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Compile Data Set for Download or QSAR

Found 322 hits of ec50 data for polymerid = 8283   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50116515
PNG
(CHEMBL3609729)
Show SMILES Cc1sc(Nc2nccc(C)n2)nc1-c1cn[nH]c1
Show InChI InChI=1S/C12H12N6S/c1-7-3-4-13-11(16-7)18-12-17-10(8(2)19-12)9-5-14-15-6-9/h3-6H,1-2H3,(H,14,15)(H,13,16,17,18)
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n/an/an/an/a 9n/an/an/an/a



Massachusetts General Hospital

Curated by ChEMBL


Assay Description
Positive allosteric modulator activity at rat mGlu4 receptor


Bioorg Med Chem Lett 25: 3956-60 (2015)


Article DOI: 10.1016/j.bmcl.2015.07.031
BindingDB Entry DOI: 10.7270/Q28C9Z1B
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50563242
PNG
(CHEMBL4744533)
Show SMILES Cc1cc(C)cc(NC(=O)[C@@H]2CSCCC(=O)N2)c1 |r|
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TBA

Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells co- expressing GIRK channel by thallium mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2021.127838
BindingDB Entry DOI: 10.7270/Q2T43XTH
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50241575
PNG
(CHEMBL4067875)
Show SMILES O\N=c1/cc(oc2ccc(OCCN3CCOCC3)cc12)-c1cc2cccn2cn1
Show InChI InChI=1S/C22H22N4O4/c27-24-19-14-22(20-12-16-2-1-5-26(16)15-23-20)30-21-4-3-17(13-18(19)21)29-11-8-25-6-9-28-10-7-25/h1-5,12-15,27H,6-11H2/b24-19+
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Prexton Therapeutics

Curated by ChEMBL


Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells co-expressing Gi/Gq assessed as increase in glutamate-induced calcium ...


J Med Chem 60: 8515-8537 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00991
BindingDB Entry DOI: 10.7270/Q2GF0WNQ
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50007548
PNG
((S)-2-Amino-4-phosphono-butyric acid | (S)-2-amino...)
Show SMILES N[C@@H](CCP(O)(O)=O)C(O)=O |r|
Show InChI InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m0/s1
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Univ. Rouen

Curated by ChEMBL


Assay Description
Agonist activity at rat mGluR4 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay


Bioorg Med Chem Lett 25: 2523-6 (2015)


Article DOI: 10.1016/j.bmcl.2015.04.043
BindingDB Entry DOI: 10.7270/Q21Z464C
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50217031
PNG
((1S,2R)-1-amino-2-phosphonomethylcyclopropane-carb...)
Show SMILES N[C@]1(C[C@H]1CP(O)(O)=O)C(O)=O
Show InChI InChI=1S/C5H10NO5P/c6-5(4(7)8)1-3(5)2-12(9,10)11/h3H,1-2,6H2,(H,7,8)(H2,9,10,11)/t3-,5-/m0/s1
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Univ. Rouen

Curated by ChEMBL


Assay Description
Agonist activity at rat mGluR4 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay


Bioorg Med Chem Lett 25: 2523-6 (2015)


Article DOI: 10.1016/j.bmcl.2015.04.043
BindingDB Entry DOI: 10.7270/Q21Z464C
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50559790
PNG
(CHEMBL4744407)
Show SMILES [Na;v0+].[#6]-[#8]-c1cc(-[#7]-[#6](=O)-c2ccccn2)ccc1-[#7]-[#6](=O)-c1ccc(-[#7]-[#6](=O)-[#6]-[#8]-[#6]-[#6](=O)-[#7]-[#6]-[#6]-[#6]-[#6]-[#6]-[#6]-[#6]-[#7]-[#6](=O)-[#6]-[#8]-c2ccc(cc2-[#6](-[#8-])=O)-c2cccc(-[#6]-[#8]-c3cc4-[#6]-[#6](-[#6]-5-[#6]-[#6]-[#6]-[#6]-5)-[#6](=O)-c4c(-[#6])c3-[#6])c2)cc1Cl
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TBA

Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glut...


