VU0483605
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
6.5
|
pKB |
35 |
|
⤷ |
pKB
6.5
[35]
|
GS39783
|
|
|
|
|
|
|
|
|
|
Rn |
Neutral
|
6.3
|
pKB |
35 |
|
⤷ |
pKB
6.3
[35]
|
PHCCC
|
|
|
|
|
|
|
|
|
|
Rn |
Neutral
|
5.6
|
pKB |
35 |
|
⤷ |
pKB
5.6
[35]
|
AZ12216052
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
5.4
|
pKB |
35 |
|
⤷ |
pKB
5.4
[35]
|
NPS 2143
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
5.1
|
pKB |
35 |
|
⤷ |
pKB
5.1
[35]
|
CPCCOEt
|
|
|
|
|
|
|
|
|
|
Rn |
Neutral
|
4.9
|
pKB |
35 |
|
⤷ |
pKB
4.9
[35]
|
CGP7930
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
4.8
|
pKB |
35 |
|
⤷ |
pKB
4.8
[35]
|
[3H]CTEP
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
8.8
|
pKd |
47 |
|
⤷ |
pKd
8.8
(Kd 1.5x10-9 M)
[47]
|
[3H]CTEP
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
8.8
|
pKd |
47 |
|
⤷ |
pKd
8.8
(Kd 1.7x10-9 M)
[47]
|
[3H]CTEP
|
|
|
|
|
|
|
|
|
|
Mm |
Negative
|
8.7
|
pKd |
47 |
|
⤷ |
pKd
8.7
(Kd 1.8x10-9 M)
[47]
|
[3H]methoxy-PEPy
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
8.5
|
pKd |
20 |
|
⤷ |
pKd
8.5
(Kd 3.4x10-9 M)
[20]
|
[3H]methoxymethyl-MTEP
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.7
|
pKd |
20 |
|
⤷ |
pKd
7.7
(Kd 2x10-8 M)
[20]
|
[3H]fenobam
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.5
|
pKd |
74 |
|
⤷ |
pKd
7.5
[74]
|
[3H]fenobam
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.3
|
pKd |
74 |
|
⤷ |
pKd
7.3
[74]
|
compound 20 [PMID: 16439120]
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
9.0
|
pKi |
13 |
|
⤷ |
pKi
9.0
(Ki 1x10-9 M)
[13]
|
BOMA
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
8.5
|
pKi |
99 |
|
⤷ |
pKi
8.5
[99]
|
AZD9272
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
8.4
|
pKi |
75 |
|
⤷ |
pKi
8.4
(Ki 3.8x10-9 M)
[75]
|
GRN-529
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
8.3
|
pKi |
38 |
|
⤷ |
pKi
8.3
(Ki 5.4x10-9 M)
[38]
|
CTEP
|
|
|
|
|
|
|
|
|
|
Mm |
Negative
|
8.0
|
pKi |
47 |
|
⤷ |
pKi
8.0
(Ki 9.5x10-9 M)
[47]
|
compound 26 [PMID: 16439120]
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
8.0
|
pKi |
13 |
|
⤷ |
pKi
8.0
(Ki 1x10-8 M)
[13]
|
compound 30 [PMID: 21757343]
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.9
|
pKi |
100 |
|
⤷ |
pKi
7.9
(Ki 1.2x10-8 M)
[100]
|
compound 10 [PMID: 15482906]
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.9
|
pKi |
36 |
|
⤷ |
pKi
7.9
(Ki 1.2x10-8 M)
[36]
|
CTEP
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.9
|
pKi |
47 |
|
⤷ |
pKi
7.9
(Ki 1.26x10-8 M)
[47]
|
compound 8 [PMID: 15482908]
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.8
|
pKi |
89 |
|
⤷ |
pKi
7.8
(Ki 1.4x10-8 M)
[89]
|
MTEP
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.8
|
pKi |
10 |
|
⤷ |
pKi
7.8
(Ki 1.6x10-8 M)
[10]
|
VU0285683
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.8
|
pKi |
76 |
|
⤷ |
pKi
7.8
(Ki 1.6x10-8 M)
[76]
|
compound 29b [PMID: 20809633]
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.8
|
pKi |
12 |
|
⤷ |
pKi
7.8
(Ki 1.7x10-8 M)
[12]
|
CTEP
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.7 – 7.8
|
pKi |
39,47 |
|
⤷ |
pKi
7.7 – 7.8
(Ki 2x10-8 – 1.64x10-8 M)
[39,47]
|
compound 10 [PMID: 15482908]
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.7
|
pKi |
89 |
|
⤷ |
pKi
7.7
(Ki 1.9x10-8 M)
[89]
|
compound 23 [PMID: 17590335]
