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Grm5 (geneid:24418) - Gene BioActivity Data
Also known as: mGluR5, mGlur5.
BioActivity Outcomes:
Probe(22)
 
 
Active(956)
 
 
Inactive(139)
 
 
Inconclusive(90)
 
 
Unspecified(448)
 
 
BioAssay Types:
Literature(1508)
 
 
 
 
 
Confirmatory(138)
 
 
 
 
 
BioActivity Types:
IC50(552)
 
 
 
 
 
 
EC50(420)
 
 
 
 
 
 
Ki(343)
 
 
 
 
 
Kd(5)
 
 
Substance Types:
Chemical(1655)
 
 
 
 
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 156    Data Row: 1655   Total Pages: 34   Display: Page     
Sort: [Click the result table header to sort]
#StructureSubstanceCompoundActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID126920341]
[CID53384864]
Average_IC50_uM 0.00483533mGluR5_3H_methoxyPEPy_Binding [AID588710, Type: confirmatory] [gi:8393490]
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2
[SID160963303]
[CID70789094]
Ki_uM 0.01Discovery of Novel Silent Allosteric Modulators (SAM) of the Metabotropic Glutamate Receptor 5: 3pt binding Assay [AID652191, Type: confirmatory] [gi:8393490]
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3
[SID160963303]
[CID70789094]
Average_Ki_uM 0.0182Discovery of Novel Silent Allosteric Modulators (SAM) of the Metabotropic Glutamate Receptor 5: full Ki determination [AID652196, Type: confirmatory] [gi:8393490]
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4
[SID144241536]
[CID4384110]
Average_EC50_uM 0.049Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5 (calcium_assay) [AID651835, Type: confirmatory] [gi:8393490]
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5
[SID144241535]
[CID1364364]
Average_EC50_uM 0.051Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5 (calcium_assay) [AID651835, Type: confirmatory] [gi:8393490]
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6
[SID125305189]
[CID53382545]
Average_IC50_uM 0.0575mGluR5_3H_methoxyPEPy_Binding [AID588710, Type: confirmatory] [gi:8393490]
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7
[SID144241562]
[CID60210908]
Average_EC50_uM 0.085Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5 (calcium_assay) [AID651835, Type: confirmatory] [gi:8393490]
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8
[SID160963303]
[CID70789094]
Average_EC50_MICROMOLAR 0.1363Discovery of Novel Silent Allosteric Modulators (SAM) of the Metabotropic Glutamate Receptor 5: Fold-shift Assay [AID652198, Type: confirmatory] [gi:8393490]
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9
[SID144241527]
[CID60210882]
Average_EC50_uM 0.298Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5 (calcium_assay) [AID651835, Type: confirmatory] [gi:8393490]
View
10
[SID144241541]
[CID60210914]
Average_EC50_uM 0.427Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5 (calcium_assay) [AID651835, Type: confirmatory] [gi:8393490]
View
11
[SID144241540]
[CID60210915]
Average_EC50_uM 0.944Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5 (calcium_assay) [AID651835, Type: confirmatory] [gi:8393490]
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12
[SID144241561]
[CID60210917]
Average_EC50_uM 1.393Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5 (calcium_assay) [AID651835, Type: confirmatory] [gi:8393490]
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13
[SID144241537]
[CID60210899]
Average_EC50_uM 1.688Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5 (calcium_assay) [AID651835, Type: confirmatory] [gi:8393490]
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14
[SID144241539]
[CID60210911]
Average_EC50_uM 1.744Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5 (calcium_assay) [AID651835, Type: confirmatory] [gi:8393490]
View
15
[SID144241564]
[CID1318633]
Average_EC50_uM 2.411Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5 (calcium_assay) [AID651835, Type: confirmatory] [gi:8393490]
View
16
[SID144241560]
[CID60210894]
Average_EC50_uM 2.456Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5 (calcium_assay) [AID651835, Type: confirmatory] [gi:8393490]
View
17
[SID144241551]
[CID60210906]
Average_EC50_uM 3.619Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5 (calcium_assay) [AID651835, Type: confirmatory] [gi:8393490]
View
18
[SID144241538]
[CID60210913]
Average_EC50_uM 4.395Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5 (calcium_assay) [AID651835, Type: confirmatory] [gi:8393490]
View
19
[SID144241553]
[CID60210918]
Average_EC50_uM 4.435Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5 (calcium_assay) [AID651835, Type: confirmatory] [gi:8393490]
View
20
[SID144241542]
[CID3433401]
Average_EC50_uM 4.53Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5 (calcium_assay) [AID651835, Type: confirmatory] [gi:8393490]
View
21
[SID144241549]
[CID60210910]
Average_EC50_uM 5.445Identification of a glycine sulfonamide based non-MPEP site positive allosteric potentiator (PAM) of mGlu5 (calcium_assay) [AID651835, Type: confirmatory] [gi:8393490]
View
22
[SID144241527]
[CID60210882]
ML332 Competition in Radioligand Binding assays (Ricerca) [AID651827, Type: other] [gi:8393490]
