ArrestinDb

Ligand source activities (1 row/activity)

Potency
Affinity

Get vendors

Show entries

Search:

Ligands (move mouse cursor over ligand name to see structure)					Receptor		Activity									Chemical information
Sel. page	Common name No matches found	GPCRdb ID No matches found	Reference ligand No matches found	Vendors	Species No matches found		Assay Type No matches found	Activity Type No matches found	Activity Relation No matches found	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description No matches found	Source No matches found	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles No matches found	DOI No matches found

Ligands (move mouse cursor over ligand name to see structure)					Receptor	Activity									Chemical information
Sel. page	Common name No matches found	GPCRdb ID No matches found	Reference ligand No matches found	Vendors	Species No matches found	Assay Type No matches found	Activity Type No matches found	Activity Relation No matches found	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description No matches found	Source No matches found	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles No matches found	DOI No matches found
	44361401	31349	None	0	Rat	Functional	pEC50	=	8	8.0	-2	5	Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells	ChEMBL	175	3	4	4	-1.9	N[C@H](C(=O)O)[C@H]1[C@@H](O)[C@@H]1C(=O)O	10.1021/jm030967o
	CHEMBL140197	31349	None	0	Rat	Functional	pEC50	=	8	8.0	-2	5	Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cellsMetabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells	ChEMBL	175	3	4	4	-1.9	N[C@H](C(=O)O)[C@H]1[C@@H](O)[C@@H]1C(=O)O	10.1021/jm030967o
	58058372	156288	None	0	Human	Functional	pEC50	=	6	6.0	-3	3	Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay	ChEMBL	302	7	3	5	1.2	N[C@@H](CCP(=O)(O)Cc1cccc([N+](=O)[O-])c1)C(=O)O	10.1021/acs.jmedchem.7b01438
	CHEMBL4064187	156288	None	0	Human	Functional	pEC50	=	6	6.0	-3	3	Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay	ChEMBL	302	7	3	5	1.2	N[C@@H](CCP(=O)(O)Cc1cccc([N+](=O)[O-])c1)C(=O)O	10.1021/acs.jmedchem.7b01438
	1408	265	None	24	Rat	Functional	pEC50	=	5	5.0	-1	7	Activity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cells	ChEMBL	217	3	4	4	-1.0	OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O	10.1016/j.bmcl.2006.06.062
	6604820	265	None	24	Rat	Functional	pEC50	=	5	5.0	-1	7	Activity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cells	ChEMBL	217	3	4	4	-1.0	OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O	10.1016/j.bmcl.2006.06.062
	CHEMBL285043	265	None	24	Rat	Functional	pEC50	=	5	5.0	-1	7	Activity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cells	ChEMBL	217	3	4	4	-1.0	OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O	10.1016/j.bmcl.2006.06.062
	CHEMBL288635	265	None	24	Rat	Functional	pEC50	=	5	5.0	-1	7	Activity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cellsActivity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cells	ChEMBL	217	3	4	4	-1.0	OC(=O)[C@@H]1C[C@](C[C@@H]1C(=O)O)(N)C(=O)O	10.1016/j.bmcl.2006.06.062
	53240406	123463	None	21	Human	Functional	pEC50	=	5	5.0	-457	4	Agonist activity at human recombinant mGlu8 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu8 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay	ChEMBL	284	4	4	6	-0.6	N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21	10.1021/acs.jmedchem.5b01124
	CHEMBL3616847	123463	None	21	Human	Functional	pEC50	=	5	5.0	-457	4	Agonist activity at human recombinant mGlu8 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assayAgonist activity at human recombinant mGlu8 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay	ChEMBL	284	4	4	6	-0.6	N[C@@]1(C(=O)O)C[C@@H](Sc2nnc[nH]2)[C@H]2[C@H](C(=O)O)[C@H]21	10.1021/acs.jmedchem.5b01124
	122197938	161033	None	0	Rat	Functional	pEC50	=	5.0	5.0	-128	3	Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.	ChEMBL	395	10	5	7	0.4	COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(F)c1OCC(=O)O	nan
	CHEMBL4115462	161033	None	0	Rat	Functional	pEC50	=	5.0	5.0	-128	3	Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.	ChEMBL	395	10	5	7	0.4	COc1cc(C(O)P(=O)(O)CC[C@@H](N)C(=O)O)cc(F)c1OCC(=O)O	nan