Citation and Details

Article DOI: 10.1016/j.bmcl.2020.127212
BindingDB Entry DOI: 10.7270/Q27H1P86
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50007548
PNG
((S)-2-Amino-4-phosphono-butyric acid | (S)-2-amino...)
Show SMILES N[C@@H](CCP(O)(O)=O)C(O)=O |r|
Show InChI InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m0/s1
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University of Copenhagen

Curated by ChEMBL


Assay Description
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay


J Med Chem 59: 914-24 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01333
BindingDB Entry DOI: 10.7270/Q2000408
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50559789
PNG
(CHEMBL4762369)
Show SMILES [Na;v0+].[#6]-[#8]-c1cc(-[#7]-[#6](=O)-c2ccccn2)ccc1-[#7]-[#6](=O)-c1ccc(-[#7]-[#6](=O)-[#6]-[#8]-[#6]-[#6](=O)-[#7]-[#6]-[#6]-[#6]-[#6]-[#6]-[#6]-[#7]-[#6](=O)-[#6]-[#8]-c2ccc(cc2-[#6](-[#8-])=O)-c2cccc(-[#6]-[#8]-c3cc4-[#6]-[#6](-[#6]-5-[#6]-[#6]-[#6]-[#6]-5)-[#6](=O)-c4c(-[#6])c3-[#6])c2)cc1Cl
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TBA

Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glut...


Citation and Details

Article DOI: 10.1016/j.bmcl.2020.127212
BindingDB Entry DOI: 10.7270/Q27H1P86
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50559791
PNG
(CHEMBL4740929)
Show SMILES [Na;v0+].[#6]-[#8]-c1cc(-[#7]-[#6](=O)-c2ccccn2)ccc1-[#7]-[#6](=O)-c1ccc(-[#7]-[#6](=O)-[#6]-[#8]-[#6]-[#6](=O)-[#7]-[#6]-[#6]-[#6]-[#6]-[#6]-[#6]-[#6]-[#6]-[#7]-[#6](=O)-[#6]-[#8]-c2ccc(cc2-[#6](-[#8-])=O)-c2cccc(-[#6]-[#8]-c3cc4-[#6]-[#6](-[#6]-5-[#6]-[#6]-[#6]-[#6]-5)-[#6](=O)-c4c(-[#6])c3-[#6])c2)cc1Cl
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TBA

Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glut...


Citation and Details

Article DOI: 10.1016/j.bmcl.2020.127212
BindingDB Entry DOI: 10.7270/Q27H1P86
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50559787
PNG
(CHEMBL4786847)
Show SMILES [Na;v0+].[#6]-[#8]-c1cc(-[#7]-[#6](=O)-c2ccccn2)ccc1-[#7]-[#6](=O)-c1ccc(-[#7]-[#6](=O)-[#6]-[#8]-[#6]-[#6](=O)-[#7]-[#6]-[#6]-[#6]-[#6]-[#7]-[#6](=O)-[#6]-[#8]-c2ccc(cc2-[#6](-[#8-])=O)-c2cccc(-[#6]-[#8]-c3cc4-[#6]-[#6](-[#6]-5-[#6]-[#6]-[#6]-[#6]-5)-[#6](=O)-c4c(-[#6])c3-[#6])c2)cc1Cl
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TBA

Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glut...


Citation and Details

Article DOI: 10.1016/j.bmcl.2020.127212
BindingDB Entry DOI: 10.7270/Q27H1P86
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50563239
PNG
(CHEMBL4758183)
Show SMILES Clc1cc(Br)cc(NC(=O)[C@@H]2CSCCC(=O)N2)c1 |r|
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TBA

Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells co- expressing GIRK channel by thallium mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2021.127838
BindingDB Entry DOI: 10.7270/Q2T43XTH
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM55082
PNG
(N-[4-[(2-chlorobenzoyl)amino]-3-methoxy-phenyl]pic...)
Show SMILES COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccccc1Cl
Show InChI InChI=1S/C20H16ClN3O3/c1-27-18-12-13(23-20(26)17-8-4-5-11-22-17)9-10-16(18)24-19(25)14-6-2-3-7-15(14)21/h2-12H,1H3,(H,23,26)(H,24,25)
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TBA

Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glut...


