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Ligand source activities (1 row/activity)

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Ligands					Receptor			Assay information							Chemical information
Sel. page	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity (Potency)	# tested GPCRs (Potency)	Species	p-value (-log)	Type	Activity Relation	Activity Value	Assay Type	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	1392	73	42	None	-323	4	Rat	4.0	pEC50	=	4	Functional	Tested for the agonistic activity against Metabotropic glutamate receptor 1Tested for the agonistic activity against Metabotropic glutamate receptor 1	ChEMBL	174	2	4	4	-1.8	OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O	10.1016/S0960-894X(97)00068-1
	5310984	73	42	None	-323	4	Rat	4.0	pEC50	=	4	Functional	Tested for the agonistic activity against Metabotropic glutamate receptor 1Tested for the agonistic activity against Metabotropic glutamate receptor 1	ChEMBL	174	2	4	4	-1.8	OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O	10.1016/S0960-894X(97)00068-1
	CHEMBL40086	73	42	None	-323	4	Rat	4.0	pEC50	=	4	Functional	Tested for the agonistic activity against Metabotropic glutamate receptor 1Tested for the agonistic activity against Metabotropic glutamate receptor 1	ChEMBL	174	2	4	4	-1.8	OC(=O)[C@@H]1NC[C@@](C1)(N)C(=O)O	10.1016/S0960-894X(97)00068-1
	44573737	192227	0	None	-	1	Rat	7.0	pEC50	=	7.0	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	378	2	1	4	4.7	O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2c(F)cccc21	10.1016/j.bmcl.2009.01.108
	CHEMBL522161	192227	0	None	-	1	Rat	7.0	pEC50	=	7.0	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	378	2	1	4	4.7	O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2c(F)cccc21	10.1016/j.bmcl.2009.01.108
	1310	2286	108	None	-741	17	Human	6.0	pEC50	=	6.0	Functional	Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/s0960-894x(99)00641-1
	1369	2286	108	None	-741	17	Human	6.0	pEC50	=	6.0	Functional	Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/s0960-894x(99)00641-1
	33032	2286	108	None	-741	17	Human	6.0	pEC50	=	6.0	Functional	Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/s0960-894x(99)00641-1
	44272391	2286	108	None	-741	17	Human	6.0	pEC50	=	6.0	Functional	Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/s0960-894x(99)00641-1
	88747398	2286	108	None	-741	17	Human	6.0	pEC50	=	6.0	Functional	Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/s0960-894x(99)00641-1
	CHEMBL575060	2286	108	None	-741	17	Human	6.0	pEC50	=	6.0	Functional	Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/s0960-894x(99)00641-1
	DB00142	2286	108	None	-741	17	Human	6.0	pEC50	=	6.0	Functional	Effect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamateEffect of compound on Metabotropic glutamate receptor 1 expressed in HEK 293 cells was determined by measuring IP production relative to glutamate	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/s0960-894x(99)00641-1
	122196105	123721	0	None	22	2	Human	7.0	pEC50	=	7.0	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	448	3	1	4	5.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(C(F)(F)F)c1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634428	123721	0	None	22	2	Human	7.0	pEC50	=	7.0	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	448	3	1	4	5.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(C(F)(F)F)c1	10.1016/j.bmcl.2015.10.013
	127032507	138495	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	380	3	1	3	5.0	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785852	138495	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	380	3	1	3	5.0	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127032507	138495	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	380	3	1	3	5.0	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785852	138495	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	380	3	1	3	5.0	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127026165	137170	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	378	3	1	4	4.1	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O	10.1016/j.bmcl.2015.12.104
	CHEMBL3758746	137170	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	378	3	1	4	4.1	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O	10.1016/j.bmcl.2015.12.104
	192790	71545	32	None	4	2	Rat	5.0	pEC50	=	5.0	Functional	Agonist activity in rat at mGlu1a receptor expressed in HEK293 cellsAgonist activity in rat at mGlu1a receptor expressed in HEK293 cells	ChEMBL	163	4	4	4	-1.8	N[C@@H](C[C@H](O)C(=O)O)C(=O)O	10.1016/s0960-894x(01)00158-5
	44286641	71545	32	None	4	2	Rat	5.0	pEC50	=	5.0	Functional	Agonist activity in rat at mGlu1a receptor expressed in HEK293 cellsAgonist activity in rat at mGlu1a receptor expressed in HEK293 cells	ChEMBL	163	4	4	4	-1.8	N[C@@H](C[C@H](O)C(=O)O)C(=O)O	10.1016/s0960-894x(01)00158-5
	CHEMBL197110	71545	32	None	4	2	Rat	5.0	pEC50	=	5.0	Functional	Agonist activity in rat at mGlu1a receptor expressed in HEK293 cellsAgonist activity in rat at mGlu1a receptor expressed in HEK293 cells	ChEMBL	163	4	4	4	-1.8	N[C@@H](C[C@H](O)C(=O)O)C(=O)O	10.1016/s0960-894x(01)00158-5
	122193176	123413	0	None	-1	3	Rat	7.0	pEC50	=	7.0	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay	ChEMBL	414	3	1	4	4.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628112	123413	0	None	-1	3	Rat	7.0	pEC50	=	7.0	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay	ChEMBL	414	3	1	4	4.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	122193179	123416	0	None	-1	2	Rat	7.0	pEC50	=	7.0	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay	ChEMBL	381	3	1	5	3.7	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628115	123416	0	None	-1	2	Rat	7.0	pEC50	=	7.0	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay	ChEMBL	381	3	1	5	3.7	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	122193176	123413	0	None	-1	3	Rat	7.0	pEC50	=	7.0	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay	ChEMBL	414	3	1	4	4.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628112	123413	0	None	-1	3	Rat	7.0	pEC50	=	7.0	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay	ChEMBL	414	3	1	4	4.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	122193179	123416	0	None	-1	2	Rat	7.0	pEC50	=	7.0	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay	ChEMBL	381	3	1	5	3.7	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628115	123416	0	None	-1	2	Rat	7.0	pEC50	=	7.0	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay	ChEMBL	381	3	1	5	3.7	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	127030066	138510	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	434	3	1	3	5.7	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(cccc3C(F)(F)F)C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785990	138510	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	434	3	1	3	5.7	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(cccc3C(F)(F)F)C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127026165	137170	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	378	3	1	4	4.1	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O	10.1016/j.bmcl.2015.12.104
	CHEMBL3758746	137170	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	378	3	1	4	4.1	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O	10.1016/j.bmcl.2015.12.104
	127030066	138510	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	434	3	1	3	5.7	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(cccc3C(F)(F)F)C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785990	138510	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	434	3	1	3	5.7	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(cccc3C(F)(F)F)C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	122196123	123738	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	364	3	1	4	3.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1F	10.1016/j.bmcl.2016.03.031
	CHEMBL3634445	123738	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	364	3	1	4	3.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1F	10.1016/j.bmcl.2016.03.031
	122196103	123719	0	None	53	2	Human	6.9	pEC50	=	6.9	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	414	3	1	4	4.7	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(C(F)(F)F)c1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634426	123719	0	None	53	2	Human	6.9	pEC50	=	6.9	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	414	3	1	4	4.7	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(C(F)(F)F)c1	10.1016/j.bmcl.2015.10.013
	127029303	137267	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	380	3	2	4	3.4	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759563	137267	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	380	3	2	4	3.4	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	44573779	187054	0	None	-	1	Rat	6.9	pEC50	=	6.9	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	328	2	1	4	3.8	O=C(Nc1ncco1)C1c2cc(F)ccc2Oc2ccc(F)cc21	10.1016/j.bmcl.2009.01.108
	CHEMBL494961	187054	0	None	-	1	Rat	6.9	pEC50	=	6.9	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	328	2	1	4	3.8	O=C(Nc1ncco1)C1c2cc(F)ccc2Oc2ccc(F)cc21	10.1016/j.bmcl.2009.01.108
	127029303	137267	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	380	3	2	4	3.4	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759563	137267	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	380	3	2	4	3.4	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127033422	138560	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	384	3	1	3	4.8	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1F	10.1016/j.bmcl.2016.03.031
	CHEMBL3786552	138560	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	384	3	1	3	4.8	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1F	10.1016/j.bmcl.2016.03.031
	127033422	138560	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	384	3	1	3	4.8	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1F	10.1016/j.bmcl.2016.03.031
	CHEMBL3786552	138560	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	384	3	1	3	4.8	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1F	10.1016/j.bmcl.2016.03.031
	127033432	138425	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	431	3	1	3	5.5	O=C(Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1)c1ncccc1Cl	10.1016/j.bmcl.2016.03.031
	CHEMBL3785119	138425	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	431	3	1	3	5.5	O=C(Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1)c1ncccc1Cl	10.1016/j.bmcl.2016.03.031
	127033432	138425	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	431	3	1	3	5.5	O=C(Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1)c1ncccc1Cl	10.1016/j.bmcl.2016.03.031
	CHEMBL3785119	138425	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	431	3	1	3	5.5	O=C(Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1)c1ncccc1Cl	10.1016/j.bmcl.2016.03.031
	127025550	137304	0	None	-1	2	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	415	3	1	5	4.3	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759867	137304	0	None	-1	2	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	415	3	1	5	4.3	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127034537	138440	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	380	3	1	3	5.1	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)CCc3ccccc32)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785267	138440	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	380	3	1	3	5.1	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)CCc3ccccc32)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	122196123	123738	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	364	3	1	4	3.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1F	10.1016/j.bmcl.2015.10.013
	CHEMBL3634445	123738	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	364	3	1	4	3.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1F	10.1016/j.bmcl.2015.10.013
	10362260	187053	0	None	-	1	Rat	6.9	pEC50	=	6.9	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	378	2	1	4	4.7	O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2c(F)cccc21	10.1016/j.bmcl.2009.01.108
	CHEMBL494960	187053	0	None	-	1	Rat	6.9	pEC50	=	6.9	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	378	2	1	4	4.7	O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2c(F)cccc21	10.1016/j.bmcl.2009.01.108
	127025550	137304	0	None	-1	2	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	415	3	1	5	4.3	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759867	137304	0	None	-1	2	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	415	3	1	5	4.3	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127034537	138440	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	380	3	1	3	5.1	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)CCc3ccccc32)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785267	138440	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	380	3	1	3	5.1	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)CCc3ccccc32)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127033962	138513	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	366	3	1	3	5.1	Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc3C2)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3786032	138513	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	366	3	1	3	5.1	Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc3C2)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	162643634	181173	0	None	-1	3	Human	6.9	pEC50	=	6.9	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	392	3	1	4	4.4	Cc1ccc2c(c1)C(=O)N(c1cc(C)c(NC(=O)c3occc3C)cc1F)C2=O	10.1016/j.bmcl.2020.127724
	CHEMBL4777502	181173	0	None	-1	3	Human	6.9	pEC50	=	6.9	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	392	3	1	4	4.4	Cc1ccc2c(c1)C(=O)N(c1cc(C)c(NC(=O)c3occc3C)cc1F)C2=O	10.1016/j.bmcl.2020.127724
	127033424	138454	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	411	3	1	3	5.1	Cc1cccnc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785387	138454	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	411	3	1	3	5.1	Cc1cccnc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127026139	137172	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	431	3	1	5	4.8	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3758756	137172	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	431	3	1	5	4.8	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127026139	137172	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	431	3	1	5	4.8	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3758756	137172	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	431	3	1	5	4.8	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	1310	2286	108	None	-794	17	Rat	4.9	pEC50	=	4.9	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	1369	2286	108	None	-794	17	Rat	4.9	pEC50	=	4.9	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	33032	2286	108	None	-794	17	Rat	4.9	pEC50	=	4.9	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	44272391	2286	108	None	-794	17	Rat	4.9	pEC50	=	4.9	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	88747398	2286	108	None	-794	17	Rat	4.9	pEC50	=	4.9	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	CHEMBL575060	2286	108	None	-794	17	Rat	4.9	pEC50	=	4.9	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	DB00142	2286	108	None	-794	17	Rat	4.9	pEC50	=	4.9	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	44573779	187054	0	None	-	1	Rat	6.9	pEC50	=	6.9	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	328	2	1	4	3.8	O=C(Nc1ncco1)C1c2cc(F)ccc2Oc2ccc(F)cc21	10.1016/j.bmcl.2009.01.108
	CHEMBL494961	187054	0	None	-	1	Rat	6.9	pEC50	=	6.9	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	328	2	1	4	3.8	O=C(Nc1ncco1)C1c2cc(F)ccc2Oc2ccc(F)cc21	10.1016/j.bmcl.2009.01.108
	4125492	139562	10	None	2	2	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	308	2	1	4	4.0	O=C(Nc1nccs1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2016.03.044
	CHEMBL3800589	139562	10	None	2	2	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	308	2	1	4	4.0	O=C(Nc1nccs1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2016.03.044
	127025831	137244	0	None	4	2	Human	6.9	pEC50	=	6.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	399	3	1	5	3.8	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759381	137244	0	None	4	2	Human	6.9	pEC50	=	6.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	399	3	1	5	3.8	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127025831	137244	0	None	4	2	Human	6.9	pEC50	=	6.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	399	3	1	5	3.8	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759381	137244	0	None	4	2	Human	6.9	pEC50	=	6.9	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	399	3	1	5	3.8	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	4125492	139562	10	None	2	2	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	308	2	1	4	4.0	O=C(Nc1nccs1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2016.03.044
	CHEMBL3800589	139562	10	None	2	2	Human	5.9	pEC50	=	5.9	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	308	2	1	4	4.0	O=C(Nc1nccs1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2016.03.044
	122196110	123725	0	None	13	2	Human	6.8	pEC50	=	6.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	394	4	1	5	3.8	COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O	10.1016/j.bmcl.2015.10.013
	CHEMBL3634432	123725	0	None	13	2	Human	6.8	pEC50	=	6.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	394	4	1	5	3.8	COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O	10.1016/j.bmcl.2015.10.013
	127033424	138454	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	411	3	1	3	5.1	Cc1cccnc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785387	138454	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	411	3	1	3	5.1	Cc1cccnc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127029002	137237	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	381	3	1	5	3.7	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759321	137237	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	381	3	1	5	3.7	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127029002	137237	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	381	3	1	5	3.7	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759321	137237	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	381	3	1	5	3.7	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	122196125	123740	0	None	40	2	Human	7.8	pEC50	=	7.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	360	3	1	4	3.9	Cc1cc(N2C(=O)c3ccccc3C2=O)ccc1NC(=O)c1occc1C	10.1016/j.bmcl.2015.10.013
	CHEMBL3634447	123740	0	None	40	2	Human	7.8	pEC50	=	7.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	360	3	1	4	3.9	Cc1cc(N2C(=O)c3ccccc3C2=O)ccc1NC(=O)c1occc1C	10.1016/j.bmcl.2015.10.013
	104766	34	36	None	-8	14	Rat	4.8	pEC50	=	4.8	Functional	Activity tested at cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cellsActivity tested at cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cells	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm0308085
	1365	34	36	None	-8	14	Rat	4.8	pEC50	=	4.8	Functional	Activity tested at cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cellsActivity tested at cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cells	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm0308085
	CHEMBL34453	34	36	None	-8	14	Rat	4.8	pEC50	=	4.8	Functional	Activity tested at cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cellsActivity tested at cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cells	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm0308085
	127029000	137240	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	396	3	1	4	4.8	Cc1sccc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759354	137240	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	396	3	1	4	4.8	Cc1sccc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127029000	137240	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	396	3	1	4	4.8	Cc1sccc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759354	137240	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	396	3	1	4	4.8	Cc1sccc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127034513	138553	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	332	3	1	3	4.0	Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2=O)cc1	10.1016/j.bmcl.2016.03.031
	CHEMBL3786494	138553	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	332	3	1	3	4.0	Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2=O)cc1	10.1016/j.bmcl.2016.03.031
	122196106	123722	0	None	18	2	Human	6.8	pEC50	=	6.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	432	3	1	4	4.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(C(F)(F)F)c1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634429	123722	0	None	18	2	Human	6.8	pEC50	=	6.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	432	3	1	4	4.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(C(F)(F)F)c1	10.1016/j.bmcl.2015.10.013
	127034513	138553	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	332	3	1	3	4.0	Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2=O)cc1	10.1016/j.bmcl.2016.03.031
	CHEMBL3786494	138553	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	332	3	1	3	4.0	Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2=O)cc1	10.1016/j.bmcl.2016.03.031
	1310	2286	108	None	-794	17	Rat	5.8	pEC50	=	5.8	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	1369	2286	108	None	-794	17	Rat	5.8	pEC50	=	5.8	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	33032	2286	108	None	-794	17	Rat	5.8	pEC50	=	5.8	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	44272391	2286	108	None	-794	17	Rat	5.8	pEC50	=	5.8	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	88747398	2286	108	None	-794	17	Rat	5.8	pEC50	=	5.8	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	CHEMBL575060	2286	108	None	-794	17	Rat	5.8	pEC50	=	5.8	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	DB00142	2286	108	None	-794	17	Rat	5.8	pEC50	=	5.8	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	122196092	123708	0	None	21	2	Human	7.8	pEC50	=	7.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	360	3	1	4	3.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)cc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634415	123708	0	None	21	2	Human	7.8	pEC50	=	7.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	360	3	1	4	3.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)cc1	10.1016/j.bmcl.2015.10.013
	122196120	123735	0	None	26	2	Human	7.8	pEC50	=	7.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	410	3	1	4	5.1	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c2ccccc12	10.1016/j.bmcl.2015.10.013
	CHEMBL3634442	123735	0	None	26	2	Human	7.8	pEC50	=	7.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	410	3	1	4	5.1	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c2ccccc12	10.1016/j.bmcl.2015.10.013
	1310	2286	108	None	-794	17	Rat	5.8	pEC50	=	5.8	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	1369	2286	108	None	-794	17	Rat	5.8	pEC50	=	5.8	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	33032	2286	108	None	-794	17	Rat	5.8	pEC50	=	5.8	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	44272391	2286	108	None	-794	17	Rat	5.8	pEC50	=	5.8	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	88747398	2286	108	None	-794	17	Rat	5.8	pEC50	=	5.8	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	CHEMBL575060	2286	108	None	-794	17	Rat	5.8	pEC50	=	5.8	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	DB00142	2286	108	None	-794	17	Rat	5.8	pEC50	=	5.8	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells by intracellular Ca2+ mobilization assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/acs.jmedchem.5b01333
	44573780	187057	0	None	-	1	Rat	6.8	pEC50	=	6.8	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	396	2	1	4	4.8	O=C(Nc1nc(C(F)(F)F)co1)C1c2cccc(F)c2Oc2c(F)cccc21	10.1016/j.bmcl.2009.01.108
	CHEMBL494967	187057	0	None	-	1	Rat	6.8	pEC50	=	6.8	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	396	2	1	4	4.8	O=C(Nc1nc(C(F)(F)F)co1)C1c2cccc(F)c2Oc2c(F)cccc21	10.1016/j.bmcl.2009.01.108
	44573738	187021	0	None	-	1	Rat	6.8	pEC50	=	6.8	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	396	2	1	4	4.8	O=C(Nc1ncc(C(F)(F)F)o1)C1c2cccc(F)c2Oc2c(F)cccc21	10.1016/j.bmcl.2009.01.108
	CHEMBL494766	187021	0	None	-	1	Rat	6.8	pEC50	=	6.8	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	396	2	1	4	4.8	O=C(Nc1ncc(C(F)(F)F)o1)C1c2cccc(F)c2Oc2c(F)cccc21	10.1016/j.bmcl.2009.01.108
	162650632	179506	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	392	3	1	4	4.0	Cc1cc(N2C(=O)Cc3ccccc3C2=O)c(F)cc1NC(=O)c1occc1C	10.1016/j.bmcl.2020.127724
	CHEMBL4748116	179506	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	392	3	1	4	4.0	Cc1cc(N2C(=O)Cc3ccccc3C2=O)c(F)cc1NC(=O)c1occc1C	10.1016/j.bmcl.2020.127724
	775428	139401	14	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	302	2	1	3	4.0	O=C(Nc1ccccn1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2016.03.044
	CHEMBL3799600	139401	14	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	302	2	1	3	4.0	O=C(Nc1ccccn1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2016.03.044
	127026137	137285	0	None	1	2	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	382	3	1	6	3.1	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759705	137285	0	None	1	2	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	382	3	1	6	3.1	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127026059	137306	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	399	3	1	5	3.8	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759878	137306	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	399	3	1	5	3.8	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	775428	139401	14	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	302	2	1	3	4.0	O=C(Nc1ccccn1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2016.03.044
	CHEMBL3799600	139401	14	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	302	2	1	3	4.0	O=C(Nc1ccccn1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2016.03.044
	127026137	137285	0	None	1	2	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	382	3	1	6	3.1	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759705	137285	0	None	1	2	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	382	3	1	6	3.1	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127032499	138515	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	352	3	1	3	5.0	Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3786060	138515	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	352	3	1	3	5.0	Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127033963	138444	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	400	3	1	3	5.3	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785321	138444	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	400	3	1	3	5.3	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127032499	138515	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	352	3	1	3	5.0	Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3786060	138515	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	352	3	1	3	5.0	Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	122196109	123557	0	None	36	2	Human	7.8	pEC50	=	7.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	410	4	1	5	4.3	COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O	10.1016/j.bmcl.2015.10.013
	CHEMBL3632642	123557	0	None	36	2	Human	7.8	pEC50	=	7.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	410	4	1	5	4.3	COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O	10.1016/j.bmcl.2015.10.013
	127047993	139121	1	None	-3	2	Rat	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	333	2	1	5	3.9	N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	CHEMBL3797793	139121	1	None	-3	2	Rat	5.8	pEC50	=	5.8	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	333	2	1	5	3.9	N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	127025563	137216	0	None	2	2	Human	6.7	pEC50	=	6.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	415	3	1	5	4.3	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759171	137216	0	None	2	2	Human	6.7	pEC50	=	6.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	415	3	1	5	4.3	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127047993	139121	1	None	-3	2	Rat	5.7	pEC50	=	5.7	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	333	2	1	5	3.9	N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	CHEMBL3797793	139121	1	None	-3	2	Rat	5.7	pEC50	=	5.7	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	333	2	1	5	3.9	N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	127025563	137216	0	None	2	2	Human	6.7	pEC50	=	6.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	415	3	1	5	4.3	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759171	137216	0	None	2	2	Human	6.7	pEC50	=	6.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	415	3	1	5	4.3	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127027100	137212	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	396	3	1	4	4.8	Cc1ccsc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759137	137212	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	396	3	1	4	4.8	Cc1ccsc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	44573737	192227	0	None	-	1	Rat	7.7	pEC50	=	7.7	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	378	2	1	4	4.7	O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2c(F)cccc21	10.1016/j.bmcl.2009.01.108
	CHEMBL522161	192227	0	None	-	1	Rat	7.7	pEC50	=	7.7	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	378	2	1	4	4.7	O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2c(F)cccc21	10.1016/j.bmcl.2009.01.108
	127027101	137135	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	382	3	1	4	3.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)cc1F	10.1016/j.bmcl.2015.12.104
	CHEMBL3758435	137135	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	382	3	1	4	3.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)cc1F	10.1016/j.bmcl.2015.12.104
	127026386	137269	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	1	6	3.6	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759573	137269	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	1	6	3.6	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	1310	2286	108	None	-741	17	Human	4.7	pEC50	=	4.7	Functional	Agonistic activity at mGlu1-alpha receptor expressed in CHO cellsAgonistic activity at mGlu1-alpha receptor expressed in CHO cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm9602569
	1369	2286	108	None	-741	17	Human	4.7	pEC50	=	4.7	Functional	Agonistic activity at mGlu1-alpha receptor expressed in CHO cellsAgonistic activity at mGlu1-alpha receptor expressed in CHO cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm9602569
	33032	2286	108	None	-741	17	Human	4.7	pEC50	=	4.7	Functional	Agonistic activity at mGlu1-alpha receptor expressed in CHO cellsAgonistic activity at mGlu1-alpha receptor expressed in CHO cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm9602569
	44272391	2286	108	None	-741	17	Human	4.7	pEC50	=	4.7	Functional	Agonistic activity at mGlu1-alpha receptor expressed in CHO cellsAgonistic activity at mGlu1-alpha receptor expressed in CHO cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm9602569
	88747398	2286	108	None	-741	17	Human	4.7	pEC50	=	4.7	Functional	Agonistic activity at mGlu1-alpha receptor expressed in CHO cellsAgonistic activity at mGlu1-alpha receptor expressed in CHO cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm9602569
	CHEMBL575060	2286	108	None	-741	17	Human	4.7	pEC50	=	4.7	Functional	Agonistic activity at mGlu1-alpha receptor expressed in CHO cellsAgonistic activity at mGlu1-alpha receptor expressed in CHO cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm9602569
	DB00142	2286	108	None	-741	17	Human	4.7	pEC50	=	4.7	Functional	Agonistic activity at mGlu1-alpha receptor expressed in CHO cellsAgonistic activity at mGlu1-alpha receptor expressed in CHO cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm9602569
	127027100	137212	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	396	3	1	4	4.8	Cc1ccsc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759137	137212	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	396	3	1	4	4.8	Cc1ccsc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127026386	137269	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	1	6	3.6	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759573	137269	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	1	6	3.6	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3cccnc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127027101	137135	0	None	-	1	Human	4.7	pEC50	=	4.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	382	3	1	4	3.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)cc1F	10.1016/j.bmcl.2015.12.104
	CHEMBL3758435	137135	0	None	-	1	Human	4.7	pEC50	=	4.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	382	3	1	4	3.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)cc1F	10.1016/j.bmcl.2015.12.104
	122196114	123729	0	None	17	2	Human	6.7	pEC50	=	6.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	365	3	1	5	3.2	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634436	123729	0	None	17	2	Human	6.7	pEC50	=	6.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	365	3	1	5	3.2	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	162652796	179873	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	420	3	1	4	4.5	Cc1ccoc1C(=O)Nc1c(F)cc(N2C(=O)CC3(CCCC3)CC2=O)c(F)c1F	10.1016/j.bmcl.2020.127724
	CHEMBL4752766	179873	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	420	3	1	4	4.5	Cc1ccoc1C(=O)Nc1c(F)cc(N2C(=O)CC3(CCCC3)CC2=O)c(F)c1F	10.1016/j.bmcl.2020.127724
	10474765	192532	0	None	-	1	Rat	7.7	pEC50	=	7.7	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	378	2	1	4	4.7	O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2ccc(F)cc21	10.1016/j.bmcl.2009.01.108
	CHEMBL522875	192532	0	None	-	1	Rat	7.7	pEC50	=	7.7	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	378	2	1	4	4.7	O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2ccc(F)cc21	10.1016/j.bmcl.2009.01.108
	122196119	123734	0	None	17	2	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	396	3	1	4	4.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c2ccccc12	10.1016/j.bmcl.2015.10.013
	CHEMBL3634441	123734	0	None	17	2	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	396	3	1	4	4.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c2ccccc12	10.1016/j.bmcl.2015.10.013
	122196122	123737	0	None	41	2	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	414	3	1	4	4.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c2ccccc12	10.1016/j.bmcl.2015.10.013
	CHEMBL3634444	123737	0	None	41	2	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	414	3	1	4	4.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c2ccccc12	10.1016/j.bmcl.2015.10.013
	10338547	3288	21	None	1	2	Rat	6.7	pEC50	=	6.7	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2009.01.108
	6204	3288	21	None	1	2	Rat	6.7	pEC50	=	6.7	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2009.01.108
	CHEMBL521982	3288	21	None	1	2	Rat	6.7	pEC50	=	6.7	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2009.01.108
	122196117	123732	0	None	12	2	Human	6.7	pEC50	=	6.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	382	3	1	6	3.1	Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(Cl)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634439	123732	0	None	12	2	Human	6.7	pEC50	=	6.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	382	3	1	6	3.1	Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(Cl)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	127034504	138455	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	391	3	1	4	4.5	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C#N)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785392	138455	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	391	3	1	4	4.5	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C#N)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	10362260	187053	0	None	-	1	Rat	7.7	pEC50	=	7.7	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	378	2	1	4	4.7	O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2c(F)cccc21	10.1016/j.bmcl.2009.01.108
	CHEMBL494960	187053	0	None	-	1	Rat	7.7	pEC50	=	7.7	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	378	2	1	4	4.7	O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2c(F)cccc21	10.1016/j.bmcl.2009.01.108
	122196100	123716	0	None	19	2	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	374	3	1	4	4.3	Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O	10.1016/j.bmcl.2015.10.013
	CHEMBL3634423	123716	0	None	19	2	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	374	3	1	4	4.3	Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O	10.1016/j.bmcl.2015.10.013
	127025479	137205	0	None	51	2	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	411	3	1	5	4.5	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	CHEMBL3759038	137205	0	None	51	2	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	411	3	1	5	4.5	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	127033963	138444	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	400	3	1	3	5.3	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785321	138444	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	400	3	1	3	5.3	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127034504	138455	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	391	3	1	4	4.5	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C#N)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785392	138455	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	391	3	1	4	4.5	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(C#N)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	162669790	182048	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	412	3	1	4	4.7	Cc1cc(N2C(=O)c3ccc(Cl)cc3C2=O)c(F)cc1NC(=O)c1occc1C	10.1016/j.bmcl.2020.127724
	CHEMBL4788523	182048	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	412	3	1	4	4.7	Cc1cc(N2C(=O)c3ccc(Cl)cc3C2=O)c(F)cc1NC(=O)c1occc1C	10.1016/j.bmcl.2020.127724
	127025479	137205	0	None	51	2	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	411	3	1	5	4.5	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	CHEMBL3759038	137205	0	None	51	2	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	411	3	1	5	4.5	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	122196095	123711	0	None	12	2	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	364	3	1	4	3.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(F)c1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634418	123711	0	None	12	2	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	364	3	1	4	3.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(F)c1	10.1016/j.bmcl.2015.10.013
	127026165	137170	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	378	3	1	4	4.1	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O	10.1016/j.bmcl.2020.127724
	CHEMBL3758746	137170	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	378	3	1	4	4.1	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O	10.1016/j.bmcl.2020.127724
	127027102	137137	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	382	3	1	4	3.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)cc1F	10.1016/j.bmcl.2015.12.104
	CHEMBL3758465	137137	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	382	3	1	4	3.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)cc1F	10.1016/j.bmcl.2015.12.104
	127025860	137203	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	2	4	3.6	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759028	137203	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	2	4	3.6	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	44573698	1064	0	None	-	1	Rat	6.7	pEC50	=	6.7	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	307	2	1	5	3.3	O=C(C1c2ccccc2Oc2c1cccc2)Nc1noc(n1)C	10.1016/j.bmcl.2009.01.108
	6205	1064	0	None	-	1	Rat	6.7	pEC50	=	6.7	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	307	2	1	5	3.3	O=C(C1c2ccccc2Oc2c1cccc2)Nc1noc(n1)C	10.1016/j.bmcl.2009.01.108
	CHEMBL492378	1064	0	None	-	1	Rat	6.7	pEC50	=	6.7	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	307	2	1	5	3.3	O=C(C1c2ccccc2Oc2c1cccc2)Nc1noc(n1)C	10.1016/j.bmcl.2009.01.108
	162666895	181939	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Negative allosteric modulation of human mGluR1 by calcium mobilization assayNegative allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	335	3	1	4	2.5	CC1(C)C2C(=O)N(c3ccc(NC(=O)c4ccccn4)cc3)C(=O)C21	10.1016/j.bmcl.2020.127724
	CHEMBL4787147	181939	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Negative allosteric modulation of human mGluR1 by calcium mobilization assayNegative allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	335	3	1	4	2.5	CC1(C)C2C(=O)N(c3ccc(NC(=O)c4ccccn4)cc3)C(=O)C21	10.1016/j.bmcl.2020.127724
	127027102	137137	0	None	-	1	Human	4.7	pEC50	=	4.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	382	3	1	4	3.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)cc1F	10.1016/j.bmcl.2015.12.104
	CHEMBL3758465	137137	0	None	-	1	Human	4.7	pEC50	=	4.7	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	382	3	1	4	3.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)cc1F	10.1016/j.bmcl.2015.12.104
	127033436	138434	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	394	3	1	4	4.2	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)Cc3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785245	138434	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	394	3	1	4	4.2	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)Cc3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127026067	137323	0	None	6	2	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	411	3	1	5	4.5	Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	CHEMBL3760018	137323	0	None	6	2	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	411	3	1	5	4.5	Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	122196121	123736	0	None	22	2	Human	7.6	pEC50	=	7.6	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	430	3	1	4	5.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c2ccccc12	10.1016/j.bmcl.2015.10.013
	CHEMBL3634443	123736	0	None	22	2	Human	7.6	pEC50	=	7.6	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	430	3	1	4	5.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c2ccccc12	10.1016/j.bmcl.2015.10.013
	122193178	123415	0	None	30	2	Human	7.6	pEC50	=	7.6	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628114	123415	0	None	30	2	Human	7.6	pEC50	=	7.6	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	1368	2258	31	None	-60	11	Rat	4.6	pEC50	=	4.6	Functional	Metabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in ratMetabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in rat	ChEMBL	159	3	3	3	-0.9	N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O	10.1021/jm030967o
	5310956	2258	31	None	-60	11	Rat	4.6	pEC50	=	4.6	Functional	Metabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in ratMetabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in rat	ChEMBL	159	3	3	3	-0.9	N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O	10.1021/jm030967o
	CHEMBL280563	2258	31	None	-60	11	Rat	4.6	pEC50	=	4.6	Functional	Metabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in ratMetabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in rat	ChEMBL	159	3	3	3	-0.9	N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O	10.1021/jm030967o
	1310	2286	108	None	-794	17	Rat	4.6	pEC50	=	4.6	Functional	Agonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmcl.2015.04.043
	1369	2286	108	None	-794	17	Rat	4.6	pEC50	=	4.6	Functional	Agonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmcl.2015.04.043
	33032	2286	108	None	-794	17	Rat	4.6	pEC50	=	4.6	Functional	Agonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmcl.2015.04.043
	44272391	2286	108	None	-794	17	Rat	4.6	pEC50	=	4.6	Functional	Agonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmcl.2015.04.043
	88747398	2286	108	None	-794	17	Rat	4.6	pEC50	=	4.6	Functional	Agonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmcl.2015.04.043
	CHEMBL575060	2286	108	None	-794	17	Rat	4.6	pEC50	=	4.6	Functional	Agonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmcl.2015.04.043
	DB00142	2286	108	None	-794	17	Rat	4.6	pEC50	=	4.6	Functional	Agonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assayAgonist activity at rat mGluR1 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmcl.2015.04.043
	127026067	137323	0	None	6	2	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	411	3	1	5	4.5	Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	CHEMBL3760018	137323	0	None	6	2	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	411	3	1	5	4.5	Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncsc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	127046038	139411	0	None	-4	2	Rat	5.6	pEC50	=	5.6	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	350	3	1	4	5.1	CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	CHEMBL3799685	139411	0	None	-4	2	Rat	5.6	pEC50	=	5.6	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	350	3	1	4	5.1	CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	122193178	123415	0	None	30	2	Human	7.6	pEC50	=	7.6	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628114	123415	0	None	30	2	Human	7.6	pEC50	=	7.6	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	122193173	123410	0	None	25	2	Human	7.6	pEC50	=	7.6	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	394	3	1	4	4.6	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628109	123410	0	None	25	2	Human	7.6	pEC50	=	7.6	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	394	3	1	4	4.6	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	122193173	123410	0	None	25	2	Human	7.6	pEC50	=	7.6	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	394	3	1	4	4.6	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628109	123410	0	None	25	2	Human	7.6	pEC50	=	7.6	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	394	3	1	4	4.6	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	127046038	139411	0	None	-4	2	Rat	5.6	pEC50	=	5.6	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	350	3	1	4	5.1	CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	CHEMBL3799685	139411	0	None	-4	2	Rat	5.6	pEC50	=	5.6	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	350	3	1	4	5.1	CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	127026059	137306	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	399	3	1	5	3.8	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759878	137306	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	399	3	1	5	3.8	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127033436	138434	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	394	3	1	4	4.2	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)Cc3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785245	138434	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	394	3	1	4	4.2	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)Cc3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127034514	138584	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	366	3	1	3	4.7	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1	10.1016/j.bmcl.2016.03.031
	CHEMBL3786739	138584	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	366	3	1	3	4.7	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1	10.1016/j.bmcl.2016.03.031
	10338547	3288	21	None	-1	2	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 minsPositive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 mins	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2016.03.044
	6204	3288	21	None	-1	2	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 minsPositive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 mins	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2016.03.044
	CHEMBL521982	3288	21	None	-1	2	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 minsPositive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 mins	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2016.03.044
	127034514	138584	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	366	3	1	3	4.7	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1	10.1016/j.bmcl.2016.03.031
	CHEMBL3786739	138584	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	366	3	1	3	4.7	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)cc1	10.1016/j.bmcl.2016.03.031
	10338547	3288	21	None	-1	2	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 minsPositive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 mins	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2016.03.044
	6204	3288	21	None	-1	2	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 minsPositive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 mins	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2016.03.044
	CHEMBL521982	3288	21	None	-1	2	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 minsPositive allosteric modulation of human mGlu1 receptor expressed in wild type T-Rex 293 cells assessed as increase in glutamate-induced calcium mobilization incubated for 2 mins before glutamate stimulation for 2.2 mins	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2016.03.044
	127033962	138513	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	366	3	1	3	5.1	Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc3C2)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3786032	138513	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	366	3	1	3	5.1	Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc3C2)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	44573738	187021	0	None	-	1	Rat	7.6	pEC50	=	7.6	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	396	2	1	4	4.8	O=C(Nc1ncc(C(F)(F)F)o1)C1c2cccc(F)c2Oc2c(F)cccc21	10.1016/j.bmcl.2009.01.108
	CHEMBL494766	187021	0	None	-	1	Rat	7.6	pEC50	=	7.6	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	396	2	1	4	4.8	O=C(Nc1ncc(C(F)(F)F)o1)C1c2cccc(F)c2Oc2c(F)cccc21	10.1016/j.bmcl.2009.01.108
	127026166	137117	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	378	3	1	4	4.1	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)cc1F	10.1016/j.bmcl.2015.12.104
	CHEMBL3758305	137117	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	378	3	1	4	4.1	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)cc1F	10.1016/j.bmcl.2015.12.104
	127026165	137170	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	378	3	1	4	4.1	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O	10.1016/j.bmcl.2016.03.031
	CHEMBL3758746	137170	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	378	3	1	4	4.1	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)c(F)c1)C2=O	10.1016/j.bmcl.2016.03.031
	127025564	137265	0	None	2	2	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	394	3	1	5	3.4	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3nccn3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	CHEMBL3759555	137265	0	None	2	2	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	394	3	1	5	3.4	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3nccn3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	127025564	137265	0	None	2	2	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	394	3	1	5	3.4	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3nccn3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	CHEMBL3759555	137265	0	None	2	2	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	394	3	1	5	3.4	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3nccn3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	127026166	137117	0	None	-	1	Human	4.6	pEC50	=	4.6	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	378	3	1	4	4.1	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)cc1F	10.1016/j.bmcl.2015.12.104
	CHEMBL3758305	137117	0	None	-	1	Human	4.6	pEC50	=	4.6	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	378	3	1	4	4.1	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)cc1F	10.1016/j.bmcl.2015.12.104
	122196096	123712	0	None	10	2	Human	7.6	pEC50	=	7.6	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	378	3	1	4	4.1	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(F)c1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634419	123712	0	None	10	2	Human	7.6	pEC50	=	7.6	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	378	3	1	4	4.1	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(F)c1	10.1016/j.bmcl.2015.10.013
	10045177	186721	0	None	-	1	Rat	6.6	pEC50	=	6.6	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	378	2	1	4	4.7	O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2cc(F)ccc21	10.1016/j.bmcl.2009.01.108
	CHEMBL492979	186721	0	None	-	1	Rat	6.6	pEC50	=	6.6	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	378	2	1	4	4.7	O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2cc(F)ccc21	10.1016/j.bmcl.2009.01.108
	127033960	138583	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	369	3	1	5	4.4	Cc1ccoc1C(=O)Nc1ccc(N2CCOc3ncccc32)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3786721	138583	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	369	3	1	5	4.4	Cc1ccoc1C(=O)Nc1ccc(N2CCOc3ncccc32)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127028298	137279	0	None	6	2	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	414	3	1	5	3.8	Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759647	137279	0	None	6	2	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	414	3	1	5	3.8	Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127033960	138583	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	369	3	1	5	4.4	Cc1ccoc1C(=O)Nc1ccc(N2CCOc3ncccc32)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3786721	138583	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	369	3	1	5	4.4	Cc1ccoc1C(=O)Nc1ccc(N2CCOc3ncccc32)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127028298	137279	0	None	6	2	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	414	3	1	5	3.8	Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759647	137279	0	None	6	2	Human	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	414	3	1	5	3.8	Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127046020	139224	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	323	2	1	5	3.7	Cc1nsc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	CHEMBL3798489	139224	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	323	2	1	5	3.7	Cc1nsc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	127046020	139224	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	323	2	1	5	3.7	Cc1nsc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	CHEMBL3798489	139224	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	323	2	1	5	3.7	Cc1nsc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	10338547	3288	21	None	1	2	Rat	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2016.03.044
	6204	3288	21	None	1	2	Rat	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2016.03.044
	CHEMBL521982	3288	21	None	1	2	Rat	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2016.03.044
	10338547	3288	21	None	1	2	Rat	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2016.03.044
	6204	3288	21	None	1	2	Rat	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2016.03.044
	CHEMBL521982	3288	21	None	1	2	Rat	6.6	pEC50	=	6.6	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2016.03.044
	122196097	123713	0	None	9	2	Human	7.6	pEC50	=	7.6	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(F)c1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634420	123713	0	None	9	2	Human	7.6	pEC50	=	7.6	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(F)c1	10.1016/j.bmcl.2015.10.013
	122196093	123709	0	None	16	2	Human	7.5	pEC50	=	7.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	380	3	1	4	4.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)cc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634416	123709	0	None	16	2	Human	7.5	pEC50	=	7.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	380	3	1	4	4.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)cc1	10.1016/j.bmcl.2015.10.013
	122196124	123739	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	380	3	1	4	4.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1Cl	10.1016/j.bmcl.2015.10.013
	CHEMBL3634446	123739	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	380	3	1	4	4.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1Cl	10.1016/j.bmcl.2015.10.013
	122193310	123420	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	393	3	1	4	3.3	O=C(Nc1ccc(N2C(=O)[C@H]3[C@H]4C=C[C@@H](C4)[C@H]3C2=O)c(Cl)c1)c1ccccn1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628280	123420	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	393	3	1	4	3.3	O=C(Nc1ccc(N2C(=O)[C@H]3[C@H]4C=C[C@@H](C4)[C@H]3C2=O)c(Cl)c1)c1ccccn1	10.1021/acs.jmedchem.5b00727
	1310	2286	108	None	-794	17	Rat	5.5	pEC50	=	5.5	Functional	Agonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/s0960-894x(01)00158-5
	1369	2286	108	None	-794	17	Rat	5.5	pEC50	=	5.5	Functional	Agonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/s0960-894x(01)00158-5
	33032	2286	108	None	-794	17	Rat	5.5	pEC50	=	5.5	Functional	Agonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/s0960-894x(01)00158-5
	44272391	2286	108	None	-794	17	Rat	5.5	pEC50	=	5.5	Functional	Agonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/s0960-894x(01)00158-5
	88747398	2286	108	None	-794	17	Rat	5.5	pEC50	=	5.5	Functional	Agonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/s0960-894x(01)00158-5
	CHEMBL575060	2286	108	None	-794	17	Rat	5.5	pEC50	=	5.5	Functional	Agonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/s0960-894x(01)00158-5
	DB00142	2286	108	None	-794	17	Rat	5.5	pEC50	=	5.5	Functional	Agonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cellsAgonist activity in rat at Metabotropic glutamate receptor 1 expressed in HEK293 cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/s0960-894x(01)00158-5
	162676671	183000	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	374	3	1	4	4.3	Cc1cc(N2C(=O)c3ccccc3C2=O)c(C)cc1NC(=O)c1occc1C	10.1016/j.bmcl.2020.127724
	CHEMBL4800540	183000	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	374	3	1	4	4.3	Cc1cc(N2C(=O)c3ccccc3C2=O)c(C)cc1NC(=O)c1occc1C	10.1016/j.bmcl.2020.127724
	122193177	123414	3	None	1	3	Human	7.5	pEC50	=	7.5	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628113	123414	3	None	1	3	Human	7.5	pEC50	=	7.5	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	122193177	123414	3	None	1	3	Human	7.5	pEC50	=	7.5	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3628113	123414	3	None	1	3	Human	7.5	pEC50	=	7.5	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	122193177	123414	3	None	1	3	Human	7.5	pEC50	=	7.5	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628113	123414	3	None	1	3	Human	7.5	pEC50	=	7.5	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	1407	2048	34	None	-1023	7	Rat	4.5	pEC50	=	4.5	Functional	Metabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in ratMetabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in rat	ChEMBL	239	4	4	4	0.2	N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O	10.1021/jm030967o
	16062593	2048	34	None	-1023	7	Rat	4.5	pEC50	=	4.5	Functional	Metabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in ratMetabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in rat	ChEMBL	239	4	4	4	0.2	N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O	10.1021/jm030967o
	CHEMBL143210	2048	34	None	-1023	7	Rat	4.5	pEC50	=	4.5	Functional	Metabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in ratMetabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in rat	ChEMBL	239	4	4	4	0.2	N[C@@H](c1ccc(c(c1)C(=O)O)C(=O)O)C(=O)O	10.1021/jm030967o
	122193175	123412	0	None	34	2	Human	7.5	pEC50	=	7.5	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	414	3	1	4	4.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628111	123412	0	None	34	2	Human	7.5	pEC50	=	7.5	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	414	3	1	4	4.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	122193175	123412	0	None	34	2	Human	7.5	pEC50	=	7.5	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	414	3	1	4	4.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628111	123412	0	None	34	2	Human	7.5	pEC50	=	7.5	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	414	3	1	4	4.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	122196127	123741	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	376	4	1	5	3.7	COc1cc(N2C(=O)c3ccccc3C2=O)ccc1NC(=O)c1occc1C	10.1016/j.bmcl.2015.10.013
	CHEMBL3634449	123741	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	376	4	1	5	3.7	COc1cc(N2C(=O)c3ccccc3C2=O)ccc1NC(=O)c1occc1C	10.1016/j.bmcl.2015.10.013
	127027327	137327	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	379	3	2	3	4.0	Cc1cc[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3760068	137327	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	379	3	2	3	4.0	Cc1cc[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127027327	137327	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	379	3	2	3	4.0	Cc1cc[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3760068	137327	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	379	3	2	3	4.0	Cc1cc[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	122196098	123714	0	None	19	2	Human	7.5	pEC50	=	7.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	382	3	1	4	3.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(F)c1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634421	123714	0	None	19	2	Human	7.5	pEC50	=	7.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	382	3	1	4	3.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(F)c1	10.1016/j.bmcl.2015.10.013
	122196113	123728	0	None	32	2	Human	7.5	pEC50	=	7.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	381	3	1	5	3.7	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634435	123728	0	None	32	2	Human	7.5	pEC50	=	7.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	381	3	1	5	3.7	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	127033437	138435	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	408	3	1	4	4.2	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)Cc3ccccc3CC2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785247	138435	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	408	3	1	4	4.2	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)Cc3ccccc3CC2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127034515	138457	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	366	3	1	3	4.7	Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)cc1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785400	138457	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	366	3	1	3	4.7	Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)cc1	10.1016/j.bmcl.2016.03.031
	127029302	137124	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	380	3	1	5	3.1	Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3758364	137124	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	380	3	1	5	3.1	Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127034515	138457	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	366	3	1	3	4.7	Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)cc1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785400	138457	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	366	3	1	3	4.7	Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)cc1	10.1016/j.bmcl.2016.03.031
	10009	3986	35	None	-1	3	Rat	6.5	pEC50	=	6.5	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay	ChEMBL	445	3	1	4	5.1	Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl	10.1021/acs.jmedchem.5b00727
	91885483	3986	35	None	-1	3	Rat	6.5	pEC50	=	6.5	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay	ChEMBL	445	3	1	4	5.1	Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl	10.1021/acs.jmedchem.5b00727
	CHEMBL3628116	3986	35	None	-1	3	Rat	6.5	pEC50	=	6.5	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay	ChEMBL	445	3	1	4	5.1	Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl	10.1021/acs.jmedchem.5b00727
	4125492	139562	10	None	-2	2	Rat	5.4	pEC50	=	5.4	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	308	2	1	4	4.0	O=C(Nc1nccs1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2016.03.044
	CHEMBL3800589	139562	10	None	-2	2	Rat	5.4	pEC50	=	5.4	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	308	2	1	4	4.0	O=C(Nc1nccs1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2016.03.044
	127033694	138494	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	368	3	1	4	5.0	Cc1ccoc1C(=O)Nc1ccc(N2CCOc3ccccc32)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785850	138494	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	368	3	1	4	5.0	Cc1ccoc1C(=O)Nc1ccc(N2CCOc3ccccc32)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127033437	138435	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	408	3	1	4	4.2	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)Cc3ccccc3CC2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785247	138435	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	408	3	1	4	4.2	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)Cc3ccccc3CC2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127033694	138494	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	368	3	1	4	5.0	Cc1ccoc1C(=O)Nc1ccc(N2CCOc3ccccc32)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785850	138494	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	368	3	1	4	5.0	Cc1ccoc1C(=O)Nc1ccc(N2CCOc3ccccc32)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	4125492	139562	10	None	-2	2	Rat	5.4	pEC50	=	5.4	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	308	2	1	4	4.0	O=C(Nc1nccs1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2016.03.044
	CHEMBL3800589	139562	10	None	-2	2	Rat	5.4	pEC50	=	5.4	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of rat mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	308	2	1	4	4.0	O=C(Nc1nccs1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2016.03.044
	127031257	138658	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	366	3	1	3	4.7	Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3787619	138658	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	366	3	1	3	4.7	Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127031257	138658	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	366	3	1	3	4.7	Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3787619	138658	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	366	3	1	3	4.7	Cc1ccoc1C(=O)Nc1ccc(N2Cc3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127029302	137124	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	380	3	1	5	3.1	Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3758364	137124	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	380	3	1	5	3.1	Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	9975764	187056	0	None	-	1	Rat	7.4	pEC50	=	7.4	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	360	2	1	4	4.6	O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2009.01.108
	CHEMBL494966	187056	0	None	-	1	Rat	7.4	pEC50	=	7.4	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	360	2	1	4	4.6	O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2009.01.108
	122196111	123726	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	347	3	1	5	3.0	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634433	123726	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	347	3	1	5	3.0	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	127032809	138452	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	444	3	1	3	5.4	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Br)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785382	138452	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	444	3	1	3	5.4	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Br)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	10009	3986	35	None	-1	3	Human	6.4	pEC50	=	6.4	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	445	3	1	4	5.1	Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl	10.1021/acs.jmedchem.5b00727