	1410	2274	None	38	Rat	Functional	pEC50	=	7.0	7.0	1	8	Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1016/j.bmcl.2015.04.043
	1412	2274	None	38	Rat	Functional	pEC50	=	7.0	7.0	1	8	Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1016/j.bmcl.2015.04.043
	179394	2274	None	38	Rat	Functional	pEC50	=	7.0	7.0	1	8	Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1016/j.bmcl.2015.04.043
	57689795	2274	None	38	Rat	Functional	pEC50	=	7.0	7.0	1	8	Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1016/j.bmcl.2015.04.043
	CHEMBL33567	2274	None	38	Rat	Functional	pEC50	=	7.0	7.0	1	8	Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1016/j.bmcl.2015.04.043
	1393	1539	None	42	Human	Functional	pEC50	=	4.9	4.9	-1047	6	Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells	ChEMBL	185	2	3	3	-0.5	OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O	10.1021/jm060917u
	1396	1539	None	42	Human	Functional	pEC50	=	4.9	4.9	-1047	6	Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells	ChEMBL	185	2	3	3	-0.5	OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O	10.1021/jm060917u
	213056	1539	None	42	Human	Functional	pEC50	=	4.9	4.9	-1047	6	Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells	ChEMBL	185	2	3	3	-0.5	OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O	10.1021/jm060917u
	CHEMBL8759	1539	None	42	Human	Functional	pEC50	=	4.9	4.9	-1047	6	Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cellsAgonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells	ChEMBL	185	2	3	3	-0.5	OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O	10.1021/jm060917u
	1393	1539	None	42	Human	Functional	pEC50	=	4.9	4.9	-1047	6	Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8	ChEMBL	185	2	3	3	-0.5	OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O	10.1021/jm980616n
	1396	1539	None	42	Human	Functional	pEC50	=	4.9	4.9	-1047	6	Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8	ChEMBL	185	2	3	3	-0.5	OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O	10.1021/jm980616n
	213056	1539	None	42	Human	Functional	pEC50	=	4.9	4.9	-1047	6	Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8	ChEMBL	185	2	3	3	-0.5	OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O	10.1021/jm980616n
	CHEMBL8759	1539	None	42	Human	Functional	pEC50	=	4.9	4.9	-1047	6	Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8	ChEMBL	185	2	3	3	-0.5	OC(=O)[C@H]1[C@H]2[C@@H]1[C@](CC2)(N)C(=O)O	10.1021/jm980616n
	122197955	160688	None	0	Rat	Functional	pEC50	=	4.9	4.9	-10	3	Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.	ChEMBL	408	10	5	8	0.8	N[C@H](CCP(=O)(O)C(O)c1ccc(SCC(=O)O)c([N+](=O)[O-])c1)C(=O)O	nan
	CHEMBL4112800	160688	None	0	Rat	Functional	pEC50	=	4.9	4.9	-10	3	Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.	ChEMBL	408	10	5	8	0.8	N[C@H](CCP(=O)(O)C(O)c1ccc(SCC(=O)O)c([N+](=O)[O-])c1)C(=O)O	nan
	46918013	158821	None	0	Human	Functional	pEC50	=	5.9	5.9	-2	3	Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay	ChEMBL	318	7	4	6	0.7	N[C@@H](CCP(=O)(O)C(O)c1cccc([N+](=O)[O-])c1)C(=O)O	10.1021/acs.jmedchem.7b01438
	CHEMBL4093492	158821	None	0	Human	Functional	pEC50	=	5.9	5.9	-2	3	Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay	ChEMBL	318	7	4	6	0.7	N[C@@H](CCP(=O)(O)C(O)c1cccc([N+](=O)[O-])c1)C(=O)O	10.1021/acs.jmedchem.7b01438
	46836872	300	None	40	Rat	Functional	pEC50	=	5.9	5.9	-138	4	Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay	ChEMBL	272	3	2	6	2.7	Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C	10.1021/acsmedchemlett.7b00317
	6238	300	None	40	Rat	Functional	pEC50	=	5.9	5.9	-138	4	Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay	ChEMBL	272	3	2	6	2.7	Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C	10.1021/acsmedchemlett.7b00317
	CHEMBL3609729	300	None	40	Rat	Functional	pEC50	=	5.9	5.9	-138	4	Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay	ChEMBL	272	3	2	6	2.7	Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C	10.1021/acsmedchemlett.7b00317
	122197956	160565	None	0	Rat	Functional	pEC50	=	5.9	5.9	-5	3	Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.	ChEMBL	363	9	5	6	0.9	N[C@H](CCP(=O)(O)C(O)c1ccc(SCC(=O)O)cc1)C(=O)O	nan