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.7
|
pKi |
57 |
|
⤷ |
pKi
7.7
(Ki 2.2x10-8 M)
[57]
|
AZD6538
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.6
|
pKi |
75 |
|
⤷ |
pKi
7.6
(Ki 2.8x10-8 M)
[75]
|
compound 24d [PMID: 23357634]
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.5
|
pKi |
106 |
|
⤷ |
pKi
7.5
(Ki 3x10-8 M)
[106]
|
basimglurant
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.4
|
pKi |
39 |
|
⤷ |
pKi
7.4
(Ki 3.6x10-8 M)
[39]
Description: Reduction of antagonist MPEP binding to mGlu5 receptors in vitro
|
compound 16m [PMID: 19931453]
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.4
|
pKi |
90 |
|
⤷ |
pKi
7.4
(Ki 3.8x10-8 M)
[90]
|
VU0366058
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.1
|
pKi |
61 |
|
⤷ |
pKi
7.1
(Ki 8.4x10-8 M)
[61]
|
compound 16a [PMID: 14697765]
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.0
|
pKi |
99 |
|
⤷ |
pKi
7.0
(Ki 9.1x10-8 M)
[99]
|
compound 42 [PMID: 17189691]
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.0
|
pKi |
14 |
|
⤷ |
pKi
7.0
(Ki 9.5x10-8 M)
[14]
|
compound 8 [PMID: 20598884]
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.0
|
pKi |
25 |
|
⤷ |
pKi
7.0
(Ki 1.02x10-7 M)
[25]
|
VU-1545
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
6.8
|
pKi |
22 |
|
⤷ |
pKi
6.8
(Ki 1.56x10-7 M)
[22]
|
compound 11a [PMID: 14697765]
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
6.8
|
pKi |
99 |
|
⤷ |
pKi
6.8
(Ki 1.59x10-7 M)
[99]
|
VU0360172
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
6.7
|
pKi |
76 |
|
⤷ |
pKi
6.7
(Ki 1.95x10-7 M)
[76]
|
compound 27 [PMID: 20598884]
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
6.7
|
pKi |
25 |
|
⤷ |
pKi
6.7
(Ki 2.06x10-7 M)
[25]
|
VU-29
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
6.6
|
pKi |
16 |
|
⤷ |
pKi
6.6
(Ki 2.44x10-7 M)
[16]
|
M-5MPEP
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
6.5
|
pKi |
77 |
|
⤷ |
pKi
6.5
(Ki 3x10-7 M)
[77]
|
Br-5MPEPy
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
6.5
|
pKi |
77 |
|
⤷ |
pKi
6.5
(Ki 3x10-7 M)
[77]
|
LSN2463359
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
6.4
|
pKi |
31 |
|
⤷ |
pKi
6.4
(Ki 3.77x10-7 M)
[31]
|
5-MPEP
|
|
|
|
|
|
|
|
|
|
Rn |
Neutral
|
6.4
|
pKi |
77 |
|
⤷ |
pKi
6.4
[77]
|
compound 18 [PMID: 21927650]
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
6.3
|
pKi |
48 |
|
⤷ |
pKi
6.3
(Ki 4.77x10-7 M)
[48]
|
LSN2814617
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
5.9
|
pKi |
31 |
|
⤷ |
pKi
5.9
(Ki 1.34x10-6 M)
[31]
|
5PAM523
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
5.7
|
pKi |
68 |
|
⤷ |
pKi
5.7
(Ki 2x10-6 M)
[68]
|
CPPZ
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
5.5
|
pKi |
91 |
|
⤷ |
pKi
5.5
(Ki 3.1x10-6 M)
[91]
|
ADX-47273
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
5.4
|
pKi |
31 |
|
⤷ |
pKi
5.4
(Ki 3.65x10-6 M)
[31]
|
cinacalcet
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
4.3
|
pKi |
35 |
|
⤷ |
pKi
4.3
[35]
|
VU0424465
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
8.8
|
pEC50 |
81 |
|
⤷ |
pEC50
8.8
(EC50 1.5x10-9 M)
[81]
|
VU0404251
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
8.1
|
pEC50 |
54 |
|
⤷ |
pEC50
8.1
(EC50 7.2x10-9 M)
[54]
|
VU-29
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
8.1
|