Citation and Details

Article DOI: 10.1016/j.bmcl.2020.127212
BindingDB Entry DOI: 10.7270/Q27H1P86
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM55087
PNG
(N-[3-chloranyl-4-[4-chloranyl-1,3-bis(oxidanyliden...)
Show SMILES Clc1cccc2C(=O)N(C(=O)c12)c1ccc(NC(=O)c2ccccn2)cc1Cl
Show InChI InChI=1S/C20H11Cl2N3O3/c21-13-5-3-4-12-17(13)20(28)25(19(12)27)16-8-7-11(10-14(16)22)24-18(26)15-6-1-2-9-23-15/h1-10H,(H,24,26)
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n/an/an/an/a 34.9n/an/an/an/a



Vanderbilt University Medical Center

Curated by ChEMBL


Assay Description
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay


J Med Chem 54: 7639-47 (2011)


Article DOI: 10.1021/jm200956q
BindingDB Entry DOI: 10.7270/Q25Q4WHD
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50559788
PNG
(CHEMBL4777845)
Show SMILES [Na;v0+].[#6]-[#8]-c1cc(-[#7]-[#6](=O)-c2ccccn2)ccc1-[#7]-[#6](=O)-c1ccc(-[#7]-[#6](=O)-[#6]-[#8]-[#6]-[#6](=O)-[#7]-[#6]-[#6]-[#6]-[#6]-[#6]-[#7]-[#6](=O)-[#6]-[#8]-c2ccc(cc2-[#6](-[#8-])=O)-c2cccc(-[#6]-[#8]-c3cc4-[#6]-[#6](-[#6]-5-[#6]-[#6]-[#6]-[#6]-5)-[#6](=O)-c4c(-[#6])c3-[#6])c2)cc1Cl
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TBA

Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glut...


Citation and Details

Article DOI: 10.1016/j.bmcl.2020.127212
BindingDB Entry DOI: 10.7270/Q27H1P86
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50563240
PNG
(CHEMBL4742127)
Show SMILES Brc1cc(Br)cc(NC(=O)[C@@H]2CSCCC(=O)N2)c1 |r|
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TBA

Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells co- expressing GIRK channel by thallium mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2021.127838
BindingDB Entry DOI: 10.7270/Q2T43XTH
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50559786
PNG
(CHEMBL4800093)
Show SMILES [Na;v0+].[#6]-[#8]-c1cc(-[#7]-[#6](=O)-c2ccccn2)ccc1-[#7]-[#6](=O)-c1ccc(-[#7]-[#6](=O)-[#6]-[#8]-[#6]-[#6](=O)-[#7]-[#6]-[#6]-[#6]-[#7]-[#6](=O)-[#6]-[#8]-c2ccc(cc2-[#6](-[#8-])=O)-c2cccc(-[#6]-[#8]-c3cc4-[#6]-[#6](-[#6]-5-[#6]-[#6]-[#6]-[#6]-5)-[#6](=O)-c4c(-[#6])c3-[#6])c2)cc1Cl
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TBA

Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing GIRK assessed as thallium influx in presence of EC20 glut...


Citation and Details

Article DOI: 10.1016/j.bmcl.2020.127212
BindingDB Entry DOI: 10.7270/Q27H1P86
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50220011
PNG
(CHEMBL243925 | L-(+)-2-amino-4-thiophosphonobutyri...)
Show SMILES N[C@@H](CCP(O)(O)=S)C(O)=O
Show InChI InChI=1S/C4H10NO4PS/c5-3(4(6)7)1-2-10(8,9)11/h3H,1-2,5H2,(H,6,7)(H2,8,9,11)/t3-/m0/s1
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Université Paris Descartes

Curated by ChEMBL


Assay Description
Agonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate production


J Med Chem 50: 4656-64 (2007)


Article DOI: 10.1021/jm070400y
BindingDB Entry DOI: 10.7270/Q2XP74NQ
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50241580
PNG
(CHEMBL4089083)
Show SMILES O\N=c1/cc(oc2ccc(CCCN3CCOCC3)cc12)-c1cc2sccc2cn1
Show InChI InChI=1S/C23H23N3O3S/c27-25-19-13-22(20-14-23-17(15-24-20)5-11-30-23)29-21-4-3-16(12-18(19)21)2-1-6-26-7-9-28-10-8-26/h3-5,11-15,27H,1-2,6-10H2/b25-19+
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Prexton Therapeutics

Curated by ChEMBL


Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells co-expressing Gi/Gq assessed as increase in glutamate-induced calcium ...