	CHEMBL4111817	160565	None	0	Rat	Functional	pEC50	=	5.9	5.9	-5	3	Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution.	ChEMBL	363	9	5	6	0.9	N[C@H](CCP(=O)(O)C(O)c1ccc(SCC(=O)O)cc1)C(=O)O	nan
	10239	4043	None	32	Rat	Functional	pEC50	=	6.9	6.9	-1	5	Agonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization by Fluo-4-AM dye based fluorescence assayAgonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization by Fluo-4-AM dye based fluorescence assay	ChEMBL	359	4	1	4	4.8	Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1	10.1039/C8MD00524A
	73058507	4043	None	32	Rat	Functional	pEC50	=	6.9	6.9	-1	5	Agonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization by Fluo-4-AM dye based fluorescence assayAgonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization by Fluo-4-AM dye based fluorescence assay	ChEMBL	359	4	1	4	4.8	Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1	10.1039/C8MD00524A
	CHEMBL4162576	4043	None	32	Rat	Functional	pEC50	=	6.9	6.9	-1	5	Agonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization by Fluo-4-AM dye based fluorescence assayAgonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization by Fluo-4-AM dye based fluorescence assay	ChEMBL	359	4	1	4	4.8	Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1	10.1039/C8MD00524A
	10239	4043	None	32	Rat	Functional	pEC50	=	6.9	6.9	-1	5	Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay	ChEMBL	359	4	1	4	4.8	Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1	10.1021/acsmedchemlett.7b00317
	73058507	4043	None	32	Rat	Functional	pEC50	=	6.9	6.9	-1	5	Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay	ChEMBL	359	4	1	4	4.8	Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1	10.1021/acsmedchemlett.7b00317
	CHEMBL4162576	4043	None	32	Rat	Functional	pEC50	=	6.9	6.9	-1	5	Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assayPositive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based fluorescence assay	ChEMBL	359	4	1	4	4.8	Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1	10.1021/acsmedchemlett.7b00317
	137640190	157046	None	0	Human	Functional	pEC50	=	5.9	5.9	-1	3	Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay	ChEMBL	318	7	4	6	0.7	N[C@@H](CCP(=O)(O)[C@H](O)c1cccc([N+](=O)[O-])c1)C(=O)O	10.1021/acs.jmedchem.7b01438
	CHEMBL4072781	157046	None	0	Human	Functional	pEC50	=	5.9	5.9	-1	3	Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assayAgonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay	ChEMBL	318	7	4	6	0.7	N[C@@H](CCP(=O)(O)[C@H](O)c1cccc([N+](=O)[O-])c1)C(=O)O	10.1021/acs.jmedchem.7b01438
	57519364	119184	None	0	Rat	Functional	pEC50	=	5.9	5.9	-2	3	Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay	ChEMBL	213	3	4	3	-0.9	NC1(C(=O)O)CC1(F)CP(=O)(O)O	10.1016/j.bmcl.2015.04.043
	CHEMBL3427499	119184	None	0	Rat	Functional	pEC50	=	5.9	5.9	-2	3	Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay	ChEMBL	213	3	4	3	-0.9	NC1(C(=O)O)CC1(F)CP(=O)(O)O	10.1016/j.bmcl.2015.04.043
	1410	2274	None	38	Rat	Functional	pEC50	=	6.9	6.9	1	8	Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate production	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1021/jm070400y
	1412	2274	None	38	Rat	Functional	pEC50	=	6.9	6.9	1	8	Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate production	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1021/jm070400y
	179394	2274	None	38	Rat	Functional	pEC50	=	6.9	6.9	1	8	Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate production	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1021/jm070400y
	57689795	2274	None	38	Rat	Functional	pEC50	=	6.9	6.9	1	8	Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate production	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1021/jm070400y
	CHEMBL33567	2274	None	38	Rat	Functional	pEC50	=	6.9	6.9	1	8	Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate productionAgonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate production	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1021/jm070400y
	57765613	158582	None	0	Human	Functional	pEC50	=	5.9	5.9	-1	3	Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting methodAgonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method	ChEMBL	336	7	4	6	0.8	N[C@@H](CCP(=O)(O)C(O)c1ccc(F)c([N+](=O)[O-])c1)C(=O)O	10.1021/acs.jmedchem.7b01438