	91885483	3986	35	None	-1	3	Human	6.4	pEC50	=	6.4	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	445	3	1	4	5.1	Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl	10.1021/acs.jmedchem.5b00727
	CHEMBL3628116	3986	35	None	-1	3	Human	6.4	pEC50	=	6.4	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	445	3	1	4	5.1	Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl	10.1021/acs.jmedchem.5b00727
	10009	3986	35	None	-1	3	Human	6.4	pEC50	=	6.4	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	445	3	1	4	5.1	Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl	10.1016/j.bmcl.2016.03.031
	91885483	3986	35	None	-1	3	Human	6.4	pEC50	=	6.4	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	445	3	1	4	5.1	Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl	10.1016/j.bmcl.2016.03.031
	CHEMBL3628116	3986	35	None	-1	3	Human	6.4	pEC50	=	6.4	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	445	3	1	4	5.1	Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl	10.1016/j.bmcl.2016.03.031
	127032809	138452	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	444	3	1	3	5.4	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Br)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785382	138452	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	444	3	1	3	5.4	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(Br)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	9975764	187056	0	None	-	1	Rat	6.4	pEC50	=	6.4	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	360	2	1	4	4.6	O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2009.01.108
	CHEMBL494966	187056	0	None	-	1	Rat	6.4	pEC50	=	6.4	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	360	2	1	4	4.6	O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2009.01.108
	10407284	186654	0	None	-	1	Rat	7.4	pEC50	=	7.4	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	378	2	1	4	4.7	O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2ccc(F)cc21	10.1016/j.bmcl.2009.01.108
	CHEMBL492570	186654	0	None	-	1	Rat	7.4	pEC50	=	7.4	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	378	2	1	4	4.7	O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2ccc(F)cc21	10.1016/j.bmcl.2009.01.108
	10045177	186721	0	None	-	1	Rat	7.4	pEC50	=	7.4	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	378	2	1	4	4.7	O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2cc(F)ccc21	10.1016/j.bmcl.2009.01.108
	CHEMBL492979	186721	0	None	-	1	Rat	7.4	pEC50	=	7.4	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	378	2	1	4	4.7	O=C(Nc1nc(C(F)(F)F)co1)C1c2ccccc2Oc2cc(F)ccc21	10.1016/j.bmcl.2009.01.108
	122193177	123414	3	None	-1	3	Rat	7.4	pEC50	=	7.4	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628113	123414	3	None	-1	3	Rat	7.4	pEC50	=	7.4	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	122193177	123414	3	None	-1	3	Rat	7.4	pEC50	=	7.4	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628113	123414	3	None	-1	3	Rat	7.4	pEC50	=	7.4	Functional	Positive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assayPositive allosteric modulation of rat mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobiliztion by cell based assay	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	127025548	137150	0	None	4	2	Human	7.4	pEC50	=	7.4	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	395	3	1	5	4.0	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	CHEMBL3758587	137150	0	None	4	2	Human	7.4	pEC50	=	7.4	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	395	3	1	5	4.0	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	127025548	137150	0	None	4	2	Human	7.4	pEC50	=	7.4	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	395	3	1	5	4.0	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	CHEMBL3758587	137150	0	None	4	2	Human	7.4	pEC50	=	7.4	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	395	3	1	5	4.0	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	162677180	182947	0	None	5	3	Human	7.4	pEC50	=	7.4	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	400	3	1	4	4.1	Cc1ccoc1C(=O)Nc1c(F)cc(N2C(=O)c3ccccc3C2=O)c(F)c1F	10.1016/j.bmcl.2020.127724
	CHEMBL4799902	182947	0	None	5	3	Human	7.4	pEC50	=	7.4	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	400	3	1	4	4.1	Cc1ccoc1C(=O)Nc1c(F)cc(N2C(=O)c3ccccc3C2=O)c(F)c1F	10.1016/j.bmcl.2020.127724
	104766	34	36	None	-8	14	Rat	4.4	pEC50	=	4.4	Functional	Tested for the agonistic activity against Metabotropic glutamate receptor 1Tested for the agonistic activity against Metabotropic glutamate receptor 1	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1016/S0960-894X(97)00068-1
	1365	34	36	None	-8	14	Rat	4.4	pEC50	=	4.4	Functional	Tested for the agonistic activity against Metabotropic glutamate receptor 1Tested for the agonistic activity against Metabotropic glutamate receptor 1	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1016/S0960-894X(97)00068-1
	CHEMBL34453	34	36	None	-8	14	Rat	4.4	pEC50	=	4.4	Functional	Tested for the agonistic activity against Metabotropic glutamate receptor 1Tested for the agonistic activity against Metabotropic glutamate receptor 1	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1016/S0960-894X(97)00068-1
	6603885	101731	17	None	-4	5	Rat	4.4	pEC50	=	4.4	Functional	Activity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulationActivity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulation	ChEMBL	158	2	3	5	-0.5	N[C@H](C(=O)O)c1cc(O)no1	10.1021/jm701394a
	6971208	101731	17	None	-4	5	Rat	4.4	pEC50	=	4.4	Functional	Activity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulationActivity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulation	ChEMBL	158	2	3	5	-0.5	N[C@H](C(=O)O)c1cc(O)no1	10.1021/jm701394a
	CHEMBL30285	101731	17	None	-4	5	Rat	4.4	pEC50	=	4.4	Functional	Activity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulationActivity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulation	ChEMBL	158	2	3	5	-0.5	N[C@H](C(=O)O)c1cc(O)no1	10.1021/jm701394a
	12310764	1939	59	None	-21	2	Rat	4.4	pEC50	=	4.4	Functional	Compound was evaluated for agonistic activity against mGluR1 alpha metabotropic receptor subtype in rat cortical slice modelCompound was evaluated for agonistic activity against mGluR1 alpha metabotropic receptor subtype in rat cortical slice model	ChEMBL	158	2	3	4	-0.9	OC(=O)C(c1o[nH]c(=O)c1)N	10.1016/s0960-894x(98)00264-9
	1233	1939	59	None	-21	2	Rat	4.4	pEC50	=	4.4	Functional	Compound was evaluated for agonistic activity against mGluR1 alpha metabotropic receptor subtype in rat cortical slice modelCompound was evaluated for agonistic activity against mGluR1 alpha metabotropic receptor subtype in rat cortical slice model	ChEMBL	158	2	3	4	-0.9	OC(=O)C(c1o[nH]c(=O)c1)N	10.1016/s0960-894x(98)00264-9
	1371	1939	59	None	-21	2	Rat	4.4	pEC50	=	4.4	Functional	Compound was evaluated for agonistic activity against mGluR1 alpha metabotropic receptor subtype in rat cortical slice modelCompound was evaluated for agonistic activity against mGluR1 alpha metabotropic receptor subtype in rat cortical slice model	ChEMBL	158	2	3	4	-0.9	OC(=O)C(c1o[nH]c(=O)c1)N	10.1016/s0960-894x(98)00264-9
	CHEMBL284895	1939	59	None	-21	2	Rat	4.4	pEC50	=	4.4	Functional	Compound was evaluated for agonistic activity against mGluR1 alpha metabotropic receptor subtype in rat cortical slice modelCompound was evaluated for agonistic activity against mGluR1 alpha metabotropic receptor subtype in rat cortical slice model	ChEMBL	158	2	3	4	-0.9	OC(=O)C(c1o[nH]c(=O)c1)N	10.1016/s0960-894x(98)00264-9
	127028301	137258	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	394	3	2	4	3.7	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759530	137258	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	394	3	2	4	3.7	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	9978023	187090	0	None	-	1	Rat	7.4	pEC50	=	7.4	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	396	2	1	4	4.8	O=C(Nc1nc(C(F)(F)F)co1)C1c2cc(F)ccc2Oc2ccc(F)cc21	10.1016/j.bmcl.2009.01.108
	CHEMBL495150	187090	0	None	-	1	Rat	7.4	pEC50	=	7.4	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	396	2	1	4	4.8	O=C(Nc1nc(C(F)(F)F)co1)C1c2cc(F)ccc2Oc2ccc(F)cc21	10.1016/j.bmcl.2009.01.108
	122196094	123710	0	None	8	2	Human	7.4	pEC50	=	7.4	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	364	3	1	4	3.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)cc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634417	123710	0	None	8	2	Human	7.4	pEC50	=	7.4	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	364	3	1	4	3.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)cc1	10.1016/j.bmcl.2015.10.013
	122193154	123408	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	383	3	1	5	3.8	O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1cscn1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628088	123408	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	383	3	1	5	3.8	O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1cscn1	10.1021/acs.jmedchem.5b00727
	122193154	123408	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	383	3	1	5	3.8	O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1cscn1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628088	123408	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	383	3	1	5	3.8	O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1cscn1	10.1021/acs.jmedchem.5b00727
	122196107	123723	0	None	25	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	376	4	1	5	3.7	COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O	10.1016/j.bmcl.2015.10.013
	CHEMBL3634430	123723	0	None	25	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	376	4	1	5	3.7	COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O	10.1016/j.bmcl.2015.10.013
	122196115	123730	0	None	1	2	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	348	3	1	6	2.4	Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3ccccc3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634437	123730	0	None	1	2	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	348	3	1	6	2.4	Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3ccccc3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	127025549	137248	0	None	1	2	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	395	3	1	5	4.0	Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	CHEMBL3759424	137248	0	None	1	2	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	395	3	1	5	4.0	Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	127033435	138634	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	417	3	1	4	5.2	Cc1scnc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3787296	138634	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	417	3	1	4	5.2	Cc1scnc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	44573780	187057	0	None	-	1	Rat	7.3	pEC50	=	7.3	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	396	2	1	4	4.8	O=C(Nc1nc(C(F)(F)F)co1)C1c2cccc(F)c2Oc2c(F)cccc21	10.1016/j.bmcl.2009.01.108
	CHEMBL494967	187057	0	None	-	1	Rat	7.3	pEC50	=	7.3	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	396	2	1	4	4.8	O=C(Nc1nc(C(F)(F)F)co1)C1c2cccc(F)c2Oc2c(F)cccc21	10.1016/j.bmcl.2009.01.108
	127025549	137248	0	None	1	2	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	395	3	1	5	4.0	Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	CHEMBL3759424	137248	0	None	1	2	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	395	3	1	5	4.0	Cc1cccc2c1C(=O)N(c1ccc(NC(=O)c3ncoc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	2862916	40460	11	None	2	2	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	358	2	1	4	5.2	O=C(Nc1nc2ccccc2s1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2016.03.044
	CHEMBL1484616	40460	11	None	2	2	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	358	2	1	4	5.2	O=C(Nc1nc2ccccc2s1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2016.03.044
	127033435	138634	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	417	3	1	4	5.2	Cc1scnc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3787296	138634	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	417	3	1	4	5.2	Cc1scnc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	122196091	123707	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	346	3	1	4	3.6	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634414	123707	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	346	3	1	4	3.6	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1	10.1016/j.bmcl.2015.10.013
	2862916	40460	11	None	2	2	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	358	2	1	4	5.2	O=C(Nc1nc2ccccc2s1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2016.03.044
	CHEMBL1484616	40460	11	None	2	2	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	358	2	1	4	5.2	O=C(Nc1nc2ccccc2s1)C1c2ccccc2Oc2ccccc21	10.1016/j.bmcl.2016.03.044
	127032506	138544	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	400	3	1	3	5.3	Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3786400	138544	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	400	3	1	3	5.3	Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127032506	138544	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	400	3	1	3	5.3	Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3786400	138544	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	400	3	1	3	5.3	Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	122196101	123717	0	None	20	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	394	3	1	4	4.6	Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O	10.1016/j.bmcl.2015.10.013
	CHEMBL3634424	123717	0	None	20	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	394	3	1	4	4.6	Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O	10.1016/j.bmcl.2015.10.013
	122196102	123718	0	None	22	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	378	3	1	4	4.1	Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O	10.1016/j.bmcl.2015.10.013
	CHEMBL3634425	123718	0	None	22	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	378	3	1	4	4.1	Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O	10.1016/j.bmcl.2015.10.013
	122196108	123724	0	None	18	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	390	4	1	5	4.0	COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O	10.1016/j.bmcl.2015.10.013
	CHEMBL3634431	123724	0	None	18	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	390	4	1	5	4.0	COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O	10.1016/j.bmcl.2015.10.013
	127028301	137258	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	394	3	2	4	3.7	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759530	137258	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	394	3	2	4	3.7	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127026167	137309	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)cc1F	10.1016/j.bmcl.2015.12.104
	CHEMBL3759901	137309	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)cc1F	10.1016/j.bmcl.2015.12.104
	127026138	137108	0	None	38	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	431	3	1	5	4.8	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3758216	137108	0	None	38	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	431	3	1	5	4.8	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	162662674	181396	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	378	3	1	4	4.1	Cc1cc(N2C(=O)c3ccccc3C2=O)c(F)cc1NC(=O)c1occc1C	10.1016/j.bmcl.2020.127724
	CHEMBL4780280	181396	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	378	3	1	4	4.1	Cc1cc(N2C(=O)c3ccccc3C2=O)c(F)cc1NC(=O)c1occc1C	10.1016/j.bmcl.2020.127724
	127026138	137108	0	None	38	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	431	3	1	5	4.8	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3758216	137108	0	None	38	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	431	3	1	5	4.8	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	44573698	1064	0	None	-	1	Rat	7.3	pEC50	=	7.3	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	307	2	1	5	3.3	O=C(C1c2ccccc2Oc2c1cccc2)Nc1noc(n1)C	10.1016/j.bmcl.2009.01.108
	6205	1064	0	None	-	1	Rat	7.3	pEC50	=	7.3	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	307	2	1	5	3.3	O=C(C1c2ccccc2Oc2c1cccc2)Nc1noc(n1)C	10.1016/j.bmcl.2009.01.108
	CHEMBL492378	1064	0	None	-	1	Rat	7.3	pEC50	=	7.3	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	307	2	1	5	3.3	O=C(C1c2ccccc2Oc2c1cccc2)Nc1noc(n1)C	10.1016/j.bmcl.2009.01.108
	127027099	137194	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	379	3	1	4	3.7	Cn1cccc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3758942	137194	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	379	3	1	4	3.7	Cn1cccc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127027099	137194	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	379	3	1	4	3.7	Cn1cccc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3758942	137194	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	379	3	1	4	3.7	Cn1cccc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	122196104	123720	0	None	10	2	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	428	3	1	4	5.0	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(C(F)(F)F)c1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634427	123720	0	None	10	2	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	428	3	1	4	5.0	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(C(F)(F)F)c1	10.1016/j.bmcl.2015.10.013
	127026167	137309	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)cc1F	10.1016/j.bmcl.2015.12.104
	CHEMBL3759901	137309	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)cc1F	10.1016/j.bmcl.2015.12.104
	122196118	123733	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	366	3	1	6	2.6	Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(F)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634440	123733	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	366	3	1	6	2.6	Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(F)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	127028303	137233	0	None	7	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	415	3	1	5	4.3	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759289	137233	0	None	7	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	415	3	1	5	4.3	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	122193174	123411	0	None	5	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	394	3	1	4	4.6	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)cc1Cl)C2=O	10.1021/acs.jmedchem.5b00727
	CHEMBL3628110	123411	0	None	5	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	394	3	1	4	4.6	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)cc1Cl)C2=O	10.1021/acs.jmedchem.5b00727
	127028303	137233	0	None	7	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	415	3	1	5	4.3	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759289	137233	0	None	7	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	415	3	1	5	4.3	Cc1ocnc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	122193174	123411	0	None	5	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	394	3	1	4	4.6	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)cc1Cl)C2=O	10.1021/acs.jmedchem.5b00727
	CHEMBL3628110	123411	0	None	5	2	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	394	3	1	4	4.6	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3occc3C)cc1Cl)C2=O	10.1021/acs.jmedchem.5b00727
	51116040	123407	5	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	366	3	1	4	4.0	O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1ccco1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628081	123407	5	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	366	3	1	4	4.0	O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1ccco1	10.1021/acs.jmedchem.5b00727
	51116040	123407	5	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	366	3	1	4	4.0	O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1ccco1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628081	123407	5	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	366	3	1	4	4.0	O=C(Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1)c1ccco1	10.1021/acs.jmedchem.5b00727
	127026471	137282	0	None	4	2	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	394	3	2	4	3.7	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3[nH]ncc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	CHEMBL3759656	137282	0	None	4	2	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	394	3	2	4	3.7	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3[nH]ncc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	10338547	3288	21	None	1	2	Rat	7.3	pEC50	=	7.3	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2009.01.108
	6204	3288	21	None	1	2	Rat	7.3	pEC50	=	7.3	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2009.01.108
	CHEMBL521982	3288	21	None	1	2	Rat	7.3	pEC50	=	7.3	Functional	Agonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assayAgonist activity at rat mGlu1 receptor expressed in HEK293 cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2009.01.108
	127029301	137160	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	397	3	1	5	4.2	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3758683	137160	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	397	3	1	5	4.2	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	162667269	181931	0	None	3	3	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	434	3	1	4	4.7	Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3cccc(Cl)c3C2=O)c(F)c1F	10.1016/j.bmcl.2020.127724
	CHEMBL4787053	181931	0	None	3	3	Human	7.3	pEC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	434	3	1	4	4.7	Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3cccc(Cl)c3C2=O)c(F)c1F	10.1016/j.bmcl.2020.127724
	127026471	137282	0	None	4	2	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	394	3	2	4	3.7	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3[nH]ncc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	CHEMBL3759656	137282	0	None	4	2	Human	6.3	pEC50	=	6.3	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	394	3	2	4	3.7	Cc1ccc2c(c1)C(=O)N(c1ccc(NC(=O)c3[nH]ncc3C)cc1Cl)C2=O	10.1016/j.bmcl.2015.12.104
	127033693	138431	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	352	3	1	3	5.2	Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc32)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785210	138431	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	352	3	1	3	5.2	Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc32)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127033693	138431	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	352	3	1	3	5.2	Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc32)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785210	138431	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	352	3	1	3	5.2	Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc32)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	162670460	182313	0	None	4	3	Human	7.2	pEC50	=	7.2	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	382	3	1	4	4.0	Cc1cc(N2C(=O)C3=C(CCCC3)C2=O)c(F)cc1NC(=O)c1occc1C	10.1016/j.bmcl.2020.127724
	CHEMBL4792152	182313	0	None	4	3	Human	7.2	pEC50	=	7.2	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	382	3	1	4	4.0	Cc1cc(N2C(=O)C3=C(CCCC3)C2=O)c(F)cc1NC(=O)c1occc1C	10.1016/j.bmcl.2020.127724
	162674997	182808	0	None	1	3	Human	7.2	pEC50	=	7.2	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	412	3	1	4	4.7	Cc1cc(N2C(=O)c3cccc(Cl)c3C2=O)c(F)cc1NC(=O)c1occc1C	10.1016/j.bmcl.2020.127724
	CHEMBL4798021	182808	0	None	1	3	Human	7.2	pEC50	=	7.2	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	412	3	1	4	4.7	Cc1cc(N2C(=O)c3cccc(Cl)c3C2=O)c(F)cc1NC(=O)c1occc1C	10.1016/j.bmcl.2020.127724
	127029301	137160	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	397	3	1	5	4.2	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3758683	137160	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	397	3	1	5	4.2	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	162645938	179000	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	400	3	1	4	4.1	Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3ccccc3C2=O)c(F)c1F	10.1016/j.bmcl.2020.127724
	CHEMBL4742005	179000	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	400	3	1	4	4.1	Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3ccccc3C2=O)c(F)c1F	10.1016/j.bmcl.2020.127724
	127025860	137203	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	2	4	3.6	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759028	137203	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	2	4	3.6	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127026140	137196	0	None	4	2	Human	7.2	pEC50	=	7.2	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	415	3	1	5	4.3	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3758967	137196	0	None	4	2	Human	7.2	pEC50	=	7.2	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	415	3	1	5	4.3	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	162648752	179372	0	None	4	3	Human	7.2	pEC50	=	7.2	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	418	3	1	4	4.2	Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3cccc(F)c3C2=O)c(F)c1F	10.1016/j.bmcl.2020.127724
	CHEMBL4746530	179372	0	None	4	3	Human	7.2	pEC50	=	7.2	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	418	3	1	4	4.2	Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3cccc(F)c3C2=O)c(F)c1F	10.1016/j.bmcl.2020.127724
	127026140	137196	0	None	4	2	Human	7.2	pEC50	=	7.2	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	415	3	1	5	4.3	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3758967	137196	0	None	4	2	Human	7.2	pEC50	=	7.2	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	415	3	1	5	4.3	Cc1scnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127026474	137243	0	None	9	2	Human	6.2	pEC50	=	6.2	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	2	4	3.6	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759376	137243	0	None	9	2	Human	6.2	pEC50	=	6.2	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	2	4	3.6	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127026474	137243	0	None	9	2	Human	6.2	pEC50	=	6.2	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	2	4	3.6	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759376	137243	0	None	9	2	Human	6.2	pEC50	=	6.2	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	2	4	3.6	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127032839	138662	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	434	3	1	3	6.0	Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1Cl	10.1016/j.bmcl.2016.03.031
	CHEMBL3787654	138662	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	434	3	1	3	6.0	Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1Cl	10.1016/j.bmcl.2016.03.031
	443586	145919	47	None	-16	3	Human	5.2	pEC50	=	5.2	Functional	Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.	ChEMBL	183	2	4	4	0.2	N[C@H](C(=O)O)c1cc(O)cc(O)c1	10.1021/jm990353c
	71668376	145919	47	None	-16	3	Human	5.2	pEC50	=	5.2	Functional	Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.	ChEMBL	183	2	4	4	0.2	N[C@H](C(=O)O)c1cc(O)cc(O)c1	10.1021/jm990353c
	CHEMBL39221	145919	47	None	-16	3	Human	5.2	pEC50	=	5.2	Functional	Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.	ChEMBL	183	2	4	4	0.2	N[C@H](C(=O)O)c1cc(O)cc(O)c1	10.1021/jm990353c
	127032839	138662	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	434	3	1	3	6.0	Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1Cl	10.1016/j.bmcl.2016.03.031
	CHEMBL3787654	138662	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	434	3	1	3	6.0	Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccc(Cl)c3C2=O)c(Cl)c1Cl	10.1016/j.bmcl.2016.03.031
	10474765	192532	0	None	-	1	Rat	7.2	pEC50	=	7.2	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	378	2	1	4	4.7	O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2ccc(F)cc21	10.1016/j.bmcl.2009.01.108
	CHEMBL522875	192532	0	None	-	1	Rat	7.2	pEC50	=	7.2	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	378	2	1	4	4.7	O=C(Nc1ncc(C(F)(F)F)o1)C1c2ccccc2Oc2ccc(F)cc21	10.1016/j.bmcl.2009.01.108
	127025847	137201	0	None	1	2	Human	6.2	pEC50	=	6.2	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	1	5	3.3	Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3758986	137201	0	None	1	2	Human	6.2	pEC50	=	6.2	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	1	5	3.3	Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127025847	137201	0	None	1	2	Human	6.2	pEC50	=	6.2	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	1	5	3.3	Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3758986	137201	0	None	1	2	Human	6.2	pEC50	=	6.2	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	398	3	1	5	3.3	Cn1ccnc1C(=O)Nc1ccc(N2C(=O)c3ccc(F)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127034512	138605	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	394	3	1	3	5.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2(C)C)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3786977	138605	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	394	3	1	3	5.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2(C)C)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127034512	138605	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	394	3	1	3	5.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2(C)C)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3786977	138605	0	None	-	1	Human	5.2	pEC50	=	5.2	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	394	3	1	3	5.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2(C)C)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127047993	139121	1	None	3	2	Human	6.2	pEC50	=	6.2	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	333	2	1	5	3.9	N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	CHEMBL3797793	139121	1	None	3	2	Human	6.2	pEC50	=	6.2	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	333	2	1	5	3.9	N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	127047993	139121	1	None	3	2	Human	6.1	pEC50	=	6.1	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	333	2	1	5	3.9	N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	CHEMBL3797793	139121	1	None	3	2	Human	6.1	pEC50	=	6.1	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	333	2	1	5	3.9	N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	1310	2286	108	None	-794	17	Rat	5.1	pEC50	=	5.1	Functional	Activity at rat mGluR1 by measuring intracellular calcium concentration in CHO cellsActivity at rat mGluR1 by measuring intracellular calcium concentration in CHO cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmcl.2005.09.014
	1369	2286	108	None	-794	17	Rat	5.1	pEC50	=	5.1	Functional	Activity at rat mGluR1 by measuring intracellular calcium concentration in CHO cellsActivity at rat mGluR1 by measuring intracellular calcium concentration in CHO cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmcl.2005.09.014
	33032	2286	108	None	-794	17	Rat	5.1	pEC50	=	5.1	Functional	Activity at rat mGluR1 by measuring intracellular calcium concentration in CHO cellsActivity at rat mGluR1 by measuring intracellular calcium concentration in CHO cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmcl.2005.09.014
	44272391	2286	108	None	-794	17	Rat	5.1	pEC50	=	5.1	Functional	Activity at rat mGluR1 by measuring intracellular calcium concentration in CHO cellsActivity at rat mGluR1 by measuring intracellular calcium concentration in CHO cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmcl.2005.09.014
	88747398	2286	108	None	-794	17	Rat	5.1	pEC50	=	5.1	Functional	Activity at rat mGluR1 by measuring intracellular calcium concentration in CHO cellsActivity at rat mGluR1 by measuring intracellular calcium concentration in CHO cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmcl.2005.09.014
	CHEMBL575060	2286	108	None	-794	17	Rat	5.1	pEC50	=	5.1	Functional	Activity at rat mGluR1 by measuring intracellular calcium concentration in CHO cellsActivity at rat mGluR1 by measuring intracellular calcium concentration in CHO cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmcl.2005.09.014
	DB00142	2286	108	None	-794	17	Rat	5.1	pEC50	=	5.1	Functional	Activity at rat mGluR1 by measuring intracellular calcium concentration in CHO cellsActivity at rat mGluR1 by measuring intracellular calcium concentration in CHO cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmcl.2005.09.014
	1310	2286	108	None	-794	17	Rat	5.1	pEC50	=	5.1	Functional	Activity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentrationActivity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentration	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmc.2007.02.040
	1369	2286	108	None	-794	17	Rat	5.1	pEC50	=	5.1	Functional	Activity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentrationActivity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentration	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmc.2007.02.040
	33032	2286	108	None	-794	17	Rat	5.1	pEC50	=	5.1	Functional	Activity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentrationActivity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentration	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmc.2007.02.040
	44272391	2286	108	None	-794	17	Rat	5.1	pEC50	=	5.1	Functional	Activity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentrationActivity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentration	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmc.2007.02.040
	88747398	2286	108	None	-794	17	Rat	5.1	pEC50	=	5.1	Functional	Activity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentrationActivity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentration	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmc.2007.02.040
	CHEMBL575060	2286	108	None	-794	17	Rat	5.1	pEC50	=	5.1	Functional	Activity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentrationActivity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentration	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmc.2007.02.040
	DB00142	2286	108	None	-794	17	Rat	5.1	pEC50	=	5.1	Functional	Activity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentrationActivity at rat recombinant mGluR1 expressed in CHO cells assessed as intracellular calcium concentration	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmc.2007.02.040
	162648102	179324	0	None	1	5	Human	7.1	pEC50	=	7.1	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	378	3	1	4	4.1	Cc1cc(NC(=O)c2occc2C)c(F)cc1N1C(=O)c2ccccc2C1=O	10.1016/j.bmcl.2020.127724
	CHEMBL4745982	179324	0	None	1	5	Human	7.1	pEC50	=	7.1	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	378	3	1	4	4.1	Cc1cc(NC(=O)c2occc2C)c(F)cc1N1C(=O)c2ccccc2C1=O	10.1016/j.bmcl.2020.127724
	122196116	123731	0	None	5	2	Human	6.1	pEC50	=	6.1	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	362	3	1	6	2.7	Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(C)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634438	123731	0	None	5	2	Human	6.1	pEC50	=	6.1	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	362	3	1	6	2.7	Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(C)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	162661457	180852	0	None	1	3	Human	7.1	pEC50	=	7.1	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	396	3	1	4	4.2	Cc1cc(N2C(=O)c3cccc(F)c3C2=O)c(F)cc1NC(=O)c1occc1C	10.1016/j.bmcl.2020.127724
	CHEMBL4764083	180852	0	None	1	3	Human	7.1	pEC50	=	7.1	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	396	3	1	4	4.2	Cc1cc(N2C(=O)c3cccc(F)c3C2=O)c(F)cc1NC(=O)c1occc1C	10.1016/j.bmcl.2020.127724
	127033961	138436	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	380	3	1	3	4.7	Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785252	138436	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	380	3	1	3	4.7	Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	162674566	182700	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	382	3	1	4	3.9	Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3ccccc3C2=O)cc1F	10.1016/j.bmcl.2020.127724
	CHEMBL4796783	182700	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	382	3	1	4	3.9	Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3ccccc3C2=O)cc1F	10.1016/j.bmcl.2020.127724
	127033961	138436	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	380	3	1	3	4.7	Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785252	138436	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	380	3	1	3	4.7	Cc1ccoc1C(=O)Nc1ccc(N2CCc3ccccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	122193176	123413	0	None	1	3	Human	7.1	pEC50	=	7.1	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	414	3	1	4	4.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628112	123413	0	None	1	3	Human	7.1	pEC50	=	7.1	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	414	3	1	4	4.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	122193176	123413	0	None	1	3	Human	7.1	pEC50	=	7.1	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	414	3	1	4	4.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628112	123413	0	None	1	3	Human	7.1	pEC50	=	7.1	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	414	3	1	4	4.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	44450470	95640	1	None	1	2	Rat	4.1	pEC50	=	4.1	Functional	Activity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulationActivity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulation	ChEMBL	160	2	3	4	-0.9	N[C@H](C(=O)O)[C@H]1CC(O)=NO1	10.1021/jm701394a
	CHEMBL260122	95640	1	None	1	2	Rat	4.1	pEC50	=	4.1	Functional	Activity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulationActivity at rat cloned mGluR1a expressed in CHO cells assessed as effect on cAMP accumulation	ChEMBL	160	2	3	4	-0.9	N[C@H](C(=O)O)[C@H]1CC(O)=NO1	10.1021/jm701394a
	127026472	137220	0	None	3	2	Human	6.1	pEC50	=	6.1	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	414	3	2	4	4.1	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759211	137220	0	None	3	2	Human	6.1	pEC50	=	6.1	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	414	3	2	4	4.1	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127026472	137220	0	None	3	2	Human	6.1	pEC50	=	6.1	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	414	3	2	4	4.1	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	CHEMBL3759211	137220	0	None	3	2	Human	6.1	pEC50	=	6.1	Functional	Positive allosteric modulation of human mGlu1 receptor by cell based calcium mobilizationPositive allosteric modulation of human mGlu1 receptor by cell based calcium mobilization	ChEMBL	414	3	2	4	4.1	Cc1cn[nH]c1C(=O)Nc1ccc(N2C(=O)c3ccc(Cl)cc3C2=O)c(Cl)c1	10.1016/j.bmcl.2015.12.104
	127031845	138524	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	384	3	1	3	4.8	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(F)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3786160	138524	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	384	3	1	3	4.8	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(F)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	122196099	123715	0	None	10	2	Human	7.1	pEC50	=	7.1	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	360	3	1	4	3.9	Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O	10.1016/j.bmcl.2015.10.013
	CHEMBL3634422	123715	0	None	10	2	Human	7.1	pEC50	=	7.1	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	360	3	1	4	3.9	Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O	10.1016/j.bmcl.2015.10.013
	127031845	138524	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	384	3	1	3	4.8	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(F)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3786160	138524	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	384	3	1	3	4.8	Cc1ccoc1C(=O)Nc1ccc(N2Cc3c(F)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	9978023	187090	0	None	-	1	Rat	7.1	pEC50	=	7.1	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	396	2	1	4	4.8	O=C(Nc1nc(C(F)(F)F)co1)C1c2cc(F)ccc2Oc2ccc(F)cc21	10.1016/j.bmcl.2009.01.108
	CHEMBL495150	187090	0	None	-	1	Rat	7.1	pEC50	=	7.1	Functional	Agonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiologyAgonist activity at rat mGlu1 receptor expressed in CHO cells assessed as reversal of glutamate-activated K+ currents by electrophysiology	ChEMBL	396	2	1	4	4.8	O=C(Nc1nc(C(F)(F)F)co1)C1c2cc(F)ccc2Oc2ccc(F)cc21	10.1016/j.bmcl.2009.01.108
	127046038	139411	0	None	4	2	Human	6.1	pEC50	=	6.1	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	350	3	1	4	5.1	CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	CHEMBL3799685	139411	0	None	4	2	Human	6.1	pEC50	=	6.1	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	350	3	1	4	5.1	CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	127046038	139411	0	None	4	2	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	350	3	1	4	5.1	CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	CHEMBL3799685	139411	0	None	4	2	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilizationPositive allosteric modulation of human mGlu1 receptor assessed as increase in glutamate-induced calcium mobilization	ChEMBL	350	3	1	4	5.1	CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	127030947	138568	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	398	5	3	4	4.4	Cc1ccoc1C(=O)Nc1ccc(NC(=O)c2ccccc2C(=O)O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3786597	138568	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	398	5	3	4	4.4	Cc1ccoc1C(=O)Nc1ccc(NC(=O)c2ccccc2C(=O)O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	104766	34	36	None	-4	14	Human	5.0	pEC50	=	5.0	Functional	Agonist activity against Metabotropic glutamate receptor 1 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulationAgonist activity against Metabotropic glutamate receptor 1 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm970207b
	1365	34	36	None	-4	14	Human	5.0	pEC50	=	5.0	Functional	Agonist activity against Metabotropic glutamate receptor 1 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulationAgonist activity against Metabotropic glutamate receptor 1 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm970207b
	CHEMBL34453	34	36	None	-4	14	Human	5.0	pEC50	=	5.0	Functional	Agonist activity against Metabotropic glutamate receptor 1 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulationAgonist activity against Metabotropic glutamate receptor 1 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm970207b
	127030947	138568	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	398	5	3	4	4.4	Cc1ccoc1C(=O)Nc1ccc(NC(=O)c2ccccc2C(=O)O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3786597	138568	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	398	5	3	4	4.4	Cc1ccoc1C(=O)Nc1ccc(NC(=O)c2ccccc2C(=O)O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	122196112	123727	0	None	52	2	Human	7.0	pEC50	=	7.0	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	361	3	1	5	3.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634434	123727	0	None	52	2	Human	7.0	pEC50	=	7.0	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	361	3	1	5	3.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	127033434	138464	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	417	3	1	4	5.2	Cc1scnc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785499	138464	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	417	3	1	4	5.2	Cc1scnc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127033434	138464	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	417	3	1	4	5.2	Cc1scnc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785499	138464	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	417	3	1	4	5.2	Cc1scnc1C(=O)Nc1ccc(N2Cc3c(Cl)cccc3C2=O)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127030048	138423	0	None	-	1	Human	5.0	pEC50	=	5.0	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	353	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccnc3C2)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785114	138423	0	None	-	1	Human	5.0	pEC50	=	5.0	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	353	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccnc3C2)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	127030048	138423	0	None	-	1	Human	5.0	pEC50	=	5.0	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	353	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccnc3C2)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	CHEMBL3785114	138423	0	None	-	1	Human	5.0	pEC50	=	5.0	Functional	Positive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 minPositive allosteric modulatory activity at human mGlu1 receptor expressed in wild type T-Rex293 cells assessed as increase in glutamate-induced calcium mobilization pre-incubated for 2.5 mins before glutamate stimulation for 1 min	ChEMBL	353	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2Cc3cccnc3C2)c(Cl)c1	10.1016/j.bmcl.2016.03.031
	52203651	123409	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	380	3	1	4	4.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628104	123409	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	380	3	1	4	4.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	52203651	123409	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	380	3	1	4	4.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628104	123409	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	380	3	1	4	4.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	122193179	123416	0	None	1	2	Human	7.0	pEC50	=	7.0	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	381	3	1	5	3.7	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628115	123416	0	None	1	2	Human	7.0	pEC50	=	7.0	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	381	3	1	5	3.7	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	122193179	123416	0	None	1	2	Human	7.0	pEC50	=	7	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	381	3	1	5	3.7	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	CHEMBL3628115	123416	0	None	1	2	Human	7.0	pEC50	=	7	Functional	Positive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisPositive allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	381	3	1	5	3.7	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccncc3C2=O)c(Cl)c1	10.1021/acs.jmedchem.5b00727
	162664872	181593	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	434	3	1	4	4.7	Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3ccc(Cl)cc3C2=O)c(F)c1F	10.1016/j.bmcl.2020.127724
	CHEMBL4782646	181593	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Positive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assayPositive allosteric modulation of human mGluR1 in presence of EC20 concentration of glutamate by calcium mobilization assay	ChEMBL	434	3	1	4	4.7	Cc1ccoc1C(=O)Nc1cc(F)c(N2C(=O)c3ccc(Cl)cc3C2=O)c(F)c1F	10.1016/j.bmcl.2020.127724
	16659643	89525	0	None	-	1	Human	9.4	pIC50	=	9.4	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	352	1	1	5	4.1	O=c1c2sc3ncc4cc[nH]c4c3c2ncn1-c1ccc(Cl)cc1	10.1021/jm070590c
	CHEMBL238077	89525	0	None	-	1	Human	9.4	pIC50	=	9.4	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	352	1	1	5	4.1	O=c1c2sc3ncc4cc[nH]c4c3c2ncn1-c1ccc(Cl)cc1	10.1021/jm070590c
	16118680	70628	0	None	-	1	Human	9.4	pIC50	=	9.4	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	355	2	0	5	4.3	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951661	70628	0	None	-	1	Human	9.4	pIC50	=	9.4	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	355	2	0	5	4.3	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	16659645	147801	0	None	-	1	Human	9.2	pIC50	=	9.2	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	332	1	1	5	3.8	Cc1ccc(-n2cnc3c(sc4ncc5cc[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	CHEMBL393705	147801	0	None	-	1	Human	9.2	pIC50	=	9.2	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	332	1	1	5	3.8	Cc1ccc(-n2cnc3c(sc4ncc5cc[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	15953801	70680	0	None	-	1	Human	9.1	pIC50	=	9.1	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	385	2	1	5	4.4	CNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951872	70680	0	None	-	1	Human	9.1	pIC50	=	9.1	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	385	2	1	5	4.4	CNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	23634171	962	1	None	-	1	Human	9.1	pIC50	=	9.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	366	3	1	6	3.7	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl	10.1016/j.bmcl.2009.04.104
	6214	962	1	None	-	1	Human	9.1	pIC50	=	9.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	366	3	1	6	3.7	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl	10.1016/j.bmcl.2009.04.104
	CHEMBL1783874	962	1	None	-	1	Human	9.1	pIC50	=	9.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	366	3	1	6	3.7	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl	10.1016/j.bmcl.2009.04.104
	57404255	72865	1	None	18	3	Rat	9.1	pIC50	=	9.1	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	302	4	1	4	3.7	COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1	10.1016/j.bmcl.2012.02.003
	CHEMBL2011870	72865	1	None	18	3	Rat	9.1	pIC50	=	9.1	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	302	4	1	4	3.7	COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1	10.1016/j.bmcl.2012.02.003
	57559287	83408	0	None	10000	2	Human	9.0	pIC50	=	9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	337	2	0	7	2.8	Cc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205921	83408	0	None	10000	2	Human	9.0	pIC50	=	9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	337	2	0	7	2.8	Cc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	23634174	83409	0	None	-	1	Human	9.0	pIC50	=	9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	357	2	0	7	3.1	CN(C)c1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	CHEMBL2205922	83409	0	None	-	1	Human	9.0	pIC50	=	9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	357	2	0	7	3.1	CN(C)c1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	23634170	83410	0	None	-	1	Human	9.0	pIC50	=	9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	401	2	0	7	3.2	CN(C)c1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	CHEMBL2205923	83410	0	None	-	1	Human	9.0	pIC50	=	9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	401	2	0	7	3.2	CN(C)c1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	11537456	207	9	None	-3	3	Human	9.0	pIC50	=	9	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	342	2	0	6	4.0	CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C	10.1021/jm0504407
	6354	207	9	None	-3	3	Human	9.0	pIC50	=	9	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	342	2	0	6	4.0	CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C	10.1021/jm0504407
	CHEMBL225032	207	9	None	-3	3	Human	9.0	pIC50	=	9	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	342	2	0	6	4.0	CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C	10.1021/jm0504407
	11559235	209	37	None	4	3	Rat	9.0	pIC50	=	9	Functional	Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells	ChEMBL	343	2	0	7	2.6	CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C	10.1016/j.bmcl.2006.06.053
	3953	209	37	None	4	3	Rat	9.0	pIC50	=	9	Functional	Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells	ChEMBL	343	2	0	7	2.6	CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C	10.1016/j.bmcl.2006.06.053
	CHEMBL386565	209	37	None	4	3	Rat	9.0	pIC50	=	9	Functional	Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells	ChEMBL	343	2	0	7	2.6	CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C	10.1016/j.bmcl.2006.06.053
	23634254	62331	0	None	-	1	Human	9.0	pIC50	=	9.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	382	4	0	6	4.3	C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783864	62331	0	None	-	1	Human	9.0	pIC50	=	9.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	382	4	0	6	4.3	C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	11313361	2103	54	None	3	2	Human	8.9	pIC50	=	8.9	Functional	Antagonist activity at human mGlu1 receptorAntagonist activity at human mGlu1 receptor	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm060950g
	1385	2103	54	None	3	2	Human	8.9	pIC50	=	8.9	Functional	Antagonist activity at human mGlu1 receptorAntagonist activity at human mGlu1 receptor	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm060950g
	CHEMBL174588	2103	54	None	3	2	Human	8.9	pIC50	=	8.9	Functional	Antagonist activity at human mGlu1 receptorAntagonist activity at human mGlu1 receptor	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm060950g
	CHEMBL254574	2103	54	None	3	2	Human	8.9	pIC50	=	8.9	Functional	Antagonist activity at human mGlu1 receptorAntagonist activity at human mGlu1 receptor	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm060950g
	16659802	1023	0	None	-	1	Human	8.9	pIC50	=	8.9	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	384	1	1	7	3.8	C[C@@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	10.1021/jm070590c
	6348	1023	0	None	-	1	Human	8.9	pIC50	=	8.9	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	384	1	1	7	3.8	C[C@@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	10.1021/jm070590c
	CHEMBL241327	1023	0	None	-	1	Human	8.9	pIC50	=	8.9	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	384	1	1	7	3.8	C[C@@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	10.1021/jm070590c
	23634169	62341	0	None	-	1	Human	8.8	pIC50	=	8.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	346	3	1	6	3.3	C#CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783875	62341	0	None	-	1	Human	8.8	pIC50	=	8.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	346	3	1	6	3.3	C#CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	44588464	174498	0	None	4	3	Mouse	8.8	pIC50	=	8.8	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	359	2	0	6	3.1	Cc1c(C2=CCN(C(=O)OC(C)(C)C)CC2)nnn1-c1ncccc1F	10.1016/j.bmc.2008.09.060
	CHEMBL456823	174498	0	None	4	3	Mouse	8.8	pIC50	=	8.8	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	359	2	0	6	3.1	Cc1c(C2=CCN(C(=O)OC(C)(C)C)CC2)nnn1-c1ncccc1F	10.1016/j.bmc.2008.09.060
	23634249	62415	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	410	3	1	6	3.8	C#CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784049	62415	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	410	3	1	6	3.8	C#CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	16660294	195702	1	None	4365	2	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	343	4	1	6	3.1	CNc1cc(-c2csc(N(C)C(=O)c3ccc(F)cc3)n2)ncn1	10.1016/j.bmcl.2009.07.097
	CHEMBL569270	195702	1	None	4365	2	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	343	4	1	6	3.1	CNc1cc(-c2csc(N(C)C(=O)c3ccc(F)cc3)n2)ncn1	10.1016/j.bmcl.2009.07.097
	23634325	62419	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	424	3	0	6	3.8	C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784053	62419	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	424	3	0	6	3.8	C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	11559235	209	37	None	-4	3	Human	8.0	pIC50	=	8	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	343	2	0	7	2.6	CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C	10.1021/jm0504407
	3953	209	37	None	-4	3	Human	8.0	pIC50	=	8	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	343	2	0	7	2.6	CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C	10.1021/jm0504407
	CHEMBL386565	209	37	None	-4	3	Human	8.0	pIC50	=	8	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	343	2	0	7	2.6	CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C	10.1021/jm0504407
	16038338	195671	0	None	-	1	Human	8.0	pIC50	=	8	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	314	3	0	5	3.0	CN(C(=O)c1ccc(F)cc1)c1nc(-c2ccncn2)cs1	10.1016/j.bmcl.2009.07.097
	CHEMBL568991	195671	0	None	-	1	Human	8.0	pIC50	=	8	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	314	3	0	5	3.0	CN(C(=O)c1ccc(F)cc1)c1nc(-c2ccncn2)cs1	10.1016/j.bmcl.2009.07.097
	16118812	70630	0	None	-	1	Human	8.0	pIC50	=	8	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	346	2	0	6	3.5	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C#N)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951663	70630	0	None	-	1	Human	8.0	pIC50	=	8	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	346	2	0	6	3.5	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C#N)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	54585406	62336	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	378	5	1	7	4.0	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783869	62336	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	378	5	1	7	4.0	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54585404	62334	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	382	4	1	6	4.6	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783867	62334	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	382	4	1	6	4.6	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54582943	62427	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	367	4	1	7	3.5	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784061	62427	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	367	4	1	7	3.5	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54584887	62418	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	376	4	0	7	3.1	C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784052	62418	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	376	4	0	7	3.1	C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	67181213	72870	0	None	-	1	Human	7.0	pIC50	=	7	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	290	3	1	3	3.9	Cc1c(-c2ccc(F)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C	10.1016/j.bmcl.2012.02.003
	CHEMBL2011875	72870	0	None	-	1	Human	7.0	pIC50	=	7	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	290	3	1	3	3.9	Cc1c(-c2ccc(F)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C	10.1016/j.bmcl.2012.02.003
	45486747	196971	0	None	-	1	Human	7.0	pIC50	=	7	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	313	3	0	4	3.6	CN(C(=O)c1cccc(F)c1)c1nc(-c2ccncc2)cs1	10.1016/j.bmcl.2009.07.097
	CHEMBL579213	196971	0	None	-	1	Human	7.0	pIC50	=	7	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	313	3	0	4	3.6	CN(C(=O)c1cccc(F)c1)c1nc(-c2ccncc2)cs1	10.1016/j.bmcl.2009.07.097
	44447970	154520	0	None	-	1	Human	6.0	pIC50	=	6	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	369	4	3	4	3.2	NC(C(=O)O)(C1CC(C(=O)O)C1)C1c2ccccc2Sc2ccccc21	10.1021/jm060950g
	CHEMBL401721	154520	0	None	-	1	Human	6.0	pIC50	=	6	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	369	4	3	4	3.2	NC(C(=O)O)(C1CC(C(=O)O)C1)C1c2ccccc2Sc2ccccc21	10.1021/jm060950g
	44588462	174978	0	None	-4	2	Mouse	6.0	pIC50	=	6	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	327	2	0	6	2.7	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccncc3)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL457873	174978	0	None	-4	2	Mouse	6.0	pIC50	=	6	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	327	2	0	6	2.7	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccncc3)nn2)CC1	10.1016/j.bmc.2008.09.060
	72163585	91601	0	None	-	1	Human	6.0	pIC50	=	6	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	369	2	0	3	3.3	O=C(N1C[C@@H]2CN(c3ncccc3F)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	CHEMBL2418382	91601	0	None	-	1	Human	6.0	pIC50	=	6	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	369	2	0	3	3.3	O=C(N1C[C@@H]2CN(c3ncccc3F)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	1418	3393	48	None	-1	2	Human	5.0	pIC50	=	5	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	10.1021/jm060950g
	5311459	3393	48	None	-1	2	Human	5.0	pIC50	=	5	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	10.1021/jm060950g
	CHEMBL94990	3393	48	None	-1	2	Human	5.0	pIC50	=	5	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	10.1021/jm060950g
	91618210	124602	0	None	-501	2	Human	5.0	pIC50	=	5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	410	2	0	6	3.2	Cc1ccc(-c2ccnc3c2CCN2C(=O)CN=C(n4cnc(C5CC5)c4)C=C32)cn1	nan
	CHEMBL3644418	124602	0	None	-501	2	Human	5.0	pIC50	=	5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	410	2	0	6	3.2	Cc1ccc(-c2ccnc3c2CCN2C(=O)CN=C(n4cnc(C5CC5)c4)C=C32)cn1	nan
	11654379	141539	0	None	1	3	Human	7.0	pIC50	=	7	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	406	6	0	6	5.0	CCCCc1nc2c(sc3nccc(N(C)C)c32)c(=O)n1-c1ccc(CC)cc1	10.1021/jm0504407
	CHEMBL387976	141539	0	None	1	3	Human	7.0	pIC50	=	7	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	406	6	0	6	5.0	CCCCc1nc2c(sc3nccc(N(C)C)c32)c(=O)n1-c1ccc(CC)cc1	10.1021/jm0504407
	44431061	86325	0	None	-	1	Rat	6.0	pIC50	=	6.0	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	293	3	2	4	2.3	O=C1NN=CC2c3cc(OCc4ccccc4)ccc3NC12	10.1016/j.bmcl.2007.01.055
	CHEMBL232013	86325	0	None	-	1	Rat	6.0	pIC50	=	6.0	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	293	3	2	4	2.3	O=C1NN=CC2c3cc(OCc4ccccc4)ccc3NC12	10.1016/j.bmcl.2007.01.055
	67425408	87089	0	None	-12	2	Human	6.0	pIC50	=	6.0	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	439	5	1	6	5.3	C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C(F)F)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2334975	87089	0	None	-12	2	Human	6.0	pIC50	=	6.0	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	439	5	1	6	5.3	C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C(F)F)n1	10.1016/j.bmcl.2013.01.009
	54582494	62338	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	396	5	1	7	4.1	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783871	62338	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	396	5	1	7	4.1	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	563298	91921	20	None	-	1	Rat	7.0	pIC50	=	7.0	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	292	3	2	2	3.0	O=C1NCCc2c1[nH]c1ccc(OCc3ccccc3)cc21	10.1016/j.bmcl.2007.01.055
	CHEMBL243043	91921	20	None	-	1	Rat	7.0	pIC50	=	7.0	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	292	3	2	2	3.0	O=C1NCCc2c1[nH]c1ccc(OCc3ccccc3)cc21	10.1016/j.bmcl.2007.01.055
	122196105	123721	0	None	22	2	Human	7.0	pIC50	=	7.0	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	448	3	1	4	5.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(C(F)(F)F)c1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634428	123721	0	None	22	2	Human	7.0	pIC50	=	7.0	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	448	3	1	4	5.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(C(F)(F)F)c1	10.1016/j.bmcl.2015.10.013
	44431049	141811	0	None	-	1	Rat	6.0	pIC50	=	6.0	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	305	2	3	2	2.7	O=C(Nc1ccccc1)c1ccc2[nH]c3c(c2c1)CCNC3=O	10.1016/j.bmcl.2007.01.055
	CHEMBL388668	141811	0	None	-	1	Rat	6.0	pIC50	=	6.0	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	305	2	3	2	2.7	O=C(Nc1ccccc1)c1ccc2[nH]c3c(c2c1)CCNC3=O	10.1016/j.bmcl.2007.01.055
	24777698	94315	1	None	-	1	Rat	5.0	pIC50	=	5.0	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	307	2	0	4	2.9	O=C1CCCc2nc(N3CCN(c4ccccc4)CC3)ccc21	10.1021/jm0611298
	CHEMBL253145	94315	1	None	-	1	Rat	5.0	pIC50	=	5.0	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	307	2	0	4	2.9	O=C1CCCc2nc(N3CCN(c4ccccc4)CC3)ccc21	10.1021/jm0611298
	49788806	17937	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology	ChEMBL	531	18	5	5	3.9	NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)CC12CC3CC(CC(C3)C1)C2	10.1021/jm100886h
	CHEMBL1269127	17937	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology	ChEMBL	531	18	5	5	3.9	NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)CC12CC3CC(CC(C3)C1)C2	10.1021/jm100886h
	89979810	132583	0	None	-22	2	Human	6.0	pIC50	=	6.0	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	419	4	0	7	2.9	COCCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4nccs4)C3=C2)cn1	nan
	CHEMBL3702444	132583	0	None	-22	2	Human	6.0	pIC50	=	6.0	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	419	4	0	7	2.9	COCCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4nccs4)C3=C2)cn1	nan
	54583942	62414	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	391	3	1	9	2.2	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784048	62414	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	391	3	1	9	2.2	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	3115037	193515	7	None	-	1	Rat	5.0	pIC50	=	5.0	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	282	4	0	3	3.8	CC(CC(=O)c1ccc2c(c1)OCCO2)c1ccccc1	10.1016/j.bmc.2009.05.072
	CHEMBL550523	193515	7	None	-	1	Rat	5.0	pIC50	=	5.0	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	282	4	0	3	3.8	CC(CC(=O)c1ccc2c(c1)OCCO2)c1ccccc1	10.1016/j.bmc.2009.05.072
	118735959	118405	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	363	4	2	5	3.2	N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1ccn[nH]1)C2	10.1016/j.ejmech.2015.04.060
	CHEMBL3422875	118405	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	363	4	2	5	3.2	N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1ccn[nH]1)C2	10.1016/j.ejmech.2015.04.060
	49788655	18131	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology	ChEMBL	423	17	5	5	1.7	NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)C1CC1	10.1021/jm100886h
	CHEMBL1270718	18131	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology	ChEMBL	423	17	5	5	1.7	NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)C1CC1	10.1021/jm100886h
	46886138	8148	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	343	1	1	7	2.9	Cc1nc(N)c2c(n1)sc1c(=O)n(-c3ccc(Cl)cc3)cnc12	10.1016/j.bmcl.2010.03.004
	CHEMBL1092277	8148	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	343	1	1	7	2.9	Cc1nc(N)c2c(n1)sc1c(=O)n(-c3ccc(Cl)cc3)cnc12	10.1016/j.bmcl.2010.03.004
	54584442	62326	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	348	4	1	6	3.9	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783859	62326	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	348	4	1	6	3.9	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	44588426	188613	0	None	5	3	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	340	2	0	5	3.6	Cc1ccccc1-n1cc(C2=CCN(C(=O)OC(C)(C)C)CC2)nn1	10.1016/j.bmc.2008.09.060
	CHEMBL511352	188613	0	None	5	3	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	340	2	0	5	3.6	Cc1ccccc1-n1cc(C2=CCN(C(=O)OC(C)(C)C)CC2)nn1	10.1016/j.bmc.2008.09.060
	45484929	195582	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	318	2	0	5	3.4	Cc1c(-c2ccc3c(c2)CC(C)(C)C3=O)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	CHEMBL568451	195582	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	318	2	0	5	3.4	Cc1c(-c2ccc3c(c2)CC(C)(C)C3=O)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	70691553	72866	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	302	4	1	4	3.7	COc1ccc(-c2nsc(NC(=O)[C@H]3C[C@@H]3C)c2C)cc1	10.1016/j.bmcl.2012.02.003
	CHEMBL2011871	72866	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	302	4	1	4	3.7	COc1ccc(-c2nsc(NC(=O)[C@H]3C[C@@H]3C)c2C)cc1	10.1016/j.bmcl.2012.02.003
	24777443	154405	0	None	-	1	Rat	7.0	pIC50	=	7.0	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	375	2	0	4	4.5	CC1(C)CC(=O)c2cc(C#N)c(N3CC=C(c4ccc(F)cc4)CC3)nc2C1	10.1021/jm0611298
	CHEMBL401096	154405	0	None	-	1	Rat	7.0	pIC50	=	7.0	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	375	2	0	4	4.5	CC1(C)CC(=O)c2cc(C#N)c(N3CC=C(c4ccc(F)cc4)CC3)nc2C1	10.1021/jm0611298
	44442432	154036	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	370	2	0	5	4.2	Cc1nc2c(cnn2-c2ccc(Cl)cc2)c(=O)n1-c1ccc(Cl)cc1	10.1016/j.bmcl.2007.05.028
	CHEMBL399127	154036	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	370	2	0	5	4.2	Cc1nc2c(cnn2-c2ccc(Cl)cc2)c(=O)n1-c1ccc(Cl)cc1	10.1016/j.bmcl.2007.05.028
	89979958	124580	0	None	-218	2	Human	6.0	pIC50	=	6.0	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	376	3	0	5	3.2	CO[C@@H](C)c1cn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)cn1	nan
	CHEMBL3644396	124580	0	None	-218	2	Human	6.0	pIC50	=	6.0	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	376	3	0	5	3.2	CO[C@@H](C)c1cn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)cn1	nan
