[125I]ZM-241385
|
|
|
|
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|
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|
|
Rn |
Antagonist |
9.2
|
pKd
|
106
|
|
⤷ |
pKd
9.2
[106]
|
[3H]ZM 241385
|
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|
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|
|
Hs |
Antagonist |
8.7 – 9.1
|
pKd
|
4,44
|
|
⤷ |
pKd
8.7 – 9.1
(Kd 1.8x10-9 – 8x10-10 M)
[4,44]
|
[3H]SCH 58261
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|
Hs |
Antagonist |
8.6 – 9.0
|
pKd
|
68,104
|
|
⤷ |
pKd
8.6 – 9.0
[68,104]
|
[3H]XAC
|
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|
|
Hs |
Antagonist |
8.0
|
pKd
|
63
|
|
⤷ |
pKd
8.0
[63]
|
SCH442416
|
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Hs |
Antagonist |
8.4 – 10.3
|
pKi
|
128,132
|
|
⤷ |
pKi
8.4 – 10.3
[128,132]
|
MRS1093
|
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|
Hs |
Antagonist |
9.2
|
pKi
|
60
|
|
⤷ |
pKi
9.2
[60]
|
preladenant
|
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|
Hs |
Antagonist |
9.1
|
pKi
|
92
|
|
⤷ |
pKi
9.1
(Ki 9x10-10 M)
[92]
|
ZM-241385
|
|
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|
|
|
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|
Hs |
Antagonist |
8.8 – 9.1
|
pKi
|
104
|
|
⤷ |
pKi
8.8 – 9.1
[104]
|
vipadenant
|
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|
Hs |
Antagonist |
8.9
|
pKi
|
48
|
|
⤷ |
pKi
8.9
(Ki 1.3x10-9 M)
[48]
|
imaradenant
|
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|
Hs |
Antagonist |
8.8
|
pKi
|
12
|
|
⤷ |
pKi
8.8
(Ki 1.7x10-9 M)
[12]
Description: Binding affinity of AZD4635 determined in a radioligand binding competition assays with membranes prepared from HEK-293-T cells stably expressing human A2AR.
|
SCH 58261
|
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Hs |
Antagonist |
8.3 – 9.2
|
pKi
|
32,68,104
|
|
⤷ |
pKi
8.3 – 9.2
[32,68,104]
|
xanthine amine congener
|
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|
Hs |
Antagonist |
8.4 – 9.0
|
pKi
|
32,67
|
|
⤷ |
pKi
8.4 – 9.0
[32,67]
|
CGS 15943
|
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|
Hs |
Antagonist |
7.7 – 9.4
|
pKi
|
32,63,67,104
|
|
⤷ |
pKi
7.7 – 9.4
[32,63,67,104]
|
istradefylline
|
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|
Rn |
Antagonist |
8.4 – 8.7
|
pKi
|
113,127
|
|
⤷ |
pKi
8.4 – 8.7
(Ki 4.46x10-9 – 2.2x10-9 M)
[113,127]
|
tozadenant
|
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|
Hs |
Antagonist |
8.3
|
pKi
|
29
|
|
⤷ |
pKi
8.3
(Ki 5x10-9 M)
[29]
|
ST-1535
|
|
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|
Hs |
Antagonist |
8.2
|
pKi
|
89
|
|
⤷ |
pKi
8.2
(Ki 6.6x10-9 M)
[89]
|
MSX-2
|
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|
Rn |
Antagonist |
8.1
|
pKi
|
94,121
|
|
⤷ |
pKi
8.1
(Ki 8.04x10-9 M)
[94,121]
|
MSX-2
|
|
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|
Hs |
Antagonist |
7.8 – 8.3
|
pKi
|
121
|
|
⤷ |
pKi
7.8 – 8.3
(Ki 1.45x10-8 – 5.38x10-9 M)
[121]
|
PBF-509
|
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|
Hs |
Antagonist |
7.6 – 7.9
|
pKi
|
49,87
|
|
⤷ |
pKi
7.9
(Ki 1.2x10-8 M)
[49,87]
Description: Determined in a competitive radioligand binding assay using membranes prepared from HeLa cells expressing human A2A receptor.