J Med Chem 60: 8515-8537 (2017)


Article DOI: 10.1021/acs.jmedchem.7b00991
BindingDB Entry DOI: 10.7270/Q2GF0WNQ
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50166956
PNG
(CHEMBL3798517)
Show SMILES CCc1cnc(Oc2ccc(NC(=O)c3ncccc3N)cc2Cl)nc1
Show InChI InChI=1S/C18H16ClN5O2/c1-2-11-9-22-18(23-10-11)26-15-6-5-12(8-13(15)19)24-17(25)16-14(20)4-3-7-21-16/h3-10H,2,20H2,1H3,(H,24,25)
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Vanderbilt University Medical Center

Curated by ChEMBL


Assay Description
Positive allosteric modulator activity at rat mGlu4 receptor


Bioorg Med Chem Lett 26: 2915-2919 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.041
BindingDB Entry DOI: 10.7270/Q2348N9V
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50503360
PNG
(CHEMBL4459205)
Show SMILES Cc1noc2c(F)cc(Nc3n[nH]c4cccnc34)cc12
Show InChI InChI=1S/C14H10FN5O/c1-7-9-5-8(6-10(15)13(9)21-20-7)17-14-12-11(18-19-14)3-2-4-16-12/h2-6H,1H3,(H2,17,18,19)
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Vanderbilt University

Curated by ChEMBL


Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK cells co-expressing GIRK1/2 assessed as increase in glutamate-induced thallium ...


J Med Chem 62: 342-358 (2019)


Article DOI: 10.1021/acs.jmedchem.8b00994
BindingDB Entry DOI: 10.7270/Q29K4FHW
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM196924
PNG
(US9212196, Derivative 20)
Show SMILES N[C@H](CCP(O)(=O)C(O)c1ccc(OCC(O)=O)c(OC(F)(F)F)c1)C(O)=O |r|
Show InChI InChI=1S/C14H17F3NO9P/c15-14(16,17)27-10-5-7(1-2-9(10)26-6-11(19)20)13(23)28(24,25)4-3-8(18)12(21)22/h1-2,5,8,13,23H,3-4,6,18H2,(H,19,20)(H,21,22)(H,24,25)/t8-,13?/m1/s1
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n/an/an/an/a 60n/an/an/an/a



UNIVERSITE PARIS DESCARTES; UNIVERSITE D'AUVERGNE

US Patent


Assay Description
Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and ...


US Patent US9212196 (2015)


BindingDB Entry DOI: 10.7270/Q28G8JJR
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50563245
PNG
(CHEMBL4743836)
Show SMILES Clc1cc(Br)cc(NC(=O)[C@H]2CSCCC(=O)N2)c1 |r|
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TBA

Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells co- expressing GIRK channel by thallium mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2021.127838
BindingDB Entry DOI: 10.7270/Q2T43XTH
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50503361
PNG
(CHEMBL4451827)
Show SMILES Cc1noc2ccc(Nc3n[nH]c4nccnc34)cc12
Show InChI InChI=1S/C13H10N6O/c1-7-9-6-8(2-3-10(9)20-19-7)16-13-11-12(17-18-13)15-5-4-14-11/h2-6H,1H3,(H2,15,16,17,18)
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Vanderbilt University

Curated by ChEMBL


Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK cells co-expressing GIRK1/2 assessed as increase in glutamate-induced thallium ...


J Med Chem 62: 342-358 (2019)


Article DOI: 10.1021/acs.jmedchem.8b00994
BindingDB Entry DOI: 10.7270/Q29K4FHW
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM55086
PNG
(N-(3-chloro-4-phthalimido-phenyl)picolinamide | N-...)
Show SMILES Clc1cc(NC(=O)c2ccccn2)ccc1N1C(=O)c2ccccc2C1=O
Show InChI InChI=1S/C20H12ClN3O3/c21-15-11-12(23-18(25)16-7-3-4-10-22-16)8-9-17(15)24-19(26)13-5-1-2-6-14(13)20(24)27/h1-11H,(H,23,25)
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n/an/an/an/a 66.8n/an/an/an/a



Vanderbilt University Medical Center

Curated by ChEMBL


Assay Description
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay


J Med Chem 54: 7639-47 (2011)


Article DOI: 10.1021/jm200956q
BindingDB Entry DOI: 10.7270/Q25Q4WHD
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50563246
PNG
(CHEMBL4742838)
Show SMILES Brc1cc(Br)cc(NC(=O)[C@H]2CSCCC(=O)N2)c1 |r|
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TBA

Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells co- expressing GIRK channel by thallium mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2021.127838
BindingDB Entry DOI: 10.7270/Q2T43XTH
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50007548
PNG
((S)-2-Amino-4-phosphono-butyric acid | (S)-2-amino...)
Show SMILES N[C@@H](CCP(O)(O)=O)C(O)=O |r|
Show InChI InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m0/s1
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n/an/an/an/a 80n/an/an/an/a



Université Paris Descartes

Curated by ChEMBL


Assay Description
Agonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate production


