Ligand |
|
|
|
|
|
|
|
|
|
|
|
[3H]QNB
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.7 – 10.5
|
pKd
|
42,73
|
|
⤷ |
pKd
9.7 – 10.5
(Kd 2x10-10 – 3.16x10-11 M)
[42,73]
|
[3H]N-methyl scopolamine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.9 – 10.2
|
pKd
|
10,42-43,47,50,98
|
|
⤷ |
pKd
9.9 – 10.2
(Kd 1.4x10-10 – 6x10-11 M)
[10,42-43,47,50,98]
|
[3H]AF DX-384
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.7
|
pKd
|
11,62,94
|
|
⤷ |
pKd
8.7
[11,62,94]
|
biperiden
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.6
|
pKd
|
2
|
|
⤷ |
pKd
8.6
(Kd 2.4x10-9 M)
[2]
|
otenzepad
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.0
|
pKd
|
27
|
|
⤷ |
pKd
7.0
[27]
|
tiotropium
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
10.2 – 10.6
|
pKi
|
86,88
|
|
⤷ |
pKi
10.2 – 10.6
[86,88]
|
3-quinuclidinyl-benzilate
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
10.4
|
pKi
|
9
|
|
⤷ |
pKi
10.4
(Ki 4x10-11 M)
[9]
|
umeclidinium
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
10.3
|
pKi
|
78
|
|
⤷ |
pKi
10.3
[78]
|
propantheline
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
10.2
|
pKi
|
41
|
|
⤷ |
pKi
10.2
[41]
|
aclidinium
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
10.0
|
pKi
|
88
|
|
⤷ |
pKi
10.0
[88]
|
oxyphenonium
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.8
|
pKi
|
9
|
|
⤷ |
pKi
9.8
(Ki 1.45x10-10 M)
[9]
|
atropine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.7
|
pKi
|
45
|
|
⤷ |
pKi
9.7
[45]
|
glycopyrrolate
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.1 – 10.0
|
pKi
|
84,86
|
|
⤷ |
pKi
9.1 – 10.0
[84,86]
|
AE9C90CB
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.5
|
pKi
|
81
|
|
⤷ |
pKi
9.5
[81]
|
mepenzolic acid
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.4
|
pKi
|
9
|
|
⤷ |
pKi
9.4
(Ki 3.6x10-10 M)
[9]
|
scopolamine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.1 – 9.5
|
pKi
|
2,41
|
|
⤷ |
pKi
9.1 – 9.5
[2,41]
|
revefenacin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.3
|
pKi
|
38
|
|
⤷ |
pKi
9.3
(Ki 5.5x10-10 M)
[38]
Description: Determined from a radioligand binding assay using membranes from CHO‐K1 cells expressing the hM4 receptor, and displacement of [3H]NMS tracer.
|
ipratropium
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
9.2
|
pKi
|
39
|
|
⤷ |
pKi
9.2
[39]
|
4-DAMP
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
9.1
|
pKi
|
45
|
|
⤷ |
pKi
9.1
[45]
|
atropine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.7 – 9.5
|
pKi
|
18,39,41,74
|
|
⤷ |
pKi
8.7 – 9.5
[18,39,41,74]
|
4-DAMP
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.9
|
pKi
|
24
|
|
⤷ |
pKi
8.9
[24]
|
oxybutynin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.4 – 8.7
|
pKi
|
23,81
|
|
⤷ |
pKi
8.4 – 8.7
[23,81]
|
muscarinic toxin 3
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.5
|
pKi
|
9
|
|
⤷ |
pKi
8.5
(Ki 3x10-9 M)
[9]
|
silahexocyclium
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.5
|
pKi
|
6
|
|
⤷ |
pKi
8.5
[6]
|
tolterodine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.3 – 8.4
|
pKi
|
31,81
|
|
⤷ |
pKi
8.3 – 8.4
[31,81]
|
UH-AH 37
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.3 – 8.4
|
pKi
|
31,104
|
|
⤷ |
pKi
8.3 – 8.4
[31,104]
|
hexocyclium
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.3
|
pKi