pKi
7.6
(Ki 2.5x10-8 M)
[49,87]
Description: Antagonism of rolipram-induced cAMP accummulation in CHO cells expressing the human A2A receptor, as measured using a proprietary enzymeimmunoassay.
|
LJ-4517
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|
Hs |
Antagonist |
7.7
|
pKi
|
129
|
|
⤷ |
pKi
7.7
(Ki 1.83x10-8 M)
[129]
Description: Displacing [3H]ZM-241385
|
KF 17837S
|
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|
Hs |
Antagonist |
7.7
|
pKi
|
32
|
|
⤷ |
pKi
7.7
[32]
|
istradefylline
|
|
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|
Hs |
Antagonist |
7.0 – 7.9
|
pKi
|
16,41
|
|
⤷ |
pKi
7.0 – 7.9
(Ki 9.12x10-8 – 1.2x10-8 M)
[16,41]
|
CSC
|
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|
Rn |
Antagonist |
7.3
|
pKi
|
54
|
|
⤷ |
pKi
7.3
(Ki 5.4x10-8 M)
[54]
|
compound 10 [PMID: 31306001]
|
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|
Hs |
Antagonist |
7.2
|
pKi
|
9
|
|
⤷ |
pKi
7.2
(Ki 6.8x10-8 M)
[9]
Description: Binding affinity calculated by measuring displacement of specific [3H]ZM24138 binding at hA2AARs expressed in CHO cells.
|
mefloquine
|
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|
Hs |
Antagonist |
7.0
|
pKi
|
145
|
|
⤷ |
pKi
7.0
(Ki 1.04x10-7 M)
[145]
Description: Binding affinity determined by displacement of [3H]-CGS21680 from human A2A receptors by increasing concentrations of racemic mefloquine.
|
DPCPX
|
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Hs |
Antagonist |
6.6 – 7.2
|
pKi
|
32,67-68,104,146
|
|
⤷ |
pKi
6.6 – 7.2
[32,67-68,104,146]
|
MRE 3008F20
|
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|
Hs |
Antagonist |
6.8
|
pKi
|
55,135-136
|
|
⤷ |
pKi
6.8
[55,135-136]
|
LUF5981
|
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|
Hs |
Antagonist |
6.7
|
pKi
|
16
|
|
⤷ |
pKi
6.7
(Ki 1.94x10-7 M)
[16]
|
rolofylline
|
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|
Hs |
Antagonist |
6.2 – 7.0
|
pKi
|
61,109
|
|
⤷ |
pKi
6.2 – 7.0
(Ki 6.37x10-7 – 1.08x10-7 M)
[61,109]
|
DPCPX
|
|
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|
Rn |
Antagonist |
6.3 – 6.8
|
pKi
|
64,94
|
|
⤷ |
pKi
6.3 – 6.8
(Ki 5x10-7 – 1.57x10-7 M)
[64,94]
|
derenofylline
|
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|
Hs |
Antagonist |
6.4
|
pKi
|
59
|
|
⤷ |
pKi
6.4
(Ki 3.98x10-7 M)
[59]
|
rolofylline
|
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|
Rn |
Antagonist |
6.3 – 6.4
|
pKi
|
62,110
|
|
⤷ |
pKi
6.3 – 6.4
(Ki 5.1x10-7 – 3.8x10-7 M)
[62,110]
|
KF26777
|
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|
Hs |
Antagonist |
6.3
|
pKi
|
116
|
|
⤷ |
pKi
6.3
(Ki 4.7x10-7 M)
[116]
|
MRS1754
|
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|
Hs |
Antagonist |
6.3
|
pKi
|
65
|
|
⤷ |
pKi
6.3
(Ki 5.03x10-7 M)
[65]
|
PSB36
|
|
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|
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|
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|
Rn |
Antagonist |
6.3
|
pKi
|
146
|
|
⤷ |
pKi
6.3
(Ki 5.52x10-7 M)
[146]
|
MRS1754
|
|
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|
Rn |
Antagonist |
6.2
|
pKi
|
65
|
|
⤷ |
pKi
6.2