	91618214	124616	0	None	-64	2	Human	6.0	pIC50	=	6.0	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	410	2	0	6	3.2	Cc1cnc(-c2cccc3c2CCN2C(=O)CN=C(n4cnc(C5CC5)c4)C=C32)cn1	nan
	CHEMBL3644432	124616	0	None	-64	2	Human	6.0	pIC50	=	6.0	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	410	2	0	6	3.2	Cc1cnc(-c2cccc3c2CCN2C(=O)CN=C(n4cnc(C5CC5)c4)C=C32)cn1	nan
	78320481	113840	3	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	318	2	0	4	4.4	Cc1ccc(-n2cnc3c(-c4ccccc4)csc3c2=O)cc1	10.1016/j.ejmech.2014.08.027
	CHEMBL3330808	113840	3	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	318	2	0	4	4.4	Cc1ccc(-n2cnc3c(-c4ccccc4)csc3c2=O)cc1	10.1016/j.ejmech.2014.08.027
	78320481	113840	3	None	-	1	Human	7.0	pIC50	=	7.0	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	318	2	0	4	4.4	Cc1ccc(-n2cnc3c(-c4ccccc4)csc3c2=O)cc1	nan
	CHEMBL3330808	113840	3	None	-	1	Human	7.0	pIC50	=	7.0	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	318	2	0	4	4.4	Cc1ccc(-n2cnc3c(-c4ccccc4)csc3c2=O)cc1	nan
	11682046	84730	0	None	1	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	362	3	0	6	3.8	CCc1ccc(-n2cnc3c(sc4nccc(N5CCC5)c43)c2=O)cc1	10.1021/jm0504407
	CHEMBL225126	84730	0	None	1	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	362	3	0	6	3.8	CCc1ccc(-n2cnc3c(sc4nccc(N5CCC5)c43)c2=O)cc1	10.1021/jm0504407
	71682959	90617	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	340	2	0	4	2.7	C[C@@H]1CN(c2cnccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397374	90617	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	340	2	0	4	2.7	C[C@@H]1CN(c2cnccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	72163835	91589	0	None	-	1	Human	4.9	pIC50	=	4.9	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	326	1	0	3	2.2	CC1(C)[C@H]2CN(C(=O)N3C[C@@H]4CN(c5ccccn5)C[C@@H]4C3)C[C@H]21	10.1016/j.bmcl.2013.07.029
	CHEMBL2418357	91589	0	None	-	1	Human	4.9	pIC50	=	4.9	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	326	1	0	3	2.2	CC1(C)[C@H]2CN(C(=O)N3C[C@@H]4CN(c5ccccn5)C[C@@H]4C3)C[C@H]21	10.1016/j.bmcl.2013.07.029
	57397023	70638	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	338	3	0	6	3.6	COc1cccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)c1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951671	70638	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	338	3	0	6	3.6	COc1cccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)c1	10.1016/j.bmcl.2011.12.131
	71682959	90617	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	340	2	0	4	2.7	C[C@@H]1CN(c2cnccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397374	90617	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	340	2	0	4	2.7	C[C@@H]1CN(c2cnccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	72163835	91589	0	None	-	1	Human	4.9	pIC50	=	4.9	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	326	1	0	3	2.2	CC1(C)[C@H]2CN(C(=O)N3C[C@@H]4CN(c5ccccn5)C[C@@H]4C3)C[C@H]21	10.1016/j.bmcl.2013.07.029
	CHEMBL2418357	91589	0	None	-	1	Human	4.9	pIC50	=	4.9	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	326	1	0	3	2.2	CC1(C)[C@H]2CN(C(=O)N3C[C@@H]4CN(c5ccccn5)C[C@@H]4C3)C[C@H]21	10.1016/j.bmcl.2013.07.029
	89980424	124589	0	None	-169	2	Human	5.9	pIC50	=	5.9	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	374	2	1	5	2.4	O=C1CN=C(n2cnc(C3(O)CC3)c2)C=C2c3cccc(C4CC4)c3CCN12	nan
	CHEMBL3644405	124589	0	None	-169	2	Human	5.9	pIC50	=	5.9	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	374	2	1	5	2.4	O=C1CN=C(n2cnc(C3(O)CC3)c2)C=C2c3cccc(C4CC4)c3CCN12	nan
	89980085	132599	0	None	-117	2	Human	4.9	pIC50	=	4.9	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	414	2	0	6	3.0	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cnc(F)nc4)c3CCN12	nan
	CHEMBL3702462	132599	0	None	-117	2	Human	4.9	pIC50	=	4.9	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	414	2	0	6	3.0	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cnc(F)nc4)c3CCN12	nan
	57881707	83401	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	383	6	2	9	2.2	COc1ccc(-n2cnc3c(sc4ncnc(NCCCO)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205913	83401	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	383	6	2	9	2.2	COc1ccc(-n2cnc3c(sc4ncnc(NCCCO)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	16659805	148080	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	384	1	1	7	3.8	C[C@H]1COc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c2N1	10.1021/jm070590c
	CHEMBL393923	148080	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	384	1	1	7	3.8	C[C@H]1COc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c2N1	10.1021/jm070590c
	16118537	964	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	363	4	1	6	4.2	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1	10.1016/j.bmcl.2011.12.131
	6357	964	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	363	4	1	6	4.2	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951683	964	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	363	4	1	6	4.2	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1	10.1016/j.bmcl.2011.12.131
	16118817	70698	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	348	3	1	6	3.9	Cc1ccc(-n2ccc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951890	70698	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	348	3	1	6	3.9	Cc1ccc(-n2ccc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	44588463	172737	0	None	-4	3	Mouse	7.9	pIC50	=	7.9	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	345	2	0	6	2.8	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ncccc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL452618	172737	0	None	-4	3	Mouse	7.9	pIC50	=	7.9	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	345	2	0	6	2.8	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ncccc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	54582002	62421	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	363	4	1	7	3.7	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784055	62421	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	363	4	1	7	3.7	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54585850	62416	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	380	4	1	7	3.2	C#CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784050	62416	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	380	4	1	7	3.2	C#CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	122196123	123738	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	364	3	1	4	3.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1F	10.1016/j.bmcl.2015.10.013
	CHEMBL3634445	123738	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	364	3	1	4	3.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1F	10.1016/j.bmcl.2015.10.013
	54580485	62328	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	412	4	1	6	4.4	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783861	62328	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	412	4	1	6	4.4	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	44588429	176259	0	None	1	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	342	3	0	4	3.5	CC(C)(C)CC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL461035	176259	0	None	1	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	342	3	0	4	3.5	CC(C)(C)CC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	44431044	88045	0	None	-	1	Rat	6.9	pIC50	=	6.9	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	327	2	2	2	3.0	CC(N(C)C(=O)c1ccc2[nH]c3c(c2c1)CCNC3=O)C(C)(C)C	10.1016/j.bmcl.2007.01.055
	CHEMBL234960	88045	0	None	-	1	Rat	6.9	pIC50	=	6.9	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	327	2	2	2	3.0	CC(N(C)C(=O)c1ccc2[nH]c3c(c2c1)CCNC3=O)C(C)(C)C	10.1016/j.bmcl.2007.01.055
	73335640	132560	0	None	-54	2	Human	5.9	pIC50	=	5.9	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	373	2	0	6	2.8	CCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4ncco4)C3=C2)cn1	nan
	CHEMBL3702422	132560	0	None	-54	2	Human	5.9	pIC50	=	5.9	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	373	2	0	6	2.8	CCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4ncco4)C3=C2)cn1	nan
	10523805	28835	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells	ChEMBL	380	5	2	6	1.9	COC(=O)[C@H](Cc1ccccc1)NC(=O)C12CC1/C(=N\O)c1ccccc1O2	10.1021/jm0009944
	CHEMBL138082	28835	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells	ChEMBL	380	5	2	6	1.9	COC(=O)[C@H](Cc1ccccc1)NC(=O)C12CC1/C(=N\O)c1ccccc1O2	10.1021/jm0009944
	44445058	94228	0	None	-	1	Rat	4.9	pIC50	=	4.9	Functional	Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay	ChEMBL	409	4	1	5	5.3	CC1(C)CC(=O)c2cc([N+](=O)[O-])c(NC3CC=C(c4ccc(F)cc4)CC3)nc2C1	10.1021/jm0611298
	CHEMBL252543	94228	0	None	-	1	Rat	4.9	pIC50	=	4.9	Functional	Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay	ChEMBL	409	4	1	5	5.3	CC1(C)CC(=O)c2cc([N+](=O)[O-])c(NC3CC=C(c4ccc(F)cc4)CC3)nc2C1	10.1021/jm0611298
	11537814	84770	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	362	2	1	7	2.9	CN(C)c1ccnc2sc3c(=O)n(-c4ccc5cn[nH]c5c4)cnc3c12	10.1021/jm0504407
	CHEMBL225438	84770	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	362	2	1	7	2.9	CN(C)c1ccnc2sc3c(=O)n(-c4ccc5cn[nH]c5c4)cnc3c12	10.1021/jm0504407
	118735953	118401	0	None	-	1	Human	4.9	pIC50	=	4.9	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	453	4	2	5	4.6	CC(C)c1cc(C(=O)N2CCc3c(sc(NC(=O)c4ccc(Cl)cc4)c3C#N)C2)[nH]n1	10.1016/j.ejmech.2015.04.060
	CHEMBL3422869	118401	0	None	-	1	Human	4.9	pIC50	=	4.9	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	453	4	2	5	4.6	CC(C)c1cc(C(=O)N2CCc3c(sc(NC(=O)c4ccc(Cl)cc4)c3C#N)C2)[nH]n1	10.1016/j.ejmech.2015.04.060
	122196103	123719	0	None	53	2	Human	6.9	pIC50	=	6.9	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	414	3	1	4	4.7	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(C(F)(F)F)c1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634426	123719	0	None	53	2	Human	6.9	pIC50	=	6.9	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	414	3	1	4	4.7	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(C(F)(F)F)c1	10.1016/j.bmcl.2015.10.013
	57403924	70648	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	367	5	2	7	3.0	COc1ccc(-n2ccc3c(sc4nccc(NCCO)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951684	70648	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	367	5	2	7	3.0	COc1ccc(-n2ccc3c(sc4nccc(NCCO)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	118735967	118410	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	392	4	1	5	4.0	N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1cnccc1F)C2	10.1016/j.ejmech.2015.04.060
	CHEMBL3422883	118410	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	392	4	1	5	4.0	N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1cnccc1F)C2	10.1016/j.ejmech.2015.04.060
	23655076	93497	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	415	3	1	7	2.2	Cc1nc2c(cnn2-c2cccc(S(N)(=O)=O)c2)c(=O)n1-c1ccc(Cl)cc1	10.1016/j.bmcl.2007.05.028
	CHEMBL248233	93497	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	415	3	1	7	2.2	Cc1nc2c(cnn2-c2cccc(S(N)(=O)=O)c2)c(=O)n1-c1ccc(Cl)cc1	10.1016/j.bmcl.2007.05.028
	78320803	113843	3	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	330	3	0	4	4.8	C=Cc1ccc(-n2cnc3c(-c4ccccc4)csc3c2=O)cc1	10.1016/j.ejmech.2014.08.027
	CHEMBL3330813	113843	3	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	330	3	0	4	4.8	C=Cc1ccc(-n2cnc3c(-c4ccccc4)csc3c2=O)cc1	10.1016/j.ejmech.2014.08.027
	54580948	62435	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	363	4	1	8	2.4	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784069	62435	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	363	4	1	8	2.4	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	11515957	84385	0	None	1	3	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	356	2	0	6	4.4	CN(C)c1ccnc2sc3c(=O)n(C4CCCCCCC4)cnc3c12	10.1021/jm0504407
	CHEMBL223399	84385	0	None	1	3	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	356	2	0	6	4.4	CN(C)c1ccnc2sc3c(=O)n(C4CCCCCCC4)cnc3c12	10.1021/jm0504407
	11515679	84678	0	None	1	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	342	2	0	6	3.8	CC1CCCCC1n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1021/jm0504407
	CHEMBL224672	84678	0	None	1	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	342	2	0	6	3.8	CC1CCCCC1n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1021/jm0504407
	45486748	195429	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	313	3	0	4	3.6	CN(C(=O)c1ccccc1F)c1nc(-c2ccncc2)cs1	10.1016/j.bmcl.2009.07.097
	CHEMBL567667	195429	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	313	3	0	4	3.6	CN(C(=O)c1ccccc1F)c1nc(-c2ccncc2)cs1	10.1016/j.bmcl.2009.07.097
	24777318	94316	0	None	-	1	Rat	6.9	pIC50	=	6.9	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	360	2	0	5	3.4	CC1(C)CC(=O)c2cc(C#N)c(N3CCN(c4ccccc4)CC3)nc2C1	10.1021/jm0611298
	CHEMBL253146	94316	0	None	-	1	Rat	6.9	pIC50	=	6.9	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	360	2	0	5	3.4	CC1(C)CC(=O)c2cc(C#N)c(N3CCN(c4ccccc4)CC3)nc2C1	10.1021/jm0611298
	73335920	124558	0	None	-181	2	Human	5.9	pIC50	=	5.9	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	385	2	0	6	3.1	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4ncco4)c3CCN12	nan
	CHEMBL3644372	124558	0	None	-181	2	Human	5.9	pIC50	=	5.9	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	385	2	0	6	3.1	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4ncco4)c3CCN12	nan
	73335035	132504	0	None	-28	2	Human	5.9	pIC50	=	5.9	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	392	6	0	5	2.9	COCCOc1cccc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)c1	nan
	CHEMBL3702366	132504	0	None	-28	2	Human	5.9	pIC50	=	5.9	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	392	6	0	5	2.9	COCCOc1cccc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)c1	nan
	86711359	132521	0	None	-5	2	Human	5.9	pIC50	=	5.9	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	418	1	0	4	2.3	Cn1ccc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)n1	nan
	CHEMBL3702383	132521	0	None	-5	2	Human	5.9	pIC50	=	5.9	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	418	1	0	4	2.3	Cn1ccc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)n1	nan
	71561287	87088	0	None	-25	2	Human	5.9	pIC50	=	5.9	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	421	5	1	6	4.8	C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(CF)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2334974	87088	0	None	-25	2	Human	5.9	pIC50	=	5.9	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	421	5	1	6	4.8	C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(CF)n1	10.1016/j.bmcl.2013.01.009
	24777816	154306	0	None	-	1	Rat	4.9	pIC50	=	4.9	Functional	Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay	ChEMBL	326	3	2	6	2.8	CC1(C)CC(=O)c2cc(-c3nn[nH]n3)c(NC3CCCC3)nc2C1	10.1021/jm0611298
	CHEMBL400505	154306	0	None	-	1	Rat	4.9	pIC50	=	4.9	Functional	Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay	ChEMBL	326	3	2	6	2.8	CC1(C)CC(=O)c2cc(-c3nn[nH]n3)c(NC3CCCC3)nc2C1	10.1021/jm0611298
	71682961	90618	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	340	2	0	4	2.7	C[C@@H]1CN(c2ccncn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397376	90618	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	340	2	0	4	2.7	C[C@@H]1CN(c2ccncn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	57400362	70650	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	381	5	2	7	3.4	COc1ccc(-n2ccc3c(sc4nccc(NC[C@@H](C)O)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951686	70650	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	381	5	2	7	3.4	COc1ccc(-n2ccc3c(sc4nccc(NC[C@@H](C)O)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	71682961	90618	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	340	2	0	4	2.7	C[C@@H]1CN(c2ccncn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397376	90618	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	340	2	0	4	2.7	C[C@@H]1CN(c2ccncn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	87550873	121692	0	None	-354	2	Rat	5.9	pIC50	=	5.9	Functional	Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis	ChEMBL	353	2	0	4	4.2	O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2cccc(Cl)c2)CC1	10.1016/j.bmc.2015.05.008
	CHEMBL3597598	121692	0	None	-354	2	Rat	5.9	pIC50	=	5.9	Functional	Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis	ChEMBL	353	2	0	4	4.2	O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2cccc(Cl)c2)CC1	10.1016/j.bmc.2015.05.008
	78324865	113832	3	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	304	2	0	4	4.1	O=c1c2scc(-c3ccccc3)c2ncn1-c1ccccc1	10.1016/j.ejmech.2014.08.027
	CHEMBL3330800	113832	3	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	304	2	0	4	4.1	O=c1c2scc(-c3ccccc3)c2ncn1-c1ccccc1	10.1016/j.ejmech.2014.08.027
	54582006	62440	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	377	3	1	9	2.2	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784074	62440	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	377	3	1	9	2.2	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	136244237	72875	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	288	3	2	4	3.4	Cc1c(-c2ccc(O)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C	10.1016/j.bmcl.2012.02.003
	CHEMBL2011880	72875	0	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	288	3	2	4	3.4	Cc1c(-c2ccc(O)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C	10.1016/j.bmcl.2012.02.003
	71683128	90605	1	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	364	2	0	4	3.2	C[C@@H]1CN(c2cnccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397345	90605	1	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	364	2	0	4	3.2	C[C@@H]1CN(c2cnccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	11681681	84584	0	None	1	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	342	3	0	6	3.7	CN(C)c1ccnc2sc3c(=O)n(CC4CCCCC4)cnc3c12	10.1021/jm0504407
	CHEMBL223868	84584	0	None	1	2	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	342	3	0	6	3.7	CN(C)c1ccnc2sc3c(=O)n(CC4CCCCC4)cnc3c12	10.1021/jm0504407
	57559648	83412	0	None	707	2	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	407	3	0	8	3.4	CN(C)c1ncnc2sc3c(=O)n(-c4ccc(OC(F)(F)F)cc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	CHEMBL2205925	83412	0	None	707	2	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	407	3	0	8	3.4	CN(C)c1ncnc2sc3c(=O)n(-c4ccc(OC(F)(F)F)cc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	16118813	70634	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	369	3	0	6	3.8	COc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)c(F)c1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951667	70634	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	369	3	0	6	3.8	COc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)c(F)c1	10.1016/j.bmcl.2011.12.131
	54584888	62423	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	427	4	1	7	4.1	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784057	62423	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	427	4	1	7	4.1	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	11493897	84639	0	None	1	3	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	342	2	0	6	3.8	CC1CCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)CC1	10.1021/jm0504407
	CHEMBL224315	84639	0	None	1	3	Human	6.9	pIC50	=	6.9	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	342	2	0	6	3.8	CC1CCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)CC1	10.1021/jm0504407
	75238115	123421	4	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Negative allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisNegative allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	369	3	1	4	3.1	CC1(C)C2C(=O)N(c3ccc(NC(=O)c4ccccn4)cc3Cl)C(=O)C21	10.1021/acs.jmedchem.5b00727
	CHEMBL3628281	123421	4	None	-	1	Human	6.9	pIC50	=	6.9	Functional	Negative allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysisNegative allosteric modulation of human mGlu1 receptor in HEK293 cells assessed as potentiation of glutamate-induced calcium mobiliztion by Fluo-4AM dye based fluorescence analysis	ChEMBL	369	3	1	4	3.1	CC1(C)C2C(=O)N(c3ccc(NC(=O)c4ccccn4)cc3Cl)C(=O)C21	10.1021/acs.jmedchem.5b00727
	86711355	132520	0	None	-9	2	Human	5.9	pIC50	=	5.9	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	444	2	0	3	3.5	COc1cccc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)c1	nan
	CHEMBL3702382	132520	0	None	-9	2	Human	5.9	pIC50	=	5.9	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	444	2	0	3	3.5	COc1cccc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)c1	nan
	73335238	132522	0	None	-109	2	Human	5.9	pIC50	=	5.9	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	445	2	0	4	2.9	COc1cc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)ccn1	nan
	CHEMBL3702384	132522	0	None	-109	2	Human	5.9	pIC50	=	5.9	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	445	2	0	4	2.9	COc1cc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)ccn1	nan
	73335547	132553	0	None	-1	2	Human	5.9	pIC50	=	5.9	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	432	0	0	4	2.8	Cc1cn(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)c(C)n1	nan
	CHEMBL3702415	132553	0	None	-1	2	Human	5.9	pIC50	=	5.9	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	432	0	0	4	2.8	Cc1cn(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)c(C)n1	nan
	10714791	167734	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells	ChEMBL	380	5	2	6	1.9	COC(=O)[C@@H](Cc1ccccc1)NC(=O)C12CC1/C(=N\O)c1ccccc1O2	10.1021/jm0009944
	CHEMBL434064	167734	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells	ChEMBL	380	5	2	6	1.9	COC(=O)[C@@H](Cc1ccccc1)NC(=O)C12CC1/C(=N\O)c1ccccc1O2	10.1021/jm0009944
	71683128	90605	1	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	364	2	0	4	3.2	C[C@@H]1CN(c2cnccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397345	90605	1	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	364	2	0	4	3.2	C[C@@H]1CN(c2cnccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	76310874	105124	0	None	-3715	2	Human	4.9	pIC50	=	4.9	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay	ChEMBL	353	6	0	6	2.7	CCN(CC)C(=O)c1nn(C)c2nc(OCc3cccc(C)n3)ccc12	10.1021/jm401622k
	CHEMBL3122223	105124	0	None	-3715	2	Human	4.9	pIC50	=	4.9	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay	ChEMBL	353	6	0	6	2.7	CCN(CC)C(=O)c1nn(C)c2nc(OCc3cccc(C)n3)ccc12	10.1021/jm401622k
	44442431	1040	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	415	3	1	7	2.2	Clc1ccc(cc1)n1c(C)nc2c(c1=O)cnn2c1ccc(cc1)S(=O)(=O)N	10.1016/j.bmcl.2007.05.028
	6342	1040	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	415	3	1	7	2.2	Clc1ccc(cc1)n1c(C)nc2c(c1=O)cnn2c1ccc(cc1)S(=O)(=O)N	10.1016/j.bmcl.2007.05.028
	CHEMBL245990	1040	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	415	3	1	7	2.2	Clc1ccc(cc1)n1c(C)nc2c(c1=O)cnn2c1ccc(cc1)S(=O)(=O)N	10.1016/j.bmcl.2007.05.028
	118735958	118404	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	377	4	2	5	3.5	Cc1cc(C(=O)N2CCc3c(sc(NCc4ccccc4)c3C#N)C2)[nH]n1	10.1016/j.ejmech.2015.04.060
	CHEMBL3422874	118404	0	None	-	1	Human	5.9	pIC50	=	5.9	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	377	4	2	5	3.5	Cc1cc(C(=O)N2CCc3c(sc(NCc4ccccc4)c3C#N)C2)[nH]n1	10.1016/j.ejmech.2015.04.060
	72163434	91597	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	365	3	0	3	3.6	O=C(CC12CC3CC(CC(C3)C1)C2)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418374	91597	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	365	3	0	3	3.6	O=C(CC12CC3CC(CC(C3)C1)C2)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	122196110	123725	0	None	13	2	Human	6.8	pIC50	=	6.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	394	4	1	5	3.8	COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O	10.1016/j.bmcl.2015.10.013
	CHEMBL3634432	123725	0	None	13	2	Human	6.8	pIC50	=	6.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	394	4	1	5	3.8	COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O	10.1016/j.bmcl.2015.10.013
	72163434	91597	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	365	3	0	3	3.6	O=C(CC12CC3CC(CC(C3)C1)C2)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418374	91597	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	365	3	0	3	3.6	O=C(CC12CC3CC(CC(C3)C1)C2)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	11652895	84644	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	334	3	0	6	3.2	CCc1ccc(-n2cnc3c(oc4nccc(N(C)C)c43)c2=O)cc1	10.1021/jm0504407
	CHEMBL224377	84644	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	334	3	0	6	3.2	CCc1ccc(-n2cnc3c(oc4nccc(N(C)C)c43)c2=O)cc1	10.1021/jm0504407
	127034284	138618	0	None	15	2	Rat	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	319	2	1	5	3.7	c1ccn2nc3c(NC45CC6CC(CC(C6)C4)C5)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	CHEMBL3787124	138618	0	None	15	2	Rat	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	319	2	1	5	3.7	c1ccn2nc3c(NC45CC6CC(CC(C6)C4)C5)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	127034284	138618	0	None	15	2	Rat	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	319	2	1	5	3.7	c1ccn2nc3c(NC45CC6CC(CC(C6)C4)C5)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	CHEMBL3787124	138618	0	None	15	2	Rat	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	319	2	1	5	3.7	c1ccn2nc3c(NC45CC6CC(CC(C6)C4)C5)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	73334761	124597	0	None	-18	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	385	2	0	7	2.0	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-n4nccn4)c3CCN12	nan
	CHEMBL3644413	124597	0	None	-18	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	385	2	0	7	2.0	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-n4nccn4)c3CCN12	nan
	57881945	83292	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	367	3	0	8	2.8	COc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)c(C)c1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205376	83292	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	367	3	0	8	2.8	COc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)c(C)c1	10.1016/j.bmcl.2012.09.048
	16118536	70646	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	351	4	1	6	4.0	CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951681	70646	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	351	4	1	6	4.0	CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	16118816	70694	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	364	4	1	7	3.6	COc1ccc(-n2ccc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951886	70694	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	364	4	1	7	3.6	COc1ccc(-n2ccc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	16118942	70697	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	336	3	1	6	3.7	CCNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951889	70697	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	336	3	1	6	3.7	CCNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	73334942	132498	0	None	2	2	Human	7.8	pIC50	=	7.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	324	2	0	4	3.0	COc1cccc2c1CCN1C(=O)CN=C(c3cccs3)C=C21	nan
	CHEMBL3702360	132498	0	None	2	2	Human	7.8	pIC50	=	7.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	324	2	0	4	3.0	COc1cccc2c1CCN1C(=O)CN=C(c3cccs3)C=C21	nan
	73335337	132524	0	None	-1	2	Human	7.8	pIC50	=	7.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	446	2	0	4	3.3	CC(C)n1cc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)cn1	nan
	CHEMBL3702386	132524	0	None	-1	2	Human	7.8	pIC50	=	7.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	446	2	0	4	3.3	CC(C)n1cc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)cn1	nan
	122196125	123740	0	None	40	2	Human	7.8	pIC50	=	7.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	360	3	1	4	3.9	Cc1cc(N2C(=O)c3ccccc3C2=O)ccc1NC(=O)c1occc1C	10.1016/j.bmcl.2015.10.013
	CHEMBL3634447	123740	0	None	40	2	Human	7.8	pIC50	=	7.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	360	3	1	4	3.9	Cc1cc(N2C(=O)c3ccccc3C2=O)ccc1NC(=O)c1occc1C	10.1016/j.bmcl.2015.10.013
	44408491	140732	0	None	-	1	Rat	7.8	pIC50	=	7.8	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	465	6	0	6	3.5	Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCCN1C(=O)c3ccccc3C1=O)CC2	10.1016/j.bmcl.2005.11.049
	CHEMBL383107	140732	0	None	-	1	Rat	7.8	pIC50	=	7.8	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	465	6	0	6	3.5	Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCCN1C(=O)c3ccccc3C1=O)CC2	10.1016/j.bmcl.2005.11.049
	122196120	123735	0	None	26	2	Human	7.8	pIC50	=	7.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	410	3	1	4	5.1	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c2ccccc12	10.1016/j.bmcl.2015.10.013
	CHEMBL3634442	123735	0	None	26	2	Human	7.8	pIC50	=	7.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	410	3	1	4	5.1	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c2ccccc12	10.1016/j.bmcl.2015.10.013
	44588460	174976	0	None	-3	3	Mouse	6.8	pIC50	=	6.8	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	327	2	0	6	2.7	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccn3)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL457872	174976	0	None	-3	3	Mouse	6.8	pIC50	=	6.8	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	327	2	0	6	2.7	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccn3)nn2)CC1	10.1016/j.bmc.2008.09.060
	73334941	132497	0	None	1	2	Human	6.8	pIC50	=	6.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	362	1	0	3	4.0	O=C1CN=C(c2cccs2)C=C2c3cccc(C(F)(F)F)c3CCN12	nan
	CHEMBL3702359	132497	0	None	1	2	Human	6.8	pIC50	=	6.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	362	1	0	3	4.0	O=C1CN=C(c2cccs2)C=C2c3cccc(C(F)(F)F)c3CCN12	nan
	45484850	196653	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	307	2	0	6	3.6	Cc1nc2cc(-c3nnn(-c4cccnc4)c3C)ccc2s1	10.1016/j.bmcl.2009.07.145
	CHEMBL576231	196653	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	307	2	0	6	3.6	Cc1nc2cc(-c3nnn(-c4cccnc4)c3C)ccc2s1	10.1016/j.bmcl.2009.07.145
	45486781	195560	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	325	4	0	5	3.5	COc1ccc(C(=O)N(C)c2nc(-c3ccncc3)cs2)cc1	10.1016/j.bmcl.2009.07.097
	CHEMBL568321	195560	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	325	4	0	5	3.5	COc1ccc(C(=O)N(C)c2nc(-c3ccncc3)cs2)cc1	10.1016/j.bmcl.2009.07.097
	45486816	196957	0	None	4	2	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	314	3	0	5	3.0	CN(C(=O)c1ccc(F)cc1)c1nc(-c2cncnc2)cs1	10.1016/j.bmcl.2009.07.097
	CHEMBL579011	196957	0	None	4	2	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	314	3	0	5	3.0	CN(C(=O)c1ccc(F)cc1)c1nc(-c2cncnc2)cs1	10.1016/j.bmcl.2009.07.097
	24777316	94279	0	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	331	1	0	4	3.7	CC1(C)CC(=O)c2cc(C#N)c(N3CCc4ccccc4C3)nc2C1	10.1021/jm0611298
	CHEMBL252942	94279	0	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	331	1	0	4	3.7	CC1(C)CC(=O)c2cc(C#N)c(N3CCc4ccccc4C3)nc2C1	10.1021/jm0611298
	86711404	124613	0	None	-758	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	362	2	1	5	2.5	CC(O)c1cn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)cn1	nan
	CHEMBL3644429	124613	0	None	-758	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	362	2	1	5	2.5	CC(O)c1cn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)cn1	nan
	89979743	132551	0	None	-7	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	434	1	1	5	1.7	O=C1CN=C(n2cnc(CO)c2)C=C2c3cccc(I)c3CCN12	nan
	CHEMBL3702413	132551	0	None	-7	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	434	1	1	5	1.7	O=C1CN=C(n2cnc(CO)c2)C=C2c3cccc(I)c3CCN12	nan
	91618209	132588	0	None	-151	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	336	3	1	4	2.7	CCCc1cccc2c1CCN1C(=O)CNC(n3cnc(C)c3)C=C21	nan
	CHEMBL3702449	132588	0	None	-151	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	336	3	1	4	2.7	CCCc1cccc2c1CCN1C(=O)CNC(n3cnc(C)c3)C=C21	nan
	89980574	132591	0	None	-501	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	363	3	0	6	2.0	COCc1ncn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)n1	nan
	CHEMBL3702452	132591	0	None	-501	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	363	3	0	6	2.0	COCc1ncn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)n1	nan
	10106002	78114	2	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells	ChEMBL	247	2	1	5	1.6	CCOC(=O)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2	10.1021/jm0009944
	CHEMBL2111945	78114	2	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells	ChEMBL	247	2	1	5	1.6	CCOC(=O)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2	10.1021/jm0009944
	24777817	166625	0	None	-	1	Rat	4.8	pIC50	=	4.8	Functional	Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay	ChEMBL	435	3	0	5	4.5	CC1(C)CC(=O)c2cc(N3CCOCC3)c(N3CC=C(c4ccc(F)cc4)CC3)nc2C1	10.1021/jm0611298
	CHEMBL429122	166625	0	None	-	1	Rat	4.8	pIC50	=	4.8	Functional	Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay	ChEMBL	435	3	0	5	4.5	CC1(C)CC(=O)c2cc(N3CCOCC3)c(N3CC=C(c4ccc(F)cc4)CC3)nc2C1	10.1021/jm0611298
	127032494	138427	0	None	-	1	Rat	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	321	2	1	5	3.8	C[C@H]1[C@H](Nc2ncnc3c2nn2ccccc32)C[C@@H]2C[C@H]1C2(C)C	10.1016/j.bmcl.2016.03.026
	CHEMBL3785139	138427	0	None	-	1	Rat	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	321	2	1	5	3.8	C[C@H]1[C@H](Nc2ncnc3c2nn2ccccc32)C[C@@H]2C[C@H]1C2(C)C	10.1016/j.bmcl.2016.03.026
	127032494	138427	0	None	-	1	Rat	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	321	2	1	5	3.8	C[C@H]1[C@H](Nc2ncnc3c2nn2ccccc32)C[C@@H]2C[C@H]1C2(C)C	10.1016/j.bmcl.2016.03.026
	CHEMBL3785139	138427	0	None	-	1	Rat	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	321	2	1	5	3.8	C[C@H]1[C@H](Nc2ncnc3c2nn2ccccc32)C[C@@H]2C[C@H]1C2(C)C	10.1016/j.bmcl.2016.03.026
	3342765	194103	11	None	-	1	Rat	4.8	pIC50	=	4.8	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	302	4	0	2	5.3	Cc1ccc(C(=O)c2ccc(Oc3ccccc3)cc2)cc1C	10.1016/j.bmc.2009.05.072
	CHEMBL557722	194103	11	None	-	1	Rat	4.8	pIC50	=	4.8	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	302	4	0	2	5.3	Cc1ccc(C(=O)c2ccc(Oc3ccccc3)cc2)cc1C	10.1016/j.bmc.2009.05.072
	57881822	83403	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	379	5	1	8	3.2	COc1ccc(-n2cnc3c(sc4ncnc(NCC5CC5)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205916	83403	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	379	5	1	8	3.2	COc1ccc(-n2cnc3c(sc4ncnc(NCC5CC5)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	122196106	123722	0	None	18	2	Human	6.8	pIC50	=	6.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	432	3	1	4	4.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(C(F)(F)F)c1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634429	123722	0	None	18	2	Human	6.8	pIC50	=	6.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	432	3	1	4	4.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(C(F)(F)F)c1	10.1016/j.bmcl.2015.10.013
	1222	101267	56	None	-3	2	Human	3.8	pIC50	=	3.8	Functional	Ability to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M ConcentrationAbility to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M Concentration	ChEMBL	209	3	3	3	0.6	CC(N)(C(=O)O)c1ccc(C(=O)O)cc1	10.1021/jm00019a002
	CHEMBL299683	101267	56	None	-3	2	Human	3.8	pIC50	=	3.8	Functional	Ability to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M ConcentrationAbility to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M Concentration	ChEMBL	209	3	3	3	0.6	CC(N)(C(=O)O)c1ccc(C(=O)O)cc1	10.1021/jm00019a002
	67424813	88646	0	None	-25	2	Human	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	418	5	2	7	4.4	CNc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2334978	88646	0	None	-25	2	Human	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	418	5	2	7	4.4	CNc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2365133	88646	0	None	-25	2	Human	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	418	5	2	7	4.4	CNc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	46886135	7839	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	309	1	1	7	2.3	Cc1nc(N)c2c(n1)sc1c(=O)n(-c3ccccc3)cnc12	10.1016/j.bmcl.2010.03.004
	CHEMBL1090247	7839	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	309	1	1	7	2.3	Cc1nc(N)c2c(n1)sc1c(=O)n(-c3ccccc3)cnc12	10.1016/j.bmcl.2010.03.004
	54586818	62429	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	406	4	1	9	4.0	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5scnc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784063	62429	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	406	4	1	9	4.0	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5scnc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	57559476	83413	0	None	630	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	391	2	0	7	3.5	CN(C)c1ncnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	CHEMBL2205926	83413	0	None	630	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	391	2	0	7	3.5	CN(C)c1ncnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	1069776	84798	11	None	1	3	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	356	2	0	6	3.7	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1021/jm0504407
	CHEMBL225589	84798	11	None	1	3	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	356	2	0	6	3.7	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1021/jm0504407
	44588425	176234	0	None	1	3	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	344	2	0	5	3.4	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccc(F)cc3)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL460827	176234	0	None	1	3	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	344	2	0	5	3.4	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccc(F)cc3)nn2)CC1	10.1016/j.bmc.2008.09.060
	11716890	94557	15	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	328	2	2	5	3.5	Cc1c(C(=O)NC2CCCCC2)sc2nc3ccc(N)cc3n12	10.1021/jm060950g
	CHEMBL254777	94557	15	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	328	2	2	5	3.5	Cc1c(C(=O)NC2CCCCC2)sc2nc3ccc(N)cc3n12	10.1021/jm060950g
	44588385	176321	0	None	-2	3	Mouse	7.8	pIC50	=	7.8	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	344	2	0	5	3.4	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL461673	176321	0	None	-2	3	Mouse	7.8	pIC50	=	7.8	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	344	2	0	5	3.4	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	1383	1421	1	None	-	1	Rat	7.8	pIC50	=	7.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	309	5	1	4	3.8	CCCOC(=O)c1[nH]c(c(c1C)C(=O)O[C@H](C(C)(C)C)C)C	10.1016/j.bmcl.2007.01.055
	44431042	1421	1	None	-	1	Rat	7.8	pIC50	=	7.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	309	5	1	4	3.8	CCCOC(=O)c1[nH]c(c(c1C)C(=O)O[C@H](C(C)(C)C)C)C	10.1016/j.bmcl.2007.01.055
	CHEMBL232052	1421	1	None	-	1	Rat	7.8	pIC50	=	7.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	309	5	1	4	3.8	CCCOC(=O)c1[nH]c(c(c1C)C(=O)O[C@H](C(C)(C)C)C)C	10.1016/j.bmcl.2007.01.055
	122196092	123708	0	None	21	2	Human	7.8	pIC50	=	7.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	360	3	1	4	3.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)cc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634415	123708	0	None	21	2	Human	7.8	pIC50	=	7.8	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	360	3	1	4	3.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)cc1	10.1016/j.bmcl.2015.10.013
	54585405	62335	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	362	4	1	6	4.3	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783868	62335	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	362	4	1	6	4.3	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	16038352	89788	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	333	1	1	6	3.2	Cc1ccc(-n2cnc3c(sc4ncc5cn[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	CHEMBL238262	89788	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	333	1	1	6	3.2	Cc1ccc(-n2cnc3c(sc4ncc5cn[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	1381	574	21	None	-3	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	278	2	0	2	3.9	C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2	10.1021/jm060950g
	9903757	574	21	None	-3	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	278	2	0	2	3.9	C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2	10.1021/jm060950g
	CHEMBL254372	574	21	None	-3	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	278	2	0	2	3.9	C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2	10.1021/jm060950g
	44588429	176259	0	None	-1	2	Mouse	6.8	pIC50	=	6.8	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	342	3	0	4	3.5	CC(C)(C)CC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL461035	176259	0	None	-1	2	Mouse	6.8	pIC50	=	6.8	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	342	3	0	4	3.5	CC(C)(C)CC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	24777699	94382	0	None	-	1	Rat	6.8	pIC50	=	6.8	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	378	2	0	5	3.6	CC1(C)CC(=O)c2cc(C#N)c(N3CCN(c4ccc(F)cc4)CC3)nc2C1	10.1021/jm0611298
	CHEMBL253568	94382	0	None	-	1	Rat	6.8	pIC50	=	6.8	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	378	2	0	5	3.6	CC1(C)CC(=O)c2cc(C#N)c(N3CCN(c4ccc(F)cc4)CC3)nc2C1	10.1021/jm0611298
	44588427	176257	0	None	-2	3	Mouse	5.8	pIC50	=	5.8	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	356	3	0	6	3.3	COc1ccccc1-n1cc(C2=CCN(C(=O)OC(C)(C)C)CC2)nn1	10.1016/j.bmc.2008.09.060
	CHEMBL461033	176257	0	None	-2	3	Mouse	5.8	pIC50	=	5.8	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	356	3	0	6	3.3	COc1ccccc1-n1cc(C2=CCN(C(=O)OC(C)(C)C)CC2)nn1	10.1016/j.bmc.2008.09.060
	73335341	132528	0	None	-2	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	319	1	0	4	2.8	N#Cc1cccc2c1CCN1C(=O)CN=C(c3cccs3)C=C21	nan
	CHEMBL3702390	132528	0	None	-2	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	319	1	0	4	2.8	N#Cc1cccc2c1CCN1C(=O)CN=C(c3cccs3)C=C21	nan
	89980234	132548	0	None	-2	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	326	0	0	4	2.5	Cc1cn(C2=NCC(=O)N3CCc4c(Cl)cccc4C3=C2)cn1	nan
	CHEMBL3702410	132548	0	None	-2	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	326	0	0	4	2.5	Cc1cn(C2=NCC(=O)N3CCc4c(Cl)cccc4C3=C2)cn1	nan
	73335734	132571	0	None	-40	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	348	3	0	5	2.4	C=Cc1cccc2c1CCN1C(=O)CN=C(n3cnc(COC)c3)C=C21	nan
	CHEMBL3702433	132571	0	None	-40	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	348	3	0	5	2.4	C=Cc1cccc2c1CCN1C(=O)CN=C(n3cnc(COC)c3)C=C21	nan
	71682340	90609	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@@H]1CN(c2ccccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397349	90609	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@@H]1CN(c2ccccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	127030349	138498	0	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	321	2	1	5	3.9	CC1(C)[C@@H]2CC[C@]1(C)[C@@H](Nc1ncnc3c1nn1ccccc31)C2	10.1016/j.bmcl.2016.03.026
	CHEMBL3785862	138498	0	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	321	2	1	5	3.9	CC1(C)[C@@H]2CC[C@]1(C)[C@@H](Nc1ncnc3c1nn1ccccc31)C2	10.1016/j.bmcl.2016.03.026
	127034264	138507	0	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	335	2	1	5	4.2	Cc1nc(N[C@H]2C[C@H]3CC[C@@]2(C)C3(C)C)c2nn3ccccc3c2n1	10.1016/j.bmcl.2016.03.026
	CHEMBL3785977	138507	0	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	335	2	1	5	4.2	Cc1nc(N[C@H]2C[C@H]3CC[C@@]2(C)C3(C)C)c2nn3ccccc3c2n1	10.1016/j.bmcl.2016.03.026
	78324871	113837	3	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	338	2	0	4	4.8	O=c1c2scc(-c3ccccc3)c2ncn1-c1ccc(Cl)cc1	10.1016/j.ejmech.2014.08.027
	CHEMBL3330805	113837	3	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	338	2	0	4	4.8	O=c1c2scc(-c3ccccc3)c2ncn1-c1ccc(Cl)cc1	10.1016/j.ejmech.2014.08.027
	71682340	90609	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@@H]1CN(c2ccccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397349	90609	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@@H]1CN(c2ccccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	127030349	138498	0	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	321	2	1	5	3.9	CC1(C)[C@@H]2CC[C@]1(C)[C@@H](Nc1ncnc3c1nn1ccccc31)C2	10.1016/j.bmcl.2016.03.026
	CHEMBL3785862	138498	0	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	321	2	1	5	3.9	CC1(C)[C@@H]2CC[C@]1(C)[C@@H](Nc1ncnc3c1nn1ccccc31)C2	10.1016/j.bmcl.2016.03.026
	127034264	138507	0	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	335	2	1	5	4.2	Cc1nc(N[C@H]2C[C@H]3CC[C@@]2(C)C3(C)C)c2nn3ccccc3c2n1	10.1016/j.bmcl.2016.03.026
	CHEMBL3785977	138507	0	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	335	2	1	5	4.2	Cc1nc(N[C@H]2C[C@H]3CC[C@@]2(C)C3(C)C)c2nn3ccccc3c2n1	10.1016/j.bmcl.2016.03.026
	89979843	124586	0	None	-29	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	386	1	0	4	3.5	O=C1CN=C(n2cnc(C(F)(F)F)c2)C=C2c3cccc(C4CC4)c3CCN12	nan
	CHEMBL3644402	124586	0	None	-29	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	386	1	0	4	3.5	O=C1CN=C(n2cnc(C(F)(F)F)c2)C=C2c3cccc(C4CC4)c3CCN12	nan
	71682342	90611	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccn1	10.1016/j.bmcl.2013.05.020
	CHEMBL2397351	90611	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccn1	10.1016/j.bmcl.2013.05.020
	73355027	90614	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	327	2	0	3	3.3	C[C@@H]1CN(c2ccccn2)CCN1C(=O)C1CC2CCCC(C2)C1	10.1016/j.bmcl.2013.05.020
	CHEMBL2397366	90614	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	327	2	0	3	3.3	C[C@@H]1CN(c2ccccn2)CCN1C(=O)C1CC2CCCC(C2)C1	10.1016/j.bmcl.2013.05.020
	71682342	90611	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccn1	10.1016/j.bmcl.2013.05.020
	CHEMBL2397351	90611	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccn1	10.1016/j.bmcl.2013.05.020
	11666576	141196	0	None	1	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	300	2	0	6	2.8	CN(C)c1ccnc2sc3c(=O)n(C4CCC4)cnc3c12	10.1021/jm0504407
	CHEMBL385776	141196	0	None	1	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	300	2	0	6	2.8	CN(C)c1ccnc2sc3c(=O)n(C4CCC4)cnc3c12	10.1021/jm0504407
	11537767	141299	0	None	-5	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	359	2	0	7	2.6	C[N+](C)([O-])c1ccnc2sc3c(=O)n(N4CCCCCC4)cnc3c12	10.1021/jm0504407
	CHEMBL386408	141299	0	None	-5	2	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	359	2	0	7	2.6	C[N+](C)([O-])c1ccnc2sc3c(=O)n(N4CCCCCC4)cnc3c12	10.1021/jm0504407
	16739288	1018	0	None	-	1	Rat	6.8	pIC50	=	6.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	306	3	2	2	3.3	Cc1cc2[nH]c3c(c2cc1OCc1ccccc1)CCNC3=O	10.1016/j.bmcl.2007.01.055
	6358	1018	0	None	-	1	Rat	6.8	pIC50	=	6.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	306	3	2	2	3.3	Cc1cc2[nH]c3c(c2cc1OCc1ccccc1)CCNC3=O	10.1016/j.bmcl.2007.01.055
	CHEMBL396712	1018	0	None	-	1	Rat	6.8	pIC50	=	6.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	306	3	2	2	3.3	Cc1cc2[nH]c3c(c2cc1OCc1ccccc1)CCNC3=O	10.1016/j.bmcl.2007.01.055
	73355027	90614	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	327	2	0	3	3.3	C[C@@H]1CN(c2ccccn2)CCN1C(=O)C1CC2CCCC(C2)C1	10.1016/j.bmcl.2013.05.020
	CHEMBL2397366	90614	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	327	2	0	3	3.3	C[C@@H]1CN(c2ccccn2)CCN1C(=O)C1CC2CCCC(C2)C1	10.1016/j.bmcl.2013.05.020
	12988076	149737	0	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	294	3	2	3	2.7	O=C1NCCC2c3cc(OCc4ccccc4)ccc3NC12	10.1016/j.bmcl.2007.01.055
	CHEMBL395256	149737	0	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	294	3	2	3	2.7	O=C1NCCC2c3cc(OCc4ccccc4)ccc3NC12	10.1016/j.bmcl.2007.01.055
	54582944	62430	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	406	4	1	9	4.0	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5ncsc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784064	62430	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	406	4	1	9	4.0	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5ncsc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	11688880	84641	0	None	1	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	350	2	0	6	3.7	Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c(C)c1	10.1021/jm0504407
	CHEMBL224356	84641	0	None	1	2	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	350	2	0	6	3.7	Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c(C)c1	10.1021/jm0504407
	16118539	70651	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	381	5	1	7	3.0	COc1ccc(-n2ccc3c(sc4nccc(N(C)CCO)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951687	70651	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	381	5	1	7	3.0	COc1ccc(-n2ccc3c(sc4nccc(N(C)CCO)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	45484897	196916	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	292	4	0	5	3.2	CCC(=O)c1ccc(-c2nnn(-c3cccnc3)c2C)cc1	10.1016/j.bmcl.2009.07.145
	CHEMBL578565	196916	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	292	4	0	5	3.2	CCC(=O)c1ccc(-c2nnn(-c3cccnc3)c2C)cc1	10.1016/j.bmcl.2009.07.145
	73335641	132561	0	None	-19	2	Human	6.8	pIC50	=	6.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	372	2	0	5	3.4	CCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4ccco4)C3=C2)cn1	nan
	CHEMBL3702423	132561	0	None	-19	2	Human	6.8	pIC50	=	6.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	372	2	0	5	3.4	CCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4ccco4)C3=C2)cn1	nan
	5766222	194238	17	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	307	3	0	2	5.1	Cc1ccc2nc(Cl)c(/C=C/C(=O)c3ccccc3)cc2c1	10.1016/j.bmc.2009.05.072
	CHEMBL559243	194238	17	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	307	3	0	2	5.1	Cc1ccc2nc(Cl)c(/C=C/C(=O)c3ccccc3)cc2c1	10.1016/j.bmc.2009.05.072
	24777696	94313	0	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	271	4	1	4	3.3	CCCCNc1nc2c(cc1C#N)C(=O)CC(C)(C)C2	10.1021/jm0611298
	CHEMBL253143	94313	0	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	271	4	1	4	3.3	CCCCNc1nc2c(cc1C#N)C(=O)CC(C)(C)C2	10.1021/jm0611298
	54582947	62446	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	374	3	1	6	4.1	C#CC(C)(C)Nc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784080	62446	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	374	3	1	6	4.1	C#CC(C)(C)Nc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	127034013	138562	0	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	2	1	5	3.6	Cc1nc(N[C@H]2CC[C@H](C)CC2)c2nn3ccccc3c2n1	10.1016/j.bmcl.2016.03.026
	CHEMBL3786560	138562	0	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	2	1	5	3.6	Cc1nc(N[C@H]2CC[C@H](C)CC2)c2nn3ccccc3c2n1	10.1016/j.bmcl.2016.03.026
	44588386	176187	0	None	2	3	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	344	2	0	5	3.4	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3cccc(F)c3)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL460391	176187	0	None	2	3	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	344	2	0	5	3.4	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3cccc(F)c3)nn2)CC1	10.1016/j.bmc.2008.09.060
	16661728	195430	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	327	4	0	4	4.0	CCN(C(=O)c1ccc(F)cc1)c1nc(-c2ccccn2)cs1	10.1016/j.bmcl.2009.07.097
	CHEMBL567668	195430	0	None	-	1	Human	7.8	pIC50	=	7.8	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	327	4	0	4	4.0	CCN(C(=O)c1ccc(F)cc1)c1nc(-c2ccccn2)cs1	10.1016/j.bmcl.2009.07.097
	122196109	123557	0	None	36	2	Human	7.7	pIC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	410	4	1	5	4.3	COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O	10.1016/j.bmcl.2015.10.013
	CHEMBL3632642	123557	0	None	36	2	Human	7.7	pIC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	410	4	1	5	4.3	COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O	10.1016/j.bmcl.2015.10.013
	11530673	165560	0	None	1	3	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	364	4	0	6	4.0	CCCc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1021/jm0504407
	CHEMBL426018	165560	0	None	1	3	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	364	4	0	6	4.0	CCCc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1021/jm0504407
	44442429	154271	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	350	2	0	5	3.8	Cc1cccc(-n2ncc3c(=O)n(-c4ccc(Cl)cc4)c(C)nc32)c1	10.1016/j.bmcl.2007.05.028
	CHEMBL400307	154271	0	None	-	1	Human	6.8	pIC50	=	6.8	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	350	2	0	5	3.8	Cc1cccc(-n2ncc3c(=O)n(-c4ccc(Cl)cc4)c(C)nc32)c1	10.1016/j.bmcl.2007.05.028
	44588461	172994	0	None	-3	3	Mouse	6.8	pIC50	=	6.8	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	327	2	0	6	2.7	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3cccnc3)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL453249	172994	0	None	-3	3	Mouse	6.8	pIC50	=	6.8	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	327	2	0	6	2.7	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3cccnc3)nn2)CC1	10.1016/j.bmc.2008.09.060
	11674352	174593	0	None	-4	3	Mouse	6.8	pIC50	=	6.8	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	331	3	0	6	2.4	CC(C)OC(=O)N1CC=C(c2cn(-c3cccnc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL457026	174593	0	None	-4	3	Mouse	6.8	pIC50	=	6.8	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	331	3	0	6	2.4	CC(C)OC(=O)N1CC=C(c2cn(-c3cccnc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	45484911	197250	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	333	3	0	5	2.9	Cc1c(-c2ccc(C(=O)N3CCCC3)cc2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	CHEMBL584610	197250	0	None	-	1	Human	5.8	pIC50	=	5.8	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	333	3	0	5	2.9	Cc1c(-c2ccc(C(=O)N3CCCC3)cc2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	91618212	124608	0	None	-177	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	385	2	0	6	3.1	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cocn4)c3CCN12	nan
	CHEMBL3644424	124608	0	None	-177	2	Human	5.8	pIC50	=	5.8	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	385	2	0	6	3.1	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cocn4)c3CCN12	nan
	127034013	138562	0	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	2	1	5	3.6	Cc1nc(N[C@H]2CC[C@H](C)CC2)c2nn3ccccc3c2n1	10.1016/j.bmcl.2016.03.026
	CHEMBL3786560	138562	0	None	-	1	Rat	5.8	pIC50	=	5.8	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	2	1	5	3.6	Cc1nc(N[C@H]2CC[C@H](C)CC2)c2nn3ccccc3c2n1	10.1016/j.bmcl.2016.03.026
	44329032	112052	0	None	-177	5	Human	4.8	pIC50	=	4.8	Functional	Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluated	ChEMBL	423	9	3	4	4.6	CCCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O	10.1016/s0960-894x(98)00510-1
	CHEMBL329920	112052	0	None	-177	5	Human	4.8	pIC50	=	4.8	Functional	Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluated	ChEMBL	423	9	3	4	4.6	CCCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O	10.1016/s0960-894x(98)00510-1
	118735971	118414	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	391	4	1	4	4.6	N#Cc1c(NCc2ccc(F)cc2)sc2c1CCN(C(=O)c1ccccc1)C2	10.1016/j.ejmech.2015.04.060
	CHEMBL3422887	118414	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	391	4	1	4	4.6	N#Cc1c(NCc2ccc(F)cc2)sc2c1CCN(C(=O)c1ccccc1)C2	10.1016/j.ejmech.2015.04.060
	89979990	132600	0	None	-83	2	Human	4.7	pIC50	=	4.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	413	2	0	5	3.6	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4ccnc(F)c4)c3CCN12	nan
	CHEMBL3702463	132600	0	None	-83	2	Human	4.7	pIC50	=	4.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	413	2	0	5	3.6	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4ccnc(F)c4)c3CCN12	nan
	11566478	84695	0	None	11	2	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	350	3	0	6	3.6	CCc1ccc(-n2cnc3c(sc4cncc(N(C)C)c43)c2=O)cc1	10.1021/jm0504407
	CHEMBL224798	84695	0	None	11	2	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	350	3	0	6	3.6	CCc1ccc(-n2cnc3c(sc4cncc(N(C)C)c43)c2=O)cc1	10.1021/jm0504407
	86729801	113839	3	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	318	2	0	4	4.4	Cc1cccc(-n2cnc3c(-c4ccccc4)csc3c2=O)c1	10.1016/j.ejmech.2014.08.027
	CHEMBL3330807	113839	3	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	318	2	0	4	4.4	Cc1cccc(-n2cnc3c(-c4ccccc4)csc3c2=O)c1	10.1016/j.ejmech.2014.08.027
	72163719	91602	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	375	2	0	3	3.7	N#Cc1ccccc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418383	91602	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	375	2	0	3	3.7	N#Cc1ccccc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1	10.1016/j.bmcl.2013.07.029
	89980679	132585	0	None	-33	2	Human	5.7	pIC50	=	5.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	419	4	0	7	3.2	CCOCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4nccs4)C3=C2)cn1	nan
	CHEMBL3702446	132585	0	None	-33	2	Human	5.7	pIC50	=	5.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	419	4	0	7	3.2	CCOCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4nccs4)C3=C2)cn1	nan
	72163719	91602	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	375	2	0	3	3.7	N#Cc1ccccc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418383	91602	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	375	2	0	3	3.7	N#Cc1ccccc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1	10.1016/j.bmcl.2013.07.029
	46886136	8146	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	339	2	1	8	2.3	COc1ccc(-n2cnc3c(sc4nc(C)nc(N)c43)c2=O)cc1	10.1016/j.bmcl.2010.03.004
	CHEMBL1092275	8146	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	339	2	1	8	2.3	COc1ccc(-n2cnc3c(sc4nc(C)nc(N)c43)c2=O)cc1	10.1016/j.bmcl.2010.03.004
	57881818	83290	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	383	4	1	8	3.1	COc1ccc(-n2cnc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1F	10.1016/j.bmcl.2012.09.048
	CHEMBL2205374	83290	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	383	4	1	8	3.1	COc1ccc(-n2cnc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1F	10.1016/j.bmcl.2012.09.048
	71455906	83398	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	367	5	1	8	3.2	CCCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	CHEMBL2205910	83398	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	367	5	1	8	3.2	CCCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	11702918	136319	0	None	42	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	343	2	0	7	3.4	CN(C)c1ccnc2sc3c(=O)n(C4CCCCCC4)nnc3c12	10.1021/jm0504407
	CHEMBL374180	136319	0	None	42	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	343	2	0	7	3.4	CN(C)c1ccnc2sc3c(=O)n(C4CCCCCC4)nnc3c12	10.1021/jm0504407
	122196122	123737	0	None	41	2	Human	7.7	pIC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	414	3	1	4	4.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c2ccccc12	10.1016/j.bmcl.2015.10.013
	CHEMBL3634444	123737	0	None	41	2	Human	7.7	pIC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	414	3	1	4	4.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c2ccccc12	10.1016/j.bmcl.2015.10.013
	44408468	75354	0	None	-	1	Rat	7.7	pIC50	=	7.7	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	318	4	0	4	3.0	C=CCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O	10.1016/j.bmcl.2005.11.049
	CHEMBL204802	75354	0	None	-	1	Rat	7.7	pIC50	=	7.7	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	318	4	0	4	3.0	C=CCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O	10.1016/j.bmcl.2005.11.049
	44408578	137987	0	None	-	1	Rat	7.7	pIC50	=	7.7	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	324	4	0	4	2.8	Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCF)CC2	10.1016/j.bmcl.2005.11.049
	CHEMBL377503	137987	0	None	-	1	Rat	7.7	pIC50	=	7.7	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	324	4	0	4	2.8	Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCF)CC2	10.1016/j.bmcl.2005.11.049
	44408599	169539	0	None	-	1	Rat	7.7	pIC50	=	7.7	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	332	4	0	4	3.3	Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CC1CC1)CC2	10.1016/j.bmcl.2005.11.049
	CHEMBL444359	169539	0	None	-	1	Rat	7.7	pIC50	=	7.7	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	332	4	0	4	3.3	Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CC1CC1)CC2	10.1016/j.bmcl.2005.11.049
	57908399	87090	0	None	-5	2	Human	6.7	pIC50	=	6.7	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	419	5	1	7	4.4	COc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2334977	87090	0	None	-5	2	Human	6.7	pIC50	=	6.7	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	419	5	1	7	4.4	COc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	24777694	94278	0	None	-	1	Rat	5.7	pIC50	=	5.7	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	331	2	1	4	3.7	CC1(C)CC(=O)c2cc(C#N)c(NC3Cc4ccccc4C3)nc2C1	10.1021/jm0611298
	CHEMBL252941	94278	0	None	-	1	Rat	5.7	pIC50	=	5.7	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	331	2	1	4	3.7	CC1(C)CC(=O)c2cc(C#N)c(NC3Cc4ccccc4C3)nc2C1	10.1021/jm0611298
	1379	2387	36	None	-	1	Human	4.7	pIC50	=	4.7	Functional	Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis	ChEMBL	209	3	3	3	0.8	OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N	10.1016/S0960-894X(97)10071-3
	5311261	2387	36	None	-	1	Human	4.7	pIC50	=	4.7	Functional	Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis	ChEMBL	209	3	3	3	0.8	OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N	10.1016/S0960-894X(97)10071-3
	CHEMBL94631	2387	36	None	-	1	Human	4.7	pIC50	=	4.7	Functional	Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis	ChEMBL	209	3	3	3	0.8	OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N	10.1016/S0960-894X(97)10071-3
	73350719	91594	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	340	1	0	3	2.7	O=C(N1CC2CCCC(C2)C1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418363	91594	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	340	1	0	3	2.7	O=C(N1CC2CCCC(C2)C1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	73350719	91594	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	340	1	0	3	2.7	O=C(N1CC2CCCC(C2)C1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418363	91594	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	340	1	0	3	2.7	O=C(N1CC2CCCC(C2)C1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	89981446	124566	0	None	-83	2	Human	5.7	pIC50	=	5.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	414	2	0	7	3.2	Cc1nc(-c2cccc3c2CCN2C(=O)CN=C(n4cnc(C5CCC5)n4)C=C32)co1	nan
	CHEMBL3644380	124566	0	None	-83	2	Human	5.7	pIC50	=	5.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	414	2	0	7	3.2	Cc1nc(-c2cccc3c2CCN2C(=O)CN=C(n4cnc(C5CCC5)n4)C=C32)co1	nan
	57881851	83285	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	419	4	1	8	4.3	COc1ccc(-n2cnc3c(sc4ncnc(Nc5cccc(F)c5)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205368	83285	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	419	4	1	8	4.3	COc1ccc(-n2cnc3c(sc4ncnc(Nc5cccc(F)c5)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	57403925	70649	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	381	6	1	7	3.7	COCCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951685	70649	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	381	6	1	7	3.7	COCCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	73336124	132581	0	None	-19	2	Human	5.7	pIC50	=	5.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	396	2	0	6	2.9	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cnccn4)c3CCN12	nan
	CHEMBL3702442	132581	0	None	-19	2	Human	5.7	pIC50	=	5.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	396	2	0	6	2.9	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cnccn4)c3CCN12	nan
	54587386	62339	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	406	4	1	8	3.8	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783872	62339	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	406	4	1	8	3.8	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	86729810	152010	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	378	3	0	7	3.9	COc1ccc(-n2cnc3c(-c4ccc5c(c4)OCO5)csc3c2=O)cc1	nan
	CHEMBL3971614	152010	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	378	3	0	7	3.9	COc1ccc(-n2cnc3c(-c4ccc5c(c4)OCO5)csc3c2=O)cc1	nan
	122196114	123729	0	None	17	2	Human	6.7	pIC50	=	6.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	365	3	1	5	3.2	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634436	123729	0	None	17	2	Human	6.7	pIC50	=	6.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	365	3	1	5	3.2	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	23634326	62325	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	364	5	1	7	3.6	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783858	62325	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	364	5	1	7	3.6	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	57559313	83407	0	None	501	2	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	353	3	0	8	2.5	COc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205920	83407	0	None	501	2	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	353	3	0	8	2.5	COc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	16118540	70655	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	341	2	1	5	4.3	CNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951690	70655	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	341	2	1	5	4.3	CNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	16118685	70689	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	399	3	1	5	4.8	CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951881	70689	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	399	3	1	5	4.8	CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	23634102	963	1	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	362	4	1	7	3.0	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC	10.1016/j.bmcl.2009.04.104
	6215	963	1	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	362	4	1	7	3.0	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC	10.1016/j.bmcl.2009.04.104
	CHEMBL1783876	963	1	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	362	4	1	7	3.0	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC	10.1016/j.bmcl.2009.04.104
	46866191	1028	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	324	1	2	8	1.9	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N	10.1016/j.bmcl.2010.03.004
	6209	1028	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	324	1	2	8	1.9	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N	10.1016/j.bmcl.2010.03.004
	CHEMBL1093560	1028	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	324	1	2	8	1.9	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N	10.1016/j.bmcl.2010.03.004
	16659803	1022	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	384	1	1	7	3.8	C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	10.1021/jm070590c
	6338	1022	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	384	1	1	7	3.8	C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	10.1021/jm070590c
	CHEMBL236180	1022	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	384	1	1	7	3.8	C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	10.1021/jm070590c
	16659966	88258	0	None	323	2	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	350	1	1	7	3.1	Cc1ccc(-n2cnc3c(sc4ncc5c(c43)NCCO5)c2=O)cc1	10.1021/jm070590c
	CHEMBL235975	88258	0	None	323	2	Human	8.7	pIC50	=	8.7	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	350	1	1	7	3.1	Cc1ccc(-n2cnc3c(sc4ncc5c(c43)NCCO5)c2=O)cc1	10.1021/jm070590c
	16118686	70690	0	None	-	1	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	411	3	1	5	4.9	O=c1c2sc3nccc(NC4CC4)c3c2ccn1-c1ccc(Br)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951882	70690	0	None	-	1	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	411	3	1	5	4.9	O=c1c2sc3nccc(NC4CC4)c3c2ccn1-c1ccc(Br)cc1	10.1016/j.bmcl.2011.12.131
	16660467	196818	0	None	-	1	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	329	3	1	6	2.6	CN(C(=O)c1ccc(F)cc1)c1nc(-c2cc(N)ncn2)cs1	10.1016/j.bmcl.2009.07.097
	CHEMBL577729	196818	0	None	-	1	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	329	3	1	6	2.6	CN(C(=O)c1ccc(F)cc1)c1nc(-c2cc(N)ncn2)cs1	10.1016/j.bmcl.2009.07.097
	23657393	88314	0	None	-	1	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	380	2	1	8	3.2	COc1ccc(-n2cnc3c(sc4ncc5c(c43)NC[C@@H](C)O5)c2=O)cc1	10.1021/jm070590c