Showing 1 to 50 of 632 entries

Previous1 2 3 4 5…13Next

Get vendors

Show entries

Search:

Ligands (move mouse cursor over ligand name to see structure)					Receptor		Activity									Chemical information
Sel. page	Common name No matches found	GPCRdb ID No matches found	Reference ligand No matches found	Vendors	Species No matches found		Assay Type No matches found	Activity Type No matches found	Activity Relation No matches found	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description No matches found	Source No matches found	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles No matches found	DOI No matches found

Ligands (move mouse cursor over ligand name to see structure)					Receptor	Activity									Chemical information
Sel. page	Common name No matches found	GPCRdb ID No matches found	Reference ligand No matches found	Vendors	Species No matches found	Assay Type No matches found	Activity Type No matches found	Activity Relation No matches found	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description No matches found	Source No matches found	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles No matches found	DOI No matches found
	139119037	90096	None	0	Human	Binding	pEC50	=	4.9	4.9	-	0	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	203	2	3	3	-0.5	N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21	10.1021/jm4000165
	15479143	90096	None	0	Human	Binding	pEC50	=	4.9	4.9	-	0	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	203	2	3	3	-0.5	N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21	10.1021/jm4000165
	CHEMBL2381652	90096	None	0	Human	Binding	pEC50	=	4.9	4.9	-	0	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	203	2	3	3	-0.5	N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21	10.1021/jm4000165
	46836872	300	None	40	Human	Binding	pEC50	=	5.9	5.9	-	1	Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (unknown origin)	ChEMBL	272	3	2	6	2.7	Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C	10.1016/j.bmcl.2022.129106
	6238	300	None	40	Human	Binding	pEC50	=	5.9	5.9	-	1	Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (unknown origin)	ChEMBL	272	3	2	6	2.7	Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C	10.1016/j.bmcl.2022.129106
	CHEMBL3609729	300	None	40	Human	Binding	pEC50	=	5.9	5.9	-	1	Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (unknown origin)	ChEMBL	272	3	2	6	2.7	Cc1ccnc(n1)Nc1sc(c(n1)c1c[nH]nc1)C	10.1016/j.bmcl.2022.129106
	71681825	90089	None	0	Human	Binding	pEC50	=	4.9	4.9	-	0	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	226	3	3	4	-0.2	[N-]=[N+]=N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12	10.1021/jm4000165
	CHEMBL2381645	90089	None	0	Human	Binding	pEC50	=	4.9	4.9	-	0	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	226	3	3	4	-0.2	[N-]=[N+]=N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12	10.1021/jm4000165
	71681823	90088	None	0	Human	Binding	pEC50	=	4.9	4.9	-	0	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	226	3	3	4	-0.2	[N-]=[N+]=N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21	10.1021/jm4000165
	CHEMBL2381644	90088	None	0	Human	Binding	pEC50	=	4.9	4.9	-	0	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	226	3	3	4	-0.2	[N-]=[N+]=N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21	10.1021/jm4000165
	10239	4043	None	32	Human	Binding	pEC50	=	6.9	6.9	-	0	Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (unknown origin)	ChEMBL	359	4	1	4	4.8	Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1	10.1016/j.bmcl.2022.129106
	73058507	4043	None	32	Human	Binding	pEC50	=	6.9	6.9	-	0	Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (unknown origin)	ChEMBL	359	4	1	4	4.8	Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1	10.1016/j.bmcl.2022.129106