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23
[SID103520919]
[CID16737207]
IC50 3.6e-05Displacement of [3H]MPEP from mGluR5 in rat brain membrane [AID291620, Type: Literature] [gi:1170947]
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24
[SID103520919]
[CID16737207]
Ki 3.6e-05Displacement of [3H]MPEP from mGluR5 in rat brain [AID570310, Type: Literature] [gi:1170947]
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25
[SID103520920]
[CID16737208]
IC50 6e-05Displacement of [3H]MPEP from mGluR5 in rat brain membrane [AID291620, Type: Literature] [gi:1170947]
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26
[SID103614357]
[CID44574111]
Ki 8e-05Displacement of [3H]MPEP from mGluR5 in rat brain [AID570310, Type: Literature] [gi:1170947]
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27
[SID131284870]
[CID53249063]
Ki 0.000106Displacement of [3H]methoxy-PEPY from rat mGluR5 expressed in human HEK-293 cells by liquid scintillation counting [AID601416, Type: Literature] [gi:1170947]
View
28
[SID131276868]
[CID53249062]
Ki 0.000127Displacement of [3H]methoxy-PEPY from rat mGluR5 expressed in human HEK-293 cells by liquid scintillation counting [AID601416, Type: Literature] [gi:1170947]
View
29
[SID131280906]
[CID46208249]
Ki 0.0002Displacement of [3H]methoxy-PEPY from rat mGluR5 expressed in human HEK-293 cells by liquid scintillation counting [AID601416, Type: Literature] [gi:1170947]
View
30
[SID103256385]
[CID3025961]
IC50 0.0002Activity at rat mGlu5 receptor expressed in CHO cells assessed as inhibition of quisqualate-stimulated calcium mobilization by FLIPR assay [AID299817, Type: Literature] [gi:1170947]
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31
[SID103520925]
[CID16736578]
IC50 0.00023Displacement of [3H]MPEP from mGluR5 in rat brain membrane [AID291620, Type: Literature] [gi:1170947]
View
32
[SID103478374]
[CID11535913]
Ki 0.00025Displacement of [3H]MPEP from mGluR5 in rat brain membranes [AID259885, Type: Literature] [gi:1170947]
View
33
[SID124968322]
[CID51050145]
Ki 0.00025Displacement of [3H]MPEP from mGluR5 in rat brain [AID570310, Type: Literature] [gi:1170947]
View
34
[SID124960417]
[CID51039242]
Ki 0.00027Displacement of [3H]MPEP from mGluR5 in rat brain [AID570310, Type: Literature] [gi:1170947]
View
35
[SID124968324]
[CID51050257]
Ki 0.00028Displacement of [3H]MPEP from mGluR5 in rat brain [AID570310, Type: Literature] [gi:1170947]
View
36
[SID131286927]
[CID53249064]
Ki 0.0003Displacement of [3H]methoxy-PEPY from rat mGluR5 expressed in human HEK-293 cells by liquid scintillation counting [AID601416, Type: Literature] [gi:1170947]
View
37
[SID131278895]
[CID53249061]
IC50 0.00032Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilization [AID601415, Type: Literature] [gi:1170947]
View
38
[SID131280842]
[CID54584297]
Ki 0.00036Displacement of [3H]methoxy-PEPY from rat mGluR5 expressed in human HEK-293 cells by liquid scintillation counting [AID601416, Type: Literature] [gi:1170947]
View
39
[SID103614357]
[CID44574111]
Ki 0.00036Displacement of [3H]methoxy-PEPY from rat mGluR5 expressed in human HEK-293 cells by liquid scintillation counting [AID601416, Type: Literature] [gi:1170947]
View
40
[SID131278896]
[CID54583366]
IC50 0.00039Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilization [AID601415, Type: Literature] [gi:1170947]
View
41
[SID124971325]
[CID51039243]
Ki 0.0004Displacement of [3H]MPEP from mGluR5 in rat brain [AID570310, Type: Literature] [gi:1170947]
View
42
[SID103447884]
[CID11378977]
IC50 0.000415Antagonist activity at rat mGluR5 expressed in HEK293A cells assessed as glutamate-induced calcium flux preincubated for 140 sec before glutamate challenge by calcium fluorescence assay [AID375051, Type: Literature] [gi:1170947]
View
43
[SID103520921]
[CID16736577]
IC50 0.00048Displacement of [3H]MPEP from mGluR5 in rat brain membrane [AID291620, Type: Literature] [gi:1170947]
View
44
[SID103520923]
[CID16737209]
IC50 0.00052Displacement of [3H]MPEP from mGluR5 in rat brain membrane [AID291620, Type: Literature] [gi:1170947]
View
45
[SID103750886]
[CID46237677]
Kd 0.0006Binding affinity to mGluR5 ligand binding site 1 in Sprague-Dawley rat brain P2 membrane after 45 mins by gamma counting [AID479139, Type: Literature] [gi:1170947]
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46
[SID131286927]
[CID53249064]
IC50 0.00061Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilization [AID601415, Type: Literature] [gi:1170947]
View
47
[SID131282902]
[CID54585280]
IC50 0.00063Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilization [AID601415, Type: Literature] [gi:1170947]
View
48
[SID131280907]
[CID54584312]
IC50 0.00066Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilization [AID601415, Type: Literature] [gi:1170947]
View
49
[SID131280906]
[CID46208249]
IC50 0.00066Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilization [AID601415, Type: Literature] [gi:1170947]
View
50
[SID131284869]
[CID54586229]
IC50 0.00066Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilization [AID601415, Type: Literature] [gi:1170947]
View