	CHEMBL236177	88314	0	None	-	1	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	380	2	1	8	3.2	COc1ccc(-n2cnc3c(sc4ncc5c(c43)NC[C@@H](C)O5)c2=O)cc1	10.1021/jm070590c
	16659967	1020	0	None	-	1	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	366	2	1	8	2.8	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	10.1021/jm070590c
	6345	1020	0	None	-	1	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	366	2	1	8	2.8	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	10.1021/jm070590c
	CHEMBL393922	1020	0	None	-	1	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	366	2	1	8	2.8	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	10.1021/jm070590c
	44588463	172737	0	None	4	3	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	345	2	0	6	2.8	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ncccc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL452618	172737	0	None	4	3	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	345	2	0	6	2.8	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ncccc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	45484935	195184	0	None	-	1	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	330	3	0	5	3.4	Cc1c(-c2ccc3c(c2)CC(C2CC2)C3=O)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	CHEMBL565943	195184	0	None	-	1	Human	8.6	pIC50	=	8.6	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	330	3	0	5	3.4	Cc1c(-c2ccc3c(c2)CC(C2CC2)C3=O)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	16659801	1021	0	None	-	1	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	370	1	1	7	3.5	Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	10.1021/jm070590c
	6346	1021	0	None	-	1	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	370	1	1	7	3.5	Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	10.1021/jm070590c
	CHEMBL236994	1021	0	None	-	1	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	370	1	1	7	3.5	Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	10.1021/jm070590c
	57559504	83417	0	None	501	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	354	3	0	9	1.9	COc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cn1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205930	83417	0	None	501	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	354	3	0	9	1.9	COc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cn1	10.1016/j.bmcl.2012.09.048
	699222	84668	11	None	1	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	322	2	0	6	3.1	CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4)cnc3c12	10.1021/jm0504407
	CHEMBL224615	84668	11	None	1	2	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	322	2	0	6	3.1	CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4)cnc3c12	10.1021/jm0504407
	122196119	123734	0	None	17	2	Human	7.7	pIC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	396	3	1	4	4.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c2ccccc12	10.1016/j.bmcl.2015.10.013
	CHEMBL3634441	123734	0	None	17	2	Human	7.7	pIC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	396	3	1	4	4.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c2ccccc12	10.1016/j.bmcl.2015.10.013
	45486758	196137	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	341	4	0	4	4.4	CC(C)N(C(=O)c1ccc(F)cc1)c1nc(-c2ccccn2)cs1	10.1016/j.bmcl.2009.07.097
	CHEMBL572144	196137	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	341	4	0	4	4.4	CC(C)N(C(=O)c1ccc(F)cc1)c1nc(-c2ccccn2)cs1	10.1016/j.bmcl.2009.07.097
	57391670	70681	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	332	2	1	6	3.5	CNc1ccnc2sc3c(=O)n(-c4ccc(C#N)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951873	70681	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	332	2	1	6	3.5	CNc1ccnc2sc3c(=O)n(-c4ccc(C#N)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	118735962	118407	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	381	4	2	5	3.3	N#Cc1c(NCc2ccc(F)cc2)sc2c1CCN(C(=O)c1ccn[nH]1)C2	10.1016/j.ejmech.2015.04.060
	CHEMBL3422878	118407	0	None	-	1	Human	5.7	pIC50	=	5.7	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	381	4	2	5	3.3	N#Cc1c(NCc2ccc(F)cc2)sc2c1CCN(C(=O)c1ccn[nH]1)C2	10.1016/j.ejmech.2015.04.060
	57559552	83416	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	324	2	0	8	1.9	CN(C)c1ncnc2sc3c(=O)n(-c4cccnc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	CHEMBL2205929	83416	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	324	2	0	8	1.9	CN(C)c1ncnc2sc3c(=O)n(-c4cccnc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	5766223	193977	24	None	-	1	Rat	4.7	pIC50	=	4.7	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	337	4	0	3	5.1	COc1ccc(C(=O)/C=C/c2cc3cc(C)ccc3nc2Cl)cc1	10.1016/j.bmc.2009.05.072
	CHEMBL556430	193977	24	None	-	1	Rat	4.7	pIC50	=	4.7	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	337	4	0	3	5.1	COc1ccc(C(=O)/C=C/c2cc3cc(C)ccc3nc2Cl)cc1	10.1016/j.bmc.2009.05.072
	86627336	121687	2	None	-524	2	Rat	6.7	pIC50	=	6.7	Functional	Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis	ChEMBL	320	2	0	5	3.0	O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2ccccn2)CC1	10.1016/j.bmc.2015.05.008
	CHEMBL3597593	121687	2	None	-524	2	Rat	6.7	pIC50	=	6.7	Functional	Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis	ChEMBL	320	2	0	5	3.0	O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2ccccn2)CC1	10.1016/j.bmc.2015.05.008
	86711408	124592	0	None	-33	2	Human	5.7	pIC50	=	5.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	376	2	0	6	2.2	COC(=O)c1cccc2c1CCN1C(=O)CN=C(n3cnc(C4CC4)c3)C=C21	nan
	CHEMBL3644408	124592	0	None	-33	2	Human	5.7	pIC50	=	5.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	376	2	0	6	2.2	COC(=O)c1cccc2c1CCN1C(=O)CN=C(n3cnc(C4CC4)c3)C=C21	nan
	89980392	124549	0	None	-346	2	Human	5.7	pIC50	=	5.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	394	3	0	5	3.3	CO[C@H](C)c1cn(C2=NCC(=O)N3CCc4c(ccc(F)c4C4CC4)C3=C2)cn1	nan
	CHEMBL3644363	124549	0	None	-346	2	Human	5.7	pIC50	=	5.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	394	3	0	5	3.3	CO[C@H](C)c1cn(C2=NCC(=O)N3CCc4c(ccc(F)c4C4CC4)C3=C2)cn1	nan
	122196117	123732	0	None	12	2	Human	6.7	pIC50	=	6.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	382	3	1	6	3.1	Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(Cl)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634439	123732	0	None	12	2	Human	6.7	pIC50	=	6.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	382	3	1	6	3.1	Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(Cl)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	54582946	62442	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	390	3	1	9	3.0	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5ncsc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784076	62442	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	390	3	1	9	3.0	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5ncsc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	49788727	18132	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology	ChEMBL	465	17	5	5	2.8	NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)C1CCCCC1	10.1021/jm100886h
	CHEMBL1270719	18132	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology	ChEMBL	465	17	5	5	2.8	NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)C1CCCCC1	10.1021/jm100886h
	54583943	62443	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	373	3	1	8	3.2	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5occc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784077	62443	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	373	3	1	8	3.2	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5occc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	11688952	80427	0	None	-	1	Rat	7.7	pIC50	=	7.7	Functional	Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells	ChEMBL	354	2	0	6	3.5	Cc1ccc(-n2cnc3c(sc4cncc(N(C)C)c43)c2=O)cc1F	10.1016/j.bmcl.2006.06.053
	CHEMBL215240	80427	0	None	-	1	Rat	7.7	pIC50	=	7.7	Functional	Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells	ChEMBL	354	2	0	6	3.5	Cc1ccc(-n2cnc3c(sc4cncc(N(C)C)c43)c2=O)cc1F	10.1016/j.bmcl.2006.06.053
	122196100	123716	0	None	19	2	Human	7.7	pIC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	374	3	1	4	4.3	Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O	10.1016/j.bmcl.2015.10.013
	CHEMBL3634423	123716	0	None	19	2	Human	7.7	pIC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	374	3	1	4	4.3	Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O	10.1016/j.bmcl.2015.10.013
	45484880	195185	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	321	4	1	5	2.8	Cc1c(-c2ccc(C(=O)NC(C)C)cc2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	CHEMBL565948	195185	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	321	4	1	5	2.8	Cc1c(-c2ccc(C(=O)NC(C)C)cc2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	45486764	195180	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	373	3	0	4	4.2	CN(C(=O)c1ccc(Br)cc1)c1nc(-c2ccncc2)cs1	10.1016/j.bmcl.2009.07.097
	CHEMBL565934	195180	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	373	3	0	4	4.2	CN(C(=O)c1ccc(Br)cc1)c1nc(-c2ccncc2)cs1	10.1016/j.bmcl.2009.07.097
	73334944	132500	0	None	-8	2	Human	6.7	pIC50	=	6.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	322	2	0	4	2.8	COc1cccc2c1CCN1C(=O)CN=C(c3ccc(C)o3)C=C21	nan
	CHEMBL3702362	132500	0	None	-8	2	Human	6.7	pIC50	=	6.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	322	2	0	4	2.8	COc1cccc2c1CCN1C(=O)CN=C(c3ccc(C)o3)C=C21	nan
	71561201	87414	0	None	-35	2	Rat	5.7	pIC50	=	5.7	Functional	Antagonist activity at rat mGluR1 expressed in HEK293 cells assessed as inhibition of Ca2+ mobilization by FLIPR assayAntagonist activity at rat mGluR1 expressed in HEK293 cells assessed as inhibition of Ca2+ mobilization by FLIPR assay	ChEMBL	374	4	2	2	4.0	O=C(N[C@@H]1CCC[C@@H](NC(=O)c2cccc(Cl)c2)C1)c1cccc(F)c1	10.1016/j.bmcl.2012.12.078
	CHEMBL2338567	87414	0	None	-35	2	Rat	5.7	pIC50	=	5.7	Functional	Antagonist activity at rat mGluR1 expressed in HEK293 cells assessed as inhibition of Ca2+ mobilization by FLIPR assayAntagonist activity at rat mGluR1 expressed in HEK293 cells assessed as inhibition of Ca2+ mobilization by FLIPR assay	ChEMBL	374	4	2	2	4.0	O=C(N[C@@H]1CCC[C@@H](NC(=O)c2cccc(Cl)c2)C1)c1cccc(F)c1	10.1016/j.bmcl.2012.12.078
	24777815	94502	0	None	2	2	Rat	4.7	pIC50	=	4.7	Functional	Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay	ChEMBL	329	3	1	4	3.3	CN(C)C(=O)c1cc2c(nc1NC1CCCC1)CC(C)(C)CC2=O	10.1021/jm0611298
	CHEMBL254429	94502	0	None	2	2	Rat	4.7	pIC50	=	4.7	Functional	Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay	ChEMBL	329	3	1	4	3.3	CN(C)C(=O)c1cc2c(nc1NC1CCCC1)CC(C)(C)CC2=O	10.1021/jm0611298
	11323495	94247	1	None	-1	2	Rat	4.7	pIC50	=	4.7	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	281	3	0	3	3.8	CC1(C)CC(=O)c2ccc(OCc3ccccc3)nc2C1	10.1021/jm0611298
	CHEMBL1204390	94247	1	None	-1	2	Rat	4.7	pIC50	=	4.7	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	281	3	0	3	3.8	CC1(C)CC(=O)c2ccc(OCc3ccccc3)nc2C1	10.1021/jm0611298
	CHEMBL252734	94247	1	None	-1	2	Rat	4.7	pIC50	=	4.7	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	281	3	0	3	3.8	CC1(C)CC(=O)c2ccc(OCc3ccccc3)nc2C1	10.1021/jm0611298
	54585852	62437	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	381	4	1	8	2.6	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784071	62437	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	381	4	1	8	2.6	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	127031562	138523	0	None	-	1	Rat	5.7	pIC50	=	5.7	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	334	2	2	6	3.1	Nc1nc(NC2C3CC4CC(C3)CC2C4)c2nn3ccccc3c2n1	10.1016/j.bmcl.2016.03.026
	CHEMBL3786157	138523	0	None	-	1	Rat	5.7	pIC50	=	5.7	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	334	2	2	6	3.1	Nc1nc(NC2C3CC4CC(C3)CC2C4)c2nn3ccccc3c2n1	10.1016/j.bmcl.2016.03.026
	127031562	138523	0	None	-	1	Rat	5.7	pIC50	=	5.7	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	334	2	2	6	3.1	Nc1nc(NC2C3CC4CC(C3)CC2C4)c2nn3ccccc3c2n1	10.1016/j.bmcl.2016.03.026
	CHEMBL3786157	138523	0	None	-	1	Rat	5.7	pIC50	=	5.7	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	334	2	2	6	3.1	Nc1nc(NC2C3CC4CC(C3)CC2C4)c2nn3ccccc3c2n1	10.1016/j.bmcl.2016.03.026
	54579959	62444	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	389	3	1	8	3.7	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5sccc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784078	62444	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	389	3	1	8	3.7	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5sccc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	45484920	195612	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	304	4	0	5	3.2	Cc1c(-c2ccc(C(=O)C3CC3)cc2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	CHEMBL568648	195612	0	None	-	1	Human	7.7	pIC50	=	7.7	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	304	4	0	5	3.2	Cc1c(-c2ccc(C(=O)C3CC3)cc2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	73335340	132527	0	None	2	2	Human	7.7	pIC50	=	7.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	318	1	0	3	3.0	C#Cc1cccc2c1CCN1C(=O)CN=C(c3cccs3)C=C21	nan
	CHEMBL3702389	132527	0	None	2	2	Human	7.7	pIC50	=	7.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	318	1	0	3	3.0	C#Cc1cccc2c1CCN1C(=O)CN=C(c3cccs3)C=C21	nan
	122196095	123711	0	None	12	2	Human	7.7	pIC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	364	3	1	4	3.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(F)c1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634418	123711	0	None	12	2	Human	7.7	pIC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	364	3	1	4	3.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)c(F)c1	10.1016/j.bmcl.2015.10.013
	122196121	123736	0	None	22	2	Human	7.7	pIC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	430	3	1	4	5.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c2ccccc12	10.1016/j.bmcl.2015.10.013
	CHEMBL3634443	123736	0	None	22	2	Human	7.7	pIC50	=	7.7	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	430	3	1	4	5.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c2ccccc12	10.1016/j.bmcl.2015.10.013
	44588462	174978	0	None	4	2	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	327	2	0	6	2.7	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccncc3)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL457873	174978	0	None	4	2	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	327	2	0	6	2.7	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccncc3)nn2)CC1	10.1016/j.bmc.2008.09.060
	44442430	154087	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	370	2	0	5	4.2	Cc1nc2c(cnn2-c2cccc(Cl)c2)c(=O)n1-c1ccc(Cl)cc1	10.1016/j.bmcl.2007.05.028
	CHEMBL399309	154087	0	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	370	2	0	5	4.2	Cc1nc2c(cnn2-c2cccc(Cl)c2)c(=O)n1-c1ccc(Cl)cc1	10.1016/j.bmcl.2007.05.028
	73335826	132589	0	None	-24	2	Human	6.7	pIC50	=	6.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	376	3	0	5	3.0	COCc1cn(C2=NCC(=O)N3CCc4c(cccc4C4CCC4)C3=C2)cn1	nan
	CHEMBL3702450	132589	0	None	-24	2	Human	6.7	pIC50	=	6.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	376	3	0	5	3.0	COCc1cn(C2=NCC(=O)N3CCc4c(cccc4C4CCC4)C3=C2)cn1	nan
	73334852	124600	0	None	-23	2	Human	5.7	pIC50	=	5.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	348	3	0	4	2.9	COc1cccc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)c1	nan
	CHEMBL3644416	124600	0	None	-23	2	Human	5.7	pIC50	=	5.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	348	3	0	4	2.9	COc1cccc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)c1	nan
	89979353	132535	0	None	-8	2	Human	5.7	pIC50	=	5.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	322	2	1	5	1.1	Cn1cc(C2=NCC(=O)N3CCc4c(CO)cccc4C3=C2)cn1	nan
	CHEMBL3702397	132535	0	None	-8	2	Human	5.7	pIC50	=	5.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	322	2	1	5	1.1	Cn1cc(C2=NCC(=O)N3CCc4c(CO)cccc4C3=C2)cn1	nan
	78321442	113845	3	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	368	3	0	5	4.8	COc1ccc(-n2cnc3c(-c4ccccc4Cl)csc3c2=O)cc1	10.1016/j.ejmech.2014.08.027
	CHEMBL3330820	113845	3	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	368	3	0	5	4.8	COc1ccc(-n2cnc3c(-c4ccccc4Cl)csc3c2=O)cc1	10.1016/j.ejmech.2014.08.027
	78322062	113847	3	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	348	3	0	5	4.4	COc1ccc(-n2cnc3c(-c4cccc(C)c4)csc3c2=O)cc1	10.1016/j.ejmech.2014.08.027
	CHEMBL3330824	113847	3	None	-	1	Human	6.7	pIC50	=	6.7	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	348	3	0	5	4.4	COc1ccc(-n2cnc3c(-c4cccc(C)c4)csc3c2=O)cc1	10.1016/j.ejmech.2014.08.027
	67425734	88658	0	None	-48	2	Human	5.7	pIC50	=	5.7	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	403	4	1	6	4.7	Cc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2334973	88658	0	None	-48	2	Human	5.7	pIC50	=	5.7	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	403	4	1	6	4.7	Cc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2365251	88658	0	None	-48	2	Human	5.7	pIC50	=	5.7	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	403	4	1	6	4.7	Cc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	127033450	138659	0	None	-	1	Rat	6.7	pIC50	=	6.7	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	281	2	1	5	3.4	c1ccn2nc3c(NC4CCCCCC4)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	CHEMBL3787631	138659	0	None	-	1	Rat	6.7	pIC50	=	6.7	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	281	2	1	5	3.4	c1ccn2nc3c(NC4CCCCCC4)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	127031256	138483	0	None	-	1	Rat	5.7	pIC50	=	5.7	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	3	1	5	3.7	C[C@H](Nc1ncnc2c1nn1ccccc21)C1CCCCC1	10.1016/j.bmcl.2016.03.026
	CHEMBL3785675	138483	0	None	-	1	Rat	5.7	pIC50	=	5.7	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	3	1	5	3.7	C[C@H](Nc1ncnc2c1nn1ccccc21)C1CCCCC1	10.1016/j.bmcl.2016.03.026
	127031256	138483	0	None	-	1	Rat	5.7	pIC50	=	5.7	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	3	1	5	3.7	C[C@H](Nc1ncnc2c1nn1ccccc21)C1CCCCC1	10.1016/j.bmcl.2016.03.026
	CHEMBL3785675	138483	0	None	-	1	Rat	5.7	pIC50	=	5.7	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	3	1	5	3.7	C[C@H](Nc1ncnc2c1nn1ccccc21)C1CCCCC1	10.1016/j.bmcl.2016.03.026
	127033450	138659	0	None	-	1	Rat	6.7	pIC50	=	6.7	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	281	2	1	5	3.4	c1ccn2nc3c(NC4CCCCCC4)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	CHEMBL3787631	138659	0	None	-	1	Rat	6.7	pIC50	=	6.7	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	281	2	1	5	3.4	c1ccn2nc3c(NC4CCCCCC4)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	3951963	194915	1	None	-	1	Rat	4.7	pIC50	=	4.7	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	379	8	0	3	6.6	CCCCCc1ccc(-c2ccc(OC(=O)C3CCC(CC)CC3)cc2)nc1	10.1016/j.bmc.2009.05.072
	CHEMBL564000	194915	1	None	-	1	Rat	4.7	pIC50	=	4.7	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	379	8	0	3	6.6	CCCCCc1ccc(-c2ccc(OC(=O)C3CCC(CC)CC3)cc2)nc1	10.1016/j.bmc.2009.05.072
	44431047	91920	0	None	-	1	Rat	6.7	pIC50	=	6.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	323	2	3	2	2.4	O=C(NC1CC2CCC1C2)c1ccc2[nH]c3c(c2c1)CCNC3=O	10.1016/j.bmcl.2007.01.055
	CHEMBL243020	91920	0	None	-	1	Rat	6.7	pIC50	=	6.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	323	2	3	2	2.4	O=C(NC1CC2CCC1C2)c1ccc2[nH]c3c(c2c1)CCNC3=O	10.1016/j.bmcl.2007.01.055
	89979891	124584	0	None	-28	2	Human	6.7	pIC50	=	6.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	359	2	0	5	2.7	O=C1CN=C(n2cnc(C3CC3)n2)C=C2c3cccc(C4CC4)c3CCN12	nan
	CHEMBL3644400	124584	0	None	-28	2	Human	6.7	pIC50	=	6.7	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	359	2	0	5	2.7	O=C1CN=C(n2cnc(C3CC3)n2)C=C2c3cccc(C4CC4)c3CCN12	nan
	159548	54424	11	None	-	1	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology	ChEMBL	435	18	6	6	1.0	CCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCNCCCCNCCCN	10.1021/jm100886h
	CHEMBL16117	54424	11	None	-	1	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology	ChEMBL	435	18	6	6	1.0	CCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCCCNCCCCNCCCN	10.1021/jm100886h
	11667270	84728	0	None	1	3	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	340	2	0	6	3.2	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1021/jm0504407
	CHEMBL225124	84728	0	None	1	3	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	340	2	0	6	3.2	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1021/jm0504407
	44442434	154037	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	337	2	0	6	2.9	Cc1nc2c(cnn2-c2cccnc2)c(=O)n1-c1ccc(Cl)cc1	10.1016/j.bmcl.2007.05.028
	CHEMBL399128	154037	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	337	2	0	6	2.9	Cc1nc2c(cnn2-c2cccnc2)c(=O)n1-c1ccc(Cl)cc1	10.1016/j.bmcl.2007.05.028
	45486755	196081	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	313	3	0	4	3.6	CN(C(=O)c1ccc(F)cc1)c1nc(-c2cccnc2)cs1	10.1016/j.bmcl.2009.07.097
	CHEMBL571687	196081	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	313	3	0	4	3.6	CN(C(=O)c1ccc(F)cc1)c1nc(-c2cccnc2)cs1	10.1016/j.bmcl.2009.07.097
	24777317	94280	0	None	-	1	Rat	5.6	pIC50	=	5.6	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	257	3	1	4	2.9	CCCNc1nc2c(cc1C#N)C(=O)CC(C)(C)C2	10.1021/jm0611298
	CHEMBL252943	94280	0	None	-	1	Rat	5.6	pIC50	=	5.6	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	257	3	1	4	2.9	CCCNc1nc2c(cc1C#N)C(=O)CC(C)(C)C2	10.1021/jm0611298
	86711394	124609	0	None	-19	2	Human	5.6	pIC50	=	5.6	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	378	2	0	4	3.5	CCc1cn(C2=NCC(=O)N3CCc4c(cccc4C4(F)CCC4)C3=C2)cn1	nan
	CHEMBL3644425	124609	0	None	-19	2	Human	5.6	pIC50	=	5.6	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	378	2	0	4	3.5	CCc1cn(C2=NCC(=O)N3CCc4c(cccc4C4(F)CCC4)C3=C2)cn1	nan
	89980108	132536	0	None	-66	2	Human	5.6	pIC50	=	5.6	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	360	3	0	4	3.1	COc1cccc(C2=NCC(=O)N3CCc4c(C(C)=O)cccc4C3=C2)c1	nan
	CHEMBL3702398	132536	0	None	-66	2	Human	5.6	pIC50	=	5.6	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	360	3	0	4	3.1	COc1cccc(C2=NCC(=O)N3CCc4c(C(C)=O)cccc4C3=C2)c1	nan
	24777814	94501	0	None	-	1	Rat	4.6	pIC50	=	4.6	Functional	Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay	ChEMBL	302	3	2	4	3.3	CC1(C)CC(=O)c2cc(C(=O)O)c(NC3CCCC3)nc2C1	10.1021/jm0611298
	CHEMBL254428	94501	0	None	-	1	Rat	4.6	pIC50	=	4.6	Functional	Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay	ChEMBL	302	3	2	4	3.3	CC1(C)CC(=O)c2cc(C(=O)O)c(NC3CCCC3)nc2C1	10.1021/jm0611298
	127033321	138526	0	None	-	1	Rat	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	279	2	1	5	2.9	c1ccn2nc3c(N[C@H]4C[C@@H]5CC[C@H]4C5)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	CHEMBL3786174	138526	0	None	-	1	Rat	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	279	2	1	5	2.9	c1ccn2nc3c(N[C@H]4C[C@@H]5CC[C@H]4C5)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	127031849	138593	0	None	8	2	Rat	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	321	2	1	5	3.8	C[C@@H]1[C@@H](Nc2ncnc3c2nn2ccccc32)C[C@H]2C[C@@H]1C2(C)C	10.1016/j.bmcl.2016.03.026
	CHEMBL3786866	138593	0	None	8	2	Rat	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	321	2	1	5	3.8	C[C@@H]1[C@@H](Nc2ncnc3c2nn2ccccc32)C[C@H]2C[C@@H]1C2(C)C	10.1016/j.bmcl.2016.03.026
	127033321	138526	0	None	-	1	Rat	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	279	2	1	5	2.9	c1ccn2nc3c(N[C@H]4C[C@@H]5CC[C@H]4C5)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	CHEMBL3786174	138526	0	None	-	1	Rat	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	279	2	1	5	2.9	c1ccn2nc3c(N[C@H]4C[C@@H]5CC[C@H]4C5)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	127031849	138593	0	None	8	2	Rat	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	321	2	1	5	3.8	C[C@@H]1[C@@H](Nc2ncnc3c2nn2ccccc32)C[C@H]2C[C@@H]1C2(C)C	10.1016/j.bmcl.2016.03.026
	CHEMBL3786866	138593	0	None	8	2	Rat	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	321	2	1	5	3.8	C[C@@H]1[C@@H](Nc2ncnc3c2nn2ccccc32)C[C@H]2C[C@@H]1C2(C)C	10.1016/j.bmcl.2016.03.026
	89979722	124583	0	None	-2344	2	Human	5.6	pIC50	=	5.6	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	385	2	0	6	3.1	O=C1CN=C(n2cnc(-c3ccno3)c2)C=C2c3cccc(C4CC4)c3CCN12	nan
	CHEMBL3644399	124583	0	None	-2344	2	Human	5.6	pIC50	=	5.6	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	385	2	0	6	3.1	O=C1CN=C(n2cnc(-c3ccno3)c2)C=C2c3cccc(C4CC4)c3CCN12	nan
	57908398	88665	0	None	-8	2	Human	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	389	4	1	6	4.4	C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1ccccn1	10.1016/j.bmcl.2013.01.009
	CHEMBL2334972	88665	0	None	-8	2	Human	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	389	4	1	6	4.4	C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1ccccn1	10.1016/j.bmcl.2013.01.009
	CHEMBL2365366	88665	0	None	-8	2	Human	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	389	4	1	6	4.4	C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1ccccn1	10.1016/j.bmcl.2013.01.009
	118735976	118417	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	409	4	1	4	4.7	N#Cc1c(NCc2cccc(F)c2)sc2c1CCN(C(=O)c1ccc(F)cc1)C2	10.1016/j.ejmech.2015.04.060
	CHEMBL3422892	118417	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	409	4	1	4	4.7	N#Cc1c(NCc2cccc(F)c2)sc2c1CCN(C(=O)c1ccc(F)cc1)C2	10.1016/j.ejmech.2015.04.060
	44431052	165954	0	None	-	1	Rat	6.6	pIC50	=	6.6	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	286	2	2	2	3.3	CC(Oc1ccc2[nH]c3c(c2c1)CCNC3=O)C(C)(C)C	10.1016/j.bmcl.2007.01.055
	CHEMBL427870	165954	0	None	-	1	Rat	6.6	pIC50	=	6.6	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	286	2	2	2	3.3	CC(Oc1ccc2[nH]c3c(c2c1)CCNC3=O)C(C)(C)C	10.1016/j.bmcl.2007.01.055
	3121216	194109	14	None	-	1	Rat	4.6	pIC50	=	4.6	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	300	6	0	3	4.4	CCCCCCc1cc2c3c(c(=O)oc2cc1OC)CCC3	10.1016/j.bmc.2009.05.072
	CHEMBL557769	194109	14	None	-	1	Rat	4.6	pIC50	=	4.6	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	300	6	0	3	4.4	CCCCCCc1cc2c3c(c(=O)oc2cc1OC)CCC3	10.1016/j.bmc.2009.05.072
	721080	194359	20	None	-	1	Rat	4.6	pIC50	=	4.6	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	346	4	0	3	5.2	O=c1cc(-c2ccccc2)c2ccc(OCc3ccc(F)cc3)cc2o1	10.1016/j.bmc.2009.05.072
	CHEMBL560273	194359	20	None	-	1	Rat	4.6	pIC50	=	4.6	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	346	4	0	3	5.2	O=c1cc(-c2ccccc2)c2ccc(OCc3ccc(F)cc3)cc2o1	10.1016/j.bmc.2009.05.072
	71682339	90608	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@H]1CN(c2ccccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397348	90608	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@H]1CN(c2ccccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	57559578	83399	0	None	-	1	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	407	4	1	8	3.4	COc1ccc(-n2cnc3c(sc4ncnc(NCC(F)(F)F)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205911	83399	0	None	-	1	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	407	4	1	8	3.4	COc1ccc(-n2cnc3c(sc4ncnc(NCC(F)(F)F)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	19705292	188614	0	None	-2	3	Mouse	7.6	pIC50	=	7.6	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	326	2	0	5	3.3	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccc3)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL511355	188614	0	None	-2	3	Mouse	7.6	pIC50	=	7.6	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	326	2	0	5	3.3	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccc3)nn2)CC1	10.1016/j.bmc.2008.09.060
	16659804	88316	0	None	-	1	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	384	1	1	7	3.8	C[C@@H]1COc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c2N1	10.1021/jm070590c
	CHEMBL236178	88316	0	None	-	1	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	384	1	1	7	3.8	C[C@@H]1COc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c2N1	10.1021/jm070590c
	44442425	93168	0	None	15	2	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	323	2	0	6	2.4	Cc1nc2c(cnn2-c2ccccc2)c(=O)n1N1CCCCCC1	10.1016/j.bmcl.2007.05.028
	CHEMBL246609	93168	0	None	15	2	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	323	2	0	6	2.4	Cc1nc2c(cnn2-c2ccccc2)c(=O)n1N1CCCCCC1	10.1016/j.bmcl.2007.05.028
	15207262	93492	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	318	2	1	6	2.6	Cc1nc2c(cnn2-c2ccccc2)c(=O)n1-c1ccc(O)cc1	10.1016/j.bmcl.2007.05.028
	CHEMBL248209	93492	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	318	2	1	6	2.6	Cc1nc2c(cnn2-c2ccccc2)c(=O)n1-c1ccc(O)cc1	10.1016/j.bmcl.2007.05.028
	45484872	195540	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	322	4	0	6	3.2	Cc1c(-c2cccc(C(=O)OC(C)C)c2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	CHEMBL568241	195540	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	322	4	0	6	3.2	Cc1c(-c2cccc(C(=O)OC(C)C)c2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	89980695	132594	0	None	-169	2	Human	5.6	pIC50	=	5.6	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	427	2	0	5	4.0	O=C1CN=C(n2cnc(C3CCC3)c2)C=C2c3cccc(-c4cccnc4F)c3CCN12	nan
	CHEMBL3702455	132594	0	None	-169	2	Human	5.6	pIC50	=	5.6	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	427	2	0	5	4.0	O=C1CN=C(n2cnc(C3CCC3)c2)C=C2c3cccc(-c4cccnc4F)c3CCN12	nan
	54586363	62340	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	392	4	1	8	3.7	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc5c(c4)OCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783873	62340	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	392	4	1	8	3.7	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc5c(c4)OCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	692972	93337	13	None	39	2	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	336	2	0	5	3.5	Cc1nc2c(cnn2-c2ccccc2)c(=O)n1-c1ccc(Cl)cc1	10.1016/j.bmcl.2007.05.028
	CHEMBL247438	93337	13	None	39	2	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	336	2	0	5	3.5	Cc1nc2c(cnn2-c2ccccc2)c(=O)n1-c1ccc(Cl)cc1	10.1016/j.bmcl.2007.05.028
	71682339	90608	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@H]1CN(c2ccccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397348	90608	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@H]1CN(c2ccccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	127034033	138502	0	None	10	2	Rat	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	301	2	1	5	2.9	c1ccc2c(c1)CC(Nc1ncnc3c1nn1ccccc31)C2	10.1016/j.bmcl.2016.03.026
	CHEMBL3785879	138502	0	None	10	2	Rat	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	301	2	1	5	2.9	c1ccc2c(c1)CC(Nc1ncnc3c1nn1ccccc31)C2	10.1016/j.bmcl.2016.03.026
	118735961	118406	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	395	4	2	5	3.6	Cc1cc(C(=O)N2CCc3c(sc(NCc4ccc(F)cc4)c3C#N)C2)[nH]n1	10.1016/j.ejmech.2015.04.060
	CHEMBL3422877	118406	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	395	4	2	5	3.6	Cc1cc(C(=O)N2CCc3c(sc(NCc4ccc(F)cc4)c3C#N)C2)[nH]n1	10.1016/j.ejmech.2015.04.060
	71683123	90620	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	363	2	0	3	3.8	C[C@@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccc1C#N	10.1016/j.bmcl.2013.05.020
	CHEMBL2397379	90620	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	363	2	0	3	3.8	C[C@@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccc1C#N	10.1016/j.bmcl.2013.05.020
	71683123	90620	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	363	2	0	3	3.8	C[C@@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccc1C#N	10.1016/j.bmcl.2013.05.020
	CHEMBL2397379	90620	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	363	2	0	3	3.8	C[C@@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccc1C#N	10.1016/j.bmcl.2013.05.020
	127034033	138502	0	None	10	2	Rat	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	301	2	1	5	2.9	c1ccc2c(c1)CC(Nc1ncnc3c1nn1ccccc31)C2	10.1016/j.bmcl.2016.03.026
	CHEMBL3785879	138502	0	None	10	2	Rat	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	301	2	1	5	2.9	c1ccc2c(c1)CC(Nc1ncnc3c1nn1ccccc31)C2	10.1016/j.bmcl.2016.03.026
	44408476	139808	0	None	-	1	Rat	7.6	pIC50	=	7.6	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	342	4	0	4	3.1	Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CC(F)F)CC2	10.1016/j.bmcl.2005.11.049
	CHEMBL380698	139808	0	None	-	1	Rat	7.6	pIC50	=	7.6	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	342	4	0	4	3.1	Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CC(F)F)CC2	10.1016/j.bmcl.2005.11.049
	45484964	196692	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	275	2	1	4	3.1	Cc1c(-c2ccc3[nH]ccc3c2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	CHEMBL576637	196692	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	275	2	1	4	3.1	Cc1c(-c2ccc3[nH]ccc3c2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	24777577	94200	0	None	-	1	Rat	5.6	pIC50	=	5.6	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	305	3	1	4	3.7	CC1(C)CC(=O)c2cc(C#N)c(NCc3ccccc3)nc2C1	10.1021/jm0611298
	CHEMBL252333	94200	0	None	-	1	Rat	5.6	pIC50	=	5.6	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	305	3	1	4	3.7	CC1(C)CC(=O)c2cc(C#N)c(NCc3ccccc3)nc2C1	10.1021/jm0611298
	3421	3488	35	None	1	4	Human	4.6	pIC50	=	4.6	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1021/jm060950g
	5311040	3488	35	None	1	4	Human	4.6	pIC50	=	4.6	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1021/jm060950g
	CHEMBL43412	3488	35	None	1	4	Human	4.6	pIC50	=	4.6	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1021/jm060950g
	24777578	94224	0	None	3	2	Rat	4.6	pIC50	=	4.6	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	291	3	0	4	3.1	CN(Cc1ccccc1)c1nc2c(cc1C#N)C(=O)CCC2	10.1021/jm0611298
	CHEMBL252531	94224	0	None	3	2	Rat	4.6	pIC50	=	4.6	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	291	3	0	4	3.1	CN(Cc1ccccc1)c1nc2c(cc1C#N)C(=O)CCC2	10.1021/jm0611298
	10444977	154225	7	None	-13	2	Rat	4.6	pIC50	=	4.6	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	253	3	0	3	3.2	O=C1CCCc2nc(OCc3ccccc3)ccc21	10.1021/jm0611298
	CHEMBL400104	154225	7	None	-13	2	Rat	4.6	pIC50	=	4.6	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	253	3	0	3	3.2	O=C1CCCc2nc(OCc3ccccc3)ccc21	10.1021/jm0611298
	22268047	46052	9	None	-	1	Human	4.6	pIC50	=	4.6	Functional	Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.	ChEMBL	185	3	3	3	-0.3	NC(C(=O)O)C12CC(C(=O)O)(C1)C2	10.1021/jm990353c
	CHEMBL153572	46052	9	None	-	1	Human	4.6	pIC50	=	4.6	Functional	Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.	ChEMBL	185	3	3	3	-0.3	NC(C(=O)O)C12CC(C(=O)O)(C1)C2	10.1021/jm990353c
	3421	3488	35	None	1	4	Human	4.6	pIC50	=	4.6	Functional	The compound was tested for inhibitory effect on second messenger formation in BHK cells expressing mGluR1aThe compound was tested for inhibitory effect on second messenger formation in BHK cells expressing mGluR1a	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1021/jm960254o
	5311040	3488	35	None	1	4	Human	4.6	pIC50	=	4.6	Functional	The compound was tested for inhibitory effect on second messenger formation in BHK cells expressing mGluR1aThe compound was tested for inhibitory effect on second messenger formation in BHK cells expressing mGluR1a	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1021/jm960254o
	CHEMBL43412	3488	35	None	1	4	Human	4.6	pIC50	=	4.6	Functional	The compound was tested for inhibitory effect on second messenger formation in BHK cells expressing mGluR1aThe compound was tested for inhibitory effect on second messenger formation in BHK cells expressing mGluR1a	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1021/jm960254o
	11501188	137018	0	None	1	2	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	350	3	0	6	3.6	CCc1ccccc1-n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1021/jm0504407
	CHEMBL375439	137018	0	None	1	2	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	350	3	0	6	3.6	CCc1ccccc1-n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1021/jm0504407
	44408492	75076	0	None	-	1	Rat	6.6	pIC50	=	6.6	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	336	5	0	5	2.5	COCCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O	10.1016/j.bmcl.2005.11.049
	CHEMBL204149	75076	0	None	-	1	Rat	6.6	pIC50	=	6.6	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	336	5	0	5	2.5	COCCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O	10.1016/j.bmcl.2005.11.049
	44408472	75211	0	None	-	1	Rat	6.6	pIC50	=	6.6	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	368	4	0	4	4.0	Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(Cc1ccccc1)CC2	10.1016/j.bmcl.2005.11.049
	CHEMBL204532	75211	0	None	-	1	Rat	6.6	pIC50	=	6.6	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	368	4	0	4	4.0	Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(Cc1ccccc1)CC2	10.1016/j.bmcl.2005.11.049
	71683124	90601	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	357	2	0	3	3.5	C[C@@H]1CN(c2cccc(F)n2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397341	90601	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	357	2	0	3	3.5	C[C@@H]1CN(c2cccc(F)n2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	78322065	113850	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	364	4	0	6	4.1	COc1ccc(-n2cnc3c(-c4cccc(OC)c4)csc3c2=O)cc1	10.1016/j.ejmech.2014.08.027
	CHEMBL3330827	113850	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	364	4	0	6	4.1	COc1ccc(-n2cnc3c(-c4cccc(OC)c4)csc3c2=O)cc1	10.1016/j.ejmech.2014.08.027
	71683124	90601	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	357	2	0	3	3.5	C[C@@H]1CN(c2cccc(F)n2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397341	90601	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	357	2	0	3	3.5	C[C@@H]1CN(c2cccc(F)n2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	11631279	141379	0	None	1	2	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	328	3	0	6	3.3	CN(C)c1ccnc2sc3c(=O)n(CC4CCCC4)cnc3c12	10.1021/jm0504407
	CHEMBL386935	141379	0	None	1	2	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	328	3	0	6	3.3	CN(C)c1ccnc2sc3c(=O)n(CC4CCCC4)cnc3c12	10.1021/jm0504407
	122196096	123712	0	None	10	2	Human	7.6	pIC50	=	7.6	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	378	3	1	4	4.1	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(F)c1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634419	123712	0	None	10	2	Human	7.6	pIC50	=	7.6	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	378	3	1	4	4.1	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(F)c1	10.1016/j.bmcl.2015.10.013
	3260619	3956	21	None	1	4	Rat	5.6	pIC50	=	5.6	Functional	Antagonist activity at rat mGluR1 expressed in Syrian golden hamster BHK cells assessed as potentiation of glutamate-induced calcium flux by fluorescence assayAntagonist activity at rat mGluR1 expressed in Syrian golden hamster BHK cells assessed as potentiation of glutamate-induced calcium flux by fluorescence assay	ChEMBL	321	2	0	5	3.7	CC1CCCN(C1)c1ncnc2c1cnn2c1ccc(cc1C)C	10.1016/j.bmcl.2008.08.087
	6227	3956	21	None	1	4	Rat	5.6	pIC50	=	5.6	Functional	Antagonist activity at rat mGluR1 expressed in Syrian golden hamster BHK cells assessed as potentiation of glutamate-induced calcium flux by fluorescence assayAntagonist activity at rat mGluR1 expressed in Syrian golden hamster BHK cells assessed as potentiation of glutamate-induced calcium flux by fluorescence assay	ChEMBL	321	2	0	5	3.7	CC1CCCN(C1)c1ncnc2c1cnn2c1ccc(cc1C)C	10.1016/j.bmcl.2008.08.087
	CHEMBL477396	3956	21	None	1	4	Rat	5.6	pIC50	=	5.6	Functional	Antagonist activity at rat mGluR1 expressed in Syrian golden hamster BHK cells assessed as potentiation of glutamate-induced calcium flux by fluorescence assayAntagonist activity at rat mGluR1 expressed in Syrian golden hamster BHK cells assessed as potentiation of glutamate-induced calcium flux by fluorescence assay	ChEMBL	321	2	0	5	3.7	CC1CCCN(C1)c1ncnc2c1cnn2c1ccc(cc1C)C	10.1016/j.bmcl.2008.08.087
	24777697	153829	0	None	-	1	Rat	5.6	pIC50	=	5.6	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	299	6	1	4	4.1	CCCCCCNc1nc2c(cc1C#N)C(=O)CC(C)(C)C2	10.1021/jm0611298
	CHEMBL398706	153829	0	None	-	1	Rat	5.6	pIC50	=	5.6	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	299	6	1	4	4.1	CCCCCCNc1nc2c(cc1C#N)C(=O)CC(C)(C)C2	10.1021/jm0611298
	89980646	124577	0	None	-109	2	Human	5.6	pIC50	=	5.6	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	376	3	0	5	3.3	C=C(C)c1cccc2c1CCN1C(=O)CN=C(n3cnc([C@H](C)OC)c3)C=C21	nan
	CHEMBL3644393	124577	0	None	-109	2	Human	5.6	pIC50	=	5.6	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	376	3	0	5	3.3	C=C(C)c1cccc2c1CCN1C(=O)CN=C(n3cnc([C@H](C)OC)c3)C=C21	nan
	71682963	90619	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	363	2	0	3	3.8	C[C@@H]1CN(c2ccccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397378	90619	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	363	2	0	3	3.8	C[C@@H]1CN(c2ccccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	71682963	90619	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	363	2	0	3	3.8	C[C@@H]1CN(c2ccccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397378	90619	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	363	2	0	3	3.8	C[C@@H]1CN(c2ccccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	127033449	138600	0	None	-	1	Rat	5.6	pIC50	=	5.6	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	267	2	1	5	3.0	c1ccn2nc3c(NC4CCCCC4)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	CHEMBL3786959	138600	0	None	-	1	Rat	5.6	pIC50	=	5.6	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	267	2	1	5	3.0	c1ccn2nc3c(NC4CCCCC4)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	46866192	1034	0	None	-	1	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	323	1	1	7	2.6	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)C	10.1016/j.bmcl.2010.03.004
	6210	1034	0	None	-	1	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	323	1	1	7	2.6	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)C	10.1016/j.bmcl.2010.03.004
	CHEMBL1093901	1034	0	None	-	1	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	323	1	1	7	2.6	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)C	10.1016/j.bmcl.2010.03.004
	16117046	70645	0	None	-	1	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	337	3	1	6	3.7	CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951680	70645	0	None	-	1	Human	7.6	pIC50	=	7.6	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	337	3	1	6	3.7	CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	73334939	132495	0	None	3	2	Human	7.6	pIC50	=	7.6	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	328	1	0	3	3.6	O=C1CN=C(c2cccs2)C=C2c3cccc(Cl)c3CCN12	nan
	CHEMBL3702357	132495	0	None	3	2	Human	7.6	pIC50	=	7.6	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	328	1	0	3	3.6	O=C1CN=C(c2cccs2)C=C2c3cccc(Cl)c3CCN12	nan
	122196097	123713	0	None	9	2	Human	7.6	pIC50	=	7.6	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(F)c1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634420	123713	0	None	9	2	Human	7.6	pIC50	=	7.6	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	398	3	1	4	4.4	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)c(F)c1	10.1016/j.bmcl.2015.10.013
	10382361	121682	0	None	-301	2	Rat	6.6	pIC50	=	6.6	Functional	Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis	ChEMBL	336	2	0	5	1.7	O=C(C#Cc1ccccc1)N1CCN(c2ncccc2[N+](=O)[O-])CC1	10.1016/j.bmc.2015.05.008
	CHEMBL3597584	121682	0	None	-301	2	Rat	6.6	pIC50	=	6.6	Functional	Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis	ChEMBL	336	2	0	5	1.7	O=C(C#Cc1ccccc1)N1CCN(c2ncccc2[N+](=O)[O-])CC1	10.1016/j.bmc.2015.05.008
	127033449	138600	0	None	-	1	Rat	5.6	pIC50	=	5.6	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	267	2	1	5	3.0	c1ccn2nc3c(NC4CCCCC4)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	CHEMBL3786959	138600	0	None	-	1	Rat	5.6	pIC50	=	5.6	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	267	2	1	5	3.0	c1ccn2nc3c(NC4CCCCC4)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	57881896	83406	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	401	4	1	8	4.1	COc1ccc(-n2cnc3c(sc4ncnc(Nc5ccccc5)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205919	83406	0	None	-	1	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	401	4	1	8	4.1	COc1ccc(-n2cnc3c(sc4ncnc(Nc5ccccc5)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	44230992	88647	0	None	-28	2	Human	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	417	5	1	6	4.9	CCc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2334976	88647	0	None	-28	2	Human	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	417	5	1	6	4.9	CCc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2365134	88647	0	None	-28	2	Human	6.6	pIC50	=	6.6	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	417	5	1	6	4.9	CCc1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	3347	2390	6	None	-	1	Human	7.6	pIC50	=	7.6	Functional	Negative allosteric modulation activity at recombinant human mGluR1a expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular Ca2+ mobilizationNegative allosteric modulation activity at recombinant human mGluR1a expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular Ca2+ mobilization	ChEMBL	341	5	2	5	3.0	OCCSc1nc(NC2Cc3c(C2)cccc3)c2c(n1)CCCC2	10.1016/j.bmcl.2016.03.026
	9840951	2390	6	None	-	1	Human	7.6	pIC50	=	7.6	Functional	Negative allosteric modulation activity at recombinant human mGluR1a expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular Ca2+ mobilizationNegative allosteric modulation activity at recombinant human mGluR1a expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular Ca2+ mobilization	ChEMBL	341	5	2	5	3.0	OCCSc1nc(NC2Cc3c(C2)cccc3)c2c(n1)CCCC2	10.1016/j.bmcl.2016.03.026
	CHEMBL3786530	2390	6	None	-	1	Human	7.6	pIC50	=	7.6	Functional	Negative allosteric modulation activity at recombinant human mGluR1a expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular Ca2+ mobilizationNegative allosteric modulation activity at recombinant human mGluR1a expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular Ca2+ mobilization	ChEMBL	341	5	2	5	3.0	OCCSc1nc(NC2Cc3c(C2)cccc3)c2c(n1)CCCC2	10.1016/j.bmcl.2016.03.026
	122196093	123709	0	None	16	2	Human	7.5	pIC50	=	7.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	380	3	1	4	4.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)cc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634416	123709	0	None	16	2	Human	7.5	pIC50	=	7.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	380	3	1	4	4.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)cc1	10.1016/j.bmcl.2015.10.013
	122196124	123739	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	380	3	1	4	4.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1Cl	10.1016/j.bmcl.2015.10.013
	CHEMBL3634446	123739	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	380	3	1	4	4.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1Cl	10.1016/j.bmcl.2015.10.013
	73335133	132511	0	None	-2	2	Human	5.6	pIC50	=	5.6	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	396	2	0	3	3.7	COc1cccc(C2=NCC(=O)N3CCc4c(Br)cccc4C3=C2)c1	nan
	CHEMBL3702373	132511	0	None	-2	2	Human	5.6	pIC50	=	5.6	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	396	2	0	3	3.7	COc1cccc(C2=NCC(=O)N3CCc4c(Br)cccc4C3=C2)c1	nan
	657896	141550	10	None	1	2	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	336	3	0	6	3.1	CN(C)c1ccnc2sc3c(=O)n(Cc4ccccc4)cnc3c12	10.1021/jm0504407
	CHEMBL388087	141550	10	None	1	2	Human	6.6	pIC50	=	6.6	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	336	3	0	6	3.1	CN(C)c1ccnc2sc3c(=O)n(Cc4ccccc4)cnc3c12	10.1021/jm0504407
	118735965	118408	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	373	4	1	4	4.4	N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1ccccc1)C2	10.1016/j.ejmech.2015.04.060
	CHEMBL3422881	118408	0	None	-	1	Human	5.6	pIC50	=	5.6	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	373	4	1	4	4.4	N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1ccccc1)C2	10.1016/j.ejmech.2015.04.060
	3483737	194176	2	None	-	1	Rat	4.6	pIC50	=	4.6	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	386	7	0	4	6.7	CCCCOc1ccc(-c2nnc(-c3ccc(-c4ccccc4)cc3)s2)cc1	10.1016/j.bmc.2009.05.072
	CHEMBL558521	194176	2	None	-	1	Rat	4.6	pIC50	=	4.6	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	386	7	0	4	6.7	CCCCOc1ccc(-c2nnc(-c3ccc(-c4ccccc4)cc3)s2)cc1	10.1016/j.bmc.2009.05.072
	44431056	151773	0	None	-	1	Rat	5.5	pIC50	=	5.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	292	3	2	2	3.0	O=C1NCCc2c1[nH]c1cc(OCc3ccccc3)ccc21	10.1016/j.bmcl.2007.01.055
	CHEMBL396956	151773	0	None	-	1	Rat	5.5	pIC50	=	5.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	292	3	2	2	3.0	O=C1NCCc2c1[nH]c1cc(OCc3ccccc3)ccc21	10.1016/j.bmcl.2007.01.055
	73336213	124605	0	None	-144	2	Human	6.5	pIC50	=	6.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	380	3	0	5	2.7	COCc1cn(C2=NCC(=O)N3CCc4c(ccc(F)c4C4CC4)C3=C2)cn1	nan
	CHEMBL3644421	124605	0	None	-144	2	Human	6.5	pIC50	=	6.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	380	3	0	5	2.7	COCc1cn(C2=NCC(=O)N3CCc4c(ccc(F)c4C4CC4)C3=C2)cn1	nan
	44588428	176258	0	None	-5	3	Mouse	6.5	pIC50	=	6.5	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	343	2	1	4	3.0	CC(C)(C)NC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL461034	176258	0	None	-5	3	Mouse	6.5	pIC50	=	6.5	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	343	2	1	4	3.0	CC(C)(C)NC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	118735968	118411	0	None	-	1	Human	5.5	pIC50	=	5.5	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	391	4	1	4	4.6	N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1cccc(F)c1)C2	10.1016/j.ejmech.2015.04.060
	CHEMBL3422884	118411	0	None	-	1	Human	5.5	pIC50	=	5.5	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	391	4	1	4	4.6	N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1cccc(F)c1)C2	10.1016/j.ejmech.2015.04.060
	72163837	91590	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	340	1	0	3	2.8	O=C(N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1)N1CCC2(CCCC2)C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418359	91590	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	340	1	0	3	2.8	O=C(N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1)N1CCC2(CCCC2)C1	10.1016/j.bmcl.2013.07.029
	72163837	91590	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	340	1	0	3	2.8	O=C(N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1)N1CCC2(CCCC2)C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418359	91590	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	340	1	0	3	2.8	O=C(N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1)N1CCC2(CCCC2)C1	10.1016/j.bmcl.2013.07.029
	5766228	193960	20	None	-	1	Rat	5.5	pIC50	=	5.5	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	313	3	0	3	5.2	Cc1ccc2cc(/C=C/C(=O)c3cccs3)c(Cl)nc2c1	10.1016/j.bmc.2009.05.072
	CHEMBL556293	193960	20	None	-	1	Rat	5.5	pIC50	=	5.5	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	313	3	0	3	5.2	Cc1ccc2cc(/C=C/C(=O)c3cccs3)c(Cl)nc2c1	10.1016/j.bmc.2009.05.072
	76321786	105126	0	None	-2041	2	Human	4.5	pIC50	=	4.5	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay	ChEMBL	351	4	0	6	2.6	C[C@@H]1CCCN1C(=O)c1nn(C)c2nc(OCc3ccccn3)ccc12	10.1021/jm401622k
	CHEMBL3122225	105126	0	None	-2041	2	Human	4.5	pIC50	=	4.5	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay	ChEMBL	351	4	0	6	2.6	C[C@@H]1CCCN1C(=O)c1nn(C)c2nc(OCc3ccccn3)ccc12	10.1021/jm401622k
	54584891	62433	0	None	-	1	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	367	3	1	7	3.1	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784067	62433	0	None	-	1	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	367	3	1	7	3.1	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	57881625	83287	0	None	3311	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	369	3	1	7	3.6	O=c1c2sc3ncnc(NC4CC4)c3c2ncn1-c1ccc(Cl)cc1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205371	83287	0	None	3311	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	369	3	1	7	3.6	O=c1c2sc3ncnc(NC4CC4)c3c2ncn1-c1ccc(Cl)cc1	10.1016/j.bmcl.2012.09.048
	57559280	83396	0	None	3311	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	367	4	0	8	2.9	CCN(C)c1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	CHEMBL2205909	83396	0	None	3311	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	367	4	0	8	2.9	CCN(C)c1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	11530404	208	11	None	1	4	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cellsAntagonist activity at human mGluR1 expressed in 1321N1 cells	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1016/j.bmcl.2006.06.053
	6211	208	11	None	1	4	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cellsAntagonist activity at human mGluR1 expressed in 1321N1 cells	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1016/j.bmcl.2006.06.053
	CHEMBL385336	208	11	None	1	4	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cellsAntagonist activity at human mGluR1 expressed in 1321N1 cells	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1016/j.bmcl.2006.06.053
	11530404	208	11	None	1	4	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1021/jm0504407
	6211	208	11	None	1	4	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1021/jm0504407
	CHEMBL385336	208	11	None	1	4	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1021/jm0504407
	16118398	70687	0	None	-	1	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	355	3	1	5	4.7	CCNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951879	70687	0	None	-	1	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	355	3	1	5	4.7	CCNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	11530404	208	11	None	1	4	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1021/jm060950g
	6211	208	11	None	1	4	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1021/jm060950g
	CHEMBL385336	208	11	None	1	4	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1021/jm060950g
	11772954	1019	0	None	1	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at mGluR1Antagonist activity at mGluR1	ChEMBL	365	8	3	7	2.0	OCCOCCNc1ncc2c(c1)c(ncn2)NC1Cc2c(C1)cccc2	10.1016/j.bmcl.2009.02.106
	6349	1019	0	None	1	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at mGluR1Antagonist activity at mGluR1	ChEMBL	365	8	3	7	2.0	OCCOCCNc1ncc2c(c1)c(ncn2)NC1Cc2c(C1)cccc2	10.1016/j.bmcl.2009.02.106
	CHEMBL469382	1019	0	None	1	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at mGluR1Antagonist activity at mGluR1	ChEMBL	365	8	3	7	2.0	OCCOCCNc1ncc2c(c1)c(ncn2)NC1Cc2c(C1)cccc2	10.1016/j.bmcl.2009.02.106
	7442	2104	3	None	-	1	Rat	8.5	pIC50	=	8.5	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	10.1021/jm0611298
	9948645	2104	3	None	-	1	Rat	8.5	pIC50	=	8.5	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	10.1021/jm0611298
	CHEMBL188906	2104	3	None	-	1	Rat	8.5	pIC50	=	8.5	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	10.1021/jm0611298
	CHEMBL253345	2104	3	None	-	1	Rat	8.5	pIC50	=	8.5	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	10.1021/jm0611298
	46886140	8389	0	None	-	1	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	341	1	2	8	2.6	Cc1ccc(-n2cnc3c(sc4nc(S)nc(N)c43)c2=O)cc1	10.1016/j.bmcl.2010.03.004
	CHEMBL1093869	8389	0	None	-	1	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	341	1	2	8	2.6	Cc1ccc(-n2cnc3c(sc4nc(S)nc(N)c43)c2=O)cc1	10.1016/j.bmcl.2010.03.004
	16118124	70636	0	None	-	1	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	378	2	0	7	4.3	CN(C)c1ccnc2sc3c(=O)n(-c4ccc5ncsc5c4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951669	70636	0	None	-	1	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	378	2	0	7	4.3	CN(C)c1ccnc2sc3c(=O)n(-c4ccc5ncsc5c4)ccc3c12	10.1016/j.bmcl.2011.12.131
	11245287	1667	29	None	1	4	Mouse	8.5	pIC50	=	8.5	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	10.1016/j.bmc.2008.09.060
	6363	1667	29	None	1	4	Mouse	8.5	pIC50	=	8.5	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	10.1016/j.bmc.2008.09.060
	CHEMBL502882	1667	29	None	1	4	Mouse	8.5	pIC50	=	8.5	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	10.1016/j.bmc.2008.09.060
	11772069	196837	0	None	331	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	337	3	0	5	2.8	CCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O	10.1016/j.bmcl.2009.07.145
	CHEMBL577833	196837	0	None	331	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	337	3	0	5	2.8	CCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O	10.1016/j.bmcl.2009.07.145
	11695894	174220	0	None	2	3	Mouse	8.5	pIC50	=	8.5	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	345	3	0	6	2.7	Cc1c(C2=CCN(C(=O)OC(C)C)CC2)nnn1-c1cccnc1F	10.1016/j.bmc.2008.09.060
	CHEMBL456196	174220	0	None	2	3	Mouse	8.5	pIC50	=	8.5	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	345	3	0	6	2.7	Cc1c(C2=CCN(C(=O)OC(C)C)CC2)nnn1-c1cccnc1F	10.1016/j.bmc.2008.09.060
	16118542	70652	0	None	-	1	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	321	2	1	5	4.0	CNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951688	70652	0	None	-	1	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	321	2	1	5	4.0	CNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	11175501	872	34	None	1819	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	349	3	0	5	2.9	O=C1N(Cc2c1ccc(c2)c1nnn(c1C)c1cccnc1F)C1CC1	10.1016/j.bmcl.2009.07.145
	6341	872	34	None	1819	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	349	3	0	5	2.9	O=C1N(Cc2c1ccc(c2)c1nnn(c1C)c1cccnc1F)C1CC1	10.1016/j.bmcl.2009.07.145
	CHEMBL578995	872	34	None	1819	2	Human	8.5	pIC50	=	8.5	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	349	3	0	5	2.9	O=C1N(Cc2c1ccc(c2)c1nnn(c1C)c1cccnc1F)C1CC1	10.1016/j.bmcl.2009.07.145
	15985249	195579	0	None	776	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	351	4	0	5	3.1	CCCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O	10.1016/j.bmcl.2009.07.145
	CHEMBL1645349	195579	0	None	776	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	351	4	0	5	3.1	CCCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O	10.1016/j.bmcl.2009.07.145
	CHEMBL568443	195579	0	None	776	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	351	4	0	5	3.1	CCCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O	10.1016/j.bmcl.2009.07.145
	15985251	2521	24	None	1	2	Rat	8.4	pIC50	=	8.4	Functional	Antagonist activity at rat mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at rat mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	368	3	0	4	3.9	Fc1ccc(c(c1)F)n1nnc(c1C)c1ccc2c(c1)CN(C2=O)C(C)C	10.1016/j.bmcl.2009.07.145
	6335	2521	24	None	1	2	Rat	8.4	pIC50	=	8.4	Functional	Antagonist activity at rat mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at rat mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	368	3	0	4	3.9	Fc1ccc(c(c1)F)n1nnc(c1C)c1ccc2c(c1)CN(C2=O)C(C)C	10.1016/j.bmcl.2009.07.145
	CHEMBL579062	2521	24	None	1	2	Rat	8.4	pIC50	=	8.4	Functional	Antagonist activity at rat mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at rat mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	368	3	0	4	3.9	Fc1ccc(c(c1)F)n1nnc(c1C)c1ccc2c(c1)CN(C2=O)C(C)C	10.1016/j.bmcl.2009.07.145
	16660140	195264	0	None	2454	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	357	5	1	6	3.4	CCNc1cc(-c2csc(N(C)C(=O)c3ccc(F)cc3)n2)ncn1	10.1016/j.bmcl.2009.07.097
	CHEMBL566374	195264	0	None	2454	2	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	357	5	1	6	3.4	CCNc1cc(-c2csc(N(C)C(=O)c3ccc(F)cc3)n2)ncn1	10.1016/j.bmcl.2009.07.097
	54586817	62417	0	None	-	1	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	380	3	0	6	3.7	C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784051	62417	0	None	-	1	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	380	3	0	6	3.7	C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54582004	62434	0	None	-	1	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	347	3	1	7	2.7	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784068	62434	0	None	-	1	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	347	3	1	7	2.7	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	16118682	70633	0	None	-	1	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	369	3	0	6	3.8	COc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1F	10.1016/j.bmcl.2011.12.131
	CHEMBL1951666	70633	0	None	-	1	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	369	3	0	6	3.8	COc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1F	10.1016/j.bmcl.2011.12.131
	57881773	83291	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	383	4	1	8	3.1	COc1ccc(-n2cnc3c(sc4ncnc(NC5CC5)c43)c2=O)c(F)c1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205375	83291	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	383	4	1	8	3.1	COc1ccc(-n2cnc3c(sc4ncnc(NC5CC5)c43)c2=O)c(F)c1	10.1016/j.bmcl.2012.09.048
	76955645	150071	3	None	-	1	Human	7.5	pIC50	=	7.5	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	356	2	0	4	4.9	O=c1c2scc(-c3ccccc3F)c2ncn1-c1ccc(Cl)cc1	nan
	CHEMBL3955218	150071	3	None	-	1	Human	7.5	pIC50	=	7.5	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	356	2	0	4	4.9	O=c1c2scc(-c3ccccc3F)c2ncn1-c1ccc(Cl)cc1	nan
	45484973	195418	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	286	2	0	4	3.8	Cc1c(-c2ccc3ccccc3c2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	CHEMBL567584	195418	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	286	2	0	4	3.8	Cc1c(-c2ccc3ccccc3c2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	10851012	187495	1	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at mGluR1Antagonist activity at mGluR1	ChEMBL	289	2	2	5	3.1	Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	CHEMBL497917	187495	1	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at mGluR1Antagonist activity at mGluR1	ChEMBL	289	2	2	5	3.1	Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	24777580	94249	0	None	-	1	Rat	5.5	pIC50	=	5.5	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	269	2	1	4	3.2	N#Cc1cc2c(nc1NC1CCCCC1)CCCC2=O	10.1021/jm0611298
	CHEMBL252736	94249	0	None	-	1	Rat	5.5	pIC50	=	5.5	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	269	2	1	4	3.2	N#Cc1cc2c(nc1NC1CCCCC1)CCCC2=O	10.1021/jm0611298
	5761323	194158	8	None	-	1	Rat	4.5	pIC50	=	4.5	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	334	5	0	2	6.0	O=C(/C=C/c1ccc(Cl)cc1)c1ccc(Oc2ccccc2)cc1	10.1016/j.bmc.2009.05.072
	CHEMBL558321	194158	8	None	-	1	Rat	4.5	pIC50	=	4.5	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	334	5	0	2	6.0	O=C(/C=C/c1ccc(Cl)cc1)c1ccc(Oc2ccccc2)cc1	10.1016/j.bmc.2009.05.072
	1893077	94199	16	None	-6	3	Rat	4.5	pIC50	=	4.5	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	294	3	0	4	3.8	N#Cc1cc2c(nc1SCc1ccccc1)CCCC2=O	10.1021/jm0611298
	CHEMBL252332	94199	16	None	-6	3	Rat	4.5	pIC50	=	4.5	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	294	3	0	4	3.8	N#Cc1cc2c(nc1SCc1ccccc1)CCCC2=O	10.1021/jm0611298
	73334943	132499	0	None	-39	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	353	2	0	4	3.0	COc1cc(C2=NCC(=O)N3CCc4c(Cl)cccc4C3=C2)ccn1	nan
	CHEMBL3702361	132499	0	None	-39	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	353	2	0	4	3.0	COc1cc(C2=NCC(=O)N3CCc4c(Cl)cccc4C3=C2)ccn1	nan
	72165213	105113	10	None	-12022	2	Human	4.5	pIC50	=	4.5	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay	ChEMBL	332	4	0	7	2.7	Cc1ccncc1-c1nn(C)c2nc(OCc3ccccn3)cnc12	10.1021/jm401622k
	CHEMBL3122212	105113	10	None	-12022	2	Human	4.5	pIC50	=	4.5	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay	ChEMBL	332	4	0	7	2.7	Cc1ccncc1-c1nn(C)c2nc(OCc3ccccn3)cnc12	10.1021/jm401622k
	11639210	143617	0	None	1	2	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	366	3	0	6	3.6	CCc1ccc(-n2cnc3c(sc4nccc([N+](C)(C)[O-])c43)c2=O)cc1	10.1021/jm0504407
	CHEMBL390391	143617	0	None	1	2	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	366	3	0	6	3.6	CCc1ccc(-n2cnc3c(sc4nccc([N+](C)(C)[O-])c43)c2=O)cc1	10.1021/jm0504407
	118735981	118419	0	None	-	1	Human	5.5	pIC50	=	5.5	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	421	5	1	5	4.6	COc1cccc(CNc2sc3c(c2C#N)CCN(C(=O)c2ccc(F)cc2)C3)c1	10.1016/j.ejmech.2015.04.060
	CHEMBL3422897	118419	0	None	-	1	Human	5.5	pIC50	=	5.5	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	421	5	1	5	4.6	COc1cccc(CNc2sc3c(c2C#N)CCN(C(=O)c2ccc(F)cc2)C3)c1	10.1016/j.ejmech.2015.04.060
	16117434	70696	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	322	2	1	6	3.3	CNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951888	70696	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	322	2	1	6	3.3	CNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	44588425	176234	0	None	-1	3	Mouse	7.5	pIC50	=	7.5	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	344	2	0	5	3.4	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccc(F)cc3)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL460827	176234	0	None	-1	3	Mouse	7.5	pIC50	=	7.5	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	344	2	0	5	3.4	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccc(F)cc3)nn2)CC1	10.1016/j.bmc.2008.09.060
	73335545	132547	0	None	-8	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	350	2	0	5	2.7	COc1cccc2c1CCN1C(=O)CN=C(n3cnc(C(C)C)c3)C=C21	nan
	CHEMBL3702409	132547	0	None	-8	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	350	2	0	5	2.7	COc1cccc2c1CCN1C(=O)CN=C(n3cnc(C(C)C)c3)C=C21	nan
	71717644	88664	0	None	-85	2	Human	5.5	pIC50	=	5.5	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	403	5	2	5	4.9	CCc1cccc(-c2c(-c3ccc4n[nH]cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2334986	88664	0	None	-85	2	Human	5.5	pIC50	=	5.5	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	403	5	2	5	4.9	CCc1cccc(-c2c(-c3ccc4n[nH]cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2365364	88664	0	None	-85	2	Human	5.5	pIC50	=	5.5	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	403	5	2	5	4.9	CCc1cccc(-c2c(-c3ccc4n[nH]cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	44431048	92872	0	None	-	1	Rat	6.5	pIC50	=	6.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	377	3	3	2	3.4	O=C(NCC12CC3CC(CC(C3)C1)C2)c1ccc2[nH]c3c(c2c1)CCNC3=O	10.1016/j.bmcl.2007.01.055
	CHEMBL245176	92872	0	None	-	1	Rat	6.5	pIC50	=	6.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	377	3	3	2	3.4	O=C(NCC12CC3CC(CC(C3)C1)C2)c1ccc2[nH]c3c(c2c1)CCNC3=O	10.1016/j.bmcl.2007.01.055
	54580949	62445	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	360	3	1	6	3.7	C#CC(C)Nc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784079	62445	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	360	3	1	6	3.7	C#CC(C)Nc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	118735970	118413	0	None	-	1	Human	5.5	pIC50	=	5.5	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	387	4	1	4	4.7	Cc1cccc(C(=O)N2CCc3c(sc(NCc4ccccc4)c3C#N)C2)c1	10.1016/j.ejmech.2015.04.060
	CHEMBL3422886	118413	0	None	-	1	Human	5.5	pIC50	=	5.5	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	387	4	1	4	4.7	Cc1cccc(C(=O)N2CCc3c(sc(NCc4ccccc4)c3C#N)C2)c1	10.1016/j.ejmech.2015.04.060
	44408692	74683	0	None	-	1	Rat	5.5	pIC50	=	5.5	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	454	7	0	6	3.4	Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCCN(C)C(=O)c1ccncc1)CC2	10.1016/j.bmcl.2005.11.049
	CHEMBL203461	74683	0	None	-	1	Rat	5.5	pIC50	=	5.5	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	454	7	0	6	3.4	Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCCN(C)C(=O)c1ccncc1)CC2	10.1016/j.bmcl.2005.11.049
	44408600	75571	0	None	-	1	Rat	5.5	pIC50	=	5.5	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	363	3	0	6	2.1	Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(N1CCOCC1)CC2	10.1016/j.bmcl.2005.11.049
	CHEMBL205075	75571	0	None	-	1	Rat	5.5	pIC50	=	5.5	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	363	3	0	6	2.1	Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(N1CCOCC1)CC2	10.1016/j.bmcl.2005.11.049
	57404255	72865	1	None	-18	3	Human	7.5	pIC50	=	7.5	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	302	4	1	4	3.7	COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1	10.1016/j.bmcl.2012.02.003
	CHEMBL2011870	72865	1	None	-18	3	Human	7.5	pIC50	=	7.5	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	302	4	1	4	3.7	COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1	10.1016/j.bmcl.2012.02.003