	CHEMBL4162576	4043	None	32	Human	Binding	pEC50	=	6.9	6.9	-	0	Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (unknown origin)	ChEMBL	359	4	1	4	4.8	Clc1ccc(nc1)Oc1ccc(cc1Cl)NC(=O)c1ccccn1	10.1016/j.bmcl.2022.129106
	70051926	90085	None	1	Human	Binding	pEC50	=	5.8	5.8	-	0	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	197	2	3	3	-0.3	C=C1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12	10.1021/jm4000165
	CHEMBL2381641	90085	None	1	Human	Binding	pEC50	=	5.8	5.8	-	0	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	197	2	3	3	-0.3	C=C1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12	10.1021/jm4000165
	1310	2315	None	61	Mouse	Binding	pEC50	=	7.7	7.7	-	18	Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	1369	2315	None	61	Mouse	Binding	pEC50	=	7.7	7.7	-	18	Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	33032	2315	None	61	Mouse	Binding	pEC50	=	7.7	7.7	-	18	Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	44272391	2315	None	61	Mouse	Binding	pEC50	=	7.7	7.7	-	18	Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	88747398	2315	None	61	Mouse	Binding	pEC50	=	7.7	7.7	-	18	Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	CHEMBL575060	2315	None	61	Mouse	Binding	pEC50	=	7.7	7.7	-	18	Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	DB00142	2315	None	61	Mouse	Binding	pEC50	=	7.7	7.7	-	18	Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	131954513	162172	None	38	Human	Binding	pEC50	=	5.6	5.6	-	1	Agonist activity at mGlu8 (unknown origin)Agonist activity at mGlu8 (unknown origin)	ChEMBL	357	2	0	4	4.3	COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1F	10.1039/C8MD00524A
	CHEMBL4160748	162172	None	38	Human	Binding	pEC50	=	5.6	5.6	-	1	Agonist activity at mGlu8 (unknown origin)Agonist activity at mGlu8 (unknown origin)	ChEMBL	357	2	0	4	4.3	COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1F	10.1039/C8MD00524A
	131954513	162172	None	38	Human	Binding	pEC50	=	5.6	5.6	-	1	Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (unknown origin)	ChEMBL	357	2	0	4	4.3	COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1F	10.1016/j.bmcl.2022.129106
	CHEMBL4160748	162172	None	38	Human	Binding	pEC50	=	5.6	5.6	-	1	Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (unknown origin)	ChEMBL	357	2	0	4	4.3	COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1F	10.1016/j.bmcl.2022.129106
	145955288	162672	None	0	Human	Binding	pEC50	=	5.5	5.5	-	0	Agonist activity at mGlu8 (unknown origin)Agonist activity at mGlu8 (unknown origin)	ChEMBL	357	2	0	4	4.3	COc1cc(F)c(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1	10.1039/C8MD00524A
	CHEMBL4168668	162672	None	0	Human	Binding	pEC50	=	5.5	5.5	-	0	Agonist activity at mGlu8 (unknown origin)Agonist activity at mGlu8 (unknown origin)	ChEMBL	357	2	0	4	4.3	COc1cc(F)c(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1	10.1039/C8MD00524A
	1407	2079	None	36	Human	Binding	pEC50	=	7.5	7.5	-	1	Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cells	ChEMBL	239	4	4	4	0.2	N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O	10.1021/acs.jmedchem.8b01120
	16062593	2079	None	36	Human	Binding	pEC50	=	7.5	7.5	-	1	Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cells	ChEMBL	239	4	4	4	0.2	N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O	10.1021/acs.jmedchem.8b01120
	CHEMBL143210	2079	None	36	Human	Binding	pEC50	=	7.5	7.5	-	1	Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cells	ChEMBL	239	4	4	4	0.2	N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O	10.1021/acs.jmedchem.8b01120
	1410	2274	None	38	Mouse	Binding	pEC50	=	6.4	6.4	-	6	Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1021/jm00009a001
	1412	2274	None	38	Mouse	Binding	pEC50	=	6.4	6.4	-	6	Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1021/jm00009a001