pEC50 |
16 |
|
⤷ |
pEC50
8.1
(EC50 9x10-9 M)
[16]
|
VU-1545
|
|
|
|
|
|
|
|
|
|
Hs |
Positive
|
8.0
|
pEC50 |
22 |
|
⤷ |
pEC50
8.0
(EC50 9.6x10-9 M)
[22]
|
VU0463841
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.9
|
pEC50 |
2 |
|
⤷ |
pEC50
7.9
(EC50 1.3x10-8 M)
[2]
|
compound 41 [PMID: 23434029]
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.9
|
pEC50 |
15 |
|
⤷ |
pEC50
7.9
(EC50 1.3x10-8 M)
[15]
|
CDPPB
|
|
|
|
|
|
|
|
|
|
Hs |
Positive
|
7.6 – 8.0
|
pEC50 |
44,49 |
|
⤷ |
pEC50
7.6 – 8.0
[44,49]
|
VU0360172
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
7.8
|
pEC50 |
76 |
|
⤷ |
pEC50
7.8
(EC50 1.6x10-8 M)
[76]
|
CDPPB
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
7.7
|
pEC50 |
49 |
|
⤷ |
pEC50
7.7
[49]
|
LSN2463359
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
7.6
|
pEC50 |
31 |
|
⤷ |
pEC50
7.6
(EC50 2.4x10-8 M)
[31]
|
LSN2463359
|
|
|
|
|
|
|
|
|
|
Hs |
Positive
|
7.5
|
pEC50 |
31 |
|
⤷ |
pEC50
7.5
(EC50 3.3x10-8 M)
[31]
|
VU0357121
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
7.5
|
pEC50 |
32 |
|
⤷ |
pEC50
7.5
(EC50 3.3x10-8 M)
[32]
|
VU0092273
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
7.5
|
pEC50 |
64 |
|
⤷ |
pEC50
7.5
(EC50 3.5x10-8 M)
[64]
|
VU0240382
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
7.4
|
pEC50 |
64 |
|
⤷ |
pEC50
7.4
(EC50 3.9x10-8 M)
[64]
|
compound 47 [PMID: 21295468]
|
|
|
|
|
|
|
|
|
|
Hs |
Positive
|
7.3
|
pEC50 |
96 |
|
⤷ |
pEC50
7.3
(EC50 5.01x10-8 M)
[96]
|
LSN2814617
|
|
|
|
|
|
|
|
|
|
Hs |
Positive
|
7.3
|
pEC50 |
31 |
|
⤷ |
pEC50
7.3
(EC50 5.2x10-8 M)
[31]
|
ADX-47273
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
7.3
|
pEC50 |
31 |
|
⤷ |
pEC50
7.3
(EC50 5.5x10-8 M)
[31]
|
VU0404251
|
|
|
|
|
|
|
|
|
|
Hs |
Positive
|
7.2
|
pEC50 |
54 |
|
⤷ |
pEC50
7.2
(EC50 7x10-8 M)
[54]
|
LSN2814617
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
7.0
|
pEC50 |
31 |
|
⤷ |
pEC50
7.0
(EC50 9.3x10-8 M)
[31]
|
VU0361747
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
6.9
|
pEC50 |
64 |
|
⤷ |
pEC50
6.9
(EC50 1.26x10-7 M)
[64]
|
ADX-47273
|
|
|
|
|
|
|
|
|
|
Hs |
Positive
|
6.8
|
pEC50 |
31 |
|
⤷ |
pEC50
6.8
(EC50 1.57x10-7 M)
[31]
|
5PAM523
|
|
|
|
|
|
|
|
|
|
Hs |
Positive
|
6.7
|
pEC50 |
68 |
|
⤷ |
pEC50
6.7
(EC50 2.01x10-7 M)
[68]
|
5PAM523
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
6.5
|
pEC50 |
68 |
|
⤷ |
pEC50
6.5
(EC50 3.11x10-7 M)
[68]
|
NCFP
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
6.0 – 6.7
|
pEC50 |
63 |
|
⤷ |
pEC50
6.7
(EC50 2.14x10-7 M)
EC50 with high mGlu5 expression
[63]
pEC50
6.4
(EC50 3.7x10-7 M)
EC50 with low mGlu5 expression
[63]
pEC50
6.0
(EC50 9.69x10-7 M)
EC50 from assay using rat astrocytes
[63]
|
CPPZ
|
|
|
|
|
|
|
|
|
|
Hs |
Positive
|
6.3
|
pEC50 |
91 |
|
⤷ |
pEC50
6.3
(EC50 5x10-7 M)
[91]
|
VU0364289
|
|
|
|
|
|
|
|
|
|
Rn |
Positive
|
5.8
|
pEC50 |
107 |
|
⤷ |
pEC50
5.8
(EC50 1.6x10-6 M)
[107]
|
SP203
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
10.4
|
pIC50 |
87 |
|
⤷ |
pIC50
10.4
(IC50 3.6x10-11 M)
[87]
|
compound 18 [PMID: 17723296]
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
9.1
|
pIC50 |
101 |
|
⤷ |
pIC50
9.1
(IC50 7.2x10-10 M)
[101]
|
compound 23 [PMID: 17590335]
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
9.1
|
pIC50 |
57 |
|
⤷ |
pIC50
9.1
(IC50 8x10-10 M)
[57]