	52941697	18117	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology	ChEMBL	425	18	5	5	2.1	CCCC(=O)N[C@@H](CC1CCCCC1)C(=O)NCCCNCCCCNCCCN	10.1021/jm100886h
	CHEMBL1270621	18117	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology	ChEMBL	425	18	5	5	2.1	CCCC(=O)N[C@@H](CC1CCCCC1)C(=O)NCCCNCCCCNCCCN	10.1021/jm100886h
	11560185	84643	0	None	1	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	390	2	0	6	4.1	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12	10.1021/jm0504407
	CHEMBL224375	84643	0	None	1	2	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	390	2	0	6	4.1	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12	10.1021/jm0504407
	73335546	132549	0	None	-5	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	472	0	0	4	3.2	O=C1CN=C(n2cnc(C(F)(F)F)c2)C=C2c3cccc(I)c3CCN12	nan
	CHEMBL3702411	132549	0	None	-5	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	472	0	0	4	3.2	O=C1CN=C(n2cnc(C(F)(F)F)c2)C=C2c3cccc(I)c3CCN12	nan
	89980768	132603	0	None	-457	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	394	3	0	5	3.3	CO[C@H](C)c1cn(C2=NCC(=O)N3CCc4c(C5CC5)ccc(F)c4C3=C2)cn1	nan
	CHEMBL3702466	132603	0	None	-457	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	394	3	0	5	3.3	CO[C@H](C)c1cn(C2=NCC(=O)N3CCc4c(C5CC5)ccc(F)c4C3=C2)cn1	nan
	46886120	8400	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	349	2	1	7	3.2	Cc1ccc(-n2cnc3c(sc4nc(C5CC5)nc(N)c43)c2=O)cc1	10.1016/j.bmcl.2010.03.004
	CHEMBL1093987	8400	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	349	2	1	7	3.2	Cc1ccc(-n2cnc3c(sc4nc(C5CC5)nc(N)c43)c2=O)cc1	10.1016/j.bmcl.2010.03.004
	54580947	62432	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	407	4	1	9	3.2	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784066	62432	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	407	4	1	9	3.2	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	45484871	195580	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	322	4	0	6	3.2	Cc1c(-c2ccc(C(=O)OC(C)C)cc2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	CHEMBL568449	195580	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	322	4	0	6	3.2	Cc1c(-c2ccc(C(=O)OC(C)C)cc2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	11537767	141299	0	None	5	2	Rat	7.5	pIC50	=	7.5	Functional	Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells	ChEMBL	359	2	0	7	2.6	C[N+](C)([O-])c1ccnc2sc3c(=O)n(N4CCCCCC4)cnc3c12	10.1016/j.bmcl.2006.06.053
	CHEMBL386408	141299	0	None	5	2	Rat	7.5	pIC50	=	7.5	Functional	Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells	ChEMBL	359	2	0	7	2.6	C[N+](C)([O-])c1ccnc2sc3c(=O)n(N4CCCCCC4)cnc3c12	10.1016/j.bmcl.2006.06.053
	86711401	124588	0	None	-660	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	388	3	0	5	3.4	CCC(=O)c1cccc2c1CCN1C(=O)CN=C(n3cnc(C4CCC4)c3)C=C21	nan
	CHEMBL3644404	124588	0	None	-660	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	388	3	0	5	3.4	CCC(=O)c1cccc2c1CCN1C(=O)CN=C(n3cnc(C4CCC4)c3)C=C21	nan
	86711388	124607	0	None	-186	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	399	2	0	6	3.4	Cc1nc(-c2cccc3c2CCN2C(=O)CN=C(n4cnc(C5CC5)c4)C=C32)co1	nan
	CHEMBL3644423	124607	0	None	-186	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	399	2	0	6	3.4	Cc1nc(-c2cccc3c2CCN2C(=O)CN=C(n4cnc(C5CC5)c4)C=C32)co1	nan
	122196127	123741	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	376	4	1	5	3.7	COc1cc(N2C(=O)c3ccccc3C2=O)ccc1NC(=O)c1occc1C	10.1016/j.bmcl.2015.10.013
	CHEMBL3634449	123741	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	376	4	1	5	3.7	COc1cc(N2C(=O)c3ccccc3C2=O)ccc1NC(=O)c1occc1C	10.1016/j.bmcl.2015.10.013
	86711405	124591	0	None	-123	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	388	3	1	5	2.9	O=C1CN=C(n2cnc(C(O)C3CC3)c2)C=C2c3cccc(C4CC4)c3CCN12	nan
	CHEMBL3644407	124591	0	None	-123	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	388	3	1	5	2.9	O=C1CN=C(n2cnc(C(O)C3CC3)c2)C=C2c3cccc(C4CC4)c3CCN12	nan
	11594849	84574	0	None	1	2	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	316	4	0	6	3.4	CCC(CC)n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1021/jm0504407
	CHEMBL223819	84574	0	None	1	2	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	316	4	0	6	3.4	CCC(CC)n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1021/jm0504407
	127033447	138511	0	None	10	2	Rat	6.5	pIC50	=	6.5	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	269	3	1	5	3.1	CC(C)(C)CCNc1ncnc2c1nn1ccccc21	10.1016/j.bmcl.2016.03.026
	CHEMBL3786024	138511	0	None	10	2	Rat	6.5	pIC50	=	6.5	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	269	3	1	5	3.1	CC(C)(C)CCNc1ncnc2c1nn1ccccc21	10.1016/j.bmcl.2016.03.026
	16117432	70693	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	352	4	1	7	3.4	CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951885	70693	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	352	4	1	7	3.4	CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	122196098	123714	0	None	19	2	Human	7.5	pIC50	=	7.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	382	3	1	4	3.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(F)c1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634421	123714	0	None	19	2	Human	7.5	pIC50	=	7.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	382	3	1	4	3.9	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)c(F)c1	10.1016/j.bmcl.2015.10.013
	122196113	123728	0	None	32	2	Human	7.5	pIC50	=	7.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	381	3	1	5	3.7	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634435	123728	0	None	32	2	Human	7.5	pIC50	=	7.5	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	381	3	1	5	3.7	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(Cl)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	89980374	124601	0	None	-47	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	350	3	0	5	2.4	COC(C)c1cccc2c1CCN1C(=O)CN=C(c3ccn(C)n3)C=C21	nan
	CHEMBL3644417	124601	0	None	-47	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	350	3	0	5	2.4	COC(C)c1cccc2c1CCN1C(=O)CN=C(c3ccn(C)n3)C=C21	nan
	73335440	132531	0	None	-107	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	386	3	0	6	2.9	CC(C)n1cc(C2=NCC(=O)N3CCc4c(cccc4-n4cccn4)C3=C2)cn1	nan
	CHEMBL3702393	132531	0	None	-107	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	386	3	0	6	2.9	CC(C)n1cc(C2=NCC(=O)N3CCc4c(cccc4-n4cccn4)C3=C2)cn1	nan
	1382	1167	29	None	-1	3	Human	5.5	pIC50	=	5.5	Functional	Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells	ChEMBL	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	10.1021/jm0009944
	6278000	1167	29	None	-1	3	Human	5.5	pIC50	=	5.5	Functional	Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells	ChEMBL	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	10.1021/jm0009944
	CHEMBL327783	1167	29	None	-1	3	Human	5.5	pIC50	=	5.5	Functional	Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells	ChEMBL	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	10.1021/jm0009944
	127033447	138511	0	None	10	2	Rat	6.5	pIC50	=	6.5	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	269	3	1	5	3.1	CC(C)(C)CCNc1ncnc2c1nn1ccccc21	10.1016/j.bmcl.2016.03.026
	CHEMBL3786024	138511	0	None	10	2	Rat	6.5	pIC50	=	6.5	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	269	3	1	5	3.1	CC(C)(C)CCNc1ncnc2c1nn1ccccc21	10.1016/j.bmcl.2016.03.026
	71683127	90604	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	364	2	0	4	3.2	C[C@@H]1CN(c2ncccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397344	90604	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	364	2	0	4	3.2	C[C@@H]1CN(c2ncccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	71683127	90604	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	364	2	0	4	3.2	C[C@@H]1CN(c2ncccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397344	90604	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	364	2	0	4	3.2	C[C@@H]1CN(c2ncccc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	16118943	70641	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	336	3	0	5	4.2	CCc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951675	70641	0	None	-	1	Human	7.5	pIC50	=	7.5	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	336	3	0	5	4.2	CCc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	86711359	132521	0	None	-5	2	Human	7.5	pIC50	=	7.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	418	1	0	4	2.3	Cn1ccc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)n1	nan
	CHEMBL3702383	132521	0	None	-5	2	Human	7.5	pIC50	=	7.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	418	1	0	4	2.3	Cn1ccc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)n1	nan
	44442428	93170	0	None	27	2	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	350	2	0	5	3.8	Cc1ccccc1-n1ncc2c(=O)n(-c3ccc(Cl)cc3)c(C)nc21	10.1016/j.bmcl.2007.05.028
	CHEMBL246611	93170	0	None	27	2	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	350	2	0	5	3.8	Cc1ccccc1-n1ncc2c(=O)n(-c3ccc(Cl)cc3)c(C)nc21	10.1016/j.bmcl.2007.05.028
	73335130	132507	0	None	-1	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	386	2	0	3	3.9	COc1cccc2c1CCN1C(=O)CN=C(c3cccc(C(F)(F)F)c3)C=C21	nan
	CHEMBL3702369	132507	0	None	-1	2	Human	5.5	pIC50	=	5.5	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	386	2	0	3	3.9	COc1cccc2c1CCN1C(=O)CN=C(c3cccc(C(F)(F)F)c3)C=C21	nan
	76325411	105122	0	None	-1548	2	Human	4.5	pIC50	=	4.5	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay	ChEMBL	353	6	1	6	2.8	CCC(C)NC(=O)c1nn(C)c2nc(OCc3cccc(C)n3)ccc12	10.1021/jm401622k
	CHEMBL3122221	105122	0	None	-1548	2	Human	4.5	pIC50	=	4.5	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay	ChEMBL	353	6	1	6	2.8	CCC(C)NC(=O)c1nn(C)c2nc(OCc3cccc(C)n3)ccc12	10.1021/jm401622k
	54582007	62447	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	402	5	1	6	4.9	C#CC(CC)(CC)Nc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784081	62447	0	None	-	1	Human	6.5	pIC50	=	6.5	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	402	5	1	6	4.9	C#CC(CC)(CC)Nc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	71682645	90613	0	None	-	1	Human	5.4	pIC50	=	5.4	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	343	2	0	3	4.0	C[C@@H]1CN(c2ccccn2)CCN1C(=O)[C@H]1CC[C@H](C(C)(C)C)CC1	10.1016/j.bmcl.2013.05.020
	CHEMBL2397364	90613	0	None	-	1	Human	5.4	pIC50	=	5.4	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	343	2	0	3	4.0	C[C@@H]1CN(c2ccccn2)CCN1C(=O)[C@H]1CC[C@H](C(C)(C)C)CC1	10.1016/j.bmcl.2013.05.020
	72163839	91592	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	368	1	0	3	3.6	O=C(N1CCC2(CCCCC2)CC1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418361	91592	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	368	1	0	3	3.6	O=C(N1CCC2(CCCCC2)CC1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	71682645	90613	0	None	-	1	Human	5.4	pIC50	=	5.4	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	343	2	0	3	4.0	C[C@@H]1CN(c2ccccn2)CCN1C(=O)[C@H]1CC[C@H](C(C)(C)C)CC1	10.1016/j.bmcl.2013.05.020
	CHEMBL2397364	90613	0	None	-	1	Human	5.4	pIC50	=	5.4	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	343	2	0	3	4.0	C[C@@H]1CN(c2ccccn2)CCN1C(=O)[C@H]1CC[C@H](C(C)(C)C)CC1	10.1016/j.bmcl.2013.05.020
	72163839	91592	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	368	1	0	3	3.6	O=C(N1CCC2(CCCCC2)CC1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418361	91592	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	368	1	0	3	3.6	O=C(N1CCC2(CCCCC2)CC1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	11639176	84423	0	None	1	3	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	364	4	0	6	4.0	CCc1ccc(-n2cnc3c(sc4nccc(N(C)CC)c43)c2=O)cc1	10.1021/jm0504407
	CHEMBL223543	84423	0	None	1	3	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	364	4	0	6	4.0	CCc1ccc(-n2cnc3c(sc4nccc(N(C)CC)c43)c2=O)cc1	10.1021/jm0504407
	16659642	89789	0	None	-	1	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	353	1	1	6	3.5	O=c1c2sc3ncc4cn[nH]c4c3c2ncn1-c1ccc(Cl)cc1	10.1021/jm070590c
	CHEMBL238263	89789	0	None	-	1	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	353	1	1	6	3.5	O=c1c2sc3ncc4cn[nH]c4c3c2ncn1-c1ccc(Cl)cc1	10.1021/jm070590c
	78324870	113836	3	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	338	2	0	4	4.8	O=c1c2scc(-c3ccccc3)c2ncn1-c1cccc(Cl)c1	10.1016/j.ejmech.2014.08.027
	CHEMBL3330804	113836	3	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	338	2	0	4	4.8	O=c1c2scc(-c3ccccc3)c2ncn1-c1cccc(Cl)c1	10.1016/j.ejmech.2014.08.027
	44431055	166047	0	None	-	1	Rat	6.4	pIC50	=	6.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	306	3	2	2	3.6	CC(Oc1ccc2[nH]c3c(c2c1)CCNC3=O)c1ccccc1	10.1016/j.bmcl.2007.01.055
	CHEMBL428040	166047	0	None	-	1	Rat	6.4	pIC50	=	6.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	306	3	2	2	3.6	CC(Oc1ccc2[nH]c3c(c2c1)CCNC3=O)c1ccccc1	10.1016/j.bmcl.2007.01.055
	73336123	132580	0	None	-114	2	Human	5.4	pIC50	=	5.4	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	415	2	0	6	3.9	Cc1ncc(-c2cccc3c2CCN2C(=O)CN=C(n4cnc(C5CC5)c4)C=C32)s1	nan
	CHEMBL3702441	132580	0	None	-114	2	Human	5.4	pIC50	=	5.4	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	415	2	0	6	3.9	Cc1ncc(-c2cccc3c2CCN2C(=O)CN=C(n4cnc(C5CC5)c4)C=C32)s1	nan
	122196111	123726	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	347	3	1	5	3.0	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634433	123726	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	347	3	1	5	3.0	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	67180972	72873	0	None	169	2	Human	7.4	pIC50	=	7.4	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	340	3	1	3	5.0	Cc1c(-c2ccc(Cl)c(Cl)c2)nsc1NC(=O)[C@@H]1C[C@H]1C	10.1016/j.bmcl.2012.02.003
	CHEMBL2011878	72873	0	None	169	2	Human	7.4	pIC50	=	7.4	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	340	3	1	3	5.0	Cc1c(-c2ccc(Cl)c(Cl)c2)nsc1NC(=O)[C@@H]1C[C@H]1C	10.1016/j.bmcl.2012.02.003
	11717319	142962	0	None	1	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	353	3	0	8	2.5	COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cn1	10.1021/jm0504407
	CHEMBL389870	142962	0	None	1	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	353	3	0	8	2.5	COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cn1	10.1021/jm0504407
	11674352	174593	0	None	4	3	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	331	3	0	6	2.4	CC(C)OC(=O)N1CC=C(c2cn(-c3cccnc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL457026	174593	0	None	4	3	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	331	3	0	6	2.4	CC(C)OC(=O)N1CC=C(c2cn(-c3cccnc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	44588386	176187	0	None	-2	3	Mouse	7.4	pIC50	=	7.4	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	344	2	0	5	3.4	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3cccc(F)c3)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL460391	176187	0	None	-2	3	Mouse	7.4	pIC50	=	7.4	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	344	2	0	5	3.4	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3cccc(F)c3)nn2)CC1	10.1016/j.bmc.2008.09.060
	25183673	121686	0	None	-13	2	Rat	7.4	pIC50	=	7.4	Functional	Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis	ChEMBL	319	2	0	4	3.6	O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2ccccc2)CC1	10.1016/j.bmc.2015.05.008
	CHEMBL3597592	121686	0	None	-13	2	Rat	7.4	pIC50	=	7.4	Functional	Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis	ChEMBL	319	2	0	4	3.6	O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2ccccc2)CC1	10.1016/j.bmc.2015.05.008
	44408471	165447	0	None	-	1	Rat	7.4	pIC50	=	7.4	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	320	4	0	4	3.3	CCCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O	10.1016/j.bmcl.2005.11.049
	CHEMBL425405	165447	0	None	-	1	Rat	7.4	pIC50	=	7.4	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	320	4	0	4	3.3	CCCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O	10.1016/j.bmcl.2005.11.049
	45484928	195581	0	None	-	1	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	340	4	0	5	3.9	Cc1c(-c2ccc(C(=O)c3ccccc3)cc2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	CHEMBL568450	195581	0	None	-	1	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	340	4	0	5	3.9	Cc1c(-c2ccc(C(=O)c3ccccc3)cc2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	5752613	194514	12	None	-	1	Rat	4.4	pIC50	=	4.4	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	337	4	0	3	5.1	COc1ccc(C(=O)/C=C/c2cc3ccc(C)cc3nc2Cl)cc1	10.1016/j.bmc.2009.05.072
	CHEMBL561391	194514	12	None	-	1	Rat	4.4	pIC50	=	4.4	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	337	4	0	3	5.1	COc1ccc(C(=O)/C=C/c2cc3ccc(C)cc3nc2Cl)cc1	10.1016/j.bmc.2009.05.072
	67424364	88636	0	None	-10	2	Human	6.4	pIC50	=	6.4	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	417	5	1	6	5.2	CC(C)c1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)C2CC2)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2334989	88636	0	None	-10	2	Human	6.4	pIC50	=	6.4	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	417	5	1	6	5.2	CC(C)c1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)C2CC2)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2365000	88636	0	None	-10	2	Human	6.4	pIC50	=	6.4	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	417	5	1	6	5.2	CC(C)c1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)C2CC2)n1	10.1016/j.bmcl.2013.01.009
	720635	5786	13	None	-1	2	Rat	6.4	pIC50	=	6.4	Functional	Antagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assayAntagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assay	ChEMBL	333	2	1	3	4.8	Clc1cccc(Nc2ncnc3ccc(Br)cc23)c1	10.1016/j.bmcl.2009.10.024
	CHEMBL1079374	5786	13	None	-1	2	Rat	6.4	pIC50	=	6.4	Functional	Antagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assayAntagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assay	ChEMBL	333	2	1	3	4.8	Clc1cccc(Nc2ncnc3ccc(Br)cc23)c1	10.1016/j.bmcl.2009.10.024
	71680758	90606	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	364	2	0	4	3.2	C[C@@H]1CN(c2ccncc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397346	90606	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	364	2	0	4	3.2	C[C@@H]1CN(c2ccncc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	44408605	74083	0	None	-	1	Rat	6.4	pIC50	=	6.4	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	421	5	1	6	3.4	Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCNC(=O)OC(C)(C)C)CC2	10.1016/j.bmcl.2005.11.049
	CHEMBL202683	74083	0	None	-	1	Rat	6.4	pIC50	=	6.4	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	421	5	1	6	3.4	Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCNC(=O)OC(C)(C)C)CC2	10.1016/j.bmcl.2005.11.049
	44408568	74901	0	None	-	1	Rat	6.4	pIC50	=	6.4	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	406	7	2	5	2.6	CCNC(=O)NCCCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O	10.1016/j.bmcl.2005.11.049
	CHEMBL203688	74901	0	None	-	1	Rat	6.4	pIC50	=	6.4	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	406	7	2	5	2.6	CCNC(=O)NCCCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O	10.1016/j.bmcl.2005.11.049
	44408569	139278	0	None	-	1	Rat	6.4	pIC50	=	6.4	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	440	7	1	6	3.1	Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCCNC(=O)c1ccncc1)CC2	10.1016/j.bmcl.2005.11.049
	CHEMBL379882	139278	0	None	-	1	Rat	6.4	pIC50	=	6.4	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	440	7	1	6	3.1	Cc1c(C(=O)OC(C)C(C)(C)C)cn2c1C(=O)N(CCCNC(=O)c1ccncc1)CC2	10.1016/j.bmcl.2005.11.049
	71680758	90606	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	364	2	0	4	3.2	C[C@@H]1CN(c2ccncc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397346	90606	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	364	2	0	4	3.2	C[C@@H]1CN(c2ccncc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	44431057	87407	0	None	-	1	Rat	5.4	pIC50	=	5.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	292	3	2	2	3.0	O=C1NCCc2c1[nH]c1cccc(OCc3ccccc3)c21	10.1016/j.bmcl.2007.01.055
	CHEMBL233851	87407	0	None	-	1	Rat	5.4	pIC50	=	5.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	292	3	2	2	3.0	O=C1NCCc2c1[nH]c1cccc(OCc3ccccc3)c21	10.1016/j.bmcl.2007.01.055
	57559545	83411	0	None	-	1	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	341	2	0	7	2.6	CN(C)c1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	CHEMBL2205924	83411	0	None	-	1	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	341	2	0	7	2.6	CN(C)c1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	11574901	84800	0	None	1	3	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	400	2	0	6	3.8	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1021/jm0504407
	CHEMBL225590	84800	0	None	1	3	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	400	2	0	6	3.8	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1021/jm0504407
	54585403	62330	0	None	-	1	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	352	4	1	6	3.7	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783863	62330	0	None	-	1	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	352	4	1	6	3.7	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	16118397	70688	0	None	-	1	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	367	3	1	5	4.8	O=c1c2sc3nccc(NC4CC4)c3c2ccn1-c1ccc(Cl)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951880	70688	0	None	-	1	Human	8.4	pIC50	=	8.4	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	367	3	1	5	4.8	O=c1c2sc3nccc(NC4CC4)c3c2ccn1-c1ccc(Cl)cc1	10.1016/j.bmcl.2011.12.131
	54582003	62425	0	None	-	1	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	349	4	1	7	3.4	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccccc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784059	62425	0	None	-	1	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	349	4	1	7	3.4	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccccc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	16118120	70626	0	None	257	2	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	335	2	0	5	4.0	Cc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951659	70626	0	None	257	2	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	335	2	0	5	4.0	Cc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	45484965	197145	0	None	-	1	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	287	2	0	5	3.2	Cc1c(-c2ccc3ncccc3c2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	CHEMBL583590	197145	0	None	-	1	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	287	2	0	5	3.2	Cc1c(-c2ccc3ncccc3c2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	16659646	89526	0	None	-	1	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	348	2	1	6	3.5	COc1ccc(-n2cnc3c(sc4ncc5cc[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	CHEMBL238079	89526	0	None	-	1	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	348	2	1	6	3.5	COc1ccc(-n2cnc3c(sc4ncc5cc[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	24777581	94277	0	None	-	1	Rat	5.4	pIC50	=	5.4	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	297	2	1	4	3.9	CC1(C)CC(=O)c2cc(C#N)c(NC3CCCCC3)nc2C1	10.1021/jm0611298
	CHEMBL252940	94277	0	None	-	1	Rat	5.4	pIC50	=	5.4	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	297	2	1	4	3.9	CC1(C)CC(=O)c2cc(C#N)c(NC3CCCCC3)nc2C1	10.1021/jm0611298
	1297	169685	33	None	1	2	Human	4.4	pIC50	=	4.4	Functional	Ability to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M ConcentrationAbility to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M Concentration	ChEMBL	211	3	4	4	0.2	NC(C(=O)O)c1ccc(C(=O)O)c(O)c1	10.1021/jm00019a002
	CHEMBL444589	169685	33	None	1	2	Human	4.4	pIC50	=	4.4	Functional	Ability to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M ConcentrationAbility to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M Concentration	ChEMBL	211	3	4	4	0.2	NC(C(=O)O)c1ccc(C(=O)O)c(O)c1	10.1021/jm00019a002
	1374	2050	31	None	-15	4	Human	4.4	pIC50	=	4.4	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	211	3	4	4	0.2	N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O	10.1021/jm060950g
	5311455	2050	31	None	-15	4	Human	4.4	pIC50	=	4.4	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	211	3	4	4	0.2	N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O	10.1021/jm060950g
	CHEMBL39372	2050	31	None	-15	4	Human	4.4	pIC50	=	4.4	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	211	3	4	4	0.2	N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O	10.1021/jm060950g
	5311460	18786	25	None	-	1	Human	4.4	pIC50	=	4.4	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	211	3	4	4	0.2	N[C@H](C(=O)O)c1ccc(O)c(C(=O)O)c1	10.1021/jm060950g
	CHEMBL128772	18786	25	None	-	1	Human	4.4	pIC50	=	4.4	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	211	3	4	4	0.2	N[C@H](C(=O)O)c1ccc(O)c(C(=O)O)c1	10.1021/jm060950g
	89979971	124599	0	None	-15	2	Human	6.4	pIC50	=	6.4	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	414	2	0	6	3.0	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cncc(F)n4)c3CCN12	nan
	CHEMBL3644415	124599	0	None	-15	2	Human	6.4	pIC50	=	6.4	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	414	2	0	6	3.0	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cncc(F)n4)c3CCN12	nan
	11552320	136304	0	None	1	3	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	364	3	0	6	4.2	CC(C)c1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1021/jm0504407
	CHEMBL374167	136304	0	None	1	3	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	364	3	0	6	4.2	CC(C)c1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1021/jm0504407
	78324869	113835	3	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	338	2	0	4	4.8	O=c1c2scc(-c3ccccc3)c2ncn1-c1ccccc1Cl	10.1016/j.ejmech.2014.08.027
	CHEMBL3330803	113835	3	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	338	2	0	4	4.8	O=c1c2scc(-c3ccccc3)c2ncn1-c1ccccc1Cl	10.1016/j.ejmech.2014.08.027
	78324866	113645	3	None	-	1	Human	6.4	pIC50	=	6.4	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	322	2	0	4	4.3	O=c1c2scc(-c3ccccc3)c2ncn1-c1ccccc1F	nan
	CHEMBL3329236	113645	3	None	-	1	Human	6.4	pIC50	=	6.4	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	322	2	0	4	4.3	O=c1c2scc(-c3ccccc3)c2ncn1-c1ccccc1F	nan
	44431053	149213	0	None	-	1	Rat	5.4	pIC50	=	5.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	278	2	2	2	3.2	O=C1NCCc2c1[nH]c1ccc(Oc3ccccc3)cc21	10.1016/j.bmcl.2007.01.055
	CHEMBL394810	149213	0	None	-	1	Rat	5.4	pIC50	=	5.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	278	2	2	2	3.2	O=C1NCCc2c1[nH]c1ccc(Oc3ccccc3)cc21	10.1016/j.bmcl.2007.01.055
	6419	1029	0	None	-20	2	Human	6.4	pIC50	=	6.4	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	431	6	1	6	5.3	CCCc1cccc(n1)c1c(snc1c1ccc2c(c1)cn(n2)C)NC(=O)[C@@H]1C[C@H]1C	10.1016/j.bmcl.2013.01.009
	71559428	1029	0	None	-20	2	Human	6.4	pIC50	=	6.4	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	431	6	1	6	5.3	CCCc1cccc(n1)c1c(snc1c1ccc2c(c1)cn(n2)C)NC(=O)[C@@H]1C[C@H]1C	10.1016/j.bmcl.2013.01.009
	CHEMBL2334980	1029	0	None	-20	2	Human	6.4	pIC50	=	6.4	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	431	6	1	6	5.3	CCCc1cccc(n1)c1c(snc1c1ccc2c(c1)cn(n2)C)NC(=O)[C@@H]1C[C@H]1C	10.1016/j.bmcl.2013.01.009
	49788731	17936	0	None	-	1	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology	ChEMBL	523	18	5	5	3.7	NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)Cc1cccc2ccccc12	10.1021/jm100886h
	CHEMBL1269126	17936	0	None	-	1	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology	ChEMBL	523	18	5	5	3.7	NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)Cc1cccc2ccccc12	10.1021/jm100886h
	11660540	84615	0	None	1	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	362	4	1	6	4.1	CCc1ccc(-n2cnc3c(sc4nccc(NC5CC5)c43)c2=O)cc1	10.1021/jm0504407
	CHEMBL224088	84615	0	None	1	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	362	4	1	6	4.1	CCc1ccc(-n2cnc3c(sc4nccc(NC5CC5)c43)c2=O)cc1	10.1021/jm0504407
	73058380	124590	0	None	-40	2	Human	7.4	pIC50	=	7.4	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	362	3	1	5	2.0	O=C1CN=C(n2cnc(CCO)c2)C=C2c3cccc(C4CC4)c3CCN12	nan
	CHEMBL3644406	124590	0	None	-40	2	Human	7.4	pIC50	=	7.4	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	362	3	1	5	2.0	O=C1CN=C(n2cnc(CCO)c2)C=C2c3cccc(C4CC4)c3CCN12	nan
	24777695	154456	0	None	-	1	Rat	4.4	pIC50	=	4.4	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	349	2	1	4	4.5	CC1(C)CC(=O)c2cc(C#N)c(NC34CC5CC(CC(C5)C3)C4)nc2C1	10.1021/jm0611298
	CHEMBL401331	154456	0	None	-	1	Rat	4.4	pIC50	=	4.4	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	349	2	1	4	4.5	CC1(C)CC(=O)c2cc(C#N)c(NC34CC5CC(CC(C5)C3)C4)nc2C1	10.1021/jm0611298
	71683125	90602	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	357	2	0	3	3.5	C[C@@H]1CN(c2ccc(F)cn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397342	90602	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	357	2	0	3	3.5	C[C@@H]1CN(c2ccc(F)cn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	71683125	90602	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	357	2	0	3	3.5	C[C@@H]1CN(c2ccc(F)cn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397342	90602	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	357	2	0	3	3.5	C[C@@H]1CN(c2ccc(F)cn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	73335642	132562	0	None	-123	2	Human	5.4	pIC50	=	5.4	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	419	4	0	7	2.9	COCCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4cscn4)C3=C2)cn1	nan
	CHEMBL3702424	132562	0	None	-123	2	Human	5.4	pIC50	=	5.4	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	419	4	0	7	2.9	COCCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4cscn4)C3=C2)cn1	nan
	54583474	62337	0	None	-	1	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	426	4	1	6	4.7	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783870	62337	0	None	-	1	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	426	4	1	6	4.7	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	11515548	210	6	None	-1	3	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	336	2	0	6	3.4	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(cnc1)N(C)C	10.1021/jm0504407
	6355	210	6	None	-1	3	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	336	2	0	6	3.4	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(cnc1)N(C)C	10.1021/jm0504407
	CHEMBL223869	210	6	None	-1	3	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	336	2	0	6	3.4	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(cnc1)N(C)C	10.1021/jm0504407
	122196094	123710	0	None	8	2	Human	7.4	pIC50	=	7.4	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	364	3	1	4	3.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)cc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634417	123710	0	None	8	2	Human	7.4	pIC50	=	7.4	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	364	3	1	4	3.8	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(F)c3C2=O)cc1	10.1016/j.bmcl.2015.10.013
	10317627	78113	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells	ChEMBL	380	5	2	6	1.9	COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2	10.1021/jm0009944
	CHEMBL2111944	78113	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Inhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis measured in CHO Metabotropic glutamate receptor 1 Expressing Cells	ChEMBL	380	5	2	6	1.9	COC(=O)[C@H](Cc1ccccc1)NC(=O)[C@]12C[C@H]1/C(=N\O)c1ccccc1O2	10.1021/jm0009944
	1373	2440	46	None	-1	4	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	209	3	3	3	0.6	OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C	10.1021/jm060950g
	139055582	2440	46	None	-1	4	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	209	3	3	3	0.6	OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C	10.1021/jm060950g
	446355	2440	46	None	-1	4	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	209	3	3	3	0.6	OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C	10.1021/jm060950g
	CHEMBL257626	2440	46	None	-1	4	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	209	3	3	3	0.6	OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C	10.1021/jm060950g
	DB04256	2440	46	None	-1	4	Human	5.4	pIC50	=	5.4	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	209	3	3	3	0.6	OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C	10.1021/jm060950g
	118735957	118403	0	None	-	1	Human	4.4	pIC50	=	4.4	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	405	5	2	5	4.3	CC(C)c1cc(C(=O)N2CCc3c(sc(NCc4ccccc4)c3C#N)C2)[nH]n1	10.1016/j.ejmech.2015.04.060
	CHEMBL3422873	118403	0	None	-	1	Human	4.4	pIC50	=	4.4	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	405	5	2	5	4.3	CC(C)c1cc(C(=O)N2CCc3c(sc(NCc4ccccc4)c3C#N)C2)[nH]n1	10.1016/j.ejmech.2015.04.060
	11501465	84679	0	None	1	3	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	364	3	0	6	3.9	CCc1ccc(-n2c(C)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1021/jm0504407
	CHEMBL224673	84679	0	None	1	3	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	364	3	0	6	3.9	CCc1ccc(-n2c(C)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1021/jm0504407
	2851338	154062	12	None	-	1	Rat	6.4	pIC50	=	6.4	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	306	2	1	2	3.9	O=C(NC12CC3CC(CC(C3)C1)C2)c1ccc2ccccc2n1	10.1021/jm0611298
	CHEMBL399161	154062	12	None	-	1	Rat	6.4	pIC50	=	6.4	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	306	2	1	2	3.9	O=C(NC12CC3CC(CC(C3)C1)C2)c1ccc2ccccc2n1	10.1021/jm0611298
	16659799	145856	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	366	1	1	7	3.2	Cc1ccc(-n2cnc3c(sc4ncc5sc(=O)[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	CHEMBL392164	145856	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	366	1	1	7	3.2	Cc1ccc(-n2cnc3c(sc4ncc5sc(=O)[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	78322374	148423	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	382	2	0	6	4.5	O=c1c2scc(-c3ccc4c(c3)OCO4)c2ncn1-c1ccc(Cl)cc1	nan
	CHEMBL3942033	148423	0	None	-	1	Human	6.4	pIC50	=	6.4	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	382	2	0	6	4.5	O=c1c2scc(-c3ccc4c(c3)OCO4)c2ncn1-c1ccc(Cl)cc1	nan
	25183668	121688	0	None	-562	2	Rat	6.4	pIC50	=	6.4	Functional	Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis	ChEMBL	334	2	0	5	3.3	Cc1cccc(C#CC=C2CCN(c3ncccc3[N+](=O)[O-])CC2)n1	10.1016/j.bmc.2015.05.008
	CHEMBL3597594	121688	0	None	-562	2	Rat	6.4	pIC50	=	6.4	Functional	Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis	ChEMBL	334	2	0	5	3.3	Cc1cccc(C#CC=C2CCN(c3ncccc3[N+](=O)[O-])CC2)n1	10.1016/j.bmc.2015.05.008
	54584892	62441	0	None	-	1	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	390	3	1	9	3.0	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5scnc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784075	62441	0	None	-	1	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	390	3	1	9	3.0	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5scnc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	11661106	84709	0	None	1	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	390	2	0	6	4.4	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4Cl)cnc3c12	10.1021/jm0504407
	CHEMBL224898	84709	0	None	1	2	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	390	2	0	6	4.4	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4Cl)cnc3c12	10.1021/jm0504407
	78322060	113846	3	None	-	1	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	348	3	0	5	4.4	COc1ccc(-n2cnc3c(-c4ccccc4C)csc3c2=O)cc1	10.1016/j.ejmech.2014.08.027
	CHEMBL3330823	113846	3	None	-	1	Human	7.4	pIC50	=	7.4	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	348	3	0	5	4.4	COc1ccc(-n2cnc3c(-c4ccccc4C)csc3c2=O)cc1	10.1016/j.ejmech.2014.08.027
	89979519	132544	0	None	-316	2	Human	5.4	pIC50	=	5.4	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	388	3	0	4	3.8	COc1cccc(C2=NCC(=O)N3CCc4c(cccc4C4CCCO4)C3=C2)c1	nan
	CHEMBL3702406	132544	0	None	-316	2	Human	5.4	pIC50	=	5.4	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	388	3	0	4	3.8	COc1cccc(C2=NCC(=O)N3CCc4c(cccc4C4CCCO4)C3=C2)c1	nan
	24777444	94248	1	None	-5	2	Rat	4.4	pIC50	=	4.4	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	280	3	1	3	3.8	CC1(C)CC(=O)c2ccc(NCc3ccccc3)nc2C1	10.1021/jm0611298
	CHEMBL252735	94248	1	None	-5	2	Rat	4.4	pIC50	=	4.4	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	280	3	1	3	3.8	CC1(C)CC(=O)c2ccc(NCc3ccccc3)nc2C1	10.1021/jm0611298
	57908404	88672	0	None	-102	2	Human	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	417	5	2	5	5.5	CC(C)c1cccc(-c2c(-c3ccc4n[nH]cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2334987	88672	0	None	-102	2	Human	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	417	5	2	5	5.5	CC(C)c1cccc(-c2c(-c3ccc4n[nH]cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2365401	88672	0	None	-102	2	Human	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	417	5	2	5	5.5	CC(C)c1cccc(-c2c(-c3ccc4n[nH]cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	122196107	123723	0	None	25	2	Human	7.3	pIC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	376	4	1	5	3.7	COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O	10.1016/j.bmcl.2015.10.013
	CHEMBL3634430	123723	0	None	25	2	Human	7.3	pIC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	376	4	1	5	3.7	COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O	10.1016/j.bmcl.2015.10.013
	127033446	138453	0	None	-	1	Rat	6.3	pIC50	=	6.3	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	3	1	5	3.7	C[C@@H](Nc1ncnc2c1nn1ccccc21)C1CCCCC1	10.1016/j.bmcl.2016.03.026
	CHEMBL3785386	138453	0	None	-	1	Rat	6.3	pIC50	=	6.3	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	3	1	5	3.7	C[C@@H](Nc1ncnc2c1nn1ccccc21)C1CCCCC1	10.1016/j.bmcl.2016.03.026
	44431051	92875	0	None	-	1	Rat	5.3	pIC50	=	5.3	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	378	2	4	2	3.5	O=C(Nc1ccc2[nH]c3c(c2c1)CCNC3=O)NC12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2007.01.055
	CHEMBL245187	92875	0	None	-	1	Rat	5.3	pIC50	=	5.3	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	378	2	4	2	3.5	O=C(Nc1ccc2[nH]c3c(c2c1)CCNC3=O)NC12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2007.01.055
	127033446	138453	0	None	-	1	Rat	6.3	pIC50	=	6.3	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	3	1	5	3.7	C[C@@H](Nc1ncnc2c1nn1ccccc21)C1CCCCC1	10.1016/j.bmcl.2016.03.026
	CHEMBL3785386	138453	0	None	-	1	Rat	6.3	pIC50	=	6.3	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	3	1	5	3.7	C[C@@H](Nc1ncnc2c1nn1ccccc21)C1CCCCC1	10.1016/j.bmcl.2016.03.026
	122196115	123730	0	None	1	2	Human	5.3	pIC50	=	5.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	348	3	1	6	2.4	Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3ccccc3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634437	123730	0	None	1	2	Human	5.3	pIC50	=	5.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	348	3	1	6	2.4	Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3ccccc3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	16117172	70684	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	364	2	1	7	4.3	CNc1ccnc2sc3c(=O)n(-c4ccc5scnc5c4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951876	70684	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	364	2	1	7	4.3	CNc1ccnc2sc3c(=O)n(-c4ccc5scnc5c4)ccc3c12	10.1016/j.bmcl.2011.12.131
	122196091	123707	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	346	3	1	4	3.6	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634414	123707	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	346	3	1	4	3.6	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3ccccc3C2=O)cc1	10.1016/j.bmcl.2015.10.013
	45484889	195189	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	278	3	0	5	2.8	CC(=O)c1ccc(-c2nnn(-c3cccnc3)c2C)cc1	10.1016/j.bmcl.2009.07.145
	CHEMBL565972	195189	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	278	3	0	5	2.8	CC(=O)c1ccc(-c2nnn(-c3cccnc3)c2C)cc1	10.1016/j.bmcl.2009.07.145
	118735969	118412	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	387	4	1	4	4.7	Cc1ccc(C(=O)N2CCc3c(sc(NCc4ccccc4)c3C#N)C2)cc1	10.1016/j.ejmech.2015.04.060
	CHEMBL3422885	118412	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	387	4	1	4	4.7	Cc1ccc(C(=O)N2CCc3c(sc(NCc4ccccc4)c3C#N)C2)cc1	10.1016/j.ejmech.2015.04.060
	72163584	91600	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	369	2	0	3	3.3	O=C(N1C[C@@H]2CN(c3ccc(F)cn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	CHEMBL2418381	91600	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	369	2	0	3	3.3	O=C(N1C[C@@H]2CN(c3ccc(F)cn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	72163584	91600	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	369	2	0	3	3.3	O=C(N1C[C@@H]2CN(c3ccc(F)cn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	CHEMBL2418381	91600	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	369	2	0	3	3.3	O=C(N1C[C@@H]2CN(c3ccc(F)cn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	127031274	138586	0	None	-	1	Rat	6.3	pIC50	=	6.3	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	335	2	2	6	2.8	OC12CC3CC(C1)CC(Nc1ncnc4c1nn1ccccc41)(C3)C2	10.1016/j.bmcl.2016.03.026
	CHEMBL3786767	138586	0	None	-	1	Rat	6.3	pIC50	=	6.3	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	335	2	2	6	2.8	OC12CC3CC(C1)CC(Nc1ncnc4c1nn1ccccc41)(C3)C2	10.1016/j.bmcl.2016.03.026
	122196101	123717	0	None	20	2	Human	7.3	pIC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	394	3	1	4	4.6	Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O	10.1016/j.bmcl.2015.10.013
	CHEMBL3634424	123717	0	None	20	2	Human	7.3	pIC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	394	3	1	4	4.6	Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(Cl)c2C1=O	10.1016/j.bmcl.2015.10.013
	122196102	123718	0	None	22	2	Human	7.3	pIC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	378	3	1	4	4.1	Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O	10.1016/j.bmcl.2015.10.013
	CHEMBL3634425	123718	0	None	22	2	Human	7.3	pIC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	378	3	1	4	4.1	Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(F)c2C1=O	10.1016/j.bmcl.2015.10.013
	122196108	123724	0	None	18	2	Human	7.3	pIC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	390	4	1	5	4.0	COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O	10.1016/j.bmcl.2015.10.013
	CHEMBL3634431	123724	0	None	18	2	Human	7.3	pIC50	=	7.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	390	4	1	5	4.0	COc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2cccc(C)c2C1=O	10.1016/j.bmcl.2015.10.013
	720466	94352	14	None	12	2	Rat	5.3	pIC50	=	5.3	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	322	3	0	4	4.4	CC1(C)CC(=O)c2cc(C#N)c(SCc3ccccc3)nc2C1	10.1021/jm0611298
	CHEMBL253349	94352	14	None	12	2	Rat	5.3	pIC50	=	5.3	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	322	3	0	4	4.4	CC1(C)CC(=O)c2cc(C#N)c(SCc3ccccc3)nc2C1	10.1021/jm0611298
	73335235	132518	0	None	-60	2	Human	5.3	pIC50	=	5.3	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	355	2	0	4	3.6	O=C1CN=C(c2ccco2)C=C2c3cccc(-c4ccncc4)c3CCN12	nan
	CHEMBL3702380	132518	0	None	-60	2	Human	5.3	pIC50	=	5.3	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	355	2	0	4	3.6	O=C1CN=C(c2ccco2)C=C2c3cccc(-c4ccncc4)c3CCN12	nan
	11681680	141824	0	None	1	3	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	342	2	0	6	3.8	CC1CCCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)C1	10.1021/jm0504407
	CHEMBL388827	141824	0	None	1	3	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	342	2	0	6	3.8	CC1CCCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)C1	10.1021/jm0504407
	127031274	138586	0	None	-	1	Rat	6.3	pIC50	=	6.3	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	335	2	2	6	2.8	OC12CC3CC(C1)CC(Nc1ncnc4c1nn1ccccc41)(C3)C2	10.1016/j.bmcl.2016.03.026
	CHEMBL3786767	138586	0	None	-	1	Rat	6.3	pIC50	=	6.3	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	335	2	2	6	2.8	OC12CC3CC(C1)CC(Nc1ncnc4c1nn1ccccc41)(C3)C2	10.1016/j.bmcl.2016.03.026
	11660511	165590	0	None	-1	3	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	361	4	1	7	3.5	CCc1ccc(-n2cnc3c(sc4nccc(NCC#N)c43)c2=O)cc1	10.1021/jm0504407
	CHEMBL426190	165590	0	None	-1	3	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	361	4	1	7	3.5	CCc1ccc(-n2cnc3c(sc4nccc(NCC#N)c43)c2=O)cc1	10.1021/jm0504407
	44588460	174976	0	None	3	3	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	327	2	0	6	2.7	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccn3)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL457872	174976	0	None	3	3	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	327	2	0	6	2.7	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccn3)nn2)CC1	10.1016/j.bmc.2008.09.060
	16661409	195559	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	314	3	0	5	3.0	CN(C(=O)c1ccc(F)cc1)c1nc(-c2cnccn2)cs1	10.1016/j.bmcl.2009.07.097
	CHEMBL568317	195559	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	314	3	0	5	3.0	CN(C(=O)c1ccc(F)cc1)c1nc(-c2cnccn2)cs1	10.1016/j.bmcl.2009.07.097
	16661726	196919	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	313	3	0	4	3.6	CN(C(=O)c1ccc(F)cc1)c1nc(-c2ccncc2)cs1	10.1016/j.bmcl.2009.07.097
	CHEMBL578580	196919	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	313	3	0	4	3.6	CN(C(=O)c1ccc(F)cc1)c1nc(-c2ccncc2)cs1	10.1016/j.bmcl.2009.07.097
	89980648	124579	0	None	-34	2	Human	6.3	pIC50	=	6.3	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	362	3	0	5	2.7	C=C(C)c1cccc2c1CCN1C(=O)CN=C(n3cnc(COC)c3)C=C21	nan
	CHEMBL3644395	124579	0	None	-34	2	Human	6.3	pIC50	=	6.3	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	362	3	0	5	2.7	C=C(C)c1cccc2c1CCN1C(=O)CN=C(n3cnc(COC)c3)C=C21	nan
	73334945	132496	0	None	-24	2	Human	5.3	pIC50	=	5.3	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	349	3	0	5	2.3	COc1cc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)ccn1	nan
	CHEMBL3702358	132496	0	None	-24	2	Human	5.3	pIC50	=	5.3	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	349	3	0	5	2.3	COc1cc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)ccn1	nan
	78320479	113838	3	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	318	2	0	4	4.4	Cc1ccccc1-n1cnc2c(-c3ccccc3)csc2c1=O	10.1016/j.ejmech.2014.08.027
	CHEMBL3330806	113838	3	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	318	2	0	4	4.4	Cc1ccccc1-n1cnc2c(-c3ccccc3)csc2c1=O	10.1016/j.ejmech.2014.08.027
	57881754	83090	0	None	-	1	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	371	3	0	8	2.6	COc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cc1F	10.1016/j.bmcl.2012.09.048
	CHEMBL2203308	83090	0	None	-	1	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	371	3	0	8	2.6	COc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cc1F	10.1016/j.bmcl.2012.09.048
	57559597	83293	0	None	1995	2	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	339	3	1	8	2.4	CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	CHEMBL2205378	83293	0	None	1995	2	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	339	3	1	8	2.4	CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	16730193	83404	0	None	-	1	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	379	4	0	8	3.0	COc1ccc(-n2cnc3c(sc4ncnc(N(C)C5CC5)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205917	83404	0	None	-	1	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	379	4	0	8	3.0	COc1ccc(-n2cnc3c(sc4ncnc(N(C)C5CC5)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	744275	84420	13	None	1	3	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	336	2	0	6	3.4	Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1021/jm0504407
	CHEMBL223496	84420	13	None	1	3	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	336	2	0	6	3.4	Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1021/jm0504407
	11609353	84669	0	None	1	3	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	314	2	0	6	3.2	CN(C)c1ccnc2sc3c(=O)n(C4CCCC4)cnc3c12	10.1021/jm0504407
	CHEMBL224617	84669	0	None	1	3	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	314	2	0	6	3.2	CN(C)c1ccnc2sc3c(=O)n(C4CCCC4)cnc3c12	10.1021/jm0504407
	16118121	70635	0	None	263	2	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	378	2	0	7	4.3	CN(C)c1ccnc2sc3c(=O)n(-c4ccc5scnc5c4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951668	70635	0	None	263	2	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	378	2	0	7	4.3	CN(C)c1ccnc2sc3c(=O)n(-c4ccc5scnc5c4)ccc3c12	10.1016/j.bmcl.2011.12.131
	11530404	208	11	None	-1	4	Rat	8.3	pIC50	=	8.3	Functional	Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1016/j.bmcl.2006.06.053
	6211	208	11	None	-1	4	Rat	8.3	pIC50	=	8.3	Functional	Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1016/j.bmcl.2006.06.053
	CHEMBL385336	208	11	None	-1	4	Rat	8.3	pIC50	=	8.3	Functional	Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1016/j.bmcl.2006.06.053
	1384	2836	54	None	-	1	Rat	8.3	pIC50	=	8.3	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	307	2	1	3	3.3	O=C(c1cnc2c(n1)cccc2)NC12CC3CC(C2)CC(C1)C3	10.1021/jm0611298
	7067728	2836	54	None	-	1	Rat	8.3	pIC50	=	8.3	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	307	2	1	3	3.3	O=C(c1cnc2c(n1)cccc2)NC12CC3CC(C2)CC(C1)C3	10.1021/jm0611298
	CHEMBL399160	2836	54	None	-	1	Rat	8.3	pIC50	=	8.3	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	307	2	1	3	3.3	O=C(c1cnc2c(n1)cccc2)NC12CC3CC(C2)CC(C1)C3	10.1021/jm0611298
	16660135	1612	30	None	2	3	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	371	5	1	6	3.8	CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C	10.1016/j.bmcl.2009.07.097
	8767	1612	30	None	2	3	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	371	5	1	6	3.8	CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C	10.1016/j.bmcl.2009.07.097
	CHEMBL566581	1612	30	None	2	3	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	371	5	1	6	3.8	CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C	10.1016/j.bmcl.2009.07.097
	16118681	70627	0	None	-	1	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	339	2	0	5	3.8	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951660	70627	0	None	-	1	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	339	2	0	5	3.8	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	16659968	88259	0	None	117	2	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	364	1	1	7	3.5	Cc1ccc(-n2cnc3c(sc4ncc5c(c43)NC[C@@H](C)O5)c2=O)cc1	10.1021/jm070590c
	CHEMBL235977	88259	0	None	117	2	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	364	1	1	7	3.5	Cc1ccc(-n2cnc3c(sc4ncc5c(c43)NC[C@@H](C)O5)c2=O)cc1	10.1021/jm070590c
	16118256	70643	0	None	-	1	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	314	2	0	5	4.1	COc1ccnc2sc3c(=O)n(C4CCCCC4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951677	70643	0	None	-	1	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	314	2	0	5	4.1	COc1ccnc2sc3c(=O)n(C4CCCCC4)ccc3c12	10.1016/j.bmcl.2011.12.131
	11325594	197226	0	None	416	2	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	351	3	0	5	3.1	Cc1c(-c2ccc3c(c2)CN(C(C)C)C3=O)nnn1-c1cccnc1F	10.1016/j.bmcl.2009.07.145
	CHEMBL584478	197226	0	None	416	2	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	351	3	0	5	3.1	Cc1c(-c2ccc3c(c2)CN(C(C)C)C3=O)nnn1-c1cccnc1F	10.1016/j.bmcl.2009.07.145
	11245287	1667	29	None	-1	4	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	10.1016/j.bmcl.2009.07.145
	6363	1667	29	None	-1	4	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	10.1016/j.bmcl.2009.07.145
	CHEMBL502882	1667	29	None	-1	4	Human	8.3	pIC50	=	8.3	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	10.1016/j.bmcl.2009.07.145
	16118123	70629	0	None	1348	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	399	2	0	5	4.4	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951662	70629	0	None	1348	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	399	2	0	5	4.4	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	11245287	1667	29	None	-1	4	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	10.1016/j.bmc.2008.09.060
	6363	1667	29	None	-1	4	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	10.1016/j.bmc.2008.09.060
	CHEMBL502882	1667	29	None	-1	4	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	10.1016/j.bmc.2008.09.060
	44435349	91556	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	420	2	1	6	4.5	CNc1c(Br)cnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1021/jm070590c
	CHEMBL241547	91556	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	420	2	1	6	4.5	CNc1c(Br)cnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1021/jm070590c
	11695588	142707	0	None	1	3	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	328	2	0	6	3.6	CN(C)c1ccnc2sc3c(=O)n(C4CCCCC4)cnc3c12	10.1021/jm0504407
	CHEMBL389655	142707	0	None	1	3	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	328	2	0	6	3.6	CN(C)c1ccnc2sc3c(=O)n(C4CCCCC4)cnc3c12	10.1021/jm0504407
	11695769	143006	0	None	1	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	338	2	1	7	2.8	CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4O)cnc3c12	10.1021/jm0504407
	CHEMBL389897	143006	0	None	1	2	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	338	2	1	7	2.8	CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4O)cnc3c12	10.1021/jm0504407
	78320170	113841	3	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	334	3	0	5	4.1	COc1ccc(-n2cnc3c(-c4ccccc4)csc3c2=O)cc1	10.1016/j.ejmech.2014.08.027
	CHEMBL3330811	113841	3	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	334	3	0	5	4.1	COc1ccc(-n2cnc3c(-c4ccccc4)csc3c2=O)cc1	10.1016/j.ejmech.2014.08.027
	44408564	75504	0	None	-	1	Rat	6.3	pIC50	=	6.3	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	377	6	1	5	2.4	CC(=O)NCCCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O	10.1016/j.bmcl.2005.11.049
	CHEMBL204878	75504	0	None	-	1	Rat	6.3	pIC50	=	6.3	Functional	Inhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation methodInhibition of rat mGluR1a in CHO cells by CDP-DAG accumulation method	ChEMBL	377	6	1	5	2.4	CC(=O)NCCCN1CCn2cc(C(=O)OC(C)C(C)(C)C)c(C)c2C1=O	10.1016/j.bmcl.2005.11.049
	89981484	124585	0	None	-46	2	Human	6.3	pIC50	=	6.3	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	349	2	0	6	1.9	COc1ncn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)n1	nan
	CHEMBL3644401	124585	0	None	-46	2	Human	6.3	pIC50	=	6.3	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	349	2	0	6	1.9	COc1ncn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)n1	nan
	73350718	91593	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	326	1	0	3	2.3	O=C(N1CC2CCC(C2)C1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418362	91593	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	326	1	0	3	2.3	O=C(N1CC2CCC(C2)C1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	72163298	91596	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	313	2	0	3	2.9	CC1(C(=O)N2C[C@@H]3CN(c4ccccn4)C[C@@H]3C2)CCCCC1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418370	91596	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	313	2	0	3	2.9	CC1(C(=O)N2C[C@@H]3CN(c4ccccn4)C[C@@H]3C2)CCCCC1	10.1016/j.bmcl.2013.07.029
	72163298	91596	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	313	2	0	3	2.9	CC1(C(=O)N2C[C@@H]3CN(c4ccccn4)C[C@@H]3C2)CCCCC1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418370	91596	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	313	2	0	3	2.9	CC1(C(=O)N2C[C@@H]3CN(c4ccccn4)C[C@@H]3C2)CCCCC1	10.1016/j.bmcl.2013.07.029
	73350718	91593	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	326	1	0	3	2.3	O=C(N1CC2CCC(C2)C1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418362	91593	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	326	1	0	3	2.3	O=C(N1CC2CCC(C2)C1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	44416780	79821	0	None	-	1	Rat	7.3	pIC50	=	7.3	Functional	Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells	ChEMBL	441	6	0	7	4.6	CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCc5ccccn5)c43)c2=O)cc1	10.1016/j.bmcl.2006.06.053
	CHEMBL213760	79821	0	None	-	1	Rat	7.3	pIC50	=	7.3	Functional	Antagonist activity at rat mGluR1 expressed in 1321N1 cellsAntagonist activity at rat mGluR1 expressed in 1321N1 cells	ChEMBL	441	6	0	7	4.6	CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCc5ccccn5)c43)c2=O)cc1	10.1016/j.bmcl.2006.06.053
	12042753	94350	0	None	-	1	Rat	7.3	pIC50	=	7.3	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	306	2	1	2	3.9	O=C(NC12CC3CC(CC(C3)C1)C2)c1cnc2ccccc2c1	10.1021/jm0611298
	CHEMBL253347	94350	0	None	-	1	Rat	7.3	pIC50	=	7.3	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	306	2	1	2	3.9	O=C(NC12CC3CC(CC(C3)C1)C2)c1cnc2ccccc2c1	10.1021/jm0611298
	44442426	154227	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	356	2	0	5	4.4	Cc1nc2c(cnn2C2CCCCCC2)c(=O)n1-c1ccc(Cl)cc1	10.1016/j.bmcl.2007.05.028
	CHEMBL400110	154227	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	356	2	0	5	4.4	Cc1nc2c(cnn2C2CCCCCC2)c(=O)n1-c1ccc(Cl)cc1	10.1016/j.bmcl.2007.05.028
	73335134	132512	0	None	-1	2	Human	5.3	pIC50	=	5.3	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	362	3	0	5	2.4	COc1cccc2c1CCN1C(=O)CN=C(c3ccnc(N(C)C)c3)C=C21	nan
	CHEMBL3702374	132512	0	None	-1	2	Human	5.3	pIC50	=	5.3	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	362	3	0	5	2.4	COc1cccc2c1CCN1C(=O)CN=C(c3ccnc(N(C)C)c3)C=C21	nan
	54580946	62428	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	383	4	1	7	4.0	C=C(C)CNc1ncnc2sc3c(=O)n(-c4cccc(Cl)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784062	62428	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	383	4	1	7	4.0	C=C(C)CNc1ncnc2sc3c(=O)n(-c4cccc(Cl)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	73335036	132505	0	None	-6	2	Human	6.3	pIC50	=	6.3	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	382	3	0	4	3.6	COc1cccc(C2=NCC(=O)N3CCc4c(ccc(Cl)c4OC)C3=C2)c1	nan
	CHEMBL3702367	132505	0	None	-6	2	Human	6.3	pIC50	=	6.3	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	382	3	0	4	3.6	COc1cccc(C2=NCC(=O)N3CCc4c(ccc(Cl)c4OC)C3=C2)c1	nan
	24777313	94201	0	None	-	1	Rat	5.3	pIC50	=	5.3	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	319	3	0	4	3.7	CN(Cc1ccccc1)c1nc2c(cc1C#N)C(=O)CC(C)(C)C2	10.1021/jm0611298
	CHEMBL252334	94201	0	None	-	1	Rat	5.3	pIC50	=	5.3	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	319	3	0	4	3.7	CN(Cc1ccccc1)c1nc2c(cc1C#N)C(=O)CC(C)(C)C2	10.1021/jm0611298
	118735975	118416	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	391	4	1	4	4.6	N#Cc1c(NCc2cccc(F)c2)sc2c1CCN(C(=O)c1ccccc1)C2	10.1016/j.ejmech.2015.04.060
	CHEMBL3422891	118416	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	391	4	1	4	4.6	N#Cc1c(NCc2cccc(F)c2)sc2c1CCN(C(=O)c1ccccc1)C2	10.1016/j.ejmech.2015.04.060
	122196104	123720	0	None	10	2	Human	6.3	pIC50	=	6.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	428	3	1	4	5.0	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(C(F)(F)F)c1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634427	123720	0	None	10	2	Human	6.3	pIC50	=	6.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	428	3	1	4	5.0	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)c(C(F)(F)F)c1	10.1016/j.bmcl.2015.10.013
	122196118	123733	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	366	3	1	6	2.6	Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(F)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634440	123733	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	366	3	1	6	2.6	Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(F)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	16118945	70640	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	352	3	0	6	3.9	COc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)c(C)c1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951674	70640	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	352	3	0	6	3.9	COc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)c(C)c1	10.1016/j.bmcl.2011.12.131
	89980399	124604	0	None	-12	2	Human	6.3	pIC50	=	6.3	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	362	3	0	5	2.6	COCc1cn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)cn1	nan
	CHEMBL3644420	124604	0	None	-12	2	Human	6.3	pIC50	=	6.3	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	362	3	0	5	2.6	COCc1cn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)cn1	nan
	16659647	166859	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	382	1	1	7	4.6	Cc1ccc(-n2cnc3c(sc4ncc5sc(=S)[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	CHEMBL429635	166859	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	382	1	1	7	4.6	Cc1ccc(-n2cnc3c(sc4ncc5sc(=S)[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	87549991	121691	0	None	-301	2	Rat	6.3	pIC50	=	6.3	Functional	Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis	ChEMBL	333	2	0	4	3.9	Cc1cccc(C#CC=C2CCN(c3ncccc3[N+](=O)[O-])CC2)c1	10.1016/j.bmc.2015.05.008
	CHEMBL3597597	121691	0	None	-301	2	Rat	6.3	pIC50	=	6.3	Functional	Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis	ChEMBL	333	2	0	4	3.9	Cc1cccc(C#CC=C2CCN(c3ncccc3[N+](=O)[O-])CC2)c1	10.1016/j.bmc.2015.05.008
	72163723	91588	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	376	2	0	4	3.1	N#Cc1ncccc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418356	91588	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	376	2	0	4	3.1	N#Cc1ncccc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1	10.1016/j.bmcl.2013.07.029
	44329031	107788	0	None	-446	7	Human	4.3	pIC50	=	4.3	Functional	Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluated	ChEMBL	437	10	3	4	5.0	CCCCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O	10.1016/s0960-894x(98)00510-1
	CHEMBL319732	107788	0	None	-446	7	Human	4.3	pIC50	=	4.3	Functional	Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluated	ChEMBL	437	10	3	4	5.0	CCCCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O	10.1016/s0960-894x(98)00510-1
	44588461	172994	0	None	3	3	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	327	2	0	6	2.7	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3cccnc3)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL453249	172994	0	None	3	3	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	327	2	0	6	2.7	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3cccnc3)nn2)CC1	10.1016/j.bmc.2008.09.060
	16117042	70647	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	365	5	1	6	4.4	CCCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951682	70647	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	365	5	1	6	4.4	CCCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	25183670	121690	0	None	-52	2	Rat	6.3	pIC50	=	6.3	Functional	Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis	ChEMBL	333	2	0	4	3.9	Cc1cccc(C#CC=C2CCN(c3ccccc3[N+](=O)[O-])CC2)n1	10.1016/j.bmc.2015.05.008
	CHEMBL3597596	121690	0	None	-52	2	Rat	6.3	pIC50	=	6.3	Functional	Negative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysisNegative allosteric modulatory activity at rat cloned mGluR1 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis	ChEMBL	333	2	0	4	3.9	Cc1cccc(C#CC=C2CCN(c3ccccc3[N+](=O)[O-])CC2)n1	10.1016/j.bmc.2015.05.008
	72163723	91588	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	376	2	0	4	3.1	N#Cc1ncccc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418356	91588	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	376	2	0	4	3.1	N#Cc1ncccc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1	10.1016/j.bmcl.2013.07.029
	44431054	92876	0	None	-	1	Rat	5.3	pIC50	=	5.3	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	298	3	2	2	3.4	O=C1NCCc2c1[nH]c1ccc(OCC3CCCCC3)cc21	10.1016/j.bmcl.2007.01.055
	CHEMBL245188	92876	0	None	-	1	Rat	5.3	pIC50	=	5.3	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	298	3	2	2	3.4	O=C1NCCc2c1[nH]c1ccc(OCC3CCCCC3)cc21	10.1016/j.bmcl.2007.01.055
	72163720	91603	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	376	2	0	4	3.1	N#Cc1cccnc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418384	91603	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	376	2	0	4	3.1	N#Cc1cccnc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1	10.1016/j.bmcl.2013.07.029
	73335829	124606	0	None	-29	2	Human	6.3	pIC50	=	6.3	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	385	2	0	6	3.1	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4ccno4)c3CCN12	nan
	CHEMBL3644422	124606	0	None	-29	2	Human	6.3	pIC50	=	6.3	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	385	2	0	6	3.1	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4ccno4)c3CCN12	nan
	127034265	138543	0	None	-	1	Rat	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	296	2	2	6	2.9	C[C@H]1CC[C@H](Nc2nc(N)nc3c2nn2ccccc32)CC1	10.1016/j.bmcl.2016.03.026
	CHEMBL3786386	138543	0	None	-	1	Rat	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	296	2	2	6	2.9	C[C@H]1CC[C@H](Nc2nc(N)nc3c2nn2ccccc32)CC1	10.1016/j.bmcl.2016.03.026
	89979991	132604	0	None	-186	2	Human	6.3	pIC50	=	6.3	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	380	3	0	5	2.7	COCc1cn(C2=NCC(=O)N3CCc4c(cc(F)cc4C4CC4)C3=C2)cn1	nan
	CHEMBL3702467	132604	0	None	-186	2	Human	6.3	pIC50	=	6.3	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	380	3	0	5	2.7	COCc1cn(C2=NCC(=O)N3CCc4c(cc(F)cc4C4CC4)C3=C2)cn1	nan
	72163720	91603	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	376	2	0	4	3.1	N#Cc1cccnc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418384	91603	0	None	-	1	Human	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	376	2	0	4	3.1	N#Cc1cccnc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1	10.1016/j.bmcl.2013.07.029
	127034265	138543	0	None	-	1	Rat	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	296	2	2	6	2.9	C[C@H]1CC[C@H](Nc2nc(N)nc3c2nn2ccccc32)CC1	10.1016/j.bmcl.2016.03.026
	CHEMBL3786386	138543	0	None	-	1	Rat	5.3	pIC50	=	5.3	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	296	2	2	6	2.9	C[C@H]1CC[C@H](Nc2nc(N)nc3c2nn2ccccc32)CC1	10.1016/j.bmcl.2016.03.026
	78322694	151625	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	348	3	0	5	4.4	COc1ccc(-n2c(C)nc3c(-c4ccccc4)csc3c2=O)cc1	nan
	CHEMBL3968177	151625	0	None	-	1	Human	6.3	pIC50	=	6.3	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	348	3	0	5	4.4	COc1ccc(-n2c(C)nc3c(-c4ccccc4)csc3c2=O)cc1	nan
	44588428	176258	0	None	5	3	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	343	2	1	4	3.0	CC(C)(C)NC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL461034	176258	0	None	5	3	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	343	2	1	4	3.0	CC(C)(C)NC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	78321115	113844	3	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	352	3	0	5	4.3	COc1ccc(-n2cnc3c(-c4ccccc4F)csc3c2=O)cc1	10.1016/j.ejmech.2014.08.027
	CHEMBL3330817	113844	3	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	352	3	0	5	4.3	COc1ccc(-n2cnc3c(-c4ccccc4F)csc3c2=O)cc1	10.1016/j.ejmech.2014.08.027
	45486817	196798	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	314	3	0	5	3.0	CN(C(=O)c1ccc(F)cc1)c1nc(-c2ncccn2)cs1	10.1016/j.bmcl.2009.07.097
	CHEMBL577505	196798	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	314	3	0	5	3.0	CN(C(=O)c1ccc(F)cc1)c1nc(-c2ncccn2)cs1	10.1016/j.bmcl.2009.07.097
	44329029	162969	0	None	-2	6	Human	5.2	pIC50	=	5.2	Functional	Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluated	ChEMBL	479	13	3	4	6.2	CCCCCCCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O	10.1016/s0960-894x(98)00510-1
	CHEMBL420262	162969	0	None	-2	6	Human	5.2	pIC50	=	5.2	Functional	Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluated	ChEMBL	479	13	3	4	6.2	CCCCCCCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O	10.1016/s0960-894x(98)00510-1
	44328753	206020	0	None	-1995	6	Human	4.2	pIC50	=	4.2	Functional	Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluated	ChEMBL	409	8	3	4	4.2	CCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O	10.1016/s0960-894x(98)00510-1
	CHEMBL95868	206020	0	None	-1995	6	Human	4.2	pIC50	=	4.2	Functional	Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluated	ChEMBL	409	8	3	4	4.2	CCCC[C@@H]1[C@H](C(=O)O)[C@H]1C(N)(CC1c2ccccc2Oc2ccccc21)C(=O)O	10.1016/s0960-894x(98)00510-1
	22884216	197040	10	None	-	1	Human	4.2	pIC50	=	4.2	Functional	In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 1 expressed in RGT cells.In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 1 expressed in RGT cells.	ChEMBL	209	4	3	3	1.3	C[C@H](Nc1ccc(C(=O)O)cc1)C(=O)O	10.1016/s0960-894x(98)00352-7