(Ki 6.12x10-7 M)
[65]
|
CPX
|
|
|
|
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|
|
|
|
|
|
Hs |
Antagonist |
6.2
|
pKi
|
63
|
|
⤷ |
pKi
6.2
[63]
|
ATL802
|
|
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|
|
|
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|
|
|
Hs |
Antagonist |
6.2
|
pKi
|
65
|
|
⤷ |
pKi
6.2
(Ki 6.54x10-7 M)
[65]
|
CPFPX
|
|
|
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|
|
|
|
|
|
Rn |
Antagonist |
6.1
|
pKi
|
51
|
|
⤷ |
pKi
6.1
(Ki 8.12x10-7 M)
[51]
|
CPFPX
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.0
|
pKi
|
51
|
|
⤷ |
pKi
6.0
(Ki 9.4x10-7 M)
[51]
|
PSB36
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.0
|
pKi
|
146
|
|
⤷ |
pKi
6.0
(Ki 9.8x10-7 M)
[146]
|
MRE 2029F20
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
<6.0
|
pKi
|
7
|
|
⤷ |
pKi
<6.0
(Ki >1x10-6 M)
[7]
|
galangin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.0
|
pKi
|
60
|
|
⤷ |
pKi
6.0
[60]
|
LAS38096
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
<6.0
|
pKi
|
34,140
|
|
⤷ |
pKi
<6.0
(Ki >1x10-6 M)
[34,140]
|
LUF7602
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
5.9
|
pKi
|
150
|
|
⤷ |
pKi
5.9
(Ki 1.259x10-6 M)
[150]
Description: Affinity determined from the displacement of specific [3H]ZM241385 binding on HEK293 cell membranes stably expressing human adenosine A2A receptors at 25 °C during 2 h of incubation.
|
FK-453
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
5.9
|
pKi
|
55
|
|
⤷ |
pKi
5.9
(Ki 1.3x10-6 M)
[55]
|
PSB-11
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
5.9
|
pKi
|
105
|
|
⤷ |
pKi
5.9
(Ki 1.28x10-6 M)
[105]
|
MRS1523
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
5.7
|
pKi
|
79
|
|
⤷ |
pKi
5.7
(Ki 2.05x10-6 M)
[79]
|
PSB-11
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
5.7
|
pKi
|
105
|
|
⤷ |
pKi
5.7
(Ki 2.1x10-6 M)
[105]
|
tonapofylline
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
5.6
|
pKi
|
61
|
|
⤷ |
pKi
5.6
(Ki 2.44x10-6 M)
[61]
|
PSB-10
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
5.6
|
pKi
|
105
|
|
⤷ |
pKi
5.6
(Ki 2.7x10-6 M)
[105]
|
MRS1041
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
5.5
|
pKi
|
60
|
|
⤷ |
pKi
5.5
[60]
|
MRS1042
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
5.5
|
pKi
|
60
|
|
⤷ |
pKi
5.5
[60]
|
flavone
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
5.5
|
pKi
|
60
|
|
⤷ |
pKi
5.5
[60]
|
theophylline
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
5.2 – 5.8
|
pKi
|
32,53,67,135
|
|
⤷ |
pKi
5.2 – 5.8
[32,53,67,135]
|
CVT-6883
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
5.5
|
pKi
|
36
|
|
⤷ |
pKi
5.5
(Ki 3.28x10-6 M)
[36]
|
MRS1523
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
5.4
|
pKi
|
79
|
|
⤷ |
pKi
5.4
(Ki 3.66x10-6 M)
[79]
|
PSB-10
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
5.2
|
pKi
|
96
|
|
⤷ |
pKi
5.2
(Ki 6.04x10-6 M)
[96]
|
MRS928
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
5.2
|
pKi
|
60
|
|
⤷ |
pKi
5.2
[60]
|
tonapofylline
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
5.2
|
pKi
|
61
|
|
⤷ |
pKi
5.2
(Ki 6.41x10-6 M)
[61]
|
caffeine
|
|
|
|
|
|
|
|
|