J Med Chem 50: 4656-64 (2007)


Article DOI: 10.1021/jm070400y
BindingDB Entry DOI: 10.7270/Q2XP74NQ
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM196910
PNG
(US9212196, Derivative 6)
Show SMILES COc1cc(cc(F)c1OCC(O)=O)C(O)P(O)(=O)CC[C@@H](N)C(O)=O |r|
Show InChI InChI=1S/C14H19FNO9P/c1-24-10-5-7(4-8(15)12(10)25-6-11(17)18)14(21)26(22,23)3-2-9(16)13(19)20/h4-5,9,14,21H,2-3,6,16H2,1H3,(H,17,18)(H,19,20)(H,22,23)/t9-,14?/m1/s1
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n/an/an/an/a 80n/an/an/an/a



UNIVERSITE PARIS DESCARTES; UNIVERSITE D'AUVERGNE

US Patent


Assay Description
Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and ...


US Patent US9212196 (2015)


BindingDB Entry DOI: 10.7270/Q28G8JJR
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50293720
PNG
(CHEMBL541754 | N-(3-(difluoromethoxy)phenyl)picoli...)
Show SMILES FC(F)Oc1cccc(NC(=O)c2ccccn2)c1
Show InChI InChI=1S/C13H10F2N2O2/c14-13(15)19-10-5-3-4-9(8-10)17-12(18)11-6-1-2-7-16-11/h1-8,13H,(H,17,18)
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Vanderbilt University Medical Center

Curated by ChEMBL


Assay Description
Activity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium flux


J Med Chem 52: 4115-8 (2009)


Article DOI: 10.1021/jm9005065
BindingDB Entry DOI: 10.7270/Q2RJ4JHT
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50293720
PNG
(CHEMBL541754 | N-(3-(difluoromethoxy)phenyl)picoli...)
Show SMILES FC(F)Oc1cccc(NC(=O)c2ccccn2)c1
Show InChI InChI=1S/C13H10F2N2O2/c14-13(15)19-10-5-3-4-9(8-10)17-12(18)11-6-1-2-7-16-11/h1-8,13H,(H,17,18)
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n/an/an/an/a 80n/an/an/an/a



Massachusetts General Hospital

Curated by ChEMBL


Assay Description
Positive allosteric modulator activity at rat mGlu4 receptor


Bioorg Med Chem Lett 25: 3956-60 (2015)


Article DOI: 10.1016/j.bmcl.2015.07.031
BindingDB Entry DOI: 10.7270/Q28C9Z1B
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM361373
PNG
(6-((1H-pyrazolo[3,4-b] pyrazin-3- yl)amino)-N-(3,3...)
Show SMILES FC1(F)CC(C1)NC(=O)c1nsc2cc(Nc3n[nH]c4nccnc34)ccc12
Show InChI InChI=1S/C17H13F2N7OS/c18-17(19)6-9(7-17)23-16(27)12-10-2-1-8(5-11(10)28-26-12)22-15-13-14(24-25-15)21-4-3-20-13/h1-5,9H,6-7H2,(H,23,27)(H2,21,22,24,25)
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Vanderbilt University

Curated by ChEMBL


Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK cells co-expressing GIRK1/2 assessed as increase in glutamate-induced thallium ...


J Med Chem 62: 342-358 (2019)


Article DOI: 10.1021/acs.jmedchem.8b00994
BindingDB Entry DOI: 10.7270/Q29K4FHW
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50516018
PNG
(CHEMBL4436022)
Show SMILES Cc1nnc2ccc(cc2c1C)C(=O)NC1CN(C1)c1ncc(Cl)cc1F
Show InChI InChI=1S/C19H17ClFN5O/c1-10-11(2)24-25-17-4-3-12(5-15(10)17)19(27)23-14-8-26(9-14)18-16(21)6-13(20)7-22-18/h3-7,14H,8-9H2,1-2H3,(H,23,27)
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Vanderbilt University

Curated by ChEMBL


Assay Description
Positive allosteric modulation of rat M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in acetylcholine-induced calcium mob...