	179394	2274	None	38	Mouse	Binding	pEC50	=	6.4	6.4	-	6	Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1021/jm00009a001
	57689795	2274	None	38	Mouse	Binding	pEC50	=	6.4	6.4	-	6	Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1021/jm00009a001
	CHEMBL33567	2274	None	38	Mouse	Binding	pEC50	=	6.4	6.4	-	6	Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouseConcentration for half maximal activation of metabotropic glutamate mGluR8 in mouse	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1021/jm00009a001
	60096211	90093	None	0	Human	Binding	pEC50	=	5.4	5.4	-	2	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	242	3	4	4	-1.4	CC(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12	10.1021/jm4000165
	CHEMBL2381649	90093	None	0	Human	Binding	pEC50	=	5.4	5.4	-	2	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	242	3	4	4	-1.4	CC(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12	10.1021/jm4000165
	1410	2274	None	38	Human	Binding	pEC50	=	7.2	7.2	2	6	Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cells	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1021/acs.jmedchem.8b01120
	1412	2274	None	38	Human	Binding	pEC50	=	7.2	7.2	2	6	Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cells	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1021/acs.jmedchem.8b01120
	179394	2274	None	38	Human	Binding	pEC50	=	7.2	7.2	2	6	Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cells	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1021/acs.jmedchem.8b01120
	57689795	2274	None	38	Human	Binding	pEC50	=	7.2	7.2	2	6	Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cells	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1021/acs.jmedchem.8b01120
	CHEMBL33567	2274	None	38	Human	Binding	pEC50	=	7.2	7.2	2	6	Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cellsActivation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cells	ChEMBL	183	4	4	3	-1.0	OC(=O)[C@H](CCP(=O)(O)O)N	10.1021/acs.jmedchem.8b01120
	9794208	90084	None	2	Human	Binding	pEC50	=	5.2	5.2	-	0	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	199	2	3	4	-1.3	N[C@@]1(C(=O)O)CC(=O)[C@@H]2[C@H]1[C@H]2C(=O)O	10.1021/jm4000165
	CHEMBL2381640	90084	None	2	Human	Binding	pEC50	=	5.2	5.2	-	0	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assayAgonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	199	2	3	4	-1.3	N[C@@]1(C(=O)O)CC(=O)[C@@H]2[C@H]1[C@H]2C(=O)O	10.1021/jm4000165
	155518354	170368	None	0	Human	Binding	pEC50	=	6.1	6.1	-	0	Agonist activity at mGlu8 (unknown origin)Agonist activity at mGlu8 (unknown origin)	ChEMBL	371	3	0	4	4.6	CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1cc(F)c(OC)cc1F	10.1039/C8MD00524A
	CHEMBL4446107	170368	None	0	Human	Binding	pEC50	=	6.1	6.1	-	0	Agonist activity at mGlu8 (unknown origin)Agonist activity at mGlu8 (unknown origin)	ChEMBL	371	3	0	4	4.6	CCc1nn2c(C(F)(F)F)cc(C)nc2c1-c1cc(F)c(OC)cc1F	10.1039/C8MD00524A
	10238	4027	None	28	Human	Binding	pEC50	=	6.1	6.1	-	0	Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (unknown origin)	ChEMBL	436	7	1	6	4.8	COC(=O)c1ccc(cc1)n1c(C)cc(c1C)C(=O)CSc1ccc(cc1)NC(=O)C	10.1016/j.bmcl.2022.129106
	4043841	4027	None	28	Human	Binding	pEC50	=	6.1	6.1	-	0	Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (unknown origin)	ChEMBL	436	7	1	6	4.8	COC(=O)c1ccc(cc1)n1c(C)cc(c1C)C(=O)CSc1ccc(cc1)NC(=O)C	10.1016/j.bmcl.2022.129106
	CHEMBL1585091	4027	None	28	Human	Binding	pEC50	=	6.1	6.1	-	0	Positive allosteric modulation of mGluR8 (unknown origin)Positive allosteric modulation of mGluR8 (unknown origin)	ChEMBL	436	7	1	6	4.8	COC(=O)c1ccc(cc1)n1c(C)cc(c1C)C(=O)CSc1ccc(cc1)NC(=O)C	10.1016/j.bmcl.2022.129106

Showing 1 to 50 of 177 entries

Previous1 2 3 4Next

Join us

Cite us

Main reference

Ligand source activities (1 row/activity)