	CHEMBL58247	197040	10	None	-	1	Human	4.2	pIC50	=	4.2	Functional	In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 1 expressed in RGT cells.In vitro antagonist activity at recombinant human Metabotropic glutamate receptor 1 expressed in RGT cells.	ChEMBL	209	4	3	3	1.3	C[C@H](Nc1ccc(C(=O)O)cc1)C(=O)O	10.1016/s0960-894x(98)00352-7
	78324867	113833	3	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	322	2	0	4	4.3	O=c1c2scc(-c3ccccc3)c2ncn1-c1cccc(F)c1	10.1016/j.ejmech.2014.08.027
	CHEMBL3330801	113833	3	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	322	2	0	4	4.3	O=c1c2scc(-c3ccccc3)c2ncn1-c1cccc(F)c1	10.1016/j.ejmech.2014.08.027
	44588426	188613	0	None	-5	3	Mouse	7.2	pIC50	=	7.2	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	340	2	0	5	3.6	Cc1ccccc1-n1cc(C2=CCN(C(=O)OC(C)(C)C)CC2)nn1	10.1016/j.bmc.2008.09.060
	CHEMBL511352	188613	0	None	-5	3	Mouse	7.2	pIC50	=	7.2	Functional	Antagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	340	2	0	5	3.6	Cc1ccccc1-n1cc(C2=CCN(C(=O)OC(C)(C)C)CC2)nn1	10.1016/j.bmc.2008.09.060
	78324870	113836	3	None	-	1	Human	7.2	pIC50	=	7.2	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	338	2	0	4	4.8	O=c1c2scc(-c3ccccc3)c2ncn1-c1cccc(Cl)c1	nan
	CHEMBL3330804	113836	3	None	-	1	Human	7.2	pIC50	=	7.2	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	338	2	0	4	4.8	O=c1c2scc(-c3ccccc3)c2ncn1-c1cccc(Cl)c1	nan
	1418	3393	48	None	-1	2	Human	4.2	pIC50	=	4.2	Functional	Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis	ChEMBL	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	10.1016/S0960-894X(97)10071-3
	5311459	3393	48	None	-1	2	Human	4.2	pIC50	=	4.2	Functional	Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis	ChEMBL	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	10.1016/S0960-894X(97)10071-3
	CHEMBL94990	3393	48	None	-1	2	Human	4.2	pIC50	=	4.2	Functional	Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis	ChEMBL	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	10.1016/S0960-894X(97)10071-3
	73334945	132496	0	None	-24	2	Human	6.2	pIC50	=	6.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	349	3	0	5	2.3	COc1cc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)ccn1	nan
	CHEMBL3702358	132496	0	None	-24	2	Human	6.2	pIC50	=	6.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	349	3	0	5	2.3	COc1cc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)ccn1	nan
	89980086	132586	0	None	-85	2	Human	5.2	pIC50	=	5.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	413	2	0	5	3.6	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cnccc4F)c3CCN12	nan
	CHEMBL3702447	132586	0	None	-85	2	Human	5.2	pIC50	=	5.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	413	2	0	5	3.6	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cnccc4F)c3CCN12	nan
	76328955	105125	0	None	-1047	2	Human	5.2	pIC50	=	5.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay	ChEMBL	339	6	0	6	2.4	CCN(CC)C(=O)c1nn(C)c2nc(OCc3ccccn3)ccc12	10.1021/jm401622k
	CHEMBL3122224	105125	0	None	-1047	2	Human	5.2	pIC50	=	5.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate-induced calcium flux after 16 to 24 hrs by FLIPR assay	ChEMBL	339	6	0	6	2.4	CCN(CC)C(=O)c1nn(C)c2nc(OCc3ccccn3)ccc12	10.1021/jm401622k
	44588427	176257	0	None	2	3	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	356	3	0	6	3.3	COc1ccccc1-n1cc(C2=CCN(C(=O)OC(C)(C)C)CC2)nn1	10.1016/j.bmc.2008.09.060
	CHEMBL461033	176257	0	None	2	3	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	356	3	0	6	3.3	COc1ccccc1-n1cc(C2=CCN(C(=O)OC(C)(C)C)CC2)nn1	10.1016/j.bmc.2008.09.060
	73335735	132572	0	None	-489	2	Human	5.2	pIC50	=	5.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	400	2	0	4	3.9	CCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4ccc(F)cc4)C3=C2)cn1	nan
	CHEMBL3702434	132572	0	None	-489	2	Human	5.2	pIC50	=	5.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	400	2	0	4	3.9	CCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4ccc(F)cc4)C3=C2)cn1	nan
	89979678	132593	0	None	-158	2	Human	5.2	pIC50	=	5.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	413	2	0	5	3.6	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cccnc4F)c3CCN12	nan
	CHEMBL3702454	132593	0	None	-158	2	Human	5.2	pIC50	=	5.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	413	2	0	5	3.6	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cccnc4F)c3CCN12	nan
	71682802	90615	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@@H]1CN(c2cccnc2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397368	90615	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@@H]1CN(c2cccnc2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	57559562	952	0	None	1659	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	365	4	1	8	3.0	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ncn1)NC1CC1	10.1016/j.bmcl.2012.09.048
	6365	952	0	None	1659	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	365	4	1	8	3.0	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ncn1)NC1CC1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205915	952	0	None	1659	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	365	4	1	8	3.0	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ncn1)NC1CC1	10.1016/j.bmcl.2012.09.048
	16661408	196134	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	313	3	0	4	3.6	CN(C(=O)c1ccc(F)cc1)c1nc(-c2ccccn2)cs1	10.1016/j.bmcl.2009.07.097
	CHEMBL572135	196134	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	313	3	0	4	3.6	CN(C(=O)c1ccc(F)cc1)c1nc(-c2ccccn2)cs1	10.1016/j.bmcl.2009.07.097
	16659963	149343	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	353	1	1	6	3.5	O=c1c2sc3ncc4nc[nH]c4c3c2ncn1-c1ccc(Cl)cc1	10.1021/jm070590c
	CHEMBL394914	149343	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	353	1	1	6	3.5	O=c1c2sc3ncc4nc[nH]c4c3c2ncn1-c1ccc(Cl)cc1	10.1021/jm070590c
	44447971	94531	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	357	4	0	5	3.2	Cc1c(C2=CCC(C(=O)N(C)C(C)C)CC2)nnn1-c1cccnc1F	10.1021/jm060950g
	CHEMBL254573	94531	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	357	4	0	5	3.2	Cc1c(C2=CCC(C(=O)N(C)C(C)C)CC2)nnn1-c1cccnc1F	10.1021/jm060950g
	9926083	94312	7	None	-	1	Rat	8.2	pIC50	=	8.2	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	292	2	0	4	2.8	CCc1nc(C#N)c(N2CCc3ccccc3CC2)nc1C	10.1021/jm0611298
	CHEMBL253142	94312	7	None	-	1	Rat	8.2	pIC50	=	8.2	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	292	2	0	4	2.8	CCc1nc(C#N)c(N2CCc3ccccc3CC2)nc1C	10.1021/jm0611298
	44588385	176321	0	None	2	3	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	344	2	0	5	3.4	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL461673	176321	0	None	2	3	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	344	2	0	5	3.4	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccc3F)nn2)CC1	10.1016/j.bmc.2008.09.060
	16118119	1127	0	None	741	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	351	3	0	6	3.7	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1016/j.bmcl.2011.12.131
	6356	1127	0	None	741	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	351	3	0	6	3.7	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1016/j.bmcl.2011.12.131
	CHEMBL1951658	1127	0	None	741	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	351	3	0	6	3.7	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1016/j.bmcl.2011.12.131
	16118126	70637	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	338	3	0	6	3.6	COc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951670	70637	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	338	3	0	6	3.6	COc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	16118815	70691	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	352	3	0	7	3.1	COc1ccc(-n2ccc3c(sc4ncnc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951883	70691	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	352	3	0	7	3.1	COc1ccc(-n2ccc3c(sc4ncnc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	16118818	70695	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	336	2	0	6	3.4	Cc1ccc(-n2ccc3c(sc4ncnc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951887	70695	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	336	2	0	6	3.4	Cc1ccc(-n2ccc3c(sc4ncnc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	23634102	963	1	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	362	4	1	7	3.0	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC	10.1016/j.ejmech.2014.08.027
	6215	963	1	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	362	4	1	7	3.0	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC	10.1016/j.ejmech.2014.08.027
	CHEMBL1783876	963	1	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	362	4	1	7	3.0	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC	10.1016/j.ejmech.2014.08.027
	54584443	62329	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	382	5	1	7	3.7	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(F)c(OC)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783862	62329	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	382	5	1	7	3.7	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(F)c(OC)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54585851	62436	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	411	3	1	7	3.2	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784070	62436	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	411	3	1	7	3.2	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54581505	62332	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	378	5	0	7	3.6	C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783865	62332	0	None	-	1	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	378	5	0	7	3.6	C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54586361	62327	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	368	4	1	6	4.2	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783860	62327	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	368	4	1	6	4.2	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	57881958	83405	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	379	4	1	8	3.4	COc1ccc(-n2cnc3c(sc4ncnc(NC5CCC5)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205918	83405	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	379	4	1	8	3.4	COc1ccc(-n2cnc3c(sc4ncnc(NC5CCC5)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	118735966	118409	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	391	4	1	4	4.6	N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1ccc(F)cc1)C2	10.1016/j.ejmech.2015.04.060
	CHEMBL3422882	118409	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assayAntagonist activity at human mGluR1 expressed in human Chem-3 cells assessed as inhibition of L-glutamate-induced calcium release by calcium-5 reagent-based fluorescence assay	ChEMBL	391	4	1	4	4.6	N#Cc1c(NCc2ccccc2)sc2c1CCN(C(=O)c1ccc(F)cc1)C2	10.1016/j.ejmech.2015.04.060
	9815955	105505	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis	ChEMBL	225	3	4	4	0.5	Cc1c(C(N)C(=O)O)ccc(C(=O)O)c1O	10.1016/S0960-894X(97)10071-3
	CHEMBL313124	105505	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis	ChEMBL	225	3	4	4	0.5	Cc1c(C(N)C(=O)O)ccc(C(=O)O)c1O	10.1016/S0960-894X(97)10071-3
	71682802	90615	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@@H]1CN(c2cccnc2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397368	90615	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@@H]1CN(c2cccnc2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	16661404	196738	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	329	3	0	4	4.1	CN(C(=O)c1ccc(Cl)cc1)c1nc(-c2ccncc2)cs1	10.1016/j.bmcl.2009.07.097
	CHEMBL577035	196738	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	329	3	0	4	4.1	CN(C(=O)c1ccc(Cl)cc1)c1nc(-c2ccncc2)cs1	10.1016/j.bmcl.2009.07.097
	18138918	58511	2	None	-1	3	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	331	2	0	4	3.0	O=C(N1CCN(c2nccs2)CC1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL1688377	58511	2	None	-1	3	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	331	2	0	4	3.0	O=C(N1CCN(c2nccs2)CC1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	18138918	58511	2	None	-1	3	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	331	2	0	4	3.0	O=C(N1CCN(c2nccs2)CC1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL1688377	58511	2	None	-1	3	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	331	2	0	4	3.0	O=C(N1CCN(c2nccs2)CC1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	11565466	84622	0	None	1	2	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	286	2	0	6	2.4	CN(C)c1ccnc2sc3c(=O)n(C4CC4)cnc3c12	10.1021/jm0504407
	CHEMBL224135	84622	0	None	1	2	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	286	2	0	6	2.4	CN(C)c1ccnc2sc3c(=O)n(C4CC4)cnc3c12	10.1021/jm0504407
	16659798	88217	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	396	2	0	8	4.6	CSc1nc2c(cnc3sc4c(=O)n(-c5ccc(C)cc5)cnc4c32)s1	10.1021/jm070590c
	CHEMBL235767	88217	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	396	2	0	8	4.6	CSc1nc2c(cnc3sc4c(=O)n(-c5ccc(C)cc5)cnc4c32)s1	10.1021/jm070590c
	73335827	132590	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	347	1	0	5	2.5	Cc1ncn(C2=NCC(=O)N3CCc4c(cccc4C4CCC4)C3=C2)n1	nan
	CHEMBL3702451	132590	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	347	1	0	5	2.5	Cc1ncn(C2=NCC(=O)N3CCc4c(cccc4C4CCC4)C3=C2)n1	nan
	73334852	124600	0	None	-23	2	Human	5.2	pIC50	=	5.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	348	3	0	4	2.9	COc1cccc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)c1	nan
	CHEMBL3644416	124600	0	None	-23	2	Human	5.2	pIC50	=	5.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	348	3	0	4	2.9	COc1cccc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)c1	nan
	91618208	132557	0	None	-239	2	Human	5.2	pIC50	=	5.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	388	3	1	6	2.1	COCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4ncc[nH]4)C3=C2)cn1	nan
	CHEMBL3702419	132557	0	None	-239	2	Human	5.2	pIC50	=	5.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	388	3	1	6	2.1	COCc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4ncc[nH]4)C3=C2)cn1	nan
	685051	91266	10	None	-25	2	Human	4.2	pIC50	=	4.2	Functional	Negative allosteric modulation of human mGluR1 expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular cAMP accumulation treated 5 mins before L-quisqualate addition by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular cAMP accumulation treated 5 mins before L-quisqualate addition by FLIPR assay	ChEMBL	248	2	1	3	3.9	Fc1ccc(Nc2nc3c(s2)CCCC3)cc1	10.1016/j.bmcl.2013.06.049
	CHEMBL2408581	91266	10	None	-25	2	Human	4.2	pIC50	=	4.2	Functional	Negative allosteric modulation of human mGluR1 expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular cAMP accumulation treated 5 mins before L-quisqualate addition by FLIPR assayNegative allosteric modulation of human mGluR1 expressed in CHO cells assessed as inhibition of L-glutamate-induced intracellular cAMP accumulation treated 5 mins before L-quisqualate addition by FLIPR assay	ChEMBL	248	2	1	3	3.9	Fc1ccc(Nc2nc3c(s2)CCCC3)cc1	10.1016/j.bmcl.2013.06.049
	44243470	88669	0	None	-33	3	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	431	5	1	6	5.5	CC(C)c1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2334981	88669	0	None	-33	3	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	431	5	1	6	5.5	CC(C)c1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2365395	88669	0	None	-33	3	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	431	5	1	6	5.5	CC(C)c1cccc(-c2c(-c3ccc4nn(C)cc4c3)nsc2NC(=O)[C@@H]2C[C@H]2C)n1	10.1016/j.bmcl.2013.01.009
	67179855	72867	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	272	3	1	3	3.7	Cc1c(-c2ccccc2)nsc1NC(=O)[C@@H]1C[C@H]1C	10.1016/j.bmcl.2012.02.003
	CHEMBL2011872	72867	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	272	3	1	3	3.7	Cc1c(-c2ccccc2)nsc1NC(=O)[C@@H]1C[C@H]1C	10.1016/j.bmcl.2012.02.003
	73335824	132587	0	None	-22	2	Human	6.2	pIC50	=	6.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	348	2	0	4	3.3	CCc1cccc2c1CCN1C(=O)CN=C(n3cnc(C(C)C)c3)C=C21	nan
	CHEMBL3702448	132587	0	None	-22	2	Human	6.2	pIC50	=	6.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	348	2	0	4	3.3	CCc1cccc2c1CCN1C(=O)CN=C(n3cnc(C(C)C)c3)C=C21	nan
	73335445	132546	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	378	4	0	5	2.9	COc1cccc(C2=NCC(=O)N3CCc4c(ccc(OC)c4OC)C3=C2)c1	nan
	CHEMBL3702408	132546	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	378	4	0	5	2.9	COc1cccc(C2=NCC(=O)N3CCc4c(ccc(OC)c4OC)C3=C2)c1	nan
	5115	111555	39	None	-	1	Human	4.2	pIC50	=	4.2	Functional	Ability to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M ConcentrationAbility to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M Concentration	ChEMBL	195	3	3	3	0.5	NC(C(=O)O)c1ccc(C(=O)O)cc1	10.1021/jm00019a002
	CHEMBL328984	111555	39	None	-	1	Human	4.2	pIC50	=	4.2	Functional	Ability to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M ConcentrationAbility to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M Concentration	ChEMBL	195	3	3	3	0.5	NC(C(=O)O)c1ccc(C(=O)O)cc1	10.1021/jm00019a002
	127033444	138504	0	None	-	1	Rat	5.2	pIC50	=	5.2	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	269	2	1	5	3.1	C[C@H](Nc1ncnc2c1nn1ccccc21)C(C)(C)C	10.1016/j.bmcl.2016.03.026
	CHEMBL3785899	138504	0	None	-	1	Rat	5.2	pIC50	=	5.2	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	269	2	1	5	3.1	C[C@H](Nc1ncnc2c1nn1ccccc21)C(C)(C)C	10.1016/j.bmcl.2016.03.026
	54586362	62333	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	426	4	0	6	4.4	C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783866	62333	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	426	4	0	6	4.4	C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	78324868	113834	3	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	322	2	0	4	4.3	O=c1c2scc(-c3ccccc3)c2ncn1-c1ccc(F)cc1	10.1016/j.ejmech.2014.08.027
	CHEMBL3330802	113834	3	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	322	2	0	4	4.3	O=c1c2scc(-c3ccccc3)c2ncn1-c1ccc(F)cc1	10.1016/j.ejmech.2014.08.027
	78324871	113837	3	None	-	1	Human	7.2	pIC50	=	7.2	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	338	2	0	4	4.8	O=c1c2scc(-c3ccccc3)c2ncn1-c1ccc(Cl)cc1	nan
	CHEMBL3330805	113837	3	None	-	1	Human	7.2	pIC50	=	7.2	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	338	2	0	4	4.8	O=c1c2scc(-c3ccccc3)c2ncn1-c1ccc(Cl)cc1	nan
	89980452	124576	0	None	-19	2	Human	6.2	pIC50	=	6.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	374	2	0	5	3.0	CC(=O)c1cccc2c1CCN1C(=O)CN=C(n3cnc(C4CCC4)c3)C=C21	nan
	CHEMBL3644392	124576	0	None	-19	2	Human	6.2	pIC50	=	6.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	374	2	0	5	3.0	CC(=O)c1cccc2c1CCN1C(=O)CN=C(n3cnc(C4CCC4)c3)C=C21	nan
	1382	1167	29	None	-1	3	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at human mGlu1b receptorAntagonist activity at human mGlu1b receptor	ChEMBL	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	10.1021/jm060950g
	6278000	1167	29	None	-1	3	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at human mGlu1b receptorAntagonist activity at human mGlu1b receptor	ChEMBL	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	10.1021/jm060950g
	CHEMBL327783	1167	29	None	-1	3	Human	5.2	pIC50	=	5.2	Functional	Antagonist activity at human mGlu1b receptorAntagonist activity at human mGlu1b receptor	ChEMBL	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	10.1021/jm060950g
	71682497	90612	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	315	2	0	3	3.5	C[C@@H]1CN(c2ccccn2)CCN1C(=O)C1CCCCCCC1	10.1016/j.bmcl.2013.05.020
	CHEMBL2397360	90612	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	315	2	0	3	3.5	C[C@@H]1CN(c2ccccn2)CCN1C(=O)C1CCCCCCC1	10.1016/j.bmcl.2013.05.020
	127033444	138504	0	None	-	1	Rat	5.2	pIC50	=	5.2	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	269	2	1	5	3.1	C[C@H](Nc1ncnc2c1nn1ccccc21)C(C)(C)C	10.1016/j.bmcl.2016.03.026
	CHEMBL3785899	138504	0	None	-	1	Rat	5.2	pIC50	=	5.2	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	269	2	1	5	3.1	C[C@H](Nc1ncnc2c1nn1ccccc21)C(C)(C)C	10.1016/j.bmcl.2016.03.026
	86729808	113848	3	None	-	1	Human	6.2	pIC50	=	6.2	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	348	3	0	5	4.4	COc1ccc(-n2cnc3c(-c4ccc(C)cc4)csc3c2=O)cc1	nan
	CHEMBL3330825	113848	3	None	-	1	Human	6.2	pIC50	=	6.2	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	348	3	0	5	4.4	COc1ccc(-n2cnc3c(-c4ccc(C)cc4)csc3c2=O)cc1	nan
	71682497	90612	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	315	2	0	3	3.5	C[C@@H]1CN(c2ccccn2)CCN1C(=O)C1CCCCCCC1	10.1016/j.bmcl.2013.05.020
	CHEMBL2397360	90612	0	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	315	2	0	3	3.5	C[C@@H]1CN(c2ccccn2)CCN1C(=O)C1CCCCCCC1	10.1016/j.bmcl.2013.05.020
	72163582	91598	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	352	2	0	4	2.6	O=C(N1C[C@@H]2CN(c3cnccn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	CHEMBL2418379	91598	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	352	2	0	4	2.6	O=C(N1C[C@@H]2CN(c3cnccn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	67181693	72874	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	336	4	1	3	4.8	Cc1c(-c2ccc(C(C)(F)F)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C	10.1016/j.bmcl.2012.02.003
	CHEMBL2011879	72874	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	336	4	1	3	4.8	Cc1c(-c2ccc(C(C)(F)F)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C	10.1016/j.bmcl.2012.02.003
	89980670	123879	0	None	-338	2	Human	6.2	pIC50	=	6.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	350	2	0	4	2.9	O=C1CN=C(n2cnc(CF)c2)C=C2c3cccc(C4CC4)c3CCN12	nan
	CHEMBL3639432	123879	0	None	-338	2	Human	6.2	pIC50	=	6.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	350	2	0	4	2.9	O=C1CN=C(n2cnc(CF)c2)C=C2c3cccc(C4CC4)c3CCN12	nan
	72163582	91598	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	352	2	0	4	2.6	O=C(N1C[C@@H]2CN(c3cnccn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	CHEMBL2418379	91598	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	352	2	0	4	2.6	O=C(N1C[C@@H]2CN(c3cnccn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	78324866	113645	3	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	322	2	0	4	4.3	O=c1c2scc(-c3ccccc3)c2ncn1-c1ccccc1F	10.1016/j.ejmech.2014.08.027
	CHEMBL3329236	113645	3	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	322	2	0	4	4.3	O=c1c2scc(-c3ccccc3)c2ncn1-c1ccccc1F	10.1016/j.ejmech.2014.08.027
	46886137	8147	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	327	1	1	7	2.4	Cc1nc(N)c2c(n1)sc1c(=O)n(-c3ccc(F)cc3)cnc12	10.1016/j.bmcl.2010.03.004
	CHEMBL1092276	8147	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	327	1	1	7	2.4	Cc1nc(N)c2c(n1)sc1c(=O)n(-c3ccc(F)cc3)cnc12	10.1016/j.bmcl.2010.03.004
	16117168	70653	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	325	2	1	5	3.8	CNc1ccnc2sc3c(=O)n(-c4ccc(F)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951689	70653	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	325	2	1	5	3.8	CNc1ccnc2sc3c(=O)n(-c4ccc(F)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	44431060	86324	0	None	-	1	Rat	6.2	pIC50	=	6.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	278	3	2	2	3.0	O=C1NCc2c1[nH]c1ccc(OCc3ccccc3)cc21	10.1016/j.bmcl.2007.01.055
	CHEMBL232012	86324	0	None	-	1	Rat	6.2	pIC50	=	6.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	278	3	2	2	3.0	O=C1NCc2c1[nH]c1ccc(OCc3ccccc3)cc21	10.1016/j.bmcl.2007.01.055
	73336217	132602	0	None	-43	2	Human	6.2	pIC50	=	6.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	380	3	0	5	2.7	COCc1cn(C2=NCC(=O)N3CCc4c(C5CC5)ccc(F)c4C3=C2)cn1	nan
	CHEMBL3702465	132602	0	None	-43	2	Human	6.2	pIC50	=	6.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	380	3	0	5	2.7	COCc1cn(C2=NCC(=O)N3CCc4c(C5CC5)ccc(F)c4C3=C2)cn1	nan
	57908400	88673	0	None	-12	2	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	443	5	1	6	5.6	C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C2CCC2)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2334983	88673	0	None	-12	2	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	443	5	1	6	5.6	C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C2CCC2)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2365403	88673	0	None	-12	2	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	443	5	1	6	5.6	C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C2CCC2)n1	10.1016/j.bmcl.2013.01.009
	45484921	196847	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	290	2	0	5	2.8	Cc1c(-c2ccc3c(c2)CCC3=O)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	CHEMBL577943	196847	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	290	2	0	5	2.8	Cc1c(-c2ccc3c(c2)CCC3=O)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	127034286	138630	0	None	1	2	Rat	7.2	pIC50	=	7.2	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	2	1	5	3.7	CC1(C)CCC(Nc2ncnc3c2nn2ccccc32)CC1	10.1016/j.bmcl.2016.03.026
	CHEMBL3787247	138630	0	None	1	2	Rat	7.2	pIC50	=	7.2	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	2	1	5	3.7	CC1(C)CCC(Nc2ncnc3c2nn2ccccc32)CC1	10.1016/j.bmcl.2016.03.026
	127034286	138630	0	None	1	2	Rat	7.2	pIC50	=	7.2	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	2	1	5	3.7	CC1(C)CCC(Nc2ncnc3c2nn2ccccc32)CC1	10.1016/j.bmcl.2016.03.026
	CHEMBL3787247	138630	0	None	1	2	Rat	7.2	pIC50	=	7.2	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	2	1	5	3.7	CC1(C)CCC(Nc2ncnc3c2nn2ccccc32)CC1	10.1016/j.bmcl.2016.03.026
	73335034	132503	0	None	-4	2	Human	6.2	pIC50	=	6.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	322	2	0	5	1.7	COc1cccc2c1CCN1C(=O)CN=C(c3ccn(C)n3)C=C21	nan
	CHEMBL3702365	132503	0	None	-4	2	Human	6.2	pIC50	=	6.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	322	2	0	5	1.7	COc1cccc2c1CCN1C(=O)CN=C(c3ccn(C)n3)C=C21	nan
	73335338	132525	0	None	-1	2	Human	5.2	pIC50	=	5.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	418	1	0	4	2.3	Cn1cnc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)c1	nan
	CHEMBL3702387	132525	0	None	-1	2	Human	5.2	pIC50	=	5.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	418	1	0	4	2.3	Cn1cnc(C2=NCC(=O)N3CCc4c(I)cccc4C3=C2)c1	nan
	67182345	72869	0	None	22	2	Human	8.2	pIC50	=	8.2	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	320	4	1	4	3.9	COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1F	10.1016/j.bmcl.2012.02.003
	CHEMBL2011874	72869	0	None	22	2	Human	8.2	pIC50	=	8.2	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	320	4	1	4	3.9	COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1F	10.1016/j.bmcl.2012.02.003
	67182239	72872	0	None	102	2	Human	8.2	pIC50	=	8.2	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	350	3	1	3	4.5	Cc1c(-c2ccc(Br)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C	10.1016/j.bmcl.2012.02.003
	CHEMBL2011877	72872	0	None	102	2	Human	8.2	pIC50	=	8.2	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	350	3	1	3	4.5	Cc1c(-c2ccc(Br)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C	10.1016/j.bmcl.2012.02.003
	16725048	1131	0	None	1412	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	371	3	0	8	2.6	COc1ccc(c(c1)F)n1cnc2c(c1=O)sc1c2c(ncn1)N(C)C	10.1016/j.bmcl.2012.09.048
	6362	1131	0	None	1412	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	371	3	0	8	2.6	COc1ccc(c(c1)F)n1cnc2c(c1=O)sc1c2c(ncn1)N(C)C	10.1016/j.bmcl.2012.09.048
	CHEMBL2205377	1131	0	None	1412	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	371	3	0	8	2.6	COc1ccc(c(c1)F)n1cnc2c(c1=O)sc1c2c(ncn1)N(C)C	10.1016/j.bmcl.2012.09.048
	57559437	83395	0	None	1412	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	353	4	1	8	2.8	CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	CHEMBL2205908	83395	0	None	1412	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	353	4	1	8	2.8	CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2012.09.048
	57881665	83415	0	None	28	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	329	2	0	7	3.0	CN(C)c1ncnc2sc3c(=O)n(C4CCCCC4)cnc3c12	10.1016/j.bmcl.2012.09.048
	CHEMBL2205928	83415	0	None	28	2	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	329	2	0	7	3.0	CN(C)c1ncnc2sc3c(=O)n(C4CCCCC4)cnc3c12	10.1016/j.bmcl.2012.09.048
	44588464	174498	0	None	-4	3	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	359	2	0	6	3.1	Cc1c(C2=CCN(C(=O)OC(C)(C)C)CC2)nnn1-c1ncccc1F	10.1016/j.bmc.2008.09.060
	CHEMBL456823	174498	0	None	-4	3	Human	8.2	pIC50	=	8.2	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	359	2	0	6	3.1	Cc1c(C2=CCN(C(=O)OC(C)(C)C)CC2)nnn1-c1ncccc1F	10.1016/j.bmc.2008.09.060
	11695894	174220	0	None	-2	3	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	345	3	0	6	2.7	Cc1c(C2=CCN(C(=O)OC(C)C)CC2)nnn1-c1cccnc1F	10.1016/j.bmc.2008.09.060
	CHEMBL456196	174220	0	None	-2	3	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	345	3	0	6	2.7	Cc1c(C2=CCN(C(=O)OC(C)C)CC2)nnn1-c1cccnc1F	10.1016/j.bmc.2008.09.060
	54579958	62420	0	None	-	1	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	383	4	1	7	4.0	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784054	62420	0	None	-	1	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	383	4	1	7	4.0	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	16118535	70685	0	None	-	1	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	335	3	1	5	4.3	CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951877	70685	0	None	-	1	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	335	3	1	5	4.3	CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	57881832	83289	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	341	3	1	7	3.5	O=c1c2sc3ncnc(NC4CC4)c3c2ncn1C1CCCCC1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205373	83289	0	None	-	1	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	341	3	1	7	3.5	O=c1c2sc3ncnc(NC4CC4)c3c2ncn1C1CCCCC1	10.1016/j.bmcl.2012.09.048
	1376	318	50	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Ability to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M ConcentrationAbility to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M Concentration	ChEMBL	221	2	3	3	0.6	OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O	10.1021/jm00019a002
	2071	318	50	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Ability to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M ConcentrationAbility to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M Concentration	ChEMBL	221	2	3	3	0.6	OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O	10.1021/jm00019a002
	CHEMBL313938	318	50	None	-	1	Human	5.2	pIC50	=	5.2	Functional	Ability to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M ConcentrationAbility to inhibit mGluR1-alpha-mediated PI (phospho inositol) hydrolysis was determined at BHK cells at 100 Micro M Concentration	ChEMBL	221	2	3	3	0.6	OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O	10.1021/jm00019a002
	2931812	94351	13	None	-	1	Rat	5.2	pIC50	=	5.2	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	257	2	1	3	2.2	O=C(NC12CC3CC(CC(C3)C1)C2)c1cnccn1	10.1021/jm0611298
	CHEMBL253348	94351	13	None	-	1	Rat	5.2	pIC50	=	5.2	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	257	2	1	3	2.2	O=C(NC12CC3CC(CC(C3)C1)C2)c1cnccn1	10.1021/jm0611298
	89980255	124581	0	None	-2290	2	Human	5.2	pIC50	=	5.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	376	3	0	5	3.2	CO[C@H](C)c1cn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)cn1	nan
	CHEMBL3644397	124581	0	None	-2290	2	Human	5.2	pIC50	=	5.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	376	3	0	5	3.2	CO[C@H](C)c1cn(C2=NCC(=O)N3CCc4c(cccc4C4CC4)C3=C2)cn1	nan
	89980164	124548	0	None	-354	2	Human	6.2	pIC50	=	6.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	368	2	0	4	3.4	O=C1CN=C(n2cnc(C(F)F)c2)C=C2c3cccc(C4CC4)c3CCN12	nan
	CHEMBL3644362	124548	0	None	-354	2	Human	6.2	pIC50	=	6.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	368	2	0	4	3.4	O=C1CN=C(n2cnc(C(F)F)c2)C=C2c3cccc(C4CC4)c3CCN12	nan
	71683126	90603	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	357	2	0	3	3.5	C[C@@H]1CN(c2ncccc2F)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397343	90603	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	357	2	0	3	3.5	C[C@@H]1CN(c2ncccc2F)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	71682806	90616	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	340	2	0	4	2.7	C[C@@H]1CN(c2ncccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397372	90616	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	340	2	0	4	2.7	C[C@@H]1CN(c2ncccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	11581985	84729	0	None	1	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	394	6	0	7	3.6	CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCOC)c43)c2=O)cc1	10.1021/jm0504407
	CHEMBL225125	84729	0	None	1	2	Human	7.2	pIC50	=	7.2	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	394	6	0	7	3.6	CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCOC)c43)c2=O)cc1	10.1021/jm0504407
	44431045	86296	0	None	-	1	Rat	7.2	pIC50	=	7.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	363	2	3	2	3.2	O=C(NC12CC3CC(CC(C3)C1)C2)c1ccc2[nH]c3c(c2c1)CCNC3=O	10.1016/j.bmcl.2007.01.055
	CHEMBL231842	86296	0	None	-	1	Rat	7.2	pIC50	=	7.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	363	2	3	2	3.2	O=C(NC12CC3CC(CC(C3)C1)C2)c1ccc2[nH]c3c(c2c1)CCNC3=O	10.1016/j.bmcl.2007.01.055
	44431050	141812	0	None	-	1	Rat	7.2	pIC50	=	7.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	363	2	3	2	3.6	O=C1NCCc2c1[nH]c1ccc(NC(=O)C34CC5CC(CC(C5)C3)C4)cc21	10.1016/j.bmcl.2007.01.055
	CHEMBL388669	141812	0	None	-	1	Rat	7.2	pIC50	=	7.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	363	2	3	2	3.6	O=C1NCCc2c1[nH]c1ccc(NC(=O)C34CC5CC(CC(C5)C3)C4)cc21	10.1016/j.bmcl.2007.01.055
	86711407	124612	0	None	-117	2	Human	6.2	pIC50	=	6.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	348	2	1	5	1.9	O=C1CN=C(n2cnc(CO)c2)C=C2c3cccc(C4CC4)c3CCN12	nan
	CHEMBL3644428	124612	0	None	-117	2	Human	6.2	pIC50	=	6.2	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	348	2	1	5	1.9	O=C1CN=C(n2cnc(CO)c2)C=C2c3cccc(C4CC4)c3CCN12	nan
	71683126	90603	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	357	2	0	3	3.5	C[C@@H]1CN(c2ncccc2F)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397343	90603	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	357	2	0	3	3.5	C[C@@H]1CN(c2ncccc2F)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	45375910	5429	2	None	-7	2	Rat	6.2	pIC50	=	6.2	Functional	Antagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assayAntagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assay	ChEMBL	317	2	1	3	4.3	Fc1ccc2ncnc(Nc3cccc(Br)c3)c2c1	10.1016/j.bmcl.2009.10.024
	CHEMBL1076333	5429	2	None	-7	2	Rat	6.2	pIC50	=	6.2	Functional	Antagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assayAntagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assay	ChEMBL	317	2	1	3	4.3	Fc1ccc2ncnc(Nc3cccc(Br)c3)c2c1	10.1016/j.bmcl.2009.10.024
	71682806	90616	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	340	2	0	4	2.7	C[C@@H]1CN(c2ncccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397372	90616	0	None	-	1	Human	6.2	pIC50	=	6.2	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	340	2	0	4	2.7	C[C@@H]1CN(c2ncccn2)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	54584889	62424	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	397	5	1	8	3.5	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784058	62424	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	397	5	1	8	3.5	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	10036599	112030	0	None	-	1	Human	4.1	pIC50	=	4.1	Functional	Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis	ChEMBL	225	3	4	4	0.5	Cc1cc(C(=O)O)c(O)cc1C(N)C(=O)O	10.1016/S0960-894X(97)10071-3
	CHEMBL329905	112030	0	None	-	1	Human	4.1	pIC50	=	4.1	Functional	Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis	ChEMBL	225	3	4	4	0.5	Cc1cc(C(=O)O)c(O)cc1C(N)C(=O)O	10.1016/S0960-894X(97)10071-3
	89980507	124562	0	None	-44	2	Human	5.1	pIC50	=	5.1	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	370	1	0	6	2.3	Cc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4cnccn4)C3=C2)cn1	nan
	CHEMBL3644376	124562	0	None	-44	2	Human	5.1	pIC50	=	5.1	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	370	1	0	6	2.3	Cc1cn(C2=NCC(=O)N3CCc4c(cccc4-c4cnccn4)C3=C2)cn1	nan
	67425269	88629	0	None	-24	2	Human	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	429	5	1	6	5.2	C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C2CC2)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2334982	88629	0	None	-24	2	Human	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	429	5	1	6	5.2	C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C2CC2)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2364958	88629	0	None	-24	2	Human	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	429	5	1	6	5.2	C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C2CC2)n1	10.1016/j.bmcl.2013.01.009
	78320802	113842	3	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	330	3	0	4	4.8	C=Cc1cccc(-n2cnc3c(-c4ccccc4)csc3c2=O)c1	10.1016/j.ejmech.2014.08.027
	CHEMBL3330812	113842	3	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	330	3	0	4	4.8	C=Cc1cccc(-n2cnc3c(-c4ccccc4)csc3c2=O)c1	10.1016/j.ejmech.2014.08.027
	78320802	113842	3	None	-	1	Human	7.1	pIC50	=	7.1	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	330	3	0	4	4.8	C=Cc1cccc(-n2cnc3c(-c4ccccc4)csc3c2=O)c1	nan
	CHEMBL3330812	113842	3	None	-	1	Human	7.1	pIC50	=	7.1	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	330	3	0	4	4.8	C=Cc1cccc(-n2cnc3c(-c4ccccc4)csc3c2=O)c1	nan
	5766229	194243	6	None	-	1	Rat	6.1	pIC50	=	6.1	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	313	3	0	3	5.2	Cc1ccc2nc(Cl)c(/C=C/C(=O)c3cccs3)cc2c1	10.1016/j.bmc.2009.05.072
	CHEMBL559310	194243	6	None	-	1	Rat	6.1	pIC50	=	6.1	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	313	3	0	3	5.2	Cc1ccc2nc(Cl)c(/C=C/C(=O)c3cccs3)cc2c1	10.1016/j.bmc.2009.05.072
	44445036	154455	0	None	-	1	Rat	5.1	pIC50	=	5.1	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	283	2	1	4	3.6	N#Cc1cc2c(nc1NC1CCCCCC1)CCCC2=O	10.1021/jm0611298
	CHEMBL401330	154455	0	None	-	1	Rat	5.1	pIC50	=	5.1	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	283	2	1	4	3.6	N#Cc1cc2c(nc1NC1CCCCCC1)CCCC2=O	10.1021/jm0611298
	78322063	113849	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	364	4	0	6	4.1	COc1ccc(-n2cnc3c(-c4ccccc4OC)csc3c2=O)cc1	10.1016/j.ejmech.2014.08.027
	CHEMBL3330826	113849	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assayAntagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay	ChEMBL	364	4	0	6	4.1	COc1ccc(-n2cnc3c(-c4ccccc4OC)csc3c2=O)cc1	10.1016/j.ejmech.2014.08.027
	16117300	70682	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	355	3	1	6	3.8	CNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951874	70682	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	355	3	1	6	3.8	CNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)ccc3c12	10.1016/j.bmcl.2011.12.131
	127034014	138479	0	None	-	1	Rat	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	335	2	1	5	4.1	Cc1nc(N[C@@H]2C[C@@H]3C[C@H]([C@H]2C)C3(C)C)c2nn3ccccc3c2n1	10.1016/j.bmcl.2016.03.026
	CHEMBL3785636	138479	0	None	-	1	Rat	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	335	2	1	5	4.1	Cc1nc(N[C@@H]2C[C@@H]3C[C@H]([C@H]2C)C3(C)C)c2nn3ccccc3c2n1	10.1016/j.bmcl.2016.03.026
	122196116	123731	0	None	5	2	Human	6.1	pIC50	=	6.1	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	362	3	1	6	2.7	Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(C)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634438	123731	0	None	5	2	Human	6.1	pIC50	=	6.1	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	362	3	1	6	2.7	Cc1ccoc1C(=O)Nc1cnc(N2C(=O)c3cccc(C)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	127034014	138479	0	None	-	1	Rat	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	335	2	1	5	4.1	Cc1nc(N[C@@H]2C[C@@H]3C[C@H]([C@H]2C)C3(C)C)c2nn3ccccc3c2n1	10.1016/j.bmcl.2016.03.026
	CHEMBL3785636	138479	0	None	-	1	Rat	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	335	2	1	5	4.1	Cc1nc(N[C@@H]2C[C@@H]3C[C@H]([C@H]2C)C3(C)C)c2nn3ccccc3c2n1	10.1016/j.bmcl.2016.03.026
	11696595	84640	0	None	1	3	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	380	2	0	6	4.0	CN(C)c1ccnc2sc3c(=O)n(C45CC6CC(CC(C6)C4)C5)cnc3c12	10.1021/jm0504407
	CHEMBL224322	84640	0	None	1	3	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	380	2	0	6	4.0	CN(C)c1ccnc2sc3c(=O)n(C45CC6CC(CC(C6)C4)C5)cnc3c12	10.1021/jm0504407
	44442423	93221	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	322	2	0	5	3.8	Cc1nc2c(cnn2-c2ccccc2)c(=O)n1C1CCCCCC1	10.1016/j.bmcl.2007.05.028
	CHEMBL246840	93221	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	322	2	0	5	3.8	Cc1nc2c(cnn2-c2ccccc2)c(=O)n1C1CCCCCC1	10.1016/j.bmcl.2007.05.028
	24777319	154136	0	None	-	1	Rat	5.1	pIC50	=	5.1	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	390	3	0	6	3.4	COc1ccc(N2CCN(c3nc4c(cc3C#N)C(=O)CC(C)(C)C4)CC2)cc1	10.1021/jm0611298
	CHEMBL399640	154136	0	None	-	1	Rat	5.1	pIC50	=	5.1	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	390	3	0	6	3.4	COc1ccc(N2CCN(c3nc4c(cc3C#N)C(=O)CC(C)(C)C4)CC2)cc1	10.1021/jm0611298
	89979742	132582	0	None	-44	2	Human	6.1	pIC50	=	6.1	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	402	2	0	7	3.0	O=C1CN=C(n2cnc(C3CC3)n2)C=C2c3cccc(-c4nccs4)c3CCN12	nan
	CHEMBL3702443	132582	0	None	-44	2	Human	6.1	pIC50	=	6.1	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	402	2	0	7	3.0	O=C1CN=C(n2cnc(C3CC3)n2)C=C2c3cccc(-c4nccs4)c3CCN12	nan
	72163838	91591	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	354	1	0	3	3.2	O=C(N1CCC2(CCCC2)CC1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418360	91591	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	354	1	0	3	3.2	O=C(N1CCC2(CCCC2)CC1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	45486778	197191	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	385	5	0	6	3.9	CC(C)N(C)c1cc(-c2csc(N(C)C(=O)c3ccc(F)cc3)n2)ncn1	10.1016/j.bmcl.2009.07.097
	CHEMBL584066	197191	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	385	5	0	6	3.9	CC(C)N(C)c1cc(-c2csc(N(C)C(=O)c3ccc(F)cc3)n2)ncn1	10.1016/j.bmcl.2009.07.097
	72163838	91591	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	354	1	0	3	3.2	O=C(N1CCC2(CCCC2)CC1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418360	91591	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	354	1	0	3	3.2	O=C(N1CCC2(CCCC2)CC1)N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1	10.1016/j.bmcl.2013.07.029
	1284324	93491	9	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	380	2	0	5	3.6	Cc1nc2c(cnn2-c2ccccc2)c(=O)n1-c1ccc(Br)cc1	10.1016/j.bmcl.2007.05.028
	CHEMBL248208	93491	9	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	380	2	0	5	3.6	Cc1nc2c(cnn2-c2ccccc2)c(=O)n1-c1ccc(Br)cc1	10.1016/j.bmcl.2007.05.028
	24777314	154226	0	None	630	2	Rat	7.1	pIC50	=	7.1	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	283	2	1	4	3.5	CC1(C)CC(=O)c2cc(C#N)c(NC3CCCC3)nc2C1	10.1021/jm0611298
	CHEMBL400105	154226	0	None	630	2	Rat	7.1	pIC50	=	7.1	Functional	Antagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphateAntagonist activity at rat mGluR1 expressed in cerebellar granule cells assessed as accumulation of [3H]inositol phosphate	ChEMBL	283	2	1	4	3.5	CC1(C)CC(=O)c2cc(C#N)c(NC3CCCC3)nc2C1	10.1021/jm0611298
	1378	2384	48	None	-1047	14	Human	5.1	pIC50	=	5.1	Functional	Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluated	ChEMBL	353	5	3	4	2.8	OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N	10.1016/s0960-894x(98)00510-1
	1399	2384	48	None	-1047	14	Human	5.1	pIC50	=	5.1	Functional	Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluated	ChEMBL	353	5	3	4	2.8	OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N	10.1016/s0960-894x(98)00510-1
	9819927	2384	48	None	-1047	14	Human	5.1	pIC50	=	5.1	Functional	Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluated	ChEMBL	353	5	3	4	2.8	OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N	10.1016/s0960-894x(98)00510-1
	CHEMBL432038	2384	48	None	-1047	14	Human	5.1	pIC50	=	5.1	Functional	Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluatedAntagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluated	ChEMBL	353	5	3	4	2.8	OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N	10.1016/s0960-894x(98)00510-1
	16118946	70642	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	348	3	0	5	4.5	COc1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951676	70642	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	348	3	0	5	4.5	COc1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	24777812	94473	0	None	-	1	Rat	5.1	pIC50	=	5.1	Functional	Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay	ChEMBL	292	2	1	3	4.2	CC1(C)CC(=O)c2cc(Cl)c(NC3CCCC3)nc2C1	10.1021/jm0611298
	CHEMBL254221	94473	0	None	-	1	Rat	5.1	pIC50	=	5.1	Functional	Antagonist activity at rat mGluR1 by FLIPR assayAntagonist activity at rat mGluR1 by FLIPR assay	ChEMBL	292	2	1	3	4.2	CC1(C)CC(=O)c2cc(Cl)c(NC3CCCC3)nc2C1	10.1021/jm0611298
	57559301	83414	0	None	1258	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	369	3	0	8	3.2	CSc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205927	83414	0	None	1258	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	369	3	0	8	3.2	CSc1ccc(-n2cnc3c(sc4ncnc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	73335237	132519	0	None	11	2	Human	8.1	pIC50	=	8.1	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	372	1	0	3	3.7	O=C1CN=C(c2cccs2)C=C2c3cccc(Br)c3CCN12	nan
	CHEMBL3702381	132519	0	None	11	2	Human	8.1	pIC50	=	8.1	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	372	1	0	3	3.7	O=C1CN=C(c2cccs2)C=C2c3cccc(Br)c3CCN12	nan
	16117979	70632	0	None	-	1	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	327	2	0	5	4.2	CN(C)c1ccnc2sc3c(=O)n(C4CCCCC4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951665	70632	0	None	-	1	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	327	2	0	5	4.2	CN(C)c1ccnc2sc3c(=O)n(C4CCCCC4)ccc3c12	10.1016/j.bmcl.2011.12.131
	54582945	62438	0	None	-	1	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	351	3	1	7	2.6	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784072	62438	0	None	-	1	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	351	3	1	7	2.6	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	16118122	70631	0	None	63	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	349	3	0	5	4.2	CCc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951664	70631	0	None	63	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	349	3	0	5	4.2	CCc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	54584890	62431	0	None	-	1	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	405	4	1	8	4.6	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5sccc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784065	62431	0	None	-	1	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	405	4	1	8	4.6	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5sccc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	16661406	196640	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	295	3	0	4	3.5	CN(C(=O)c1ccccc1)c1nc(-c2ccncc2)cs1	10.1016/j.bmcl.2009.07.097
	CHEMBL576121	196640	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	295	3	0	4	3.5	CN(C(=O)c1ccccc1)c1nc(-c2ccncc2)cs1	10.1016/j.bmcl.2009.07.097
	86729807	149927	3	None	-	1	Human	7.1	pIC50	=	7.1	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	352	2	0	4	5.1	Cc1ccc(-c2csc3c(=O)n(-c4ccc(Cl)cc4)cnc23)cc1	nan
	CHEMBL3954190	149927	3	None	-	1	Human	7.1	pIC50	=	7.1	Functional	FLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and diluteFLIPR Calcium 5 Assay: Cells of Chem3 Cell Line (HTS145C:Millipore) in which mGluR1 was stably expressed were adjusted to a density of 2×106/ml. 50 μl of the cells were plated in each well of a 96-well plate, and stabilized at 5% CO2 and 37° C. for 1 hr. The cells were allowed to react with an HBSS buffer containing a Ca2+ fluorescent dye (FLIPR Calcium 5 assay kit: Molecular Devices) under the conditions of 5% CO2 and 37° C. for 30 min. As a result of the reaction, the cells were labeled with the fluorescent dye. Separately from the 96-well plate containing the fluorescently labeled cells, another 96-well plate was prepared that contained L-Glutamate (final concentration=30 μM) activating mGluR1 and a blocking drug to be screened. Most cell-based HTS systems have liquid application systems necessary for drug injection but no liquid inhalation systems. For this reason, 25 μl of each of the blocking drug and L-Glutamate was prepared at a 6-fold higher concentration in an HBSS buffer and dilute	ChEMBL	352	2	0	4	5.1	Cc1ccc(-c2csc3c(=O)n(-c4ccc(Cl)cc4)cnc23)cc1	nan
	44442422	93220	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	354	2	0	5	3.7	Cc1nc2c(cnn2-c2ccccc2)c(=O)n1-c1ccc(Cl)c(F)c1	10.1016/j.bmcl.2007.05.028
	CHEMBL246839	93220	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	354	2	0	5	3.7	Cc1nc2c(cnn2-c2ccccc2)c(=O)n1-c1ccc(Cl)c(F)c1	10.1016/j.bmcl.2007.05.028
	89980420	132510	0	None	5	2	Human	6.1	pIC50	=	6.1	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	312	1	0	3	3.1	O=C1CN=C(c2cccs2)C=C2c3cccc(F)c3CCN12	nan
	CHEMBL3702372	132510	0	None	5	2	Human	6.1	pIC50	=	6.1	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	312	1	0	3	3.1	O=C1CN=C(c2cccs2)C=C2c3cccc(F)c3CCN12	nan
	16661729	195433	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	341	5	0	4	4.4	CCCN(C(=O)c1ccc(F)cc1)c1nc(-c2ccccn2)cs1	10.1016/j.bmcl.2009.07.097
	CHEMBL567673	195433	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	341	5	0	4	4.4	CCCN(C(=O)c1ccc(F)cc1)c1nc(-c2ccccn2)cs1	10.1016/j.bmcl.2009.07.097
	89980559	124551	0	None	-407	2	Human	6.1	pIC50	=	6.1	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	381	3	0	6	2.1	COCc1ncn(C2=NCC(=O)N3CCc4c(ccc(F)c4C4CC4)C3=C2)n1	nan
	CHEMBL3644365	124551	0	None	-407	2	Human	6.1	pIC50	=	6.1	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	381	3	0	6	2.1	COCc1ncn(C2=NCC(=O)N3CCc4c(ccc(F)c4C4CC4)C3=C2)n1	nan
	57881906	83288	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	353	3	1	7	3.1	O=c1c2sc3ncnc(NC4CC4)c3c2ncn1-c1ccc(F)cc1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205372	83288	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	353	3	1	7	3.1	O=c1c2sc3ncnc(NC4CC4)c3c2ncn1-c1ccc(F)cc1	10.1016/j.bmcl.2012.09.048
	11493585	84629	0	None	11	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	326	2	0	6	3.4	CC1CCC(n2cnc3c(oc4nccc(N(C)C)c43)c2=O)CC1	10.1021/jm0504407
	CHEMBL224200	84629	0	None	11	2	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	326	2	0	6	3.4	CC1CCC(n2cnc3c(oc4nccc(N(C)C)c43)c2=O)CC1	10.1021/jm0504407
	89979749	132598	0	None	-66	2	Human	5.1	pIC50	=	5.1	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	384	2	1	5	2.8	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cc[nH]n4)c3CCN12	nan
	CHEMBL3702461	132598	0	None	-66	2	Human	5.1	pIC50	=	5.1	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	384	2	1	5	2.8	O=C1CN=C(n2cnc(C3CC3)c2)C=C2c3cccc(-c4cc[nH]n4)c3CCN12	nan
	16661405	196974	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	309	3	0	4	3.8	Cc1ccc(C(=O)N(C)c2nc(-c3ccncc3)cs2)cc1	10.1016/j.bmcl.2009.07.097
	CHEMBL579225	196974	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	309	3	0	4	3.8	Cc1ccc(C(=O)N(C)c2nc(-c3ccncc3)cs2)cc1	10.1016/j.bmcl.2009.07.097
	127034283	138533	0	None	20	2	Rat	7.1	pIC50	=	7.1	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	319	2	1	5	3.5	c1ccn2nc3c(NC4C5CC6CC(C5)CC4C6)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	CHEMBL3786284	138533	0	None	20	2	Rat	7.1	pIC50	=	7.1	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	319	2	1	5	3.5	c1ccn2nc3c(NC4C5CC6CC(C5)CC4C6)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	72163721	91604	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	376	2	0	4	3.1	N#Cc1ccncc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418385	91604	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	376	2	0	4	3.1	N#Cc1ccncc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1	10.1016/j.bmcl.2013.07.029
	72163721	91604	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	376	2	0	4	3.1	N#Cc1ccncc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1	10.1016/j.bmcl.2013.07.029
	CHEMBL2418385	91604	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	376	2	0	4	3.1	N#Cc1ccncc1N1C[C@H]2CN(C(=O)C34CC5CC(CC(C5)C3)C4)C[C@H]2C1	10.1016/j.bmcl.2013.07.029
	11530971	84736	0	None	1	3	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	378	4	0	6	4.2	CCc1ccc(-n2c(CC)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1021/jm0504407
	CHEMBL225201	84736	0	None	1	3	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	378	4	0	6	4.2	CCc1ccc(-n2c(CC)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1021/jm0504407
	127034283	138533	0	None	20	2	Rat	7.1	pIC50	=	7.1	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	319	2	1	5	3.5	c1ccn2nc3c(NC4C5CC6CC(C5)CC4C6)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	CHEMBL3786284	138533	0	None	20	2	Rat	7.1	pIC50	=	7.1	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	319	2	1	5	3.5	c1ccn2nc3c(NC4C5CC6CC(C5)CC4C6)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	54582005	62439	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	381	4	1	8	2.6	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4F)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784073	62439	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	381	4	1	8	2.6	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4F)cnc3c12	10.1016/j.bmcl.2009.04.104
	16118949	70639	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	322	2	0	5	3.9	COc1ccnc2sc3c(=O)n(-c4ccccc4C)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951673	70639	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	322	2	0	5	3.9	COc1ccnc2sc3c(=O)n(-c4ccccc4C)ccc3c12	10.1016/j.bmcl.2011.12.131
	72163432	91595	0	None	39	3	Human	7.1	pIC50	=	7.1	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	351	2	0	3	3.2	O=C(N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	CHEMBL2418364	91595	0	None	39	3	Human	7.1	pIC50	=	7.1	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	351	2	0	3	3.2	O=C(N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	72163432	91595	0	None	39	3	Human	7.1	pIC50	=	7.1	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	351	2	0	3	3.2	O=C(N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	CHEMBL2418364	91595	0	None	39	3	Human	7.1	pIC50	=	7.1	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	351	2	0	3	3.2	O=C(N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	5766225	194475	9	None	-	1	Rat	5.1	pIC50	=	5.1	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	307	3	0	2	5.1	Cc1cccc2cc(/C=C/C(=O)c3ccccc3)c(Cl)nc12	10.1016/j.bmc.2009.05.072
	CHEMBL561189	194475	9	None	-	1	Rat	5.1	pIC50	=	5.1	Functional	Allosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation countingAllosteric antagonist activity at mGluR1 in Sprague-Dawley rat cerebellar granule cells assessed as accumulation of [3H]inositol phosphate by liquid scintillation counting	ChEMBL	307	3	0	2	5.1	Cc1cccc2cc(/C=C/C(=O)c3ccccc3)c(Cl)nc12	10.1016/j.bmc.2009.05.072
	44421618	84771	0	None	1	2	Human	5.1	pIC50	=	5.1	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	378	2	0	6	4.4	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(C)(C)C)cc4)cnc3c12	10.1021/jm0504407
	CHEMBL225439	84771	0	None	1	2	Human	5.1	pIC50	=	5.1	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	378	2	0	6	4.4	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(C)(C)C)cc4)cnc3c12	10.1021/jm0504407
	57559370	83400	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	369	5	2	9	1.8	COc1ccc(-n2cnc3c(sc4ncnc(NCCO)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205912	83400	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	369	5	2	9	1.8	COc1ccc(-n2cnc3c(sc4ncnc(NCCO)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	49788729	17935	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology	ChEMBL	535	18	5	5	4.2	NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(-c2ccccc2)cc1	10.1021/jm100886h
	CHEMBL1269125	17935	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiologyAntagonist activity at GluR1 expressed in Xenopus laevis oocytes assessed as inhibition of glutamate-induced current at -60mV holding potential by two-electrode voltage-clamp electrophysiology	ChEMBL	535	18	5	5	4.2	NCCCNCCCCNCCCNC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccc(-c2ccccc2)cc1	10.1021/jm100886h
	11588590	141503	0	None	1	3	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	362	3	0	6	3.9	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)cnc3c12	10.1021/jm0504407
	CHEMBL387687	141503	0	None	1	3	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	362	3	0	6	3.9	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)cnc3c12	10.1021/jm0504407
	16117303	70683	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	355	3	1	6	3.8	CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4F)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951875	70683	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	355	3	1	6	3.8	CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4F)ccc3c12	10.1016/j.bmcl.2011.12.131
	16117433	70692	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	338	3	1	7	3.0	CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951884	70692	0	None	-	1	Human	7.1	pIC50	=	7.1	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	338	3	1	7	3.0	CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	45484905	196675	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	335	4	0	5	3.1	Cc1c(-c2ccc(C(=O)N(C)C(C)C)cc2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	CHEMBL576434	196675	0	None	-	1	Human	6.1	pIC50	=	6.1	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPRAntagonist activity at human mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR	ChEMBL	335	4	0	5	3.1	Cc1c(-c2ccc(C(=O)N(C)C(C)C)cc2)nnn1-c1cccnc1	10.1016/j.bmcl.2009.07.145
	1379	2387	36	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis	ChEMBL	209	3	3	3	0.8	OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N	10.1016/S0960-894X(97)10071-3
	5311261	2387	36	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis	ChEMBL	209	3	3	3	0.8	OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N	10.1016/S0960-894X(97)10071-3
	CHEMBL94631	2387	36	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysisCompound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis	ChEMBL	209	3	3	3	0.8	OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N	10.1016/S0960-894X(97)10071-3
	1379	2387	36	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.	ChEMBL	209	3	3	3	0.8	OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N	10.1021/jm990353c
	5311261	2387	36	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.	ChEMBL	209	3	3	3	0.8	OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N	10.1021/jm990353c
	CHEMBL94631	2387	36	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.	ChEMBL	209	3	3	3	0.8	OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N	10.1021/jm990353c
	127033445	138458	0	None	-	1	Rat	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	269	2	1	5	3.1	C[C@@H](Nc1ncnc2c1nn1ccccc21)C(C)(C)C	10.1016/j.bmcl.2016.03.026
	CHEMBL3785407	138458	0	None	-	1	Rat	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	269	2	1	5	3.1	C[C@@H](Nc1ncnc2c1nn1ccccc21)C(C)(C)C	10.1016/j.bmcl.2016.03.026
	122196099	123715	0	None	10	2	Human	7.1	pIC50	=	7.1	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	360	3	1	4	3.9	Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O	10.1016/j.bmcl.2015.10.013
	CHEMBL3634422	123715	0	None	10	2	Human	7.1	pIC50	=	7.1	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	360	3	1	4	3.9	Cc1cc(NC(=O)c2occc2C)ccc1N1C(=O)c2ccccc2C1=O	10.1016/j.bmcl.2015.10.013
	89980785	124578	0	None	-125	2	Human	6.1	pIC50	=	6.1	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	388	3	0	5	3.3	COCc1cn(C2=NCC(=O)N3CCc4c(C5=CCCC5)cccc4C3=C2)cn1	nan
	CHEMBL3644394	124578	0	None	-125	2	Human	6.1	pIC50	=	6.1	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	388	3	0	5	3.3	COCc1cn(C2=NCC(=O)N3CCc4c(C5=CCCC5)cccc4C3=C2)cn1	nan
	89979907	132545	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	335	2	1	5	2.0	COc1cccc2c1CCN1C(=O)CN=C(c3cccc(O)n3)C=C21	nan
	CHEMBL3702407	132545	0	None	-	1	Human	5.1	pIC50	=	5.1	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	335	2	1	5	2.0	COc1cccc2c1CCN1C(=O)CN=C(c3cccc(O)n3)C=C21	nan
	71559536	87092	0	None	-33	2	Human	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	457	5	1	6	6.0	C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C2CCCC2)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2334984	87092	0	None	-33	2	Human	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	457	5	1	6	6.0	C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(C2CCCC2)n1	10.1016/j.bmcl.2013.01.009
	127033445	138458	0	None	-	1	Rat	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	269	2	1	5	3.1	C[C@@H](Nc1ncnc2c1nn1ccccc21)C(C)(C)C	10.1016/j.bmcl.2016.03.026
	CHEMBL3785407	138458	0	None	-	1	Rat	6.1	pIC50	=	6.1	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	269	2	1	5	3.1	C[C@@H](Nc1ncnc2c1nn1ccccc21)C(C)(C)C	10.1016/j.bmcl.2016.03.026
	57404255	72865	1	None	-18	3	Human	8.1	pIC50	=	8.1	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	302	4	1	4	3.7	COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1	10.1016/j.bmcl.2012.02.003
	CHEMBL2011870	72865	1	None	-18	3	Human	8.1	pIC50	=	8.1	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	302	4	1	4	3.7	COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1	10.1016/j.bmcl.2012.02.003
	24884476	72871	0	None	138	2	Human	8.1	pIC50	=	8.1	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	306	3	1	3	4.4	Cc1c(-c2ccc(Cl)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C	10.1016/j.bmcl.2012.02.003
	CHEMBL2011876	72871	0	None	138	2	Human	8.1	pIC50	=	8.1	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	306	3	1	3	4.4	Cc1c(-c2ccc(Cl)cc2)nsc1NC(=O)[C@@H]1C[C@H]1C	10.1016/j.bmcl.2012.02.003
	57559572	83286	0	None	1122	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	349	3	1	7	3.3	Cc1ccc(-n2cnc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205370	83286	0	None	1122	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	349	3	1	7	3.3	Cc1ccc(-n2cnc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	57881727	83402	0	None	-	1	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	397	7	2	9	2.6	COc1ccc(-n2cnc3c(sc4ncnc(NCCCCO)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205914	83402	0	None	-	1	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	397	7	2	9	2.6	COc1ccc(-n2cnc3c(sc4ncnc(NCCCCO)c43)c2=O)cc1	10.1016/j.bmcl.2012.09.048
	11717278	84614	0	None	1	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	350	3	0	6	3.6	CCc1cccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c1	10.1021/jm0504407
	CHEMBL224084	84614	0	None	1	2	Human	8.1	pIC50	=	8.1	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	350	3	0	6	3.6	CCc1cccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c1	10.1021/jm0504407
	57404255	72865	1	None	-18	3	Human	8.1	pIC50	=	8.1	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	302	4	1	4	3.7	COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1	10.1016/j.bmcl.2013.01.009
	CHEMBL2011870	72865	1	None	-18	3	Human	8.1	pIC50	=	8.1	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	302	4	1	4	3.7	COc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1	10.1016/j.bmcl.2013.01.009
	1208332	166502	12	None	1047	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	352	3	0	7	3.1	COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2009.04.104
	1208332	166502	12	None	1047	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	352	3	0	7	3.1	COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2010.03.004
	CHEMBL428909	166502	12	None	1047	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	352	3	0	7	3.1	COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2009.04.104
	CHEMBL428909	166502	12	None	1047	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	352	3	0	7	3.1	COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2010.03.004
	1208332	166502	12	None	1047	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	352	3	0	7	3.1	COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1021/jm070590c
	CHEMBL428909	166502	12	None	1047	2	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	352	3	0	7	3.1	COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1021/jm070590c
	54582942	62422	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	379	5	1	8	3.4	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784056	62422	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	379	5	1	8	3.4	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	19705292	188614	0	None	2	3	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	326	2	0	5	3.3	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccc3)nn2)CC1	10.1016/j.bmc.2008.09.060
	CHEMBL511355	188614	0	None	2	3	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assayAntagonist activity at human mGluR1 expressed in CHO cells assessed as calcium flux by FLIPR assay	ChEMBL	326	2	0	5	3.3	CC(C)(C)OC(=O)N1CC=C(c2cn(-c3ccccc3)nn2)CC1	10.1016/j.bmc.2008.09.060
	16659964	89529	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	367	1	0	7	3.5	Cn1cnc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c21	10.1021/jm070590c
	CHEMBL238090	89529	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assayAntagonist activity at human mGluR1a expressed in CHO cells assessed by measuring intracellular calcium by FLIPR assay	ChEMBL	367	1	0	7	3.5	Cn1cnc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c21	10.1021/jm070590c
	16118400	70686	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	347	3	1	5	4.5	Cc1ccc(-n2ccc3c(sc4nccc(NC5CC5)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951878	70686	0	None	-	1	Human	8.0	pIC50	=	8.0	Functional	Antagonist activity at human metabotropic glutamate receptor 1Antagonist activity at human metabotropic glutamate receptor 1	ChEMBL	347	3	1	5	4.5	Cc1ccc(-n2ccc3c(sc4nccc(NC5CC5)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	44442424	93455	0	None	30	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	309	2	0	6	2.0	Cc1nc2c(cnn2-c2ccccc2)c(=O)n1N1CCCCC1	10.1016/j.bmcl.2007.05.028
	CHEMBL248052	93455	0	None	30	2	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	309	2	0	6	2.0	Cc1nc2c(cnn2-c2ccccc2)c(=O)n1N1CCCCC1	10.1016/j.bmcl.2007.05.028
	67181122	72868	0	None	-4	2	Human	7.0	pIC50	=	7.0	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	316	5	1	4	4.1	CCOc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1	10.1016/j.bmcl.2012.02.003
	CHEMBL2011873	72868	0	None	-4	2	Human	7.0	pIC50	=	7.0	Functional	Allosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assayAllosteric antagonist activity at human recombinant mGluR1 expressed in AV12 cells assessed as intracellular calcium concentration using Fluo-3 dye by FLIPR assay	ChEMBL	316	5	1	4	4.1	CCOc1ccc(-c2nsc(NC(=O)[C@@H]3C[C@H]3C)c2C)cc1	10.1016/j.bmcl.2012.02.003
	44431046	86297	0	None	-	1	Rat	7.0	pIC50	=	7.0	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	363	2	3	2	3.0	O=C(NC1C2CC3CC(C2)CC1C3)c1ccc2[nH]c3c(c2c1)CCNC3=O	10.1016/j.bmcl.2007.01.055
	CHEMBL231843	86297	0	None	-	1	Rat	7.0	pIC50	=	7.0	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of intracellular calcium ion mobilization by FLIPR assay	ChEMBL	363	2	3	2	3.0	O=C(NC1C2CC3CC(C2)CC1C3)c1ccc2[nH]c3c(c2c1)CCNC3=O	10.1016/j.bmcl.2007.01.055
	73335239	132523	0	None	-2	2	Human	7.0	pIC50	=	7.0	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	404	1	0	3	3.1	O=C1CN=C(c2ccoc2)C=C2c3cccc(I)c3CCN12	nan
	CHEMBL3702385	132523	0	None	-2	2	Human	7.0	pIC50	=	7.0	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	404	1	0	3	3.1	O=C1CN=C(c2ccoc2)C=C2c3cccc(I)c3CCN12	nan