Bioorg Med Chem Lett 29: (2019)


Article DOI: 10.1016/j.bmcl.2019.126678
BindingDB Entry DOI: 10.7270/Q26D5XB5
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM361347
PNG
(6-((1H-pyrazolo[4,3-b] pyridin- 3-yl)amino)-N-(3,3...)
Show SMILES FC1(F)CC(C1)NC(=O)c1nsc2cc(Nc3n[nH]c4cccnc34)ccc12
Show InChI InChI=1S/C18H14F2N6OS/c19-18(20)7-10(8-18)23-17(27)14-11-4-3-9(6-13(11)28-26-14)22-16-15-12(24-25-16)2-1-5-21-15/h1-6,10H,7-8H2,(H,23,27)(H2,22,24,25)
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n/an/an/an/a 83n/an/an/an/a



Vanderbilt University

Curated by ChEMBL


Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK cells co-expressing GIRK1/2 assessed as increase in glutamate-induced thallium ...


J Med Chem 62: 342-358 (2019)


Article DOI: 10.1021/acs.jmedchem.8b00994
BindingDB Entry DOI: 10.7270/Q29K4FHW
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50503364
PNG
(CHEMBL4522695)
Show SMILES Cc1noc2ccc(Nc3n[nH]c4cccnc34)cc12
Show InChI InChI=1S/C14H11N5O/c1-8-10-7-9(4-5-12(10)20-19-8)16-14-13-11(17-18-14)3-2-6-15-13/h2-7H,1H3,(H2,16,17,18)
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Vanderbilt University

Curated by ChEMBL


Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK cells co-expressing GIRK1/2 assessed as increase in glutamate-induced thallium ...


J Med Chem 62: 342-358 (2019)


Article DOI: 10.1021/acs.jmedchem.8b00994
BindingDB Entry DOI: 10.7270/Q29K4FHW
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50007548
PNG
((S)-2-Amino-4-phosphono-butyric acid | (S)-2-amino...)
Show SMILES N[C@@H](CCP(O)(O)=O)C(O)=O |r|
Show InChI InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m0/s1
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Universite Paris Descartes

Curated by ChEMBL


Assay Description
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular ...


J Med Chem 53: 2797-813 (2010)


Article DOI: 10.1021/jm901523t
BindingDB Entry DOI: 10.7270/Q28W3F7Q
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM196907
PNG
(US9212196, Derivative 3)
Show SMILES COc1cc(ccc1OCC(O)=O)C(O)P(O)(=O)CC[C@@H](N)C(O)=O |r|
Show InChI InChI=1S/C14H20NO9P/c1-23-11-6-8(2-3-10(11)24-7-12(16)17)14(20)25(21,22)5-4-9(15)13(18)19/h2-3,6,9,14,20H,4-5,7,15H2,1H3,(H,16,17)(H,18,19)(H,21,22)/t9-,14?/m1/s1
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n/an/an/an/a 100n/an/an/an/a



UNIVERSITE PARIS DESCARTES; UNIVERSITE D'AUVERGNE

US Patent


Assay Description
Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and ...


US Patent US9212196 (2015)


BindingDB Entry DOI: 10.7270/Q28G8JJR
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50088290
PNG
(CHEMBL3427499)
Show SMILES NC1(CC1(F)CP(O)(O)=O)C(O)=O
Show InChI InChI=1S/C5H9FNO5P/c6-4(2-13(10,11)12)1-5(4,7)3(8)9/h1-2,7H2,(H,8,9)(H2,10,11,12)
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Univ. Rouen

Curated by ChEMBL


Assay Description
Agonist activity at rat mGluR4 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay


Bioorg Med Chem Lett 25: 2523-6 (2015)


Article DOI: 10.1016/j.bmcl.2015.04.043
BindingDB Entry DOI: 10.7270/Q21Z464C
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50358177
PNG
(CHEMBL1921952)
Show SMILES O=C(Nc1ccc(cc1)N1S(=O)(=O)c2ccccc2S1(=O)=O)c1cscn1
Show InChI InChI=1S/C16H11N3O5S3/c20-16(13-9-25-10-17-13)18-11-5-7-12(8-6-11)19-26(21,22)14-3-1-2-4-15(14)27(19,23)24/h1-10H,(H,18,20)
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n/an/an/an/a 105n/an/an/an/a



Vanderbilt University Medical Center

Curated by ChEMBL


Assay Description
Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay


J Med Chem 54: 7639-47 (2011)


Article DOI: 10.1021/jm200956q
BindingDB Entry DOI: 10.7270/Q25Q4WHD
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM55082
PNG
(N-[4-[(2-chlorobenzoyl)amino]-3-methoxy-phenyl]pic...)
Show SMILES COc1cc(NC(=O)c2ccccn2)ccc1NC(=O)c1ccccc1Cl
Show InChI InChI=1S/C20H16ClN3O3/c1-27-18-12-13(23-20(26)17-8-4-5-11-22-17)9-10-16(18)24-19(25)14-6-2-3-7-15(14)21/h2-12H,1H3,(H,23,26)(H,24,25)
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n/an/an/an/a 106n/an/an/an/a



