Drug Information

Drug (ID: DG01680) and It's Reported Resistant Information
Name
AEB071/Binimetinib
Synonyms
AEB071/Binimetinib
    Click to Show/Hide
Type(s) of Resistant Mechanism of This Drug
  ADTT: Aberration of the Drug's Therapeutic Target
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
Click to Show/Hide the Resistance Disease of This Class
Uveal melanoma [ICD-11: 2D0Y]
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
  Aberration of the Drug's Therapeutic Target (ADTT) Click to Show/Hide
Key Molecule: Guanine nucleotide-binding protein subunit alpha-11 (GNA11) [1]
Sensitive Disease Uveal melanoma [ICD-11: 2D0Y.0]
 Disease Info 
Molecule Alteration Missense mutation
p.Q209L (c.626A>T)
 Molecule Info 
Wild Type Structure Method: Electron microscopy Resolution: 3.50  Å
PDB: 6VU5
Mutant Type Structure Method: Electron microscopy Resolution: 2.90  Å
PDB: 7F6G
   Download The Information of Sequence       Download The Structure File   
RMSD: 1.91
TM score: 0.72705
Amino acid change:
Q209L
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
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M
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H
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H
-
H
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H
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H
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H
-
H
-
H
0
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-
H
M
H
T
T
L
L
E
E
S
S
I
I
M
M
A
A
C
C
10
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C
C
L
L
S
S
E
E
E
E
A
A
K
K
E
E
A
A
R
R
20
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R
R
I
I
N
N
D
D
E
E
I
I
E
E
R
R
Q
Q
L
L
30
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R
R
R
R
D
D
K
K
R
R
D
D
A
A
R
R
R
R
E
E
40
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L
L
K
K
L
L
L
L
L
L
L
L
G
G
T
T
G
G
E
E
50
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S
S
G
G
K
K
S
S
T
T
F
F
I
I
K
K
Q
Q
M
M
60
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R
R
I
I
I
I
H
H
G
G
S
S
G
G
Y
Y
S
S
D
D
70
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E
E
D
D
K
K
R
R
G
G
F
F
T
T
K
K
L
L
V
V
80
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Y
Y
Q
Q
N
N
I
I
F
F
T
T
A
A
M
M
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Q
A
A
90
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M
M
I
I
R
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A
A
M
M
D
D
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T
L
L
K
K
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100
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P
P
Y
Y
K
K
Y
Y
E
E
H
H
N
N
K
K
A
A
H
H
110
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A
A
Q
Q
L
L
V
V
R
R
E
E
V
V
D
D
V
V
E
E
120
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K
K
V
V
S
S
A
A
F
F
E
E
N
N
P
P
Y
Y
V
V
130
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D
D
A
A
I
I
K
K
S
S
L
L
W
W
N
N
D
D
P
P
140
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G
G
I
I
Q
Q
E
E
C
C
Y
Y
D
D
R
R
R
R
R
R
150
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E
E
Y
Y
Q
Q
L
L
S
S
D
D
S
S
T
T
K
K
Y
Y
160
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Y
Y
L
L
N
N
D
D
L
L
D
D
R
R
V
V
A
A
D
D
170
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P
P
A
A
Y
Y
L
L
P
P
T
T
Q
Q
Q
Q
D
D
V
V
180
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L
L
R
R
V
V
R
Q
V
V
P
P
T
T
T
T
G
G
I
I
190
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I
I
E
E
Y
Y
P
P
F
F
D
D
L
L
Q
Q
S
S
V
V
200
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I
I
F
F
R
R
M
M
V
V
D
D
V
V
G
G
G
G
Q
L
210
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R
R
S
S
E
E
R
R
R
R
K
K
W
W
I
I
H
H
C
C
220
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F
F
E
E
N
N
V
V
T
T
S
S
I
I
M
M
F
F
L
L
230
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V
V
A
A
L
L
S
S
E
E
Y
Y
D
D
Q
Q
V
V
L
L
240
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V
V
E
E
S
S
D
D
N
N
E
E
N
N
R
R
M
M
E
E
250
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E
E
S
S
K
K
A
A
L
L
F
F
R
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T
I
I
I
I
260
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T
T
Y
Y
P
P
W
W
F
F
Q
Q
N
N
S
S
S
S
V
V
270
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I
I
L
L
F
F
L
L
N
N
K
K
K
K
D
D
L
L
L
L
280
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E
E
E
E
K
K
I
I
M
M
Y
Y
S
S
H
H
L
L
V
V
290
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D
D
Y
Y
F
F
P
P
E
E
Y
Y
D
D
G
G
P
P
Q
Q
300
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R
R
D
D
A
A
Q
Q
A
A
A
A
R
R
E
E
F
F
I
I
310
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L
L
K
K
M
M
F
F
V
V
D
D
L
L
N
N
P
P
D
D
320
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S
S
D
D
K
K
I
I
I
I
Y
Y
S
S
H
H
F
F
T
T
330
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C
C
A
A
T
T
D
D
T
T
E
E
N
N
I
I
R
R
F
F
340
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V
V
F
F
A
A
A
A
V
V
K
K
D
D
T
T
I
I
L
L
350
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Q
Q
L
L
N
N
L
L
K
K
E
E
Y
Y
N
N
L
L
V
V
Click to Show/Hide the Structure
Experimental Note Identified from the Human Clinical Data
In Vitro Model OMM-GN11 N.A. Mus musculus (Mouse) N.A.
OMM13 N.A. N.A. N.A.
Mel202 Eye Homo sapiens (Human) CVCL_C301
GNAQ cells N.A. N.A. N.A.
Mel270 cells Skin Homo sapiens (Human) CVCL_C302
GNA11 cells N.A. N.A. N.A.
UPMD-1 cells Skin Homo sapiens (Human) CVCL_C297
92-1 cells Bladder Homo sapiens (Human) CVCL_W909
Mel202 Eye Homo sapiens (Human) CVCL_C301
In Vivo Model C57/BL6 mouse model Mus musculus
Experiment for
Molecule Alteration		 Western blot analysis
Experiment for
Drug Resistance		 Cell proliferation assay
References
Ref 1 Combined PKC and MEK inhibition in uveal melanoma with GNAQ and GNA11 mutationsOncogene. 2014 Sep 25;33(39):4724-34. doi: 10.1038/onc.2013.418. Epub 2013 Oct 21.

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