	72163583	91599	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	369	2	0	3	3.3	O=C(N1C[C@@H]2CN(c3cccc(F)n3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	CHEMBL2418380	91599	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	369	2	0	3	3.3	O=C(N1C[C@@H]2CN(c3cccc(F)n3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	127030962	138516	0	None	24	2	Rat	7.0	pIC50	=	7.0	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	281	2	1	5	3.3	C[C@H]1CC[C@H](Nc2ncnc3c2nn2ccccc32)CC1	10.1016/j.bmcl.2016.03.026
	CHEMBL3786063	138516	0	None	24	2	Rat	7.0	pIC50	=	7.0	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	281	2	1	5	3.3	C[C@H]1CC[C@H](Nc2ncnc3c2nn2ccccc32)CC1	10.1016/j.bmcl.2016.03.026
	72163583	91599	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	369	2	0	3	3.3	O=C(N1C[C@@H]2CN(c3cccc(F)n3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	CHEMBL2418380	91599	0	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	369	2	0	3	3.3	O=C(N1C[C@@H]2CN(c3cccc(F)n3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	127030962	138516	0	None	24	2	Rat	7.0	pIC50	=	7.0	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	281	2	1	5	3.3	C[C@H]1CC[C@H](Nc2ncnc3c2nn2ccccc32)CC1	10.1016/j.bmcl.2016.03.026
	CHEMBL3786063	138516	0	None	24	2	Rat	7.0	pIC50	=	7.0	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	281	2	1	5	3.3	C[C@H]1CC[C@H](Nc2ncnc3c2nn2ccccc32)CC1	10.1016/j.bmcl.2016.03.026
	127033451	138637	0	None	35	2	Rat	7.0	pIC50	=	7.0	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	2	1	5	3.8	c1ccn2nc3c(NC4CCCCCCC4)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	CHEMBL3787343	138637	0	None	35	2	Rat	7.0	pIC50	=	7.0	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	2	1	5	3.8	c1ccn2nc3c(NC4CCCCCCC4)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	10809781	78112	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Inhibition of Quisqualate-Induced PI Hydrolysis Measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis Measured in CHO Metabotropic glutamate receptor 1 Expressing Cells	ChEMBL	380	5	2	6	1.9	COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@]12C[C@@H]1/C(=N\O)c1ccccc1O2	10.1021/jm0009944
	CHEMBL2111943	78112	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Inhibition of Quisqualate-Induced PI Hydrolysis Measured in CHO Metabotropic glutamate receptor 1 Expressing CellsInhibition of Quisqualate-Induced PI Hydrolysis Measured in CHO Metabotropic glutamate receptor 1 Expressing Cells	ChEMBL	380	5	2	6	1.9	COC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@]12C[C@@H]1/C(=N\O)c1ccccc1O2	10.1021/jm0009944
	73336019	124571	0	None	-177	2	Human	5.0	pIC50	=	5.0	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	376	2	0	5	3.0	CCc1cn(C2=NCC(=O)N3CCc4c(cccc4C4CCCO4)C3=C2)cn1	nan
	CHEMBL3644387	124571	0	None	-177	2	Human	5.0	pIC50	=	5.0	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	376	2	0	5	3.0	CCc1cn(C2=NCC(=O)N3CCc4c(cccc4C4CCCO4)C3=C2)cn1	nan
	11777615	98405	0	None	-2	2	Rat	4.0	pIC50	=	4.0	Functional	Antagonistic activity against Metabotropic glutamate receptor 1 was determinedAntagonistic activity against Metabotropic glutamate receptor 1 was determined	ChEMBL	265	2	3	4	1.2	CC1(C)CC(N)(C(=O)O)c2ccc(C(=O)O)cc2O1	10.1016/S0960-894X(97)00177-7
	CHEMBL278949	98405	0	None	-2	2	Rat	4.0	pIC50	=	4.0	Functional	Antagonistic activity against Metabotropic glutamate receptor 1 was determinedAntagonistic activity against Metabotropic glutamate receptor 1 was determined	ChEMBL	265	2	3	4	1.2	CC1(C)CC(N)(C(=O)O)c2ccc(C(=O)O)cc2O1	10.1016/S0960-894X(97)00177-7
	127033451	138637	0	None	35	2	Rat	7.0	pIC50	=	7.0	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	2	1	5	3.8	c1ccn2nc3c(NC4CCCCCCC4)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	CHEMBL3787343	138637	0	None	35	2	Rat	7.0	pIC50	=	7.0	Functional	Negative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assayNegative allosteric modulation of rat mGluR1 expressed in HEK293 cells assessed as inhibition of glutamate induced calcium mobilization by calcium mobilization assay	ChEMBL	295	2	1	5	3.8	c1ccn2nc3c(NC4CCCCCCC4)ncnc3c2c1	10.1016/j.bmcl.2016.03.026
	73335033	132502	0	None	-2	2	Human	6.0	pIC50	=	6.0	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	347	3	0	4	2.9	CCc1cc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)ccn1	nan
	CHEMBL3702364	132502	0	None	-2	2	Human	6.0	pIC50	=	6.0	Functional	Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).Fluorometric Imaging Plate Reader (FLIPR) Assay: Activity of compounds of the present invention was examined by determination to what extent the glutamate-induced elevation of the intracellular calcium concentration in L(tk-) cells expressing human mGluR5a receptors (see L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886, 1995) is inhibited by utilizing methods as described e.g. by L. P. Daggett et al., Neuropharm. Vol. 34, pages 871-886 (1995) and P. J. Flor et al., J. Neurochem. Vol. 67, pages 58-63 (1996). Activity of compounds of the present invention with respect to mGluR1 antagonism was examined by an assay based on measurements of L-glutamate induced intracellular calcium increases using a 96 well plate-based Fluorometric Imaging Plate Reader (FLIPR).	ChEMBL	347	3	0	4	2.9	CCc1cc(C2=NCC(=O)N3CCc4c(OC)cccc4C3=C2)ccn1	nan
	11703031	143033	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	349	3	0	5	4.2	CCc1ccc(-n2cnc3c(sc4cccc(N(C)C)c43)c2=O)cc1	10.1021/jm0504407
	CHEMBL389918	143033	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	349	3	0	5	4.2	CCc1ccc(-n2cnc3c(sc4cccc(N(C)C)c43)c2=O)cc1	10.1021/jm0504407
	122196112	123727	0	None	52	2	Human	7.0	pIC50	=	7.0	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	361	3	1	5	3.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	CHEMBL3634434	123727	0	None	52	2	Human	7.0	pIC50	=	7.0	Functional	Positive allosteric modulation of human mGluR1 by calcium mobilization assayPositive allosteric modulation of human mGluR1 by calcium mobilization assay	ChEMBL	361	3	1	5	3.3	Cc1ccoc1C(=O)Nc1ccc(N2C(=O)c3cccc(C)c3C2=O)nc1	10.1016/j.bmcl.2015.10.013
	67425323	87091	0	None	-478	2	Human	5.0	pIC50	=	5.0	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	432	5	1	7	4.4	C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(N(C)C)n1	10.1016/j.bmcl.2013.01.009
	CHEMBL2334979	87091	0	None	-478	2	Human	5.0	pIC50	=	5.0	Functional	Negative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assayNegative allosteric modulation of human recombinant mGlu1 receptor expressed in Syrian hamster AV12 cells assessed as receptor-mediated changes in intracellular calcium concentration by FLIPR assay	ChEMBL	432	5	1	7	4.4	C[C@@H]1C[C@H]1C(=O)Nc1snc(-c2ccc3nn(C)cc3c2)c1-c1cccc(N(C)C)n1	10.1016/j.bmcl.2013.01.009
	54580945	62426	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	350	4	1	8	2.8	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccncc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784060	62426	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human mGluR1Antagonist activity at human mGluR1	ChEMBL	350	4	1	8	2.8	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccncc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	11056756	5402	0	None	-7	2	Rat	6.0	pIC50	=	6.0	Functional	Antagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assayAntagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assay	ChEMBL	333	2	1	3	4.8	Clc1ccc2ncnc(Nc3cccc(Br)c3)c2c1	10.1016/j.bmcl.2009.10.024
	CHEMBL1075626	5402	0	None	-7	2	Rat	6.0	pIC50	=	6.0	Functional	Antagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assayAntagonist activity at rat mGluR1 expressed in BHK cells by calcium mobilization assay	ChEMBL	333	2	1	3	4.8	Clc1ccc2ncnc(Nc3cccc(Br)c3)c2c1	10.1016/j.bmcl.2009.10.024
	3346	2391	10	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	281	4	1	5	3.4	COc1ccc(cc1)Nc1ncnc2c1cc(OC)cc2	10.1021/jm060950g
	9926999	2391	10	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	281	4	1	5	3.4	COc1ccc(cc1)Nc1ncnc2c1cc(OC)cc2	10.1021/jm060950g
	CHEMBL254575	2391	10	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at mGlu1 receptorAntagonist activity at mGlu1 receptor	ChEMBL	281	4	1	5	3.4	COc1ccc(cc1)Nc1ncnc2c1cc(OC)cc2	10.1021/jm060950g
	71680760	90607	9	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	364	2	0	4	3.2	C[C@@H]1CN(c2cccnc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397347	90607	9	None	-	1	Human	7.0	pIC50	=	7.0	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	364	2	0	4	3.2	C[C@@H]1CN(c2cccnc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	71682341	90610	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccn1	10.1016/j.bmcl.2013.05.020
	CHEMBL2397350	90610	0	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccn1	10.1016/j.bmcl.2013.05.020
	11681575	136653	0	None	1	3	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	336	3	1	6	3.6	CCc1ccc(-n2cnc3c(sc4nccc(NC)c43)c2=O)cc1	10.1021/jm0504407
	CHEMBL374815	136653	0	None	1	3	Human	7.0	pIC50	=	7.0	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	336	3	1	6	3.6	CCc1ccc(-n2cnc3c(sc4nccc(NC)c43)c2=O)cc1	10.1021/jm0504407
	2660431	196138	7	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	299	3	1	4	3.6	O=C(Nc1nc(-c2ccccn2)cs1)c1ccc(F)cc1	10.1016/j.bmcl.2009.07.097
	CHEMBL572145	196138	7	None	-	1	Human	6.0	pIC50	=	6.0	Functional	Antagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in CHO cells by FLIPR assay	ChEMBL	299	3	1	4	3.6	O=C(Nc1nc(-c2ccccn2)cs1)c1ccc(F)cc1	10.1016/j.bmcl.2009.07.097
	44442435	93304	0	None	-	1	Human	5.0	pIC50	=	5.0	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	338	2	0	7	2.3	Cc1nc2c(cnn2-c2cncnc2)c(=O)n1-c1ccc(Cl)cc1	10.1016/j.bmcl.2007.05.028
	CHEMBL247216	93304	0	None	-	1	Human	5.0	pIC50	=	5.0	Functional	Antagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assayAntagonist activity at human mGluR1 receptor expressed in 132N1 cells assessed as inhibition of glutamate-induced calcium flux by FLIPR assay	ChEMBL	338	2	0	7	2.3	Cc1nc2c(cnn2-c2cncnc2)c(=O)n1-c1ccc(Cl)cc1	10.1016/j.bmcl.2007.05.028
	71682341	90610	0	None	-	1	Human	6.0	pIC50	=	6	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccn1	10.1016/j.bmcl.2013.05.020
	CHEMBL2397350	90610	0	None	-	1	Human	6.0	pIC50	=	6	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	339	2	0	3	3.3	C[C@H]1CN(C(=O)C23CC4CC(CC(C4)C2)C3)CCN1c1ccccn1	10.1016/j.bmcl.2013.05.020
	11582178	137400	0	None	1	2	Human	7.0	pIC50	=	7	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	404	4	1	6	4.5	CCc1ccc(-n2cnc3c(sc4nccc(NCC(F)(F)F)c43)c2=O)cc1	10.1021/jm0504407
	CHEMBL376372	137400	0	None	1	2	Human	7.0	pIC50	=	7	Functional	Antagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilizationAntagonist activity at human mGluR1 expressed in 1321N1 cells assessed as effect on L-glutamate-induced calcium mobilization	ChEMBL	404	4	1	6	4.5	CCc1ccc(-n2cnc3c(sc4nccc(NCC(F)(F)F)c43)c2=O)cc1	10.1021/jm0504407
	71680760	90607	9	None	-	1	Human	7.0	pIC50	=	7	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	364	2	0	4	3.2	C[C@@H]1CN(c2cccnc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	CHEMBL2397347	90607	9	None	-	1	Human	7.0	pIC50	=	7	Functional	Negative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 minsNegative allosteric modulation of human mGlu1 receptor expressed in HEK293A TREx cells assessed as calcium flux after 45 mins	ChEMBL	364	2	0	4	3.2	C[C@@H]1CN(c2cccnc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	71680760	90607	9	None	-	1	Human	7.0	pIC50	=	7	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	364	2	0	4	3.2	C[C@@H]1CN(c2cccnc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	CHEMBL2397347	90607	9	None	-	1	Human	7.0	pIC50	=	7	Functional	Negative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilizationNegative allosteric modulation of human mGluR1 expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization	ChEMBL	364	2	0	4	3.2	C[C@@H]1CN(c2cccnc2C#N)CCN1C(=O)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.05.020
	54585405	62335	0	None	-	1	Rat	9.7	pKi	=	9.7	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	362	4	1	6	4.3	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783868	62335	0	None	-	1	Rat	9.7	pKi	=	9.7	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	362	4	1	6	4.3	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54585406	62336	0	None	-	1	Rat	9.4	pKi	=	9.4	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	378	5	1	7	4.0	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783869	62336	0	None	-	1	Rat	9.4	pKi	=	9.4	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	378	5	1	7	4.0	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	16118123	70629	0	None	-	2	Rat	9.4	pKi	=	9.4	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	399	2	0	5	4.4	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951662	70629	0	None	-	2	Rat	9.4	pKi	=	9.4	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	399	2	0	5	4.4	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	23634171	962	1	None	-	1	Rat	9.2	pKi	=	9.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	366	3	1	6	3.7	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl	10.1016/j.bmcl.2009.04.104
	6214	962	1	None	-	1	Rat	9.2	pKi	=	9.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	366	3	1	6	3.7	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl	10.1016/j.bmcl.2009.04.104
	CHEMBL1783874	962	1	None	-	1	Rat	9.2	pKi	=	9.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	366	3	1	6	3.7	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl	10.1016/j.bmcl.2009.04.104
	54580485	62328	0	None	-	1	Rat	9.2	pKi	=	9.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	412	4	1	6	4.4	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783861	62328	0	None	-	1	Rat	9.2	pKi	=	9.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	412	4	1	6	4.4	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	23634249	62415	0	None	-	1	Rat	9.2	pKi	=	9.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	410	3	1	6	3.8	C#CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784049	62415	0	None	-	1	Rat	9.2	pKi	=	9.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	410	3	1	6	3.8	C#CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	23634326	62325	0	None	-	1	Rat	9.0	pKi	=	9.0	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	364	5	1	7	3.6	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783858	62325	0	None	-	1	Rat	9.0	pKi	=	9.0	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	364	5	1	7	3.6	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54586361	62327	0	None	-	1	Rat	9.0	pKi	=	9.0	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	368	4	1	6	4.2	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783860	62327	0	None	-	1	Rat	9.0	pKi	=	9.0	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	368	4	1	6	4.2	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54585404	62334	0	None	-	1	Rat	8.9	pKi	=	8.9	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	382	4	1	6	4.6	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783867	62334	0	None	-	1	Rat	8.9	pKi	=	8.9	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	382	4	1	6	4.6	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54583474	62337	0	None	-	1	Rat	8.8	pKi	=	8.8	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	426	4	1	6	4.7	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783870	62337	0	None	-	1	Rat	8.8	pKi	=	8.8	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	426	4	1	6	4.7	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	23634169	62341	0	None	-	1	Rat	8.8	pKi	=	8.8	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	346	3	1	6	3.3	C#CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783875	62341	0	None	-	1	Rat	8.8	pKi	=	8.8	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	346	3	1	6	3.3	C#CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	16118120	70626	0	None	-	2	Rat	8.7	pKi	=	8.7	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	335	2	0	5	4.0	Cc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951659	70626	0	None	-	2	Rat	8.7	pKi	=	8.7	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	335	2	0	5	4.0	Cc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	16118680	70628	0	None	-	1	Rat	8.7	pKi	=	8.7	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	355	2	0	5	4.3	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951661	70628	0	None	-	1	Rat	8.7	pKi	=	8.7	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	355	2	0	5	4.3	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	44592072	178478	0	None	-	0	Rat	8.0	pKi	=	8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	356	6	2	7	2.5	c1nc(NC2CCCCC2)c2cc(NCCN3CCOCC3)ncc2n1	10.1016/j.bmcl.2009.02.106
	CHEMBL471435	178478	0	None	-	0	Rat	8.0	pKi	=	8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	356	6	2	7	2.5	c1nc(NC2CCCCC2)c2cc(NCCN3CCOCC3)ncc2n1	10.1016/j.bmcl.2009.02.106
	54580945	62426	0	None	-	1	Rat	6.0	pKi	=	6	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	350	4	1	8	2.8	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccncc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784060	62426	0	None	-	1	Rat	6.0	pKi	=	6	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	350	4	1	8	2.8	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccncc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	1310	2286	108	None	-741	17	Human	5.0	pKi	=	5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm000007r
	1369	2286	108	None	-741	17	Human	5.0	pKi	=	5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm000007r
	33032	2286	108	None	-741	17	Human	5.0	pKi	=	5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm000007r
	44272391	2286	108	None	-741	17	Human	5.0	pKi	=	5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm000007r
	88747398	2286	108	None	-741	17	Human	5.0	pKi	=	5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm000007r
	CHEMBL575060	2286	108	None	-741	17	Human	5.0	pKi	=	5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm000007r
	DB00142	2286	108	None	-741	17	Human	5.0	pKi	=	5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm000007r
	3246152	160745	27	None	-	0	Human	5.0	pKi	=	5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	161	4	3	3	-0.5	C[C@@H](C[C@H](N)C(=O)O)C(=O)O	10.1021/jm000007r
	CHEMBL41221	160745	27	None	-	0	Human	5.0	pKi	=	5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	161	4	3	3	-0.5	C[C@@H](C[C@H](N)C(=O)O)C(=O)O	10.1021/jm000007r
	44592033	178510	0	None	-	0	Rat	7.0	pKi	=	7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	302	6	1	6	2.8	COCCOc1cc2c(NC3CCCCC3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	CHEMBL471666	178510	0	None	-	0	Rat	7.0	pKi	=	7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	302	6	1	6	2.8	COCCOc1cc2c(NC3CCCCC3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	44592030	178262	0	None	-	0	Rat	7.0	pKi	=	7.0	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	348	6	2	6	2.6	CN(C)CCNc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	CHEMBL469381	178262	0	None	-	0	Rat	7.0	pKi	=	7.0	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	348	6	2	6	2.6	CN(C)CCNc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	54582946	62442	0	None	-	1	Rat	7.0	pKi	=	7.0	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	390	3	1	9	3.0	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5ncsc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784076	62442	0	None	-	1	Rat	7.0	pKi	=	7.0	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	390	3	1	9	3.0	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5ncsc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	57403925	70649	0	None	-	1	Rat	7.0	pKi	=	7.0	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	381	6	1	7	3.7	COCCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951685	70649	0	None	-	1	Rat	7.0	pKi	=	7.0	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	381	6	1	7	3.7	COCCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	44438573	93274	0	None	-	0	Rat	6.0	pKi	=	6.0	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	404	3	0	6	2.5	CN1CCN(c2nccn3cc(C(=O)N4CCCC(c5ccccc5)C4)nc23)CC1	10.1016/j.bmcl.2006.10.015
	CHEMBL247092	93274	0	None	-	0	Rat	6.0	pKi	=	6.0	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	404	3	0	6	2.5	CN1CCN(c2nccn3cc(C(=O)N4CCCC(c5ccccc5)C4)nc23)CC1	10.1016/j.bmcl.2006.10.015
	44438588	93063	2	None	-	0	Rat	8.0	pKi	=	8.0	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	338	5	1	4	3.2	CC(C)(CNC(=O)c1cncc(N2CCCCC2)n1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	CHEMBL246245	93063	2	None	-	0	Rat	8.0	pKi	=	8.0	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	338	5	1	4	3.2	CC(C)(CNC(=O)c1cncc(N2CCCCC2)n1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	44592031	178263	0	None	-	0	Rat	8.0	pKi	=	8.0	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	301	6	2	6	2.8	COCCNc1cc2c(NC3CCCCC3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	CHEMBL469383	178263	0	None	-	0	Rat	8.0	pKi	=	8.0	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	301	6	2	6	2.8	COCCNc1cc2c(NC3CCCCC3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	16117979	70632	0	None	-	1	Rat	8.0	pKi	=	8.0	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	327	2	0	5	4.2	CN(C)c1ccnc2sc3c(=O)n(C4CCCCC4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951665	70632	0	None	-	1	Rat	8.0	pKi	=	8.0	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	327	2	0	5	4.2	CN(C)c1ccnc2sc3c(=O)n(C4CCCCC4)ccc3c12	10.1016/j.bmcl.2011.12.131
	16118121	70635	0	None	-	2	Rat	8.0	pKi	=	8.0	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	378	2	0	7	4.3	CN(C)c1ccnc2sc3c(=O)n(-c4ccc5scnc5c4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951668	70635	0	None	-	2	Rat	8.0	pKi	=	8.0	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	378	2	0	7	4.3	CN(C)c1ccnc2sc3c(=O)n(-c4ccc5scnc5c4)ccc3c12	10.1016/j.bmcl.2011.12.131
	1370	3212	62	None	-11	6	Human	6.0	pKi	=	6.0	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm000007r
	1372	3212	62	None	-11	6	Human	6.0	pKi	=	6.0	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm000007r
	40539	3212	62	None	-11	6	Human	6.0	pKi	=	6.0	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm000007r
	6971145	3212	62	None	-11	6	Human	6.0	pKi	=	6.0	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm000007r
	CHEMBL279956	3212	62	None	-11	6	Human	6.0	pKi	=	6.0	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm000007r
	DB02999	3212	62	None	-11	6	Human	6.0	pKi	=	6.0	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm000007r
	44591866	188888	0	None	-	0	Rat	6.9	pKi	=	6.9	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	292	3	1	5	2.6	COc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	CHEMBL513761	188888	0	None	-	0	Rat	6.9	pKi	=	6.9	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	292	3	1	5	2.6	COc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	16118946	70642	0	None	-	1	Rat	6.9	pKi	=	6.9	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	348	3	0	5	4.5	COc1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951676	70642	0	None	-	1	Rat	6.9	pKi	=	6.9	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	348	3	0	5	4.5	COc1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	16118124	70636	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	378	2	0	7	4.3	CN(C)c1ccnc2sc3c(=O)n(-c4ccc5ncsc5c4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951669	70636	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	378	2	0	7	4.3	CN(C)c1ccnc2sc3c(=O)n(-c4ccc5ncsc5c4)ccc3c12	10.1016/j.bmcl.2011.12.131
	16118400	70686	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	347	3	1	5	4.5	Cc1ccc(-n2ccc3c(sc4nccc(NC5CC5)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951878	70686	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	347	3	1	5	4.5	Cc1ccc(-n2ccc3c(sc4nccc(NC5CC5)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	44438576	93418	0	None	-	0	Rat	5.9	pKi	=	5.9	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	378	5	1	6	2.0	CC(CNC(=O)c1cn2ccnc(N3CCN(C)CC3)c2n1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	CHEMBL247862	93418	0	None	-	0	Rat	5.9	pKi	=	5.9	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	378	5	1	6	2.0	CC(CNC(=O)c1cn2ccnc(N3CCN(C)CC3)c2n1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	44438586	152582	4	None	-	0	Rat	5.9	pKi	=	5.9	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	291	5	1	3	3.7	CC(C)(CNCc1cnc2ccccc2n1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	CHEMBL397639	152582	4	None	-	0	Rat	5.9	pKi	=	5.9	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	291	5	1	3	3.7	CC(C)(CNCc1cnc2ccccc2n1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	44438577	169715	3	None	-	0	Rat	6.9	pKi	=	6.9	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	317	2	0	3	3.7	O=C(c1cnc2ccccc2n1)N1CCCC(c2ccccc2)C1	10.1016/j.bmcl.2006.10.015
	CHEMBL444629	169715	3	None	-	0	Rat	6.9	pKi	=	6.9	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	317	2	0	3	3.7	O=C(c1cnc2ccccc2n1)N1CCCC(c2ccccc2)C1	10.1016/j.bmcl.2006.10.015
	44591992	188809	0	None	-	0	Rat	6.9	pKi	=	6.9	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	321	5	3	6	2.0	OCCNc1ncnc2cnc(NC3Cc4ccccc4C3)cc12	10.1016/j.bmcl.2009.02.106
	CHEMBL513032	188809	0	None	-	0	Rat	6.9	pKi	=	6.9	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	321	5	3	6	2.0	OCCNc1ncnc2cnc(NC3Cc4ccccc4C3)cc12	10.1016/j.bmcl.2009.02.106
	54582494	62338	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	396	5	1	7	4.1	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783871	62338	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	396	5	1	7	4.1	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54587386	62339	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	406	4	1	8	3.8	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783872	62339	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	406	4	1	8	3.8	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	16118682	70633	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	369	3	0	6	3.8	COc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1F	10.1016/j.bmcl.2011.12.131
	CHEMBL1951666	70633	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	369	3	0	6	3.8	COc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1F	10.1016/j.bmcl.2011.12.131
	16118540	70655	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	341	2	1	5	4.3	CNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951690	70655	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	341	2	1	5	4.3	CNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	16118816	70694	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	364	4	1	7	3.6	COc1ccc(-n2ccc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951886	70694	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	364	4	1	7	3.6	COc1ccc(-n2ccc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	16725048	1131	0	None	-	2	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	371	3	0	8	2.6	COc1ccc(c(c1)F)n1cnc2c(c1=O)sc1c2c(ncn1)N(C)C	10.1016/j.bmcl.2012.09.048
	6362	1131	0	None	-	2	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	371	3	0	8	2.6	COc1ccc(c(c1)F)n1cnc2c(c1=O)sc1c2c(ncn1)N(C)C	10.1016/j.bmcl.2012.09.048
	CHEMBL2205377	1131	0	None	-	2	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	371	3	0	8	2.6	COc1ccc(c(c1)F)n1cnc2c(c1=O)sc1c2c(ncn1)N(C)C	10.1016/j.bmcl.2012.09.048
	57403924	70648	0	None	-	1	Rat	6.9	pKi	=	6.9	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	367	5	2	7	3.0	COc1ccc(-n2ccc3c(sc4nccc(NCCO)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951684	70648	0	None	-	1	Rat	6.9	pKi	=	6.9	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	367	5	2	7	3.0	COc1ccc(-n2ccc3c(sc4nccc(NCCO)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	54584443	62329	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	382	5	1	7	3.7	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(F)c(OC)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783862	62329	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	382	5	1	7	3.7	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(F)c(OC)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54586363	62340	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	392	4	1	8	3.7	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc5c(c4)OCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783873	62340	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	392	4	1	8	3.7	C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc5c(c4)OCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	44438598	147214	0	None	-	0	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	337	7	1	5	2.5	CN(CCC#N)c1cnc(C(=O)NCC(C)(C)c2ccccc2)cn1	10.1016/j.bmcl.2006.10.015
	CHEMBL393237	147214	0	None	-	0	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	337	7	1	5	2.5	CN(CCC#N)c1cnc(C(=O)NCC(C)(C)c2ccccc2)cn1	10.1016/j.bmcl.2006.10.015
	44591865	178631	0	None	-	0	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	291	3	2	5	2.6	CNc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	CHEMBL472490	178631	0	None	-	0	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	291	3	2	5	2.6	CNc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	16118256	70643	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	314	2	0	5	4.1	COc1ccnc2sc3c(=O)n(C4CCCCC4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951677	70643	0	None	-	1	Rat	7.9	pKi	=	7.9	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	314	2	0	5	4.1	COc1ccnc2sc3c(=O)n(C4CCCCC4)ccc3c12	10.1016/j.bmcl.2011.12.131
	57559562	952	0	None	-	2	Rat	7.8	pKi	=	7.8	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	365	4	1	8	3.0	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ncn1)NC1CC1	10.1016/j.bmcl.2012.09.048
	6365	952	0	None	-	2	Rat	7.8	pKi	=	7.8	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	365	4	1	8	3.0	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ncn1)NC1CC1	10.1016/j.bmcl.2012.09.048
	CHEMBL2205915	952	0	None	-	2	Rat	7.8	pKi	=	7.8	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	365	4	1	8	3.0	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ncn1)NC1CC1	10.1016/j.bmcl.2012.09.048
	44592518	187497	0	None	-	0	Rat	5.9	pKi	=	5.9	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	293	4	1	5	3.3	C[C@H](Nc1ncnc2cnc(N(C)C)cc12)c1ccccc1	10.1016/j.bmcl.2009.02.106
	CHEMBL497919	187497	0	None	-	0	Rat	5.9	pKi	=	5.9	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	293	4	1	5	3.3	C[C@H](Nc1ncnc2cnc(N(C)C)cc12)c1ccccc1	10.1016/j.bmcl.2009.02.106
	44438580	93019	3	None	-	0	Rat	7.8	pKi	=	7.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	321	5	1	4	2.9	COC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	CHEMBL246024	93019	3	None	-	0	Rat	7.8	pKi	=	7.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	321	5	1	4	2.9	COC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	439282	141052	6	None	-	0	Human	6.8	pKi	=	6.8	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	159	4	3	3	-0.6	C=C(C[C@H](N)C(=O)O)C(=O)O	10.1021/jm000007r
	CHEMBL38499	141052	6	None	-	0	Human	6.8	pKi	=	6.8	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	159	4	3	3	-0.6	C=C(C[C@H](N)C(=O)O)C(=O)O	10.1021/jm000007r
	16118542	70652	0	None	-	1	Rat	7.8	pKi	=	7.8	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	321	2	1	5	4.0	CNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951688	70652	0	None	-	1	Rat	7.8	pKi	=	7.8	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	321	2	1	5	4.0	CNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	54583942	62414	0	None	-	1	Rat	6.8	pKi	=	6.8	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	391	3	1	9	2.2	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784048	62414	0	None	-	1	Rat	6.8	pKi	=	6.8	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	391	3	1	9	2.2	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	44591991	171425	0	None	-	0	Rat	6.8	pKi	=	6.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	291	3	2	5	2.6	CNc1ncnc2cnc(NC3Cc4ccccc4C3)cc12	10.1016/j.bmcl.2009.02.106
	CHEMBL447113	171425	0	None	-	0	Rat	6.8	pKi	=	6.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	291	3	2	5	2.6	CNc1ncnc2cnc(NC3Cc4ccccc4C3)cc12	10.1016/j.bmcl.2009.02.106
	44322921	205110	1	None	-	0	Human	5.8	pKi	=	5.8	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	185	2	3	3	-0.5	N[C@@]1(C(=O)O)CC2CC1[C@H]2C(=O)O	10.1021/jm000007r
	CHEMBL90501	205110	1	None	-	0	Human	5.8	pKi	=	5.8	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	185	2	3	3	-0.5	N[C@@]1(C(=O)O)CC2CC1[C@H]2C(=O)O	10.1021/jm000007r
	44591990	178344	1	None	-	0	Rat	5.8	pKi	=	5.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	260	2	1	2	3.8	c1ccc2c(c1)CC(Nc1nccc3ccccc13)C2	10.1016/j.bmcl.2009.02.106
	CHEMBL470205	178344	1	None	-	0	Rat	5.8	pKi	=	5.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	260	2	1	2	3.8	c1ccc2c(c1)CC(Nc1nccc3ccccc13)C2	10.1016/j.bmcl.2009.02.106
	44438589	168955	2	None	-	0	Rat	7.8	pKi	=	7.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	338	5	1	4	3.2	CC(C)(CNC(=O)c1cnc(N2CCCCC2)cn1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	CHEMBL443489	168955	2	None	-	0	Rat	7.8	pKi	=	7.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	338	5	1	4	3.2	CC(C)(CNC(=O)c1cnc(N2CCCCC2)cn1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	16118119	1127	0	None	-	2	Rat	7.8	pKi	=	7.8	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	351	3	0	6	3.7	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1016/j.bmcl.2011.12.131
	6356	1127	0	None	-	2	Rat	7.8	pKi	=	7.8	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	351	3	0	6	3.7	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1016/j.bmcl.2011.12.131
	CHEMBL1951658	1127	0	None	-	2	Rat	7.8	pKi	=	7.8	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	351	3	0	6	3.7	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1016/j.bmcl.2011.12.131
	44592032	178264	0	None	-	0	Rat	6.8	pKi	=	6.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	288	5	2	6	2.1	OCCOc1cc2c(NC3CCCCC3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	CHEMBL469386	178264	0	None	-	0	Rat	6.8	pKi	=	6.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	288	5	2	6	2.1	OCCOc1cc2c(NC3CCCCC3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	44438585	93344	3	None	-	0	Rat	6.8	pKi	=	6.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	331	5	1	3	3.9	CC(C)(CNC(=O)c1cnc(-c2ccccc2)cn1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	CHEMBL247476	93344	3	None	-	0	Rat	6.8	pKi	=	6.8	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	331	5	1	3	3.9	CC(C)(CNC(=O)c1cnc(-c2ccccc2)cn1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	54586817	62417	0	None	-	1	Rat	7.8	pKi	=	7.8	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	380	3	0	6	3.7	C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784051	62417	0	None	-	1	Rat	7.8	pKi	=	7.8	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	380	3	0	6	3.7	C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	16118122	70631	0	None	-	2	Rat	7.8	pKi	=	7.8	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	349	3	0	5	4.2	CCc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951664	70631	0	None	-	2	Rat	7.8	pKi	=	7.8	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	349	3	0	5	4.2	CCc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	16117046	70645	0	None	-	1	Rat	7.8	pKi	=	7.8	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	337	3	1	6	3.7	CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951680	70645	0	None	-	1	Rat	7.8	pKi	=	7.8	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	337	3	1	6	3.7	CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	44592520	187351	0	None	-	0	Rat	6.7	pKi	=	6.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	305	3	1	5	2.7	CN(C)c1cc2c(NC3Cc4ccccc4C3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	CHEMBL496897	187351	0	None	-	0	Rat	6.7	pKi	=	6.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	305	3	1	5	2.7	CN(C)c1cc2c(NC3Cc4ccccc4C3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	16118813	70634	0	None	-	1	Rat	7.7	pKi	=	7.7	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	369	3	0	6	3.8	COc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)c(F)c1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951667	70634	0	None	-	1	Rat	7.7	pKi	=	7.7	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	369	3	0	6	3.8	COc1ccc(-n2ccc3c(sc4nccc(N(C)C)c43)c2=O)c(F)c1	10.1016/j.bmcl.2011.12.131
	16118815	70691	0	None	-	1	Rat	7.7	pKi	=	7.7	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	352	3	0	7	3.1	COc1ccc(-n2ccc3c(sc4ncnc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951883	70691	0	None	-	1	Rat	7.7	pKi	=	7.7	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	352	3	0	7	3.1	COc1ccc(-n2ccc3c(sc4ncnc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	44592517	187496	0	None	-	0	Rat	6.7	pKi	=	6.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	271	3	1	5	2.8	CN(C)c1cc2c(NC3CCCCC3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	CHEMBL497918	187496	0	None	-	0	Rat	6.7	pKi	=	6.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	271	3	1	5	2.8	CN(C)c1cc2c(NC3CCCCC3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	44438579	93018	3	None	-	0	Rat	8.7	pKi	=	8.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	323	4	1	3	3.5	CC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccc(F)cc1	10.1016/j.bmcl.2006.10.015
	CHEMBL246023	93018	3	None	-	0	Rat	8.7	pKi	=	8.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	323	4	1	3	3.5	CC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccc(F)cc1	10.1016/j.bmcl.2006.10.015
	44438587	93062	0	None	-	0	Rat	8.7	pKi	=	8.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	309	4	1	3	3.1	CC(C)(CNC(=O)c1cnc2c(n1)CCCC2)c1ccccc1	10.1016/j.bmcl.2006.10.015
	CHEMBL246244	93062	0	None	-	0	Rat	8.7	pKi	=	8.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	309	4	1	3	3.1	CC(C)(CNC(=O)c1cnc2c(n1)CCCC2)c1ccccc1	10.1016/j.bmcl.2006.10.015
	54579958	62420	0	None	-	1	Rat	8.7	pKi	=	8.7	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	383	4	1	7	4.0	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784054	62420	0	None	-	1	Rat	8.7	pKi	=	8.7	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	383	4	1	7	4.0	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54584890	62431	0	None	-	1	Rat	8.6	pKi	=	8.6	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	405	4	1	8	4.6	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5sccc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784065	62431	0	None	-	1	Rat	8.6	pKi	=	8.6	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	405	4	1	8	4.6	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5sccc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54584442	62326	0	None	-	1	Rat	8.6	pKi	=	8.6	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	348	4	1	6	3.9	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783859	62326	0	None	-	1	Rat	8.6	pKi	=	8.6	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	348	4	1	6	3.9	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54582002	62421	0	None	-	1	Rat	8.5	pKi	=	8.5	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	363	4	1	7	3.7	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784055	62421	0	None	-	1	Rat	8.5	pKi	=	8.5	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	363	4	1	7	3.7	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	11451117	178535	0	None	-	0	Rat	7.7	pKi	=	7.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	355	6	1	6	2.8	O=C1CCCN1CCOc1cc2c(NC3CCCCC3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	CHEMBL471875	178535	0	None	-	0	Rat	7.7	pKi	=	7.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	355	6	1	6	2.8	O=C1CCCN1CCOc1cc2c(NC3CCCCC3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	44592071	178477	0	None	-	0	Rat	6.7	pKi	=	6.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	300	6	3	6	2.5	NCCCNc1cc2c(NC3CCCCC3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	CHEMBL471434	178477	0	None	-	0	Rat	6.7	pKi	=	6.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	300	6	3	6	2.5	NCCCNc1cc2c(NC3CCCCC3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	16118949	70639	0	None	-	1	Rat	6.7	pKi	=	6.7	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	322	2	0	5	3.9	COc1ccnc2sc3c(=O)n(-c4ccccc4C)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951673	70639	0	None	-	1	Rat	6.7	pKi	=	6.7	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	322	2	0	5	3.9	COc1ccnc2sc3c(=O)n(-c4ccccc4C)ccc3c12	10.1016/j.bmcl.2011.12.131
	44591995	178278	0	None	-	0	Rat	7.7	pKi	=	7.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	321	5	3	6	2.0	OCCNc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	CHEMBL469588	178278	0	None	-	0	Rat	7.7	pKi	=	7.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	321	5	3	6	2.0	OCCNc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	22136331	91574	1	None	-	0	Rat	7.7	pKi	=	7.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	291	4	1	3	3.2	CC(CNC(=O)c1cnc2ccccc2n1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	CHEMBL241699	91574	1	None	-	0	Rat	7.7	pKi	=	7.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	291	4	1	3	3.2	CC(CNC(=O)c1cnc2ccccc2n1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	16118817	70698	0	None	-	1	Rat	7.7	pKi	=	7.7	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	348	3	1	6	3.9	Cc1ccc(-n2ccc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951890	70698	0	None	-	1	Rat	7.7	pKi	=	7.7	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	348	3	1	6	3.9	Cc1ccc(-n2ccc3c(sc4ncnc(NC5CC5)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	44592070	188434	0	None	-	0	Rat	5.7	pKi	=	5.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	286	5	3	6	2.1	NCCNc1cc2c(NC3CCCCC3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	CHEMBL509066	188434	0	None	-	0	Rat	5.7	pKi	=	5.7	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	286	5	3	6	2.1	NCCNc1cc2c(NC3CCCCC3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	16117042	70647	0	None	-	1	Rat	7.6	pKi	=	7.6	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	365	5	1	6	4.4	CCCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951682	70647	0	None	-	1	Rat	7.6	pKi	=	7.6	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	365	5	1	6	4.4	CCCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	54582003	62425	0	None	-	1	Rat	7.6	pKi	=	7.6	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	349	4	1	7	3.4	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccccc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784059	62425	0	None	-	1	Rat	7.6	pKi	=	7.6	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	349	4	1	7	3.4	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccccc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54580948	62435	0	None	-	1	Rat	7.6	pKi	=	7.6	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	363	4	1	8	2.4	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784069	62435	0	None	-	1	Rat	7.6	pKi	=	7.6	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	363	4	1	8	2.4	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	3421	3488	35	None	1	4	Human	4.6	pKi	=	4.6	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1021/jm000007r
	5311040	3488	35	None	1	4	Human	4.6	pKi	=	4.6	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1021/jm000007r
	CHEMBL43412	3488	35	None	1	4	Human	4.6	pKi	=	4.6	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1021/jm000007r
	54584887	62418	0	None	-	1	Rat	7.6	pKi	=	7.6	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	376	4	0	7	3.1	C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784052	62418	0	None	-	1	Rat	7.6	pKi	=	7.6	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	376	4	0	7	3.1	C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	44438590	93126	0	None	-	0	Rat	7.6	pKi	=	7.6	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	390	8	3	5	3.3	CC(C)(CNC(=O)c1cncc(N[C@@H](CO)c2ccccc2)n1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	CHEMBL246449	93126	0	None	-	0	Rat	7.6	pKi	=	7.6	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	390	8	3	5	3.3	CC(C)(CNC(=O)c1cncc(N[C@@H](CO)c2ccccc2)n1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	44438599	93127	0	None	-	0	Rat	7.6	pKi	=	7.6	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	369	8	1	5	2.6	CC(CN(C)C)N(C)c1cnc(C(=O)NCC(C)(C)c2ccccc2)cn1	10.1016/j.bmcl.2006.10.015
	CHEMBL246455	93127	0	None	-	0	Rat	7.6	pKi	=	7.6	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	369	8	1	5	2.6	CC(CN(C)C)N(C)c1cnc(C(=O)NCC(C)(C)c2ccccc2)cn1	10.1016/j.bmcl.2006.10.015
	13231190	188805	14	None	-	0	Rat	7.6	pKi	=	7.6	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	227	2	1	3	3.4	c1ccc2c(NC3CCCCC3)ncnc2c1	10.1016/j.bmcl.2009.02.106
	CHEMBL513012	188805	14	None	-	0	Rat	7.6	pKi	=	7.6	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	227	2	1	3	3.4	c1ccc2c(NC3CCCCC3)ncnc2c1	10.1016/j.bmcl.2009.02.106
	16117168	70653	0	None	-	1	Rat	6.6	pKi	=	6.6	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	325	2	1	5	3.8	CNc1ccnc2sc3c(=O)n(-c4ccc(F)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951689	70653	0	None	-	1	Rat	6.6	pKi	=	6.6	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	325	2	1	5	3.8	CNc1ccnc2sc3c(=O)n(-c4ccc(F)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	54585850	62416	0	None	-	1	Rat	7.6	pKi	=	7.6	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	380	4	1	7	3.2	C#CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784050	62416	0	None	-	1	Rat	7.6	pKi	=	7.6	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	380	4	1	7	3.2	C#CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	16118818	70695	0	None	-	1	Rat	7.6	pKi	=	7.6	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	336	2	0	6	3.4	Cc1ccc(-n2ccc3c(sc4ncnc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951887	70695	0	None	-	1	Rat	7.6	pKi	=	7.6	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	336	2	0	6	3.4	Cc1ccc(-n2ccc3c(sc4ncnc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	54585851	62436	0	None	-	1	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	411	3	1	7	3.2	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784070	62436	0	None	-	1	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	411	3	1	7	3.2	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	16118681	70627	0	None	-	1	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	339	2	0	5	3.8	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951660	70627	0	None	-	1	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	339	2	0	5	3.8	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	44438578	92978	3	None	-	0	Rat	8.5	pKi	=	8.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	305	4	1	3	3.3	CC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	CHEMBL245819	92978	3	None	-	0	Rat	8.5	pKi	=	8.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	305	4	1	3	3.3	CC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	44438596	93065	2	None	-	0	Rat	8.5	pKi	=	8.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	302	3	1	4	2.8	C[C@H]1CC[C@H](NC(=O)c2cnc(N3CCCCC3)cn2)CC1	10.1016/j.bmcl.2006.10.015
	CHEMBL246250	93065	2	None	-	0	Rat	8.5	pKi	=	8.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	302	3	1	4	2.8	C[C@H]1CC[C@H](NC(=O)c2cnc(N3CCCCC3)cn2)CC1	10.1016/j.bmcl.2006.10.015
	11772954	1019	0	None	-1	2	Rat	8.5	pKi	=	8.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	365	8	3	7	2.0	OCCOCCNc1ncc2c(c1)c(ncn2)NC1Cc2c(C1)cccc2	10.1016/j.bmcl.2009.02.106
	6349	1019	0	None	-1	2	Rat	8.5	pKi	=	8.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	365	8	3	7	2.0	OCCOCCNc1ncc2c(c1)c(ncn2)NC1Cc2c(C1)cccc2	10.1016/j.bmcl.2009.02.106
	CHEMBL469382	1019	0	None	-1	2	Rat	8.5	pKi	=	8.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	365	8	3	7	2.0	OCCOCCNc1ncc2c(c1)c(ncn2)NC1Cc2c(C1)cccc2	10.1016/j.bmcl.2009.02.106
	54586362	62333	0	None	-	1	Rat	8.5	pKi	=	8.5	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	426	4	0	6	4.4	C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783866	62333	0	None	-	1	Rat	8.5	pKi	=	8.5	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	426	4	0	6	4.4	C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	16118686	70690	0	None	-	1	Rat	8.5	pKi	=	8.5	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	411	3	1	5	4.9	O=c1c2sc3nccc(NC4CC4)c3c2ccn1-c1ccc(Br)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951882	70690	0	None	-	1	Rat	8.5	pKi	=	8.5	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	411	3	1	5	4.9	O=c1c2sc3nccc(NC4CC4)c3c2ccn1-c1ccc(Br)cc1	10.1016/j.bmcl.2011.12.131
	23634102	963	1	None	-	1	Rat	8.5	pKi	=	8.5	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	362	4	1	7	3.0	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC	10.1016/j.bmcl.2009.04.104
	6215	963	1	None	-	1	Rat	8.5	pKi	=	8.5	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	362	4	1	7	3.0	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC	10.1016/j.bmcl.2009.04.104
	CHEMBL1783876	963	1	None	-	1	Rat	8.5	pKi	=	8.5	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	362	4	1	7	3.0	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC	10.1016/j.bmcl.2009.04.104
	54584888	62423	0	None	-	1	Rat	8.4	pKi	=	8.4	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	427	4	1	7	4.1	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784057	62423	0	None	-	1	Rat	8.4	pKi	=	8.4	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	427	4	1	7	4.1	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	44438591	152583	4	None	-	0	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	304	6	1	4	3.2	CCCCN(C)c1cncc(C(=O)NC2CCCCCC2)n1	10.1016/j.bmcl.2006.10.015
	CHEMBL397640	152583	4	None	-	0	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	304	6	1	4	3.2	CCCCN(C)c1cncc(C(=O)NC2CCCCCC2)n1	10.1016/j.bmcl.2006.10.015
	44591863	188679	0	None	-	0	Rat	6.5	pKi	=	6.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	319	3	0	5	2.7	CN(C)c1cc2c(N(C)C3Cc4ccccc4C3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	CHEMBL511838	188679	0	None	-	0	Rat	6.5	pKi	=	6.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	319	3	0	5	2.7	CN(C)c1cc2c(N(C)C3Cc4ccccc4C3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	1426	2575	59	None	-	4	Human	4.5	pKi	=	4.5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	193	0	0	1	2.8	Cc1cccc(n1)C#Cc1ccccc1	10.1021/jm000007r
	3025961	2575	59	None	-	4	Human	4.5	pKi	=	4.5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	193	0	0	1	2.8	Cc1cccc(n1)C#Cc1ccccc1	10.1021/jm000007r
	CHEMBL66654	2575	59	None	-	4	Human	4.5	pKi	=	4.5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	193	0	0	1	2.8	Cc1cccc(n1)C#Cc1ccccc1	10.1021/jm000007r
	1297	169685	33	None	1	2	Human	4.5	pKi	=	4.5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	211	3	4	4	0.2	NC(C(=O)O)c1ccc(C(=O)O)c(O)c1	10.1021/jm000007r
	CHEMBL444589	169685	33	None	1	2	Human	4.5	pKi	=	4.5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	211	3	4	4	0.2	NC(C(=O)O)c1ccc(C(=O)O)c(O)c1	10.1021/jm000007r
	57391670	70681	0	None	-	1	Rat	6.5	pKi	=	6.5	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	332	2	1	6	3.5	CNc1ccnc2sc3c(=O)n(-c4ccc(C#N)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951873	70681	0	None	-	1	Rat	6.5	pKi	=	6.5	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	332	2	1	6	3.5	CNc1ccnc2sc3c(=O)n(-c4ccc(C#N)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	44591994	188806	0	None	-	0	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	393	4	2	5	4.2	c1ccc2c(c1)CC(Nc1cc3c(NC4Cc5ccccc5C4)ncnc3cn1)C2	10.1016/j.bmcl.2009.02.106
	CHEMBL513018	188806	0	None	-	0	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	393	4	2	5	4.2	c1ccc2c(c1)CC(Nc1cc3c(NC4Cc5ccccc5C4)ncnc3cn1)C2	10.1016/j.bmcl.2009.02.106
	44438584	93343	3	None	-	0	Rat	6.5	pKi	=	6.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	331	5	1	3	3.9	CC(C)(CNC(=O)c1cncc(-c2ccccc2)n1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	CHEMBL247475	93343	3	None	-	0	Rat	6.5	pKi	=	6.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	331	5	1	3	3.9	CC(C)(CNC(=O)c1cncc(-c2ccccc2)n1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	54582005	62439	0	None	-	1	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	381	4	1	8	2.6	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4F)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784073	62439	0	None	-	1	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	381	4	1	8	2.6	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4F)cnc3c12	10.1016/j.bmcl.2009.04.104
	16118945	70640	0	None	-	1	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	352	3	0	6	3.9	COc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)c(C)c1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951674	70640	0	None	-	1	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	352	3	0	6	3.9	COc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)c(C)c1	10.1016/j.bmcl.2011.12.131
	16117303	70683	0	None	-	1	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	355	3	1	6	3.8	CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4F)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951875	70683	0	None	-	1	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	355	3	1	6	3.8	CNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4F)ccc3c12	10.1016/j.bmcl.2011.12.131
	16117432	70693	0	None	-	1	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	352	4	1	7	3.4	CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951885	70693	0	None	-	1	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	352	4	1	7	3.4	CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	44592069	188709	0	None	-	0	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	302	6	2	6	2.5	OCCCOc1cc2c(NC3CCCCC3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	CHEMBL512178	188709	0	None	-	0	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	302	6	2	6	2.5	OCCCOc1cc2c(NC3CCCCC3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	23186964	178451	1	None	-	0	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	261	2	1	3	3.2	c1ccc2c(c1)CC(Nc1ncnc3ccccc13)C2	10.1016/j.bmcl.2009.02.106
	CHEMBL471242	178451	1	None	-	0	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	261	2	1	3	3.2	c1ccc2c(c1)CC(Nc1ncnc3ccccc13)C2	10.1016/j.bmcl.2009.02.106
	44438600	93128	0	None	-	0	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	368	6	2	5	2.4	CC(C)(CNC(=O)c1cnc(N2CCC(CO)CC2)cn1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	CHEMBL246456	93128	0	None	-	0	Rat	7.5	pKi	=	7.5	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	368	6	2	5	2.4	CC(C)(CNC(=O)c1cnc(N2CCC(CO)CC2)cn1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	5311262	205397	9	None	-	0	Human	6.5	pKi	=	6.5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	383	5	3	4	3.6	N[C@](CC1c2ccccc2Sc2ccccc21)(C(=O)O)[C@H]1C[C@@H](C(=O)O)C1	10.1021/jm000007r
	CHEMBL92162	205397	9	None	-	0	Human	6.5	pKi	=	6.5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	383	5	3	4	3.6	N[C@](CC1c2ccccc2Sc2ccccc21)(C(=O)O)[C@H]1C[C@@H](C(=O)O)C1	10.1021/jm000007r
	1426	2575	59	None	-	4	Human	7.4	pKi	=	7.4	Functional	Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1	ChEMBL	193	0	0	1	2.8	Cc1cccc(n1)C#Cc1ccccc1	10.1016/j.bmcl.2010.06.075
	3025961	2575	59	None	-	4	Human	7.4	pKi	=	7.4	Functional	Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1	ChEMBL	193	0	0	1	2.8	Cc1cccc(n1)C#Cc1ccccc1	10.1016/j.bmcl.2010.06.075
	CHEMBL66654	2575	59	None	-	4	Human	7.4	pKi	=	7.4	Functional	Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1	ChEMBL	193	0	0	1	2.8	Cc1cccc(n1)C#Cc1ccccc1	10.1016/j.bmcl.2010.06.075
	54582943	62427	0	None	-	1	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	367	4	1	7	3.5	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784061	62427	0	None	-	1	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	367	4	1	7	3.5	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54582945	62438	0	None	-	1	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	351	3	1	7	2.6	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784072	62438	0	None	-	1	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	351	3	1	7	2.6	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54581505	62332	0	None	-	1	Rat	8.4	pKi	=	8.4	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	378	5	0	7	3.6	C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783865	62332	0	None	-	1	Rat	8.4	pKi	=	8.4	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	378	5	0	7	3.6	C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54584891	62433	0	None	-	1	Rat	8.4	pKi	=	8.4	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	367	3	1	7	3.1	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784067	62433	0	None	-	1	Rat	8.4	pKi	=	8.4	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	367	3	1	7	3.1	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	44438582	93020	2	None	-	0	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	306	4	1	4	2.7	CC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccccn1	10.1016/j.bmcl.2006.10.015
	CHEMBL246025	93020	2	None	-	0	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	306	4	1	4	2.7	CC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccccn1	10.1016/j.bmcl.2006.10.015
	44438592	93346	0	None	-	0	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	296	4	1	4	1.8	CCN(C)c1cncc(C(=O)NC2Cc3ccccc3C2)n1	10.1016/j.bmcl.2006.10.015
	CHEMBL247485	93346	0	None	-	0	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	296	4	1	4	1.8	CCN(C)c1cncc(C(=O)NC2Cc3ccccc3C2)n1	10.1016/j.bmcl.2006.10.015
	9948445	147768	0	None	-	0	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	305	4	1	3	3.4	CC(C)(Cc1ccccc1)NC(=O)c1cnc2ccccc2n1	10.1016/j.bmcl.2006.10.015
	CHEMBL393681	147768	0	None	-	0	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	305	4	1	3	3.4	CC(C)(Cc1ccccc1)NC(=O)c1cnc2ccccc2n1	10.1016/j.bmcl.2006.10.015
	16117300	70682	0	None	-	1	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	355	3	1	6	3.8	CNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951874	70682	0	None	-	1	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	355	3	1	6	3.8	CNc1ccnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)ccc3c12	10.1016/j.bmcl.2011.12.131
	44438572	93230	0	None	-	0	Rat	6.4	pKi	=	6.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	420	3	0	8	1.2	CN1CCN(c2nccn3cc(C(=O)N4CCCN(c5ccccn5)CC4)nc23)CC1	10.1016/j.bmcl.2006.10.015
	CHEMBL246890	93230	0	None	-	0	Rat	6.4	pKi	=	6.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	420	3	0	8	1.2	CN1CCN(c2nccn3cc(C(=O)N4CCCN(c5ccccn5)CC4)nc23)CC1	10.1016/j.bmcl.2006.10.015
	44592073	188750	0	None	-	0	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	357	6	1	7	2.5	c1nc(NC2CCCCC2)c2cc(OCCN3CCOCC3)ncc2n1	10.1016/j.bmcl.2009.02.106
	CHEMBL512523	188750	0	None	-	0	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	357	6	1	7	2.5	c1nc(NC2CCCCC2)c2cc(OCCN3CCOCC3)ncc2n1	10.1016/j.bmcl.2009.02.106
	16118943	70641	0	None	-	1	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	336	3	0	5	4.2	CCc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951675	70641	0	None	-	1	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	336	3	0	5	4.2	CCc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	104766	34	36	None	-4	14	Human	4.4	pKi	=	4.4	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm000007r
	1365	34	36	None	-4	14	Human	4.4	pKi	=	4.4	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm000007r
	CHEMBL34453	34	36	None	-4	14	Human	4.4	pKi	=	4.4	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm000007r
	54586818	62429	0	None	-	1	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	406	4	1	9	4.0	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5scnc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784063	62429	0	None	-	1	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	406	4	1	9	4.0	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5scnc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	44438593	93347	0	None	-	0	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	328	7	2	5	1.6	CN(CCO)c1cncc(C(=O)NCC(C)(C)c2ccccc2)n1	10.1016/j.bmcl.2006.10.015
	CHEMBL247487	93347	0	None	-	0	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	328	7	2	5	1.6	CN(CCO)c1cncc(C(=O)NCC(C)(C)c2ccccc2)n1	10.1016/j.bmcl.2006.10.015
	12310764	1939	59	None	-	2	Human	4.4	pKi	=	4.4	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	158	2	3	4	-0.9	OC(=O)C(c1o[nH]c(=O)c1)N	10.1021/jm000007r
	1233	1939	59	None	-	2	Human	4.4	pKi	=	4.4	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	158	2	3	4	-0.9	OC(=O)C(c1o[nH]c(=O)c1)N	10.1021/jm000007r
	1371	1939	59	None	-	2	Human	4.4	pKi	=	4.4	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	158	2	3	4	-0.9	OC(=O)C(c1o[nH]c(=O)c1)N	10.1021/jm000007r
	CHEMBL284895	1939	59	None	-	2	Human	4.4	pKi	=	4.4	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	158	2	3	4	-0.9	OC(=O)C(c1o[nH]c(=O)c1)N	10.1021/jm000007r
	44438594	146931	0	None	-	0	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	312	7	3	5	2.0	O=C(NCC1CC1)c1cncc(NCCc2cccc(O)c2)n1	10.1016/j.bmcl.2006.10.015
	CHEMBL393029	146931	0	None	-	0	Rat	7.4	pKi	=	7.4	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	312	7	3	5	2.0	O=C(NCC1CC1)c1cncc(NCCc2cccc(O)c2)n1	10.1016/j.bmcl.2006.10.015
	54582944	62430	0	None	-	1	Rat	7.3	pKi	=	7.3	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	406	4	1	9	4.0	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5ncsc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784064	62430	0	None	-	1	Rat	7.3	pKi	=	7.3	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	406	4	1	9	4.0	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5ncsc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	11404904	188602	0	None	-	0	Rat	8.3	pKi	=	8.3	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	335	6	2	6	2.7	COCCNc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	CHEMBL511266	188602	0	None	-	0	Rat	8.3	pKi	=	8.3	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	335	6	2	6	2.7	COCCNc1cc2c(NC3Cc4ccccc4C3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	16118537	964	0	None	-	1	Rat	8.3	pKi	=	8.3	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	363	4	1	6	4.2	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1	10.1016/j.bmcl.2011.12.131
	6357	964	0	None	-	1	Rat	8.3	pKi	=	8.3	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	363	4	1	6	4.2	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951683	964	0	None	-	1	Rat	8.3	pKi	=	8.3	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	363	4	1	6	4.2	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1	10.1016/j.bmcl.2011.12.131
	23634254	62331	0	None	-	1	Rat	8.3	pKi	=	8.3	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	382	4	0	6	4.3	C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783864	62331	0	None	-	1	Rat	8.3	pKi	=	8.3	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	382	4	0	6	4.3	C=CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	1368	2258	31	None	-	11	Human	4.3	pKi	=	4.3	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	159	3	3	3	-0.9	N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O	10.1021/jm000007r
	5310956	2258	31	None	-	11	Human	4.3	pKi	=	4.3	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	159	3	3	3	-0.9	N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O	10.1021/jm000007r
	CHEMBL280563	2258	31	None	-	11	Human	4.3	pKi	=	4.3	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	159	3	3	3	-0.9	N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O	10.1021/jm000007r
	44438581	147556	3	None	-	0	Rat	6.3	pKi	=	6.3	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	320	5	2	4	2.5	CNC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	CHEMBL393507	147556	3	None	-	0	Rat	6.3	pKi	=	6.3	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	320	5	2	4	2.5	CNC(C)(CNC(=O)c1cnc2ccccc2n1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	16118942	70697	0	None	-	1	Rat	7.3	pKi	=	7.3	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	336	3	1	6	3.7	CCNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951889	70697	0	None	-	1	Rat	7.3	pKi	=	7.3	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	336	3	1	6	3.7	CCNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	44591864	178630	0	None	-	0	Rat	7.3	pKi	=	7.3	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	305	3	1	5	2.7	CNc1cc2c(N(C)C3Cc4ccccc4C3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	CHEMBL472489	178630	0	None	-	0	Rat	7.3	pKi	=	7.3	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	305	3	1	5	2.7	CNc1cc2c(N(C)C3Cc4ccccc4C3)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	44438595	93064	0	None	-	0	Rat	7.3	pKi	=	7.3	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	365	6	1	5	2.3	O=C(NCC1CC1)c1cncc(N2CCCN(Cc3ccccc3)CC2)n1	10.1016/j.bmcl.2006.10.015
	CHEMBL246249	93064	0	None	-	0	Rat	7.3	pKi	=	7.3	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	365	6	1	5	2.3	O=C(NCC1CC1)c1cncc(N2CCCN(Cc3ccccc3)CC2)n1	10.1016/j.bmcl.2006.10.015
	16118812	70630	0	None	-	1	Rat	7.3	pKi	=	7.3	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	346	2	0	6	3.5	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C#N)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951663	70630	0	None	-	1	Rat	7.3	pKi	=	7.3	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	346	2	0	6	3.5	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C#N)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	57397023	70638	0	None	-	1	Rat	6.3	pKi	=	6.3	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	338	3	0	6	3.6	COc1cccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)c1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951671	70638	0	None	-	1	Rat	6.3	pKi	=	6.3	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	338	3	0	6	3.6	COc1cccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)c1	10.1016/j.bmcl.2011.12.131
	9844204	205387	2	None	-	0	Human	5.2	pKi	=	5.2	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	405	5	3	4	4.3	NC(CC1c2ccccc2Sc2ccccc21)(C(=O)O)c1ccc(C(=O)O)cc1	10.1021/jm000007r
	CHEMBL92118	205387	2	None	-	0	Human	5.2	pKi	=	5.2	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	405	5	3	4	4.3	NC(CC1c2ccccc2Sc2ccccc21)(C(=O)O)c1ccc(C(=O)O)cc1	10.1021/jm000007r
	11337722	1053	0	None	-	1	Rat	8.2	pKi	=	8.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	371	6	1	7	2.9	C1CCCC(CC1)Nc1ncnc2c1cc(OCCN1CCOCC1)nc2	10.1016/j.bmcl.2009.02.106
	6351	1053	0	None	-	1	Rat	8.2	pKi	=	8.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	371	6	1	7	2.9	C1CCCC(CC1)Nc1ncnc2c1cc(OCCN1CCOCC1)nc2	10.1016/j.bmcl.2009.02.106
	CHEMBL470396	1053	0	None	-	1	Rat	8.2	pKi	=	8.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	371	6	1	7	2.9	C1CCCC(CC1)Nc1ncnc2c1cc(OCCN1CCOCC1)nc2	10.1016/j.bmcl.2009.02.106
	15953801	70680	0	None	-	1	Rat	8.2	pKi	=	8.2	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	385	2	1	5	4.4	CNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951872	70680	0	None	-	1	Rat	8.2	pKi	=	8.2	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	385	2	1	5	4.4	CNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	16118126	70637	0	None	-	1	Rat	8.2	pKi	=	8.2	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	338	3	0	6	3.6	COc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951670	70637	0	None	-	1	Rat	8.2	pKi	=	8.2	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	338	3	0	6	3.6	COc1ccc(-n2ccc3c(sc4nccc(OC)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	135413554	1597	54	None	-	2	Human	8.2	pKi	=	8.2	Functional	Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1	ChEMBL	266	1	2	3	1.3	O=C(NC1=NC(=O)CN1C)Nc1cccc(c1)Cl	10.1016/j.bmcl.2010.06.075
	135497698	1597	54	None	-	2	Human	8.2	pKi	=	8.2	Functional	Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1	ChEMBL	266	1	2	3	1.3	O=C(NC1=NC(=O)CN1C)Nc1cccc(c1)Cl	10.1016/j.bmcl.2010.06.075
	135659063	1597	54	None	-	2	Human	8.2	pKi	=	8.2	Functional	Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1	ChEMBL	266	1	2	3	1.3	O=C(NC1=NC(=O)CN1C)Nc1cccc(c1)Cl	10.1016/j.bmcl.2010.06.075
	1433	1597	54	None	-	2	Human	8.2	pKi	=	8.2	Functional	Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1	ChEMBL	266	1	2	3	1.3	O=C(NC1=NC(=O)CN1C)Nc1cccc(c1)Cl	10.1016/j.bmcl.2010.06.075