Vanderbilt University Medical Center

Curated by ChEMBL


Assay Description
Positive allosteric modulation of rat mGluR4 expressed in CHO cells coexpressing Gqi5 assessed as calcium mobilization


J Med Chem 54: 1106-10 (2011)


Article DOI: 10.1021/jm101271s
BindingDB Entry DOI: 10.7270/Q27P90C1
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50293721
PNG
(CHEMBL562551 | N-(4-chloro-3-methoxyphenyl)picolin...)
Show SMILES COc1cc(NC(=O)c2ccccn2)ccc1Cl
Show InChI InChI=1S/C13H11ClN2O2/c1-18-12-8-9(5-6-10(12)14)16-13(17)11-4-2-3-7-15-11/h2-8H,1H3,(H,16,17)
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Vanderbilt University Medical Center

Curated by ChEMBL


Assay Description
Activity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium flux


J Med Chem 52: 4115-8 (2009)


Article DOI: 10.1021/jm9005065
BindingDB Entry DOI: 10.7270/Q2RJ4JHT
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM196906
PNG
(US9212196, Derivative 2)
Show SMILES N[C@@H](CCP(O)(=O)C(O)c1ccc(OCC(O)=O)cc1)C(O)=O |r|
Show InChI InChI=1S/C13H18NO8P/c14-10(12(17)18)5-6-23(20,21)13(19)8-1-3-9(4-2-8)22-7-11(15)16/h1-4,10,13,19H,5-7,14H2,(H,15,16)(H,17,18)(H,20,21)/t10-,13?/m0/s1
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n/an/an/an/a 110n/an/an/an/a



UNIVERSITE PARIS DESCARTES; UNIVERSITE D'AUVERGNE

US Patent


Assay Description
Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and ...


US Patent US9212196 (2015)


BindingDB Entry DOI: 10.7270/Q28G8JJR
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50563241
PNG
(CHEMBL4763684)
Show SMILES Brc1cc(I)cc(NC(=O)[C@@H]2CSCCC(=O)N2)c1 |r|
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TBA

Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells co- expressing GIRK channel by thallium mobilization assay


Citation and Details

Article DOI: 10.1016/j.bmcl.2021.127838
BindingDB Entry DOI: 10.7270/Q2T43XTH
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50088290
PNG
(CHEMBL3427499)
Show SMILES NC1(CC1(F)CP(O)(O)=O)C(O)=O
Show InChI InChI=1S/C5H9FNO5P/c6-4(2-13(10,11)12)1-5(4,7)3(8)9/h1-2,7H2,(H,8,9)(H2,10,11,12)
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Univ. Rouen

Curated by ChEMBL


Assay Description
Agonist activity at rat mGluR4 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay


Bioorg Med Chem Lett 25: 2523-6 (2015)


Article DOI: 10.1016/j.bmcl.2015.04.043
BindingDB Entry DOI: 10.7270/Q21Z464C
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50088290
PNG
(CHEMBL3427499)
Show SMILES NC1(CC1(F)CP(O)(O)=O)C(O)=O
Show InChI InChI=1S/C5H9FNO5P/c6-4(2-13(10,11)12)1-5(4,7)3(8)9/h1-2,7H2,(H,8,9)(H2,10,11,12)
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Univ. Rouen

Curated by ChEMBL


Assay Description
Agonist activity at rat mGluR4 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay


Bioorg Med Chem Lett 25: 2523-6 (2015)


Article DOI: 10.1016/j.bmcl.2015.04.043
BindingDB Entry DOI: 10.7270/Q21Z464C
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50503365
PNG
(CHEMBL4483053)
Show SMILES Cc1noc2ccc(Nc3n[nH]c4cc(F)cnc34)cc12
Show InChI InChI=1S/C14H10FN5O/c1-7-10-5-9(2-3-12(10)21-20-7)17-14-13-11(18-19-14)4-8(15)6-16-13/h2-6H,1H3,(H2,17,18,19)
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Vanderbilt University

Curated by ChEMBL


Assay Description
Positive allosteric modulation of rat mGlu4 receptor expressed in HEK cells co-expressing GIRK1/2 assessed as increase in glutamate-induced thallium ...