|
6
|
|
⤷ |
pKi
8.3
[6]
|
dicyclomine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.3
|
pKi
|
9
|
|
⤷ |
pKi
8.3
(Ki 5x10-9 M)
[9]
|
PCS1055
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.2
|
pKi
|
18
|
|
⤷ |
pKi
8.2
[18]
|
himbacine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.9 – 8.4
|
pKi
|
9,24,44,61
|
|
⤷ |
pKi
8.4
(Ki 4x10-9 M)
[9]
pKi
7.9 – 8.2
[24,44,61]
|
amitriptyline
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
8.1
|
pKi
|
82
|
|
⤷ |
pKi
8.1
(Ki 7.2x10-9 M)
[82]
|
AQ-RA 741
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.8 – 8.2
|
pKi
|
24,31
|
|
⤷ |
pKi
7.8 – 8.2
[24,31]
|
tripitramine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.9
|
pKi
|
63
|
|
⤷ |
pKi
7.9
[63]
|
darifenacin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.3 – 8.1
|
pKi
|
31,39,81
|
|
⤷ |
pKi
7.3 – 8.1
[31,39,81]
|
hexahydrosiladifenidol
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.7
|
pKi
|
45
|
|
⤷ |
pKi
7.7
[45]
|
AFDX384
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.3 – 8.0
|
pKi
|
18,24
|
|
⤷ |
pKi
7.3 – 8.0
[18,24]
|
pirenzepine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.0 – 8.1
|
pKi
|
9,24,37,41,44,104
|
|
⤷ |
pKi
8.1
(Ki 8x10-9 M)
[9]
pKi
7.0 – 7.6
[24,37,41,44,104]
|
PD 102807
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.4 – 7.6
|
pKi
|
18,68
|
|
⤷ |
pKi
7.4 – 7.6
[18,68]
|
p-F-HHSiD
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.1 – 7.5
|
pKi
|
27,41
|
|
⤷ |
pKi
7.1 – 7.5
[27,41]
|
dosulepin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.2
|
pKi
|
82
|
|
⤷ |
pKi
7.2
(Ki 6.1x10-8 M)
[82]
|
hexahydrosiladifenidol
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.5 – 7.7
|
pKi
|
6,27
|
|
⤷ |
pKi
6.5 – 7.7
[6,27]
|
muscarinic toxin 1
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.1
|
pKi
|
35
|
|
⤷ |
pKi
7.1
[35]
|
hexahydrodifenidol
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
7.1
|
pKi
|
6
|
|
⤷ |
pKi
7.1
[6]
|
pirenzepine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
7.1
|
pKi
|
45
|
|
⤷ |
pKi
7.1
[45]
|
methoctramine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.6 – 7.5
|
pKi
|
6,24,27,37
|
|
⤷ |
pKi
6.6 – 7.5
[6,24,27,37]
|
tropicamide
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.9
|
pKi
|
9
|
|
⤷ |
pKi
6.9
[9]
|
solifenacin
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.8
|
pKi
|
81
|
|
⤷ |
pKi
6.8
[81]
|
(S)-dimetindene
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
6.5
|
pKi
|
8
|
|
⤷ |
pKi
6.5
(Ki 2.951x10-7 M)
[8]
Description: Binding to hM4 receptors expressed in CHO cells.
|
otenzepad
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
6.5
|
pKi
|
45
|
|
⤷ |
pKi
6.5
[45]
|
guanylpirenzepine
|
|
|
|
|
|
|
|
|
|
|
Rn |
Antagonist |
6.2
|
pKi
|
97
|
|
⤷ |
pKi
6.2
[97]
|
muscarinic toxin 2
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
5.9
|
pKi
|
35
|
|
⤷ |
pKi
5.9
[35]
|
VU0255035
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
5.9
|
pKi
|
80
|
|
⤷ |
pKi
5.9
[80]
|
lithocholylcholine
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
5.3
|
pKi
|
13
|
|
⤷ |
pKi
5.3
[13]
|
muscarinic toxin 7
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
<5.0
|
pKi
|
64
|
|
⤷ |
pKi
<5.0
[64]
|
ML381
|
|
|
|
|
|
|
|
|
|
|
Hs |
Antagonist |
>4.5
|
pKi
|
30
|
|
⤷ |
pKi
>4.5
(Ki <3x10-5 M)
[30]
|
|