.4
(IC50 4x10-9 M)
[4]
Description: Inhibition of FLT3-ITD catalytic activity
|
compound 2c [PMID: 24900538]
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.7
|
pIC50 |
66 |
|
⤷ |
pIC50
8.7
(IC50 2.1x10-9 M)
[66]
|
ENMD-2076
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.5
|
pIC50 |
56 |
|
⤷ |
pIC50
8.5
(IC50 3x10-9 M)
[56]
|
linifanib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.4
|
pIC50 |
2 |
|
⤷ |
pIC50
8.4
(IC50 4x10-9 M)
[2]
|
URMC-099
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.4
|
pIC50 |
23 |
|
⤷ |
pIC50
8.4
(IC50 4x10-9 M)
[23]
|
compound 18e [PMID: 31670517]
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.4
|
pIC50 |
78 |
|
⤷ |
pIC50
8.4
(IC50 4x10-9 M)
[78]
|
quizartinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.4
|
pIC50 |
81 |
|
⤷ |
pIC50
8.4
(IC50 4.2x10-9 M)
[81]
|
mivavotinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.3
|
pIC50 |
35 |
|
⤷ |
pIC50
8.3
(IC50 4.6x10-9 M)
[35]
Description: In vitro potency
|
AKN-028
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.2
|
pIC50 |
16 |
|
⤷ |
pIC50
8.2
(IC50 6x10-9 M)
[16]
|
sunitinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.2
|
pIC50 |
31 |
|
⤷ |
pIC50
8.2
(IC50 6.5x10-9 M)
[31]
|
KW-2449
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.2
|
pIC50 |
60 |
|
⤷ |
pIC50
8.2
(IC50 6.6x10-9 M)
[60]
|
sitravatinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.1
|
pIC50 |
54 |
|
⤷ |
pIC50
8.1
(IC50 8x10-9 M)
[54]
Description: In a biochemical enzyme activity assay.
|
compound 25ap [PMID: 37796543]
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
8.0
|
pIC50 |
82 |
|
⤷ |
pIC50
8.0
(IC50 1.09x10-8 M)
[82]
|
compound 7d [PMID: 29672049]
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.9
|
pIC50 |
26 |
|
⤷ |
pIC50
7.9
(IC50 1.3x10-8 M)
[26]
Description: In a biochemical assay.
|
MELK-TI
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.7
|
pIC50 |
29 |
|
⤷ |
pIC50
7.7
(IC50 1.8x10-8 M)
[29]
Description: Measured in a MIllipore kinase screening panel assay
|
tafetinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.7
|
pIC50 |
65 |
|
⤷ |
pIC50
7.7
(IC50 2.08x10-8 M)
[65]
Description: In a radiometric biochemical protein kinase assay.
|
pacritinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.7
|
pIC50 |
71 |
|
⤷ |
pIC50
7.7
(IC50 2.2x10-8 M)
[71]
|
MK-2461
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.7
|
pIC50 |
51 |
|
⤷ |
pIC50
7.7
(IC50 2.2x10-8 M)
[51]
|
JNJ-28312141
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.5
|
pIC50 |
46 |
|
⤷ |
pIC50
7.5
(IC50 3x10-8 M)
[46]
|
merestinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.5
|
pIC50 |
76 |
|
⤷ |
pIC50
7.5
(IC50 3.1x10-8 M)
[76]
Description: Inhibition of in vitro biochemical activity by EMD Millipore assay.
|
zotiraciclib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.3 – 7.7
|
pIC50 |
22,72 |
|
⤷ |
pIC50
7.3 – 7.7
(IC50 5.6x10-8 – 1.9x10-8 M)
[22,72]
|
Flt-3 inhibitor II
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.5
|
pIC50 |
45 |
|
⤷ |
pIC50
7.5
(IC50 3.3x10-8 M)
[45]
|
Flt-3 inhibitor
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.4
|
pIC50 |
52 |
|
⤷ |
pIC50
7.4
(IC50 4.2x10-8 M)
[52]
|
SGI-1776
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.4
|
pIC50 |
15 |
|
⤷ |
pIC50
7.4
(IC50 4.4x10-8 M)
[15]
|
sorafenib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.2 – 7.5
|
pIC50 |
70,80 |
|
⤷ |
pIC50
7.5
(IC50 3.3x10-8 M)
[80]
pIC50
7.2
(IC50 5.8x10-8 M)
[70]
|
Flt-3 inhibitor III
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.3
|
pIC50 |
18 |
|
⤷ |
pIC50
7.3
(IC50 5x10-8 M)
[18]
|
ruserontinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.3
|
pIC50 |
8 |
|
⤷ |
pIC50
7.3
(IC50 5.5x10-8 M)
[8]
|
ceritinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.2
|
pIC50 |
48 |
|
⤷ |
pIC50
7.2
(IC50 6x10-8 M)
[48]
|
compound 13ac [PMID: 33256400]
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.2
|
pIC50 |
77 |
|
⤷ |
pIC50
7.2
(IC50 6.2x10-8 M)
[77]
|
UNC8969
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.2
|
pIC50 |
34 |
|
⤷ |
pIC50
7.2
(IC50 7x10-8 M)
[34]
|
PF-562271
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.0
|
pIC50 |
58 |
|
⤷ |
pIC50
7.0
(IC50 9.7x10-8 M)
[58]
|
compound 14k [PMID: 21982499]
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.0
|
pIC50 |
55 |
|
⤷ |
pIC50
7.0
(IC50 1.04x10-7 M)
[55]
|
BMS-690514
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
7.0
|
pIC50 |
47 |
|
⤷ |
pIC50
7.0
(IC50 1.1x10-7 M)
[47]
|
BAY-985
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
6.9
|
pIC50 |
38 |
|
⤷ |
pIC50
6.9
(IC50 1.23x10-7 M)
[38]
|
pexidartinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
6.8
|
pIC50 |
61 |
|
⤷ |
pIC50
6.8
(IC50 1.6x10-7 M)
[61]
|
edicotinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
6.7
|
pIC50 |
20 |
|
⤷ |
pIC50
6.7
(IC50 1.9x10-7 M)
[20]
|
tandutinib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
6.7
|
pIC50 |
30 |
|
⤷ |
pIC50
6.7
(IC50 2.2x10-7 M)
[30]
|
nuvisertib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
6.6
|
pIC50 |
17 |
|
⤷ |
pIC50
6.6
(IC50 2.79x10-7 M)
[17]
|
GTP-14564
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
6.5
|
pIC50 |
50 |
|
⤷ |
pIC50
6.5
(IC50 3x10-7 M)
[50]
|
onvansertib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
6.3
|
pIC50 |
6 |
|
⤷ |
pIC50
6.3
(IC50 5.1x10-7 M)
[6]
|
AST-487
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
6.3
|
pIC50 |
1 |
|
⤷ |
pIC50
6.3
(IC50 5.2x10-7 M)
[1]
|
midostaurin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
6.3
|
pIC50 |
68 |
|
⤷ |
pIC50
6.3
(IC50 5.28x10-7 M)
[68]
|
cediranib
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
<6.0
|
pIC50 |
67 |
|
⤷ |
pIC50
<6.0
(IC50 >1x10-6 M)
[67]
|
compound 1 [Cruz-López et al., 2019]
|
|
|
|
|
|
|
|
|
|
|
Hs |
Inhibition
|
4.3
|
pIC50 |
12 |
|
⤷ |
pIC50
4.3
(IC50 5.35x10-5 M)
[12]
|