J Med Chem 62: 342-358 (2019)


Article DOI: 10.1021/acs.jmedchem.8b00994
BindingDB Entry DOI: 10.7270/Q29K4FHW
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50166968
PNG
(CHEMBL3798234)
Show SMILES Nc1cccnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1
Show InChI InChI=1S/C20H13ClN4O3/c21-14-10-11(24-18(26)17-15(22)6-3-9-23-17)7-8-16(14)25-19(27)12-4-1-2-5-13(12)20(25)28/h1-10H,22H2,(H,24,26)
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n/an/an/an/a 128n/an/an/an/a



Vanderbilt University Medical Center

Curated by ChEMBL


Assay Description
Positive allosteric modulator activity at rat mGlu4 receptor


Bioorg Med Chem Lett 26: 2915-2919 (2016)


Article DOI: 10.1016/j.bmcl.2016.04.041
BindingDB Entry DOI: 10.7270/Q2348N9V
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50007548
PNG
((S)-2-Amino-4-phosphono-butyric acid | (S)-2-amino...)
Show SMILES N[C@@H](CCP(O)(O)=O)C(O)=O |r|
Show InChI InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m0/s1
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n/an/an/an/a 130n/an/an/an/a



Universite Paris Descartes

Curated by ChEMBL


Assay Description
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular ...


J Med Chem 53: 2797-813 (2010)


Article DOI: 10.1021/jm901523t
BindingDB Entry DOI: 10.7270/Q28W3F7Q
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50007548
PNG
((S)-2-Amino-4-phosphono-butyric acid | (S)-2-amino...)
Show SMILES N[C@@H](CCP(O)(O)=O)C(O)=O |r|
Show InChI InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m0/s1
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n/an/an/an/a 130n/an/an/an/a



INSA de Rouen and Universit£ de Rouen

Curated by ChEMBL


Assay Description
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured e...


Bioorg Med Chem 20: 4716-26 (2012)


Article DOI: 10.1016/j.bmc.2012.06.006
BindingDB Entry DOI: 10.7270/Q2BG2Q2W
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM82006
PNG
(D-AP4 | D-APB | US9212196, L-AP4)
Show SMILES N[C@H](CCP(O)(O)=O)C(O)=O |r|
Show InChI InChI=1S/C4H10NO5P/c5-3(4(6)7)1-2-11(8,9)10/h3H,1-2,5H2,(H,6,7)(H2,8,9,10)/t3-/m1/s1
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n/an/an/an/a 130n/an/an/an/a



UNIVERSITE PARIS DESCARTES; UNIVERSITE D'AUVERGNE

US Patent


Assay Description
Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and ...


US Patent US9212196 (2015)


BindingDB Entry DOI: 10.7270/Q28G8JJR
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM50159148
PNG
(CHEMBL3786667)
Show SMILES [H][C@]1(C[C@]1(C[C@H](N)C(O)=O)C(O)=O)C(O)=O |r|
Show InChI InChI=1S/C8H11NO6/c9-4(6(12)13)2-8(7(14)15)1-3(8)5(10)11/h3-4H,1-2,9H2,(H,10,11)(H,12,13)(H,14,15)/t3-,4-,8+/m0/s1
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n/an/an/an/a 130n/an/an/an/a



University of Copenhagen

Curated by ChEMBL


Assay Description
Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay


J Med Chem 59: 914-24 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01333
BindingDB Entry DOI: 10.7270/Q2000408
More data for this
Ligand-Target Pair
Metabotropic glutamate receptor 4


(Rattus norvegicus (Rat))
BDBM196911
PNG
(US9212196, Derivative 7)
Show SMILES COc1cc(cc(Cl)c1OCC(O)=O)C(O)P(O)(=O)CC[C@@H](N)C(O)=O |r|
Show InChI InChI=1S/C14H19ClNO9P/c1-24-10-5-7(4-8(15)12(10)25-6-11(17)18)14(21)26(22,23)3-2-9(16)13(19)20/h4-5,9,14,21H,2-3,6,16H2,1H3,(H,17,18)(H,19,20)(H,22,23)/t9-,14?/m1/s1
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n/an/an/an/a 130n/an/an/an/a



UNIVERSITE PARIS DESCARTES; UNIVERSITE D'AUVERGNE

US Patent


Assay Description
Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and ...


US Patent US9212196 (2015)


BindingDB Entry DOI: 10.7270/Q28G8JJR
More data for this
Ligand-Target Pair
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