|
MTEB
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
8.7
|
pIC50 |
99 |
|
⤷ |
pIC50
8.7
[99]
|
GRN-529
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
8.6
|
pIC50 |
38 |
|
⤷ |
pIC50
8.6
(IC50 2.6x10-9 M)
[38]
|
compound 8 [PMID: 15482908]
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
8.4
|
pIC50 |
89 |
|
⤷ |
pIC50
8.4
(IC50 3.9x10-9 M)
[89]
|
[3H]M-MPEP
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
8.3 – 8.4
|
pIC50 |
29,65 |
|
⤷ |
pIC50
8.4
[29]
pIC50
8.3
[65]
|
compound 10 [PMID: 15482906]
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
8.2
|
pIC50 |
36 |
|
⤷ |
pIC50
8.2
(IC50 6.7x10-9 M)
[36]
|
AZD9272
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
8.1
|
pIC50 |
75 |
|
⤷ |
pIC50
8.1
(IC50 7.6x10-9 M)
[75]
|
alloswitch-1
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
8.1
|
pIC50 |
73 |
|
⤷ |
pIC50
8.1
(IC50 8.6x10-9 M)
[73]
Description: Inhibition of agonist-induced IP accumulation.
|
CTEP
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.9 – 8.2
|
pIC50 |
47 |
|
⤷ |
pIC50
7.9 – 8.2
(IC50 1.14x10-8 – 6.4x10-9 M)
[47]
|
compound 30 [PMID: 21757343]
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.9
|
pIC50 |
100 |
|
⤷ |
pIC50
7.9
(IC50 1.2x10-8 M)
[100]
|
VU0463841
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.9
|
pIC50 |
2 |
|
⤷ |
pIC50
7.9
(IC50 1.3x10-8 M)
[2]
|
AZD6538
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.9
|
pIC50 |
75 |
|
⤷ |
pIC50
7.9
(IC50 1.34x10-8 M)
[75]
|
compound 29b [PMID: 20809633]
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.8
|
pIC50 |
12 |
|
⤷ |
pIC50
7.8
(IC50 1.6x10-8 M)
[12]
|
compound 30 [PMID: 21757343]
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.8
|
pIC50 |
100 |
|
⤷ |
pIC50
7.8
(IC50 1.7x10-8 M)
[100]
|
compound 24 [PMID: 23374867]
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.7
|
pIC50 |
33 |
|
⤷ |
pIC50
7.7
(IC50 1.9x10-8 M)
[33]
|
[14C]MTEP
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.7
|
pIC50 |
3 |
|
⤷ |
pIC50
7.7
[3]
|
dipraglurant
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.7
|
pIC50 |
15 |
|
⤷ |
pIC50
7.7
(IC50 2x10-8 M)
[15]
|
compound 16a [PMID: 14697765]
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.7
|
pIC50 |
99 |
|
⤷ |
pIC50
7.7
(IC50 2.2x10-8 M)
[99]
|
compound 24d [PMID: 23357634]
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.6
|
pIC50 |
106 |
|
⤷ |
pIC50
7.6
(IC50 2.3x10-8 M)
[106]
|
VU0285683
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.6
|
pIC50 |
76 |
|
⤷ |
pIC50
7.6
(IC50 2.44x10-8 M)
[76]
|
MPEP
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.4 – 7.7
|
pIC50 |
29-30 |
|
⤷ |
pIC50
7.4 – 7.7
[29-30]
|
compound 13 [PMID: 15686941]
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.6
|
pIC50 |
6 |
|
⤷ |
pIC50
7.6
(IC50 2.8x10-8 M)
[6]
|
methoxymethyl-MTEP
|
|
|
|
|
|
|
|
|
|
Rn |
Negative
|
7.5
|
pIC50 |
3 |
|
⤷ |
pIC50
7.5
(IC50 3x10-8 M)
[3]
|
compound 16m [PMID: 19931453]
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.5
|
pIC50 |
90 |
|
⤷ |
pIC50
7.5
(IC50 3.2x10-8 M)
[90]
|
compound 11a [PMID: 14697765]
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.4
|
pIC50 |
99 |
|
⤷ |
pIC50
7.4
(IC50 4.1x10-8 M)
[99]
|
GSK2210875
|
|
|
|
|
|
|
|
|
|
Hs |
Negative
|
7.4
|
pIC50 |
70 |
|
⤷ |
pIC50
7.4
(IC50 4x10-8 M)
[70]
|
compound |