	1434	1597	54	None	-	2	Human	8.2	pKi	=	8.2	Functional	Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1	ChEMBL	266	1	2	3	1.3	O=C(NC1=NC(=O)CN1C)Nc1cccc(c1)Cl	10.1016/j.bmcl.2010.06.075
	162834	1597	54	None	-	2	Human	8.2	pKi	=	8.2	Functional	Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1	ChEMBL	266	1	2	3	1.3	O=C(NC1=NC(=O)CN1C)Nc1cccc(c1)Cl	10.1016/j.bmcl.2010.06.075
	CHEMBL239800	1597	54	None	-	2	Human	8.2	pKi	=	8.2	Functional	Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1	ChEMBL	266	1	2	3	1.3	O=C(NC1=NC(=O)CN1C)Nc1cccc(c1)Cl	10.1016/j.bmcl.2010.06.075
	DB12931	1597	54	None	-	2	Human	8.2	pKi	=	8.2	Functional	Antagonist activity at human mGLUR1Antagonist activity at human mGLUR1	ChEMBL	266	1	2	3	1.3	O=C(NC1=NC(=O)CN1C)Nc1cccc(c1)Cl	10.1016/j.bmcl.2010.06.075
	9815955	105505	0	None	-	1	Human	5.2	pKi	=	5.2	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	225	3	4	4	0.5	Cc1c(C(N)C(=O)O)ccc(C(=O)O)c1O	10.1021/jm000007r
	CHEMBL313124	105505	0	None	-	1	Human	5.2	pKi	=	5.2	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	225	3	4	4	0.5	Cc1c(C(N)C(=O)O)ccc(C(=O)O)c1O	10.1021/jm000007r
	44591993	188525	0	None	-	0	Rat	5.2	pKi	=	5.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	249	6	4	7	-0.2	OCCNc1cc2c(NCCO)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	CHEMBL510310	188525	0	None	-	0	Rat	5.2	pKi	=	5.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	249	6	4	7	-0.2	OCCNc1cc2c(NCCO)ncnc2cn1	10.1016/j.bmcl.2009.02.106
	44591867	172073	2	None	-	0	Rat	5.2	pKi	=	5.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	226	2	1	2	4.0	c1ccc2c(NC3CCCCC3)ccnc2c1	10.1016/j.bmcl.2009.02.106
	CHEMBL449616	172073	2	None	-	0	Rat	5.2	pKi	=	5.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	226	2	1	2	4.0	c1ccc2c(NC3CCCCC3)ccnc2c1	10.1016/j.bmcl.2009.02.106
	54580946	62428	0	None	-	1	Rat	7.2	pKi	=	7.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	383	4	1	7	4.0	C=C(C)CNc1ncnc2sc3c(=O)n(-c4cccc(Cl)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784062	62428	0	None	-	1	Rat	7.2	pKi	=	7.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	383	4	1	7	4.0	C=C(C)CNc1ncnc2sc3c(=O)n(-c4cccc(Cl)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54583943	62443	0	None	-	1	Rat	7.2	pKi	=	7.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	373	3	1	8	3.2	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5occc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784077	62443	0	None	-	1	Rat	7.2	pKi	=	7.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	373	3	1	8	3.2	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5occc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	16118539	70651	0	None	-	1	Rat	7.2	pKi	=	7.2	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	381	5	1	7	3.0	COc1ccc(-n2ccc3c(sc4nccc(N(C)CCO)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951687	70651	0	None	-	1	Rat	7.2	pKi	=	7.2	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	381	5	1	7	3.0	COc1ccc(-n2ccc3c(sc4nccc(N(C)CCO)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	54580947	62432	0	None	-	1	Rat	7.2	pKi	=	7.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	407	4	1	9	3.2	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784066	62432	0	None	-	1	Rat	7.2	pKi	=	7.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	407	4	1	9	3.2	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	54584892	62441	0	None	-	1	Rat	7.2	pKi	=	7.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	390	3	1	9	3.0	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5scnc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784075	62441	0	None	-	1	Rat	7.2	pKi	=	7.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	390	3	1	9	3.0	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5scnc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	44438575	145505	0	None	-	0	Rat	6.2	pKi	=	6.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	434	3	0	8	1.5	Cc1cccc(N2CCCN(C(=O)c3cn4ccnc(N5CCN(C)CC5)c4n3)CC2)n1	10.1016/j.bmcl.2006.10.015
	CHEMBL391879	145505	0	None	-	0	Rat	6.2	pKi	=	6.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	434	3	0	8	1.5	Cc1cccc(N2CCCN(C(=O)c3cn4ccnc(N5CCN(C)CC5)c4n3)CC2)n1	10.1016/j.bmcl.2006.10.015
	36039661	93021	4	None	-	0	Rat	5.2	pKi	=	5.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	255	4	1	3	2.2	CC(C)(CNC(=O)c1cnccn1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	CHEMBL246026	93021	4	None	-	0	Rat	5.2	pKi	=	5.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	255	4	1	3	2.2	CC(C)(CNC(=O)c1cnccn1)c1ccccc1	10.1016/j.bmcl.2006.10.015
	443586	145919	47	None	-16	3	Human	5.2	pKi	=	5.2	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	183	2	4	4	0.2	N[C@H](C(=O)O)c1cc(O)cc(O)c1	10.1021/jm000007r
	71668376	145919	47	None	-16	3	Human	5.2	pKi	=	5.2	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	183	2	4	4	0.2	N[C@H](C(=O)O)c1cc(O)cc(O)c1	10.1021/jm000007r
	CHEMBL39221	145919	47	None	-16	3	Human	5.2	pKi	=	5.2	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	183	2	4	4	0.2	N[C@H](C(=O)O)c1cc(O)cc(O)c1	10.1021/jm000007r
	54584889	62424	0	None	-	1	Rat	7.2	pKi	=	7.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	397	5	1	8	3.5	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784058	62424	0	None	-	1	Rat	7.2	pKi	=	7.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	397	5	1	8	3.5	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	1378	2384	48	None	-1047	14	Human	5.2	pKi	=	5.2	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	353	5	3	4	2.8	OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N	10.1021/jm000007r
	1399	2384	48	None	-1047	14	Human	5.2	pKi	=	5.2	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	353	5	3	4	2.8	OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N	10.1021/jm000007r
	9819927	2384	48	None	-1047	14	Human	5.2	pKi	=	5.2	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	353	5	3	4	2.8	OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N	10.1021/jm000007r
	CHEMBL432038	2384	48	None	-1047	14	Human	5.2	pKi	=	5.2	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	353	5	3	4	2.8	OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N	10.1021/jm000007r
	54579959	62444	0	None	-	1	Rat	7.2	pKi	=	7.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	389	3	1	8	3.7	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5sccc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784078	62444	0	None	-	1	Rat	7.2	pKi	=	7.2	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	389	3	1	8	3.7	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5sccc5c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	5300647	92979	15	None	-	0	Rat	7.2	pKi	=	7.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	277	4	1	3	2.6	O=C(NCCc1ccccc1)c1cnc2ccccc2n1	10.1016/j.bmcl.2006.10.015
	CHEMBL245820	92979	15	None	-	0	Rat	7.2	pKi	=	7.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	277	4	1	3	2.6	O=C(NCCc1ccccc1)c1cnc2ccccc2n1	10.1016/j.bmcl.2006.10.015
	44591868	178533	0	None	-	0	Rat	6.2	pKi	=	6.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	228	2	0	3	3.3	c1ccc2c(OC3CCCCC3)ncnc2c1	10.1016/j.bmcl.2009.02.106
	CHEMBL471866	178533	0	None	-	0	Rat	6.2	pKi	=	6.2	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	228	2	0	3	3.3	c1ccc2c(OC3CCCCC3)ncnc2c1	10.1016/j.bmcl.2009.02.106
	16118397	70688	0	None	-	1	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	367	3	1	5	4.8	O=c1c2sc3nccc(NC4CC4)c3c2ccn1-c1ccc(Cl)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951880	70688	0	None	-	1	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	367	3	1	5	4.8	O=c1c2sc3nccc(NC4CC4)c3c2ccn1-c1ccc(Cl)cc1	10.1016/j.bmcl.2011.12.131
	16118685	70689	0	None	-	1	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	399	3	1	5	4.8	CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951881	70689	0	None	-	1	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	399	3	1	5	4.8	CCNc1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	54582942	62422	0	None	-	1	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	379	5	1	8	3.4	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784056	62422	0	None	-	1	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	379	5	1	8	3.4	C=C(C)CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	54585403	62330	0	None	-	1	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	352	4	1	6	3.7	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1783863	62330	0	None	-	1	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	352	4	1	6	3.7	C=CCNc1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	1208332	166502	12	None	-	2	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	352	3	0	7	3.1	COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2009.04.104
	CHEMBL428909	166502	12	None	-	2	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	352	3	0	7	3.1	COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.bmcl.2009.04.104
	16117172	70684	0	None	-	1	Rat	7.2	pKi	=	7.2	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	364	2	1	7	4.3	CNc1ccnc2sc3c(=O)n(-c4ccc5scnc5c4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951876	70684	0	None	-	1	Rat	7.2	pKi	=	7.2	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	364	2	1	7	4.3	CNc1ccnc2sc3c(=O)n(-c4ccc5scnc5c4)ccc3c12	10.1016/j.bmcl.2011.12.131
	54585852	62437	0	None	-	1	Rat	7.1	pKi	=	7.1	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	381	4	1	8	2.6	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784071	62437	0	None	-	1	Rat	7.1	pKi	=	7.1	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	381	4	1	8	2.6	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(OC)c(F)c4)cnc3c12	10.1016/j.bmcl.2009.04.104
	16117433	70692	0	None	-	1	Rat	7.1	pKi	=	7.1	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	338	3	1	7	3.0	CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951884	70692	0	None	-	1	Rat	7.1	pKi	=	7.1	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	338	3	1	7	3.0	CNc1ncnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	57402169	70644	0	None	-	0	Rat	6.1	pKi	=	6.1	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	260	2	0	5	2.6	CCn1ccc2c(sc3nccc(OC)c32)c1=O	10.1016/j.bmcl.2011.12.131
	CHEMBL1951678	70644	0	None	-	0	Rat	6.1	pKi	=	6.1	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	260	2	0	5	2.6	CCn1ccc2c(sc3nccc(OC)c32)c1=O	10.1016/j.bmcl.2011.12.131
	23634325	62419	0	None	-	1	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	424	3	0	6	3.8	C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784053	62419	0	None	-	1	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	424	3	0	6	3.8	C#CCN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	44438597	93066	3	None	-	0	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	302	3	1	4	2.9	O=C(NC1CCCCCC1)c1cnc(N2CCCCC2)cn1	10.1016/j.bmcl.2006.10.015
	CHEMBL246251	93066	3	None	-	0	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	302	3	1	4	2.9	O=C(NC1CCCCCC1)c1cnc(N2CCCCC2)cn1	10.1016/j.bmcl.2006.10.015
	54582004	62434	0	None	-	1	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	347	3	1	7	2.7	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784068	62434	0	None	-	1	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	347	3	1	7	2.7	C#CCNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12	10.1016/j.bmcl.2009.04.104
	16118536	70646	0	None	-	1	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	351	4	1	6	4.0	CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951681	70646	0	None	-	1	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	351	4	1	6	4.0	CCNc1ccnc2sc3c(=O)n(-c4ccc(OC)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	1418	3393	48	None	-1	2	Human	4.1	pKi	=	4.1	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	10.1021/jm000007r
	5311459	3393	48	None	-1	2	Human	4.1	pKi	=	4.1	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	10.1021/jm000007r
	CHEMBL94990	3393	48	None	-1	2	Human	4.1	pKi	=	4.1	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	10.1021/jm000007r
	44592519	192790	0	None	-	0	Rat	6.1	pKi	=	6.1	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	259	5	1	5	2.7	CCCC(C)Nc1ncnc2cnc(N(C)C)cc12	10.1016/j.bmcl.2009.02.106
	CHEMBL525546	192790	0	None	-	0	Rat	6.1	pKi	=	6.1	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challengeAntagonist activity at rat mGluR1a expressed in CHO cells assessed as inhibition of glutamate-evoked increase in calcium internalization preincubated 5 mins before glutamate challenge	ChEMBL	259	5	1	5	2.7	CCCC(C)Nc1ncnc2cnc(N(C)C)cc12	10.1016/j.bmcl.2009.02.106
	57400362	70650	0	None	-	1	Rat	7.1	pKi	=	7.1	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	381	5	2	7	3.4	COc1ccc(-n2ccc3c(sc4nccc(NC[C@@H](C)O)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	CHEMBL1951686	70650	0	None	-	1	Rat	7.1	pKi	=	7.1	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	381	5	2	7	3.4	COc1ccc(-n2ccc3c(sc4nccc(NC[C@@H](C)O)c43)c2=O)cc1	10.1016/j.bmcl.2011.12.131
	3931705	106569	21	None	-	0	Human	5.1	pKi	=	5.1	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	209	3	3	3	0.8	Cc1cc(C(=O)O)ccc1C(N)C(=O)O	10.1021/jm000007r
	CHEMBL315591	106569	21	None	-	0	Human	5.1	pKi	=	5.1	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	209	3	3	3	0.8	Cc1cc(C(=O)O)ccc1C(N)C(=O)O	10.1021/jm000007r
	16216350	93067	0	None	-	0	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	332	4	2	5	2.0	C[C@H]1CC[C@H](NC(=O)c2cnc(N3CCC(CO)CC3)cn2)CC1	10.1016/j.bmcl.2006.10.015
	CHEMBL246252	93067	0	None	-	0	Rat	8.1	pKi	=	8.1	Functional	Antagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assayAntagonist activity at rat mGluR1a expressed in CHO cells assessed as increase in calcium internalization by FLIPR assay	ChEMBL	332	4	2	5	2.0	C[C@H]1CC[C@H](NC(=O)c2cnc(N3CCC(CO)CC3)cn2)CC1	10.1016/j.bmcl.2006.10.015
	16118398	70687	0	None	-	1	Rat	8.0	pKi	=	8.0	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	355	3	1	5	4.7	CCNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951879	70687	0	None	-	1	Rat	8.0	pKi	=	8.0	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	355	3	1	5	4.7	CCNc1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	16118535	70685	0	None	-	1	Rat	8.0	pKi	=	8.0	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	335	3	1	5	4.3	CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951877	70685	0	None	-	1	Rat	8.0	pKi	=	8.0	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	335	3	1	5	4.3	CCNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	16117434	70696	0	None	-	1	Rat	7.0	pKi	=	7.0	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	322	2	1	6	3.3	CNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	CHEMBL1951888	70696	0	None	-	1	Rat	7.0	pKi	=	7.0	Functional	Antagonist activity at rat metabotropic glutamate receptor 1Antagonist activity at rat metabotropic glutamate receptor 1	ChEMBL	322	2	1	6	3.3	CNc1ncnc2sc3c(=O)n(-c4ccc(C)cc4)ccc3c12	10.1016/j.bmcl.2011.12.131
	1382	1167	29	None	-1	3	Human	5.0	pKi	=	5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	10.1021/jm000007r
	6278000	1167	29	None	-1	3	Human	5.0	pKi	=	5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	10.1021/jm000007r
	CHEMBL327783	1167	29	None	-1	3	Human	5.0	pKi	=	5	Functional	Agonist potency against cloned human metabotropic glutamate receptor 1Agonist potency against cloned human metabotropic glutamate receptor 1	ChEMBL	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	10.1021/jm000007r
	54582006	62440	0	None	-	1	Rat	6.0	pKi	=	6	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	377	3	1	9	2.2	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	CHEMBL1784074	62440	0	None	-	1	Rat	6.0	pKi	=	6	Functional	Antagonist activity at rat mGluR1Antagonist activity at rat mGluR1	ChEMBL	377	3	1	9	2.2	C#CCNc1ncnc2sc3c(=O)n(-c4ccc5c(c4)OCO5)cnc3c12	10.1016/j.bmcl.2009.04.104
	1376	318	50	None	-	1	Human	4.2	pA2	=	4.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	221	2	3	3	0.6	OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O	9152378
	2071	318	50	None	-	1	Human	4.2	pA2	=	4.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	221	2	3	3	0.6	OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O	9152378
	CHEMBL313938	318	50	None	-	1	Human	4.2	pA2	=	4.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	221	2	3	3	0.6	OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O	9152378
	1310	2286	108	None	-794	17	Rat	8.3	pEC50	=	8.3	Functional	NoneNone	Drug Central	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	1369	2286	108	None	-794	17	Rat	8.3	pEC50	=	8.3	Functional	NoneNone	Drug Central	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	33032	2286	108	None	-794	17	Rat	8.3	pEC50	=	8.3	Functional	NoneNone	Drug Central	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	44272391	2286	108	None	-794	17	Rat	8.3	pEC50	=	8.3	Functional	NoneNone	Drug Central	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	88747398	2286	108	None	-794	17	Rat	8.3	pEC50	=	8.3	Functional	NoneNone	Drug Central	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	CHEMBL575060	2286	108	None	-794	17	Rat	8.3	pEC50	=	8.3	Functional	NoneNone	Drug Central	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	DB00142	2286	108	None	-794	17	Rat	8.3	pEC50	=	8.3	Functional	NoneNone	Drug Central	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	1310	2286	108	None	-741	17	Human	4.9	pEC50	=	4.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10443583
	1369	2286	108	None	-741	17	Human	4.9	pEC50	=	4.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10443583
	33032	2286	108	None	-741	17	Human	4.9	pEC50	=	4.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10443583
	44272391	2286	108	None	-741	17	Human	4.9	pEC50	=	4.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10443583
	88747398	2286	108	None	-741	17	Human	4.9	pEC50	=	4.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10443583
	CHEMBL575060	2286	108	None	-741	17	Human	4.9	pEC50	=	4.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10443583
	DB00142	2286	108	None	-741	17	Human	4.9	pEC50	=	4.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10443583
	1382	1167	29	None	1	3	Rat	5.3	pEC50	=	5.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	11961143
	6278000	1167	29	None	1	3	Rat	5.3	pEC50	=	5.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	11961143
	CHEMBL327783	1167	29	None	1	3	Rat	5.3	pEC50	=	5.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	11961143
	11523834	3994	0	None	-	1	Rat	5.6	pEC50	=	5.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	384	5	1	5	4.7	O=C(c1ccc(cc1)N(=O)=O)Nc1c(cnn1c1ccccc1)c1ccccc1	16099654
	6207	3994	0	None	-	1	Rat	5.6	pEC50	=	5.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	384	5	1	5	4.7	O=C(c1ccc(cc1)N(=O)=O)Nc1c(cnn1c1ccccc1)c1ccccc1	16099654
	CHEMBL377636	3994	0	None	-	1	Rat	5.6	pEC50	=	5.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	384	5	1	5	4.7	O=C(c1ccc(cc1)N(=O)=O)Nc1c(cnn1c1ccccc1)c1ccccc1	16099654
	10009	3986	35	None	-1	3	Human	6.4	pEC50	=	6.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	445	3	1	4	5.1	Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl	25137254
	91885483	3986	35	None	-1	3	Human	6.4	pEC50	=	6.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	445	3	1	4	5.1	Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl	25137254
	CHEMBL3628116	3986	35	None	-1	3	Human	6.4	pEC50	=	6.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	445	3	1	4	5.1	Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl	25137254
	44573698	1064	0	None	-	1	Rat	7.2	pEC50	=	7.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	307	2	1	5	3.3	O=C(C1c2ccccc2Oc2c1cccc2)Nc1noc(n1)C	16099654
	6205	1064	0	None	-	1	Rat	7.2	pEC50	=	7.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	307	2	1	5	3.3	O=C(C1c2ccccc2Oc2c1cccc2)Nc1noc(n1)C	16099654
	CHEMBL492378	1064	0	None	-	1	Rat	7.2	pEC50	=	7.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	307	2	1	5	3.3	O=C(C1c2ccccc2Oc2c1cccc2)Nc1noc(n1)C	16099654
	6206	1087	0	None	-	1	Rat	7.2	pEC50	=	7.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	321	3	1	6	2.6	CCn1nnc(n1)NC(=O)C1c2ccccc2Oc2c1cccc2	16099654
	9923127	1087	0	None	-	1	Rat	7.2	pEC50	=	7.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	321	3	1	6	2.6	CCn1nnc(n1)NC(=O)C1c2ccccc2Oc2c1cccc2	16099654
	10338547	3288	21	None	1	2	Rat	7.3	pEC50	=	7.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	19233648
	6204	3288	21	None	1	2	Rat	7.3	pEC50	=	7.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	19233648
	CHEMBL521982	3288	21	None	1	2	Rat	7.3	pEC50	=	7.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	19233648
	3421	3488	35	None	-1	4	Rat	4.2	pIC50	=	4.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10428410
	5311040	3488	35	None	-1	4	Rat	4.2	pIC50	=	4.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10428410
	CHEMBL43412	3488	35	None	-1	4	Rat	4.2	pIC50	=	4.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10428410
	10058919	3634	10	None	1	2	Rat	4.2	pIC50	=	4.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	209	3	3	5	-1.0	OC(=O)[C@H](C12CC(C1)(C2)c1n[nH]nn1)N	11249114
	3419	3634	10	None	1	2	Rat	4.2	pIC50	=	4.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	209	3	3	5	-1.0	OC(=O)[C@H](C12CC(C1)(C2)c1n[nH]nn1)N	11249114
	CHEMBL2204334	3634	10	None	1	2	Rat	4.2	pIC50	=	4.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	209	3	3	5	-1.0	OC(=O)[C@H](C12CC(C1)(C2)c1n[nH]nn1)N	11249114
	1379	2387	36	None	-	1	Human	5.1	pIC50	=	5.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	209	3	3	3	0.8	OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N	None
	5311261	2387	36	None	-	1	Human	5.1	pIC50	=	5.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	209	3	3	3	0.8	OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N	None
	CHEMBL94631	2387	36	None	-	1	Human	5.1	pIC50	=	5.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	209	3	3	3	0.8	OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N	None
	10398360	105	0	None	-	1	Rat	5.2	pIC50	=	5.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	215	3	3	4	0.8	OC(=O)c1cc(c(s1)C(C(=O)O)N)C	12015200
	3396	105	0	None	-	1	Rat	5.2	pIC50	=	5.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	215	3	3	4	0.8	OC(=O)c1cc(c(s1)C(C(=O)O)N)C	12015200
	CHEMBL1322301	105	0	None	-	1	Rat	5.2	pIC50	=	5.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	215	3	3	4	0.8	OC(=O)c1cc(c(s1)C(C(=O)O)N)C	12015200
	1382	1167	29	None	-1	3	Human	5.5	pIC50	=	5.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	10051528
	6278000	1167	29	None	-1	3	Human	5.5	pIC50	=	5.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	10051528
	CHEMBL327783	1167	29	None	-1	3	Human	5.5	pIC50	=	5.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	10051528
	16739288	1018	0	None	-	1	Rat	6.8	pIC50	=	6.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	306	3	2	2	3.3	Cc1cc2[nH]c3c(c2cc1OCc1ccccc1)CCNC3=O	17276684
	6358	1018	0	None	-	1	Rat	6.8	pIC50	=	6.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	306	3	2	2	3.3	Cc1cc2[nH]c3c(c2cc1OCc1ccccc1)CCNC3=O	17276684
	CHEMBL396712	1018	0	None	-	1	Rat	6.8	pIC50	=	6.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	306	3	2	2	3.3	Cc1cc2[nH]c3c(c2cc1OCc1ccccc1)CCNC3=O	17276684
	1390	1526	0	None	-	1	Rat	6.9	pIC50	=	6.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	308	2	0	5	2.0	CCn1c(C)nc(c(c1=O)C#N)N1CCc2c(CC1)cccc2	12509432
	3363	1526	0	None	-	1	Rat	6.9	pIC50	=	6.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	308	2	0	5	2.0	CCn1c(C)nc(c(c1=O)C#N)N1CCc2c(CC1)cccc2	12509432
	9904703	1526	0	None	-	1	Rat	6.9	pIC50	=	6.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	308	2	0	5	2.0	CCn1c(C)nc(c(c1=O)C#N)N1CCc2c(CC1)cccc2	12509432
	3346	2391	10	None	-	1	Human	6.9	pIC50	=	6.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	281	4	1	5	3.4	COc1ccc(cc1)Nc1ncnc2c1cc(OC)cc2	24798819
	9926999	2391	10	None	-	1	Human	6.9	pIC50	=	6.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	281	4	1	5	3.4	COc1ccc(cc1)Nc1ncnc2c1cc(OC)cc2	24798819
	CHEMBL254575	2391	10	None	-	1	Human	6.9	pIC50	=	6.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	281	4	1	5	3.4	COc1ccc(cc1)Nc1ncnc2c1cc(OC)cc2	24798819
	1389	4055	0	None	-7	2	Human	6.9	pIC50	=	6.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	342	2	1	5	3.8	CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1	19559036
	5392	4055	0	None	-7	2	Human	6.9	pIC50	=	6.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	342	2	1	5	3.8	CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1	19559036
	9819432	4055	0	None	-7	2	Human	6.9	pIC50	=	6.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	342	2	1	5	3.8	CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1	19559036
	CHEMBL1517556	4055	0	None	-7	2	Human	6.9	pIC50	=	6.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	342	2	1	5	3.8	CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1	19559036
	6337	3985	0	None	-	1	Human	7.0	pIC50	=	7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	378	2	0	4	3.5	N#Cc1ncccc1N1CCN([C@@H](C1)C)C(=O)C12CC3CC(C2)C(C(C1)C3)C	23727046
	73755207	3985	0	None	-	1	Human	7.0	pIC50	=	7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	378	2	0	4	3.5	N#Cc1ncccc1N1CCN([C@@H](C1)C)C(=O)C12CC3CC(C2)C(C(C1)C3)C	23727046
	10245890	1951	7	None	3	2	Human	7.0	pIC50	=	7.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	327	5	0	4	4.2	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC	15771457
	6474	1951	7	None	3	2	Human	7.0	pIC50	=	7.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	327	5	0	4	4.2	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC	15771457
	CHEMBL175643	1951	7	None	3	2	Human	7.0	pIC50	=	7.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	327	5	0	4	4.2	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC	15771457
	6340	871	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	389	5	0	5	4.0	Cc1c(OCCN2CCOCC2)cc2c(c1F)c(=O)c(co2)C1CCCCC1	19559036
	73755208	871	0	None	-	1	Human	7.3	pIC50	=	7.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	389	5	0	5	4.0	Cc1c(OCCN2CCOCC2)cc2c(c1F)c(=O)c(co2)C1CCCCC1	19559036
	11515548	210	6	None	-1	3	Human	7.4	pIC50	=	7.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	336	2	0	6	3.4	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(cnc1)N(C)C	16279797
	6355	210	6	None	-1	3	Human	7.4	pIC50	=	7.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	336	2	0	6	3.4	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(cnc1)N(C)C	16279797
	CHEMBL223869	210	6	None	-1	3	Human	7.4	pIC50	=	7.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	336	2	0	6	3.4	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(cnc1)N(C)C	16279797
	11515548	210	6	None	1	3	Rat	7.4	pIC50	=	7.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	336	2	0	6	3.4	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(cnc1)N(C)C	18054908
	6355	210	6	None	1	3	Rat	7.4	pIC50	=	7.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	336	2	0	6	3.4	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(cnc1)N(C)C	18054908
	CHEMBL223869	210	6	None	1	3	Rat	7.4	pIC50	=	7.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	336	2	0	6	3.4	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(cnc1)N(C)C	18054908
	1381	574	21	None	3	2	Rat	7.4	pIC50	=	7.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	278	2	0	2	3.9	C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2	11306677
	1381	574	21	None	3	2	Rat	7.4	pIC50	=	7.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	278	2	0	2	3.9	C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2	12695537
	9903757	574	21	None	3	2	Rat	7.4	pIC50	=	7.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	278	2	0	2	3.9	C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2	11306677
	9903757	574	21	None	3	2	Rat	7.4	pIC50	=	7.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	278	2	0	2	3.9	C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2	12695537
	CHEMBL254372	574	21	None	3	2	Rat	7.4	pIC50	=	7.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	278	2	0	2	3.9	C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2	11306677
	CHEMBL254372	574	21	None	3	2	Rat	7.4	pIC50	=	7.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	278	2	0	2	3.9	C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2	12695537
	3347	2390	6	None	-	1	Human	7.6	pIC50	=	7.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	341	5	2	5	3.0	OCCSc1nc(NC2Cc3c(C2)cccc3)c2c(n1)CCCC2	19559036
	9840951	2390	6	None	-	1	Human	7.6	pIC50	=	7.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	341	5	2	5	3.0	OCCSc1nc(NC2Cc3c(C2)cccc3)c2c(n1)CCCC2	19559036
	CHEMBL3786530	2390	6	None	-	1	Human	7.6	pIC50	=	7.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	341	5	2	5	3.0	OCCSc1nc(NC2Cc3c(C2)cccc3)c2c(n1)CCCC2	19559036
	46866192	1034	0	None	-	1	Human	7.6	pIC50	=	7.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	323	1	1	7	2.6	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)C	20346665
	6210	1034	0	None	-	1	Human	7.6	pIC50	=	7.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	323	1	1	7	2.6	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)C	20346665
	CHEMBL1093901	1034	0	None	-	1	Human	7.6	pIC50	=	7.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	323	1	1	7	2.6	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)C	20346665
	11722867	95	2	None	-	1	Rat	7.8	pIC50	=	7.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	309	5	1	4	3.8	CCCOC(=O)c1[nH]c(c(c1C)C(=O)OC(C(C)(C)C)C)C	12470711
	3397	95	2	None	-	1	Rat	7.8	pIC50	=	7.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	309	5	1	4	3.8	CCCOC(=O)c1[nH]c(c(c1C)C(=O)OC(C(C)(C)C)C)C	12470711
	CHEMBL304824	95	2	None	-	1	Rat	7.8	pIC50	=	7.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	309	5	1	4	3.8	CCCOC(=O)c1[nH]c(c(c1C)C(=O)OC(C(C)(C)C)C)C	12470711
	6364	1070	0	None	-	1	Rat	7.8	pIC50	=	7.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	295	5	1	4	3.4	CCCOC(=O)c1[nH]c(c(c1C)C(=O)OCC(C)(C)C)C	12470711
	73755211	1070	0	None	-	1	Rat	7.8	pIC50	=	7.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	295	5	1	4	3.4	CCCOC(=O)c1[nH]c(c(c1C)C(=O)OCC(C)(C)C)C	12470711
	1389	4055	0	None	7	2	Rat	7.8	pIC50	=	7.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	342	2	1	5	3.8	CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1	15976016
	5392	4055	0	None	7	2	Rat	7.8	pIC50	=	7.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	342	2	1	5	3.8	CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1	15976016
	9819432	4055	0	None	7	2	Rat	7.8	pIC50	=	7.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	342	2	1	5	3.8	CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1	15976016
	CHEMBL1517556	4055	0	None	7	2	Rat	7.8	pIC50	=	7.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	342	2	1	5	3.8	CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1	15976016
	16118537	964	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	363	4	1	6	4.2	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1	22266036
	6357	964	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	363	4	1	6	4.2	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1	22266036
	CHEMBL1951683	964	0	None	-	1	Human	7.9	pIC50	=	7.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	363	4	1	6	4.2	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1	22266036
	10470232	3218	18	None	-1	2	Human	8.0	pIC50	=	8.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	12695537
	1391	3218	18	None	-1	2	Human	8.0	pIC50	=	8.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	12695537
	6336	3218	18	None	-1	2	Human	8.0	pIC50	=	8.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	12695537
	CHEMBL369459	3218	18	None	-1	2	Human	8.0	pIC50	=	8.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	12695537
	11537456	207	9	None	-3	3	Human	8.0	pIC50	=	8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	342	2	0	6	4.0	CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C	16279797
	6354	207	9	None	-3	3	Human	8.0	pIC50	=	8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	342	2	0	6	4.0	CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C	16279797
	CHEMBL225032	207	9	None	-3	3	Human	8.0	pIC50	=	8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	342	2	0	6	4.0	CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C	16279797
	11559235	209	37	None	-4	3	Human	8.0	pIC50	=	8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	343	2	0	7	2.6	CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C	16279797
	3953	209	37	None	-4	3	Human	8.0	pIC50	=	8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	343	2	0	7	2.6	CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C	16279797
	CHEMBL386565	209	37	None	-4	3	Human	8.0	pIC50	=	8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	343	2	0	7	2.6	CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C	16279797
	6208	1038	0	None	-	1	Rat	8.1	pIC50	=	8.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	318	4	2	5	1.7	OCC1CCN(CC1)c1ncc(nc1)C(=O)NC1CCCCC1	17064898
	73755189	1038	0	None	-	1	Rat	8.1	pIC50	=	8.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	318	4	2	5	1.7	OCC1CCN(CC1)c1ncc(nc1)C(=O)NC1CCCCC1	17064898
	10409562	4053	0	None	-	1	Rat	8.1	pIC50	=	8.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	414	7	0	6	4.0	COCCN(Cc1ccc2c(c1)nc1n2cc(s1)C(=O)N(C1CCCCC1)C)C	18164695
	6361	4053	0	None	-	1	Rat	8.1	pIC50	=	8.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	414	7	0	6	4.0	COCCN(Cc1ccc2c(c1)nc1n2cc(s1)C(=O)N(C1CCCCC1)C)C	18164695
	16725048	1131	0	None	1412	2	Human	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	371	3	0	8	2.6	COc1ccc(c(c1)F)n1cnc2c(c1=O)sc1c2c(ncn1)N(C)C	23084894
	6362	1131	0	None	1412	2	Human	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	371	3	0	8	2.6	COc1ccc(c(c1)F)n1cnc2c(c1=O)sc1c2c(ncn1)N(C)C	23084894
	CHEMBL2205377	1131	0	None	1412	2	Human	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	371	3	0	8	2.6	COc1ccc(c(c1)F)n1cnc2c(c1=O)sc1c2c(ncn1)N(C)C	23084894
	16118119	1127	0	None	741	2	Human	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	351	3	0	6	3.7	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C	22266036
	6356	1127	0	None	741	2	Human	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	351	3	0	6	3.7	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C	22266036
	CHEMBL1951658	1127	0	None	741	2	Human	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	351	3	0	6	3.7	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C	22266036
	57559562	952	0	None	1659	2	Human	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	365	4	1	8	3.0	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ncn1)NC1CC1	23084894
	6365	952	0	None	1659	2	Human	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	365	4	1	8	3.0	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ncn1)NC1CC1	23084894
	CHEMBL2205915	952	0	None	1659	2	Human	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	365	4	1	8	3.0	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ncn1)NC1CC1	23084894
	11337722	1053	0	None	-	1	Rat	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	371	6	1	7	2.9	C1CCCC(CC1)Nc1ncnc2c1cc(OCCN1CCOCC1)nc2	19289283
	6351	1053	0	None	-	1	Rat	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	371	6	1	7	2.9	C1CCCC(CC1)Nc1ncnc2c1cc(OCCN1CCOCC1)nc2	19289283
	CHEMBL470396	1053	0	None	-	1	Rat	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	371	6	1	7	2.9	C1CCCC(CC1)Nc1ncnc2c1cc(OCCN1CCOCC1)nc2	19289283
	11245287	1667	29	None	-1	4	Human	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	17360958
	6363	1667	29	None	-1	4	Human	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	17360958
	CHEMBL502882	1667	29	None	-1	4	Human	8.2	pIC50	=	8.2	Functional	UnclassifiedUnclassified	Guide to Pharmacology	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	17360958
	6343	957	0	None	-	1	Human	8.3	pIC50	=	8.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	352	2	1	6	2.6	COc1ccc(cc1)N1C=NC2C(C1=O)Sc1c2c2NCCc2cn1	17929793
	73755209	957	0	None	-	1	Human	8.3	pIC50	=	8.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	352	2	1	6	2.6	COc1ccc(cc1)N1C=NC2C(C1=O)Sc1c2c2NCCc2cn1	17929793
	11245287	1667	29	None	-1	4	Rat	8.3	pIC50	=	8.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	17360958
	6363	1667	29	None	-1	4	Rat	8.3	pIC50	=	8.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	17360958
	CHEMBL502882	1667	29	None	-1	4	Rat	8.3	pIC50	=	8.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	17360958
	11530404	208	11	None	-1	4	Rat	8.3	pIC50	=	8.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	18054908
	6211	208	11	None	-1	4	Rat	8.3	pIC50	=	8.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	18054908
	CHEMBL385336	208	11	None	-1	4	Rat	8.3	pIC50	=	8.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	18054908
	15985251	2521	24	None	-1	2	Human	8.4	pIC50	=	8.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	368	3	0	4	3.9	Fc1ccc(c(c1)F)n1nnc(c1C)c1ccc2c(c1)CN(C2=O)C(C)C	20524178
	6335	2521	24	None	-1	2	Human	8.4	pIC50	=	8.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	368	3	0	4	3.9	Fc1ccc(c(c1)F)n1nnc(c1C)c1ccc2c(c1)CN(C2=O)C(C)C	20524178
	CHEMBL579062	2521	24	None	-1	2	Human	8.4	pIC50	=	8.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	368	3	0	4	3.9	Fc1ccc(c(c1)F)n1nnc(c1C)c1ccc2c(c1)CN(C2=O)C(C)C	20524178
	11530404	208	11	None	1	4	Human	8.5	pIC50	=	8.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	16279797
	6211	208	11	None	1	4	Human	8.5	pIC50	=	8.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	16279797
	CHEMBL385336	208	11	None	1	4	Human	8.5	pIC50	=	8.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	16279797
	11772954	1019	0	None	-1	2	Rat	8.5	pIC50	=	8.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	365	8	3	7	2.0	OCCOCCNc1ncc2c(c1)c(ncn2)NC1Cc2c(C1)cccc2	19289283
	6349	1019	0	None	-1	2	Rat	8.5	pIC50	=	8.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	365	8	3	7	2.0	OCCOCCNc1ncc2c(c1)c(ncn2)NC1Cc2c(C1)cccc2	19289283
	CHEMBL469382	1019	0	None	-1	2	Rat	8.5	pIC50	=	8.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	365	8	3	7	2.0	OCCOCCNc1ncc2c(c1)c(ncn2)NC1Cc2c(C1)cccc2	19289283
	16659801	1021	0	None	-	1	Human	8.5	pIC50	=	8.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	370	1	1	7	3.5	Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	17929793
	6346	1021	0	None	-	1	Human	8.5	pIC50	=	8.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	370	1	1	7	3.5	Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	17929793
	CHEMBL236994	1021	0	None	-	1	Human	8.5	pIC50	=	8.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	370	1	1	7	3.5	Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	17929793
	11175501	872	34	None	1819	2	Human	8.6	pIC50	=	8.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	349	3	0	5	2.9	O=C1N(Cc2c1ccc(c2)c1nnn(c1C)c1cccnc1F)C1CC1	19359526
	6341	872	34	None	1819	2	Human	8.6	pIC50	=	8.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	349	3	0	5	2.9	O=C1N(Cc2c1ccc(c2)c1nnn(c1C)c1cccnc1F)C1CC1	19359526
	CHEMBL578995	872	34	None	1819	2	Human	8.6	pIC50	=	8.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	349	3	0	5	2.9	O=C1N(Cc2c1ccc(c2)c1nnn(c1C)c1cccnc1F)C1CC1	19359526
	16659967	1020	0	None	-	1	Human	8.6	pIC50	=	8.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	366	2	1	8	2.8	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	17929793
	6345	1020	0	None	-	1	Human	8.6	pIC50	=	8.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	366	2	1	8	2.8	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	17929793
	CHEMBL393922	1020	0	None	-	1	Human	8.6	pIC50	=	8.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	366	2	1	8	2.8	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	17929793
	16659803	1022	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	384	1	1	7	3.8	C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	17929793
	6338	1022	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	384	1	1	7	3.8	C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	17929793
	CHEMBL236180	1022	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	384	1	1	7	3.8	C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	17929793
	23634102	963	1	None	-	1	Human	8.7	pIC50	=	8.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	362	4	1	7	3.0	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC	19433355
	6215	963	1	None	-	1	Human	8.7	pIC50	=	8.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	362	4	1	7	3.0	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC	19433355
	CHEMBL1783876	963	1	None	-	1	Human	8.7	pIC50	=	8.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	362	4	1	7	3.0	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC	19433355
	46866191	1028	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	324	1	2	8	1.9	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N	20346665
	6209	1028	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	324	1	2	8	1.9	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N	20346665
	CHEMBL1093560	1028	0	None	-	1	Human	8.7	pIC50	=	8.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	324	1	2	8	1.9	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N	20346665
	16659802	1023	0	None	-	1	Human	8.9	pIC50	=	8.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	384	1	1	7	3.8	C[C@@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	17929793
	6348	1023	0	None	-	1	Human	8.9	pIC50	=	8.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	384	1	1	7	3.8	C[C@@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	17929793
	CHEMBL241327	1023	0	None	-	1	Human	8.9	pIC50	=	8.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	384	1	1	7	3.8	C[C@@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	17929793
	11313361	2103	54	None	3	2	Human	8.9	pIC50	=	8.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	15555631
	1385	2103	54	None	3	2	Human	8.9	pIC50	=	8.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	15555631
	CHEMBL174588	2103	54	None	3	2	Human	8.9	pIC50	=	8.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	15555631
	CHEMBL254574	2103	54	None	3	2	Human	8.9	pIC50	=	8.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	15555631
	11559235	209	37	None	4	3	Rat	9.0	pIC50	=	9.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	343	2	0	7	2.6	CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C	16809035
	11559235	209	37	None	4	3	Rat	9.0	pIC50	=	9.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	343	2	0	7	2.6	CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C	18054908
	3953	209	37	None	4	3	Rat	9.0	pIC50	=	9.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	343	2	0	7	2.6	CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C	16809035
	3953	209	37	None	4	3	Rat	9.0	pIC50	=	9.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	343	2	0	7	2.6	CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C	18054908
	CHEMBL386565	209	37	None	4	3	Rat	9.0	pIC50	=	9.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	343	2	0	7	2.6	CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C	16809035
	CHEMBL386565	209	37	None	4	3	Rat	9.0	pIC50	=	9.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	343	2	0	7	2.6	CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C	18054908
	23634171	962	1	None	-	1	Human	9.1	pIC50	=	9.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	366	3	1	6	3.7	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl	19433355
	6214	962	1	None	-	1	Human	9.1	pIC50	=	9.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	366	3	1	6	3.7	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl	19433355
	CHEMBL1783874	962	1	None	-	1	Human	9.1	pIC50	=	9.1	Functional	UnclassifiedUnclassified	Guide to Pharmacology	366	3	1	6	3.7	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl	19433355
	1366	2049	39	None	-1	3	Rat	4.9	pIC50	None	4.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	167	2	3	3	0.5	OC(=O)[C@H](c1cccc(c1)O)N	11080213
	40428795	2049	39	None	-1	3	Rat	4.9	pIC50	None	4.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	167	2	3	3	0.5	OC(=O)[C@H](c1cccc(c1)O)N	11080213
	6604712	2049	39	None	-1	3	Rat	4.9	pIC50	None	4.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	167	2	3	3	0.5	OC(=O)[C@H](c1cccc(c1)O)N	11080213
	CHEMBL442347	2049	39	None	-1	3	Rat	4.9	pIC50	None	4.9	Functional	UnclassifiedUnclassified	Guide to Pharmacology	167	2	3	3	0.5	OC(=O)[C@H](c1cccc(c1)O)N	11080213
	1383	1421	1	None	-	1	Rat	7.8	pIC50	None	7.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	309	5	1	4	3.8	CCCOC(=O)c1[nH]c(c(c1C)C(=O)O[C@H](C(C)(C)C)C)C	12470711
	44431042	1421	1	None	-	1	Rat	7.8	pIC50	None	7.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	309	5	1	4	3.8	CCCOC(=O)c1[nH]c(c(c1C)C(=O)O[C@H](C(C)(C)C)C)C	12470711
	CHEMBL232052	1421	1	None	-	1	Rat	7.8	pIC50	None	7.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	309	5	1	4	3.8	CCCOC(=O)c1[nH]c(c(c1C)C(=O)O[C@H](C(C)(C)C)C)C	12470711
	10009	3986	35	None	-1	3	Human	6.0	pKB	=	6.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	445	3	1	4	5.1	Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl	29514854
	91885483	3986	35	None	-1	3	Human	6.0	pKB	=	6.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	445	3	1	4	5.1	Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl	29514854
	CHEMBL3628116	3986	35	None	-1	3	Human	6.0	pKB	=	6.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	445	3	1	4	5.1	Clc1cc(ccc1N1C(=O)c2c(C1=O)c(Cl)ccc2)NC(=O)c1ncccc1Cl	29514854

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Ligands					Receptor			Assay information							Chemical information
Sel. page	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity (Affinity)	# tested GPCRs (Affinity)	Species	p-value (-log)	Type	Activity Relation	Activity Value	Assay Type	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	52942855	17116	0	None	-	0	Human	6.0	pEC50	=	6	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	441	6	2	6	2.8	NC(=O)c1c(NC(=O)Cn2cc(CN3CCC3)c(C(F)(F)F)n2)sc2c1CCCC2	10.1016/j.bmcl.2010.08.063
	CHEMBL1257182	17116	0	None	-	0	Human	6.0	pEC50	=	6	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	441	6	2	6	2.8	NC(=O)c1c(NC(=O)Cn2cc(CN3CCC3)c(C(F)(F)F)n2)sc2c1CCCC2	10.1016/j.bmcl.2010.08.063
	44237734	17500	0	None	-	0	Human	6.0	pEC50	=	6	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	427	4	3	6	2.2	NC(=O)c1c(NC(=O)Cn2nc(C(F)(F)F)c3c2CCNC3)sc2c1CCCC2	10.1016/j.bmcl.2010.08.063
	CHEMBL1258461	17500	0	None	-	0	Human	6.0	pEC50	=	6	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	427	4	3	6	2.2	NC(=O)c1c(NC(=O)Cn2nc(C(F)(F)F)c3c2CCNC3)sc2c1CCCC2	10.1016/j.bmcl.2010.08.063
	1310	2286	108	None	-4	18	Rat	5.0	pEC50	=	5	Binding	Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm020122x
	1369	2286	108	None	-4	18	Rat	5.0	pEC50	=	5	Binding	Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm020122x
	33032	2286	108	None	-4	18	Rat	5.0	pEC50	=	5	Binding	Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm020122x
	44272391	2286	108	None	-4	18	Rat	5.0	pEC50	=	5	Binding	Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm020122x
	88747398	2286	108	None	-4	18	Rat	5.0	pEC50	=	5	Binding	Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm020122x
	CHEMBL575060	2286	108	None	-4	18	Rat	5.0	pEC50	=	5	Binding	Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm020122x
	DB00142	2286	108	None	-4	18	Rat	5.0	pEC50	=	5	Binding	Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1Compound was evaluated for the inhibitory activity against cloned Metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm020122x
	139054390	203215	101	None	-	5	Rat	5.0	pEC50	=	5	Binding	Effect on Metabotropic glutamate receptor 1Effect on Metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	N[C@H](CCC(=O)O)C(=O)O	10.1021/jm9703597
	23327	203215	101	None	-	5	Rat	5.0	pEC50	=	5	Binding	Effect on Metabotropic glutamate receptor 1Effect on Metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	N[C@H](CCC(=O)O)C(=O)O	10.1021/jm9703597
	CHEMBL76232	203215	101	None	-	5	Rat	5.0	pEC50	=	5	Binding	Effect on Metabotropic glutamate receptor 1Effect on Metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	N[C@H](CCC(=O)O)C(=O)O	10.1021/jm9703597
	1310	2286	108	None	-4	18	Rat	4.9	pEC50	=	4.9	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	1369	2286	108	None	-4	18	Rat	4.9	pEC50	=	4.9	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	33032	2286	108	None	-4	18	Rat	4.9	pEC50	=	4.9	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	44272391	2286	108	None	-4	18	Rat	4.9	pEC50	=	4.9	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	88747398	2286	108	None	-4	18	Rat	4.9	pEC50	=	4.9	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	CHEMBL575060	2286	108	None	-4	18	Rat	4.9	pEC50	=	4.9	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	DB00142	2286	108	None	-4	18	Rat	4.9	pEC50	=	4.9	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	49800187	17571	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	415	6	3	6	2.3	CNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	CHEMBL1258681	17571	0	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	415	6	3	6	2.3	CNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	1310	2286	108	None	-4	18	Rat	4.9	pEC50	=	4.9	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	1369	2286	108	None	-4	18	Rat	4.9	pEC50	=	4.9	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	33032	2286	108	None	-4	18	Rat	4.9	pEC50	=	4.9	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	44272391	2286	108	None	-4	18	Rat	4.9	pEC50	=	4.9	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	88747398	2286	108	None	-4	18	Rat	4.9	pEC50	=	4.9	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	CHEMBL575060	2286	108	None	-4	18	Rat	4.9	pEC50	=	4.9	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	DB00142	2286	108	None	-4	18	Rat	4.9	pEC50	=	4.9	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	10338547	3288	21	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2016.03.044
	6204	3288	21	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2016.03.044
	CHEMBL521982	3288	21	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2016.03.044
	10338547	3288	21	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2016.03.044
	6204	3288	21	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2016.03.044
	CHEMBL521982	3288	21	None	-	0	Human	6.9	pEC50	=	6.9	Binding	Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)	ChEMBL	360	2	1	4	4.6	O=C(C1c2ccccc2Oc2c1cccc2)Nc1occ(n1)C(F)(F)F	10.1016/j.bmcl.2016.03.044
	104766	34	36	None	-26	11	Human	4.8	pEC50	=	4.8	Binding	Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm970719q
	1365	34	36	None	-26	11	Human	4.8	pEC50	=	4.8	Binding	Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm970719q
	CHEMBL34453	34	36	None	-26	11	Human	4.8	pEC50	=	4.8	Binding	Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm970719q
	52946206	17181	0	None	-	0	Human	5.8	pEC50	=	5.8	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	429	7	3	6	3.1	CC(C)(C)c1nn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)cc1CNC1CC1	10.1016/j.bmcl.2010.08.063
	CHEMBL1257414	17181	0	None	-	0	Human	5.8	pEC50	=	5.8	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	429	7	3	6	3.1	CC(C)(C)c1nn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)cc1CNC1CC1	10.1016/j.bmcl.2010.08.063
	52941383	17223	0	None	-	0	Human	5.8	pEC50	=	5.8	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	431	7	3	6	3.4	CC(C)NCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(C)(C)C	10.1016/j.bmcl.2010.08.063
	CHEMBL1257527	17223	0	None	-	0	Human	5.8	pEC50	=	5.8	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	431	7	3	6	3.4	CC(C)NCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(C)(C)C	10.1016/j.bmcl.2010.08.063
	52947461	17224	0	None	-	0	Human	5.8	pEC50	=	5.8	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	429	7	3	6	2.7	CNCc1cn(CCC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	CHEMBL1257528	17224	0	None	-	0	Human	5.8	pEC50	=	5.8	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	429	7	3	6	2.7	CNCc1cn(CCC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	52945583	17299	0	None	-	0	Human	5.8	pEC50	=	5.8	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	429	6	3	6	2.6	CNCc1cn(CC(=O)Nc2sc3c(c2C(=O)NC)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	CHEMBL1257768	17299	0	None	-	0	Human	5.8	pEC50	=	5.8	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	429	6	3	6	2.6	CNCc1cn(CC(=O)Nc2sc3c(c2C(=O)NC)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	52947637	17642	0	None	-	0	Human	5.8	pEC50	=	5.8	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	459	9	3	7	2.3	COCCNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	CHEMBL1258915	17642	0	None	-	0	Human	5.8	pEC50	=	5.8	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	459	9	3	7	2.3	COCCNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	1310	2286	108	None	-1	18	Human	5.8	pEC50	=	5.8	Binding	Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1039/C1MD00186H
	1369	2286	108	None	-1	18	Human	5.8	pEC50	=	5.8	Binding	Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1039/C1MD00186H
	33032	2286	108	None	-1	18	Human	5.8	pEC50	=	5.8	Binding	Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1039/C1MD00186H
	44272391	2286	108	None	-1	18	Human	5.8	pEC50	=	5.8	Binding	Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1039/C1MD00186H
	88747398	2286	108	None	-1	18	Human	5.8	pEC50	=	5.8	Binding	Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1039/C1MD00186H
	CHEMBL575060	2286	108	None	-1	18	Human	5.8	pEC50	=	5.8	Binding	Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1039/C1MD00186H
	DB00142	2286	108	None	-1	18	Human	5.8	pEC50	=	5.8	Binding	Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1039/C1MD00186H
	10846649	100761	4	None	-	0	Human	5.8	pEC50	=	5.8	Binding	Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1	ChEMBL	185	2	3	3	-0.5	N[C@@]1(C(=O)O)C[C@@H]2C[C@H]1[C@H]2C(=O)O	10.1021/jm970719q
	CHEMBL296054	100761	4	None	-	0	Human	5.8	pEC50	=	5.8	Binding	Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1	ChEMBL	185	2	3	3	-0.5	N[C@@]1(C(=O)O)C[C@@H]2C[C@H]1[C@H]2C(=O)O	10.1021/jm970719q
	1370	3212	62	None	44	8	Rat	4.8	pEC50	=	4.8	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in humanConcentration for half maximal activation of metabotropic glutamate mGluR1b in human	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	1372	3212	62	None	44	8	Rat	4.8	pEC50	=	4.8	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in humanConcentration for half maximal activation of metabotropic glutamate mGluR1b in human	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	40539	3212	62	None	44	8	Rat	4.8	pEC50	=	4.8	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in humanConcentration for half maximal activation of metabotropic glutamate mGluR1b in human	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	6971145	3212	62	None	44	8	Rat	4.8	pEC50	=	4.8	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in humanConcentration for half maximal activation of metabotropic glutamate mGluR1b in human	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	CHEMBL279956	3212	62	None	44	8	Rat	4.8	pEC50	=	4.8	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in humanConcentration for half maximal activation of metabotropic glutamate mGluR1b in human	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	DB02999	3212	62	None	44	8	Rat	4.8	pEC50	=	4.8	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in humanConcentration for half maximal activation of metabotropic glutamate mGluR1b in human	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	127047993	139121	1	None	-	0	Human	6.7	pEC50	=	6.7	Binding	Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)	ChEMBL	333	2	1	5	3.9	N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	CHEMBL3797793	139121	1	None	-	0	Human	6.7	pEC50	=	6.7	Binding	Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)	ChEMBL	333	2	1	5	3.9	N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	127047993	139121	1	None	-	0	Human	6.7	pEC50	=	6.7	Binding	Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)	ChEMBL	333	2	1	5	3.9	N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	CHEMBL3797793	139121	1	None	-	0	Human	6.7	pEC50	=	6.7	Binding	Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)	ChEMBL	333	2	1	5	3.9	N#Cc1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	52949928	17263	0	None	-	0	Human	5.7	pEC50	=	5.7	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	471	9	2	6	3.8	CCN(CC)Cc1cn(CCC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	CHEMBL1257646	17263	0	None	-	0	Human	5.7	pEC50	=	5.7	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	471	9	2	6	3.8	CCN(CC)Cc1cn(CCC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	1370	3212	62	None	44	8	Rat	6.7	pEC50	=	6.7	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	1372	3212	62	None	44	8	Rat	6.7	pEC50	=	6.7	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	40539	3212	62	None	44	8	Rat	6.7	pEC50	=	6.7	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	6971145	3212	62	None	44	8	Rat	6.7	pEC50	=	6.7	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	CHEMBL279956	3212	62	None	44	8	Rat	6.7	pEC50	=	6.7	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	DB02999	3212	62	None	44	8	Rat	6.7	pEC50	=	6.7	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	1370	3212	62	None	-66	8	Human	6.7	pEC50	=	6.7	Binding	Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm9601718
	1372	3212	62	None	-66	8	Human	6.7	pEC50	=	6.7	Binding	Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm9601718
	40539	3212	62	None	-66	8	Human	6.7	pEC50	=	6.7	Binding	Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm9601718
	6971145	3212	62	None	-66	8	Human	6.7	pEC50	=	6.7	Binding	Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm9601718
	CHEMBL279956	3212	62	None	-66	8	Human	6.7	pEC50	=	6.7	Binding	Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm9601718
	DB02999	3212	62	None	-66	8	Human	6.7	pEC50	=	6.7	Binding	Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm9601718
	127046038	139411	0	None	-	0	Human	6.7	pEC50	=	6.7	Binding	Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)	ChEMBL	350	3	1	4	5.1	CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	CHEMBL3799685	139411	0	None	-	0	Human	6.7	pEC50	=	6.7	Binding	Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate pEC50 at 10 uM (Rvb = 6.007 +/- 0.076 No_unit)	ChEMBL	350	3	1	4	5.1	CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	127046038	139411	0	None	-	0	Human	6.7	pEC50	=	6.7	Binding	Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)	ChEMBL	350	3	1	4	5.1	CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	CHEMBL3799685	139411	0	None	-	0	Human	6.7	pEC50	=	6.7	Binding	Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)Positive allosteric modulation of human mGlu1 receptor assessed as glutamate EC50 at 10 uM (Rvb = 983.4 nM)	ChEMBL	350	3	1	4	5.1	CC(C)c1csc(NC(=O)C2c3ccccc3Oc3ccccc32)n1	10.1016/j.bmcl.2016.03.044
	104766	34	36	None	3	11	Rat	4.7	pEC50	=	4.7	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm00009a001
	1365	34	36	None	3	11	Rat	4.7	pEC50	=	4.7	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm00009a001
	CHEMBL34453	34	36	None	3	11	Rat	4.7	pEC50	=	4.7	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm00009a001
	104766	34	36	None	-26	11	Human	4.7	pEC50	=	4.7	Binding	Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm9601718
	1365	34	36	None	-26	11	Human	4.7	pEC50	=	4.7	Binding	Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm9601718
	CHEMBL34453	34	36	None	-26	11	Human	4.7	pEC50	=	4.7	Binding	Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm9601718
	1370	3212	62	None	44	8	Rat	5.6	pEC50	=	5.6	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	1372	3212	62	None	44	8	Rat	5.6	pEC50	=	5.6	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	40539	3212	62	None	44	8	Rat	5.6	pEC50	=	5.6	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	6971145	3212	62	None	44	8	Rat	5.6	pEC50	=	5.6	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	CHEMBL279956	3212	62	None	44	8	Rat	5.6	pEC50	=	5.6	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	DB02999	3212	62	None	44	8	Rat	5.6	pEC50	=	5.6	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	46947824	16304	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	495	5	3	6	3.5	O=C(Cn1nc(C(F)(F)F)c2c1CCCC2)Nc1sc2c(c1C(=O)N[C@@H]1CCNC1)CCCC2	10.1016/j.bmcl.2010.08.063
	CHEMBL1234889	16304	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	495	5	3	6	3.5	O=C(Cn1nc(C(F)(F)F)c2c1CCCC2)Nc1sc2c(c1C(=O)N[C@@H]1CCNC1)CCCC2	10.1016/j.bmcl.2010.08.063
	52945134	17536	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	413	4	2	5	3.9	O=C(Cn1nc(C(F)(F)F)c2c1CCCC2)Nc1sc2c(c1CO)CCCC2	10.1016/j.bmcl.2010.08.063
	CHEMBL1258570	17536	0	None	-	0	Human	6.6	pEC50	=	6.6	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	413	4	2	5	3.9	O=C(Cn1nc(C(F)(F)F)c2c1CCCC2)Nc1sc2c(c1CO)CCCC2	10.1016/j.bmcl.2010.08.063
	52948725	17262	0	None	-	0	Human	5.6	pEC50	=	5.6	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	443	8	3	6	3.1	CCNCc1cn(CCC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	CHEMBL1257645	17262	0	None	-	0	Human	5.6	pEC50	=	5.6	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	443	8	3	6	3.1	CCNCc1cn(CCC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	118718092	120084	0	None	-	1	Human	5.5	pEC50	=	5.5	Binding	Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells	ChEMBL	215	3	3	6	-0.4	N[C@]1(C(=O)O)C[C@H]1Cc1nsnc1O	10.1039/C1MD00186H
	CHEMBL3347672	120084	0	None	-	1	Human	5.5	pEC50	=	5.5	Binding	Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells	ChEMBL	215	3	3	6	-0.4	N[C@]1(C(=O)O)C[C@H]1Cc1nsnc1O	10.1039/C1MD00186H
	CHEMBL3545861	120084	0	None	-	1	Human	5.5	pEC50	=	5.5	Binding	Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells	ChEMBL	215	3	3	6	-0.4	N[C@]1(C(=O)O)C[C@H]1Cc1nsnc1O	10.1039/C1MD00186H
	46870038	16303	0	None	-	0	Human	6.5	pEC50	=	6.5	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	403	6	3	6	2.6	CNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(C)(C)C	10.1016/j.bmcl.2010.08.063
	CHEMBL1234888	16303	0	None	-	0	Human	6.5	pEC50	=	6.5	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	403	6	3	6	2.6	CNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(C)(C)C	10.1016/j.bmcl.2010.08.063
	24967422	17146	0	None	-	0	Human	6.5	pEC50	=	6.5	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	417	6	2	6	2.9	CN(C)Cc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(C)(C)C	10.1016/j.bmcl.2010.08.063
	CHEMBL1257298	17146	0	None	-	0	Human	6.5	pEC50	=	6.5	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	417	6	2	6	2.9	CN(C)Cc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(C)(C)C	10.1016/j.bmcl.2010.08.063
	52942778	17610	0	None	-	0	Human	5.5	pEC50	=	5.5	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	443	7	3	6	3.1	CC(C)NCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	CHEMBL1258796	17610	0	None	-	0	Human	5.5	pEC50	=	5.5	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	443	7	3	6	3.1	CC(C)NCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	6603885	101731	17	None	-	0	Rat	4.5	pEC50	=	4.5	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	158	2	3	5	-0.5	N[C@H](C(=O)O)c1cc(O)no1	10.1021/jm00009a001
	6971208	101731	17	None	-	0	Rat	4.5	pEC50	=	4.5	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	158	2	3	5	-0.5	N[C@H](C(=O)O)c1cc(O)no1	10.1021/jm00009a001
	CHEMBL30285	101731	17	None	-	0	Rat	4.5	pEC50	=	4.5	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	158	2	3	5	-0.5	N[C@H](C(=O)O)c1cc(O)no1	10.1021/jm00009a001
	6603885	101731	17	None	-	0	Rat	4.4	pEC50	=	4.4	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat	ChEMBL	158	2	3	5	-0.5	N[C@H](C(=O)O)c1cc(O)no1	10.1021/jm00009a001
	6971208	101731	17	None	-	0	Rat	4.4	pEC50	=	4.4	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat	ChEMBL	158	2	3	5	-0.5	N[C@H](C(=O)O)c1cc(O)no1	10.1021/jm00009a001
	CHEMBL30285	101731	17	None	-	0	Rat	4.4	pEC50	=	4.4	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat	ChEMBL	158	2	3	5	-0.5	N[C@H](C(=O)O)c1cc(O)no1	10.1021/jm00009a001
	1310	2286	108	None	-1	18	Human	5.3	pEC50	=	5.3	Binding	Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm970719q
	1369	2286	108	None	-1	18	Human	5.3	pEC50	=	5.3	Binding	Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm970719q
	33032	2286	108	None	-1	18	Human	5.3	pEC50	=	5.3	Binding	Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm970719q
	44272391	2286	108	None	-1	18	Human	5.3	pEC50	=	5.3	Binding	Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm970719q
	88747398	2286	108	None	-1	18	Human	5.3	pEC50	=	5.3	Binding	Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm970719q
	CHEMBL575060	2286	108	None	-1	18	Human	5.3	pEC50	=	5.3	Binding	Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm970719q
	DB00142	2286	108	None	-1	18	Human	5.3	pEC50	=	5.3	Binding	Compound was tested for the inhibition of Metabotropic glutamate receptor 1Compound was tested for the inhibition of Metabotropic glutamate receptor 1	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm970719q
	104766	34	36	None	3	11	Rat	4.3	pEC50	=	4.3	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm00009a001
	1365	34	36	None	3	11	Rat	4.3	pEC50	=	4.3	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm00009a001
	CHEMBL34453	34	36	None	3	11	Rat	4.3	pEC50	=	4.3	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	10.1021/jm00009a001
	52947627	17609	0	None	-	0	Human	6.3	pEC50	=	6.3	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	429	6	2	6	2.6	CN(C)Cc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	CHEMBL1258795	17609	0	None	-	0	Human	6.3	pEC50	=	6.3	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	429	6	2	6	2.6	CN(C)Cc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	1310	2286	108	None	-4	18	Rat	4.3	pEC50	=	4.3	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	1369	2286	108	None	-4	18	Rat	4.3	pEC50	=	4.3	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	33032	2286	108	None	-4	18	Rat	4.3	pEC50	=	4.3	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	44272391	2286	108	None	-4	18	Rat	4.3	pEC50	=	4.3	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	88747398	2286	108	None	-4	18	Rat	4.3	pEC50	=	4.3	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	CHEMBL575060	2286	108	None	-4	18	Rat	4.3	pEC50	=	4.3	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	DB00142	2286	108	None	-4	18	Rat	4.3	pEC50	=	4.3	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1b in ratConcentration for half maximal activation of metabotropic glutamate mGluR1b in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	6603885	101731	17	None	-	0	Rat	5.2	pEC50	=	5.2	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	158	2	3	5	-0.5	N[C@H](C(=O)O)c1cc(O)no1	10.1021/jm00009a001
	6971208	101731	17	None	-	0	Rat	5.2	pEC50	=	5.2	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	158	2	3	5	-0.5	N[C@H](C(=O)O)c1cc(O)no1	10.1021/jm00009a001
	CHEMBL30285	101731	17	None	-	0	Rat	5.2	pEC50	=	5.2	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	158	2	3	5	-0.5	N[C@H](C(=O)O)c1cc(O)no1	10.1021/jm00009a001
	6603885	101731	17	None	-	0	Human	5.2	pEC50	=	5.2	Binding	Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)	ChEMBL	158	2	3	5	-0.5	N[C@H](C(=O)O)c1cc(O)no1	10.1021/jm9601718
	6971208	101731	17	None	-	0	Human	5.2	pEC50	=	5.2	Binding	Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)	ChEMBL	158	2	3	5	-0.5	N[C@H](C(=O)O)c1cc(O)no1	10.1021/jm9601718
	CHEMBL30285	101731	17	None	-	0	Human	5.2	pEC50	=	5.2	Binding	Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)	ChEMBL	158	2	3	5	-0.5	N[C@H](C(=O)O)c1cc(O)no1	10.1021/jm9601718
	6603885	101731	17	None	-	0	Rat	4.2	pEC50	=	4.2	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat	ChEMBL	158	2	3	5	-0.5	N[C@H](C(=O)O)c1cc(O)no1	10.1021/jm00009a001
	6971208	101731	17	None	-	0	Rat	4.2	pEC50	=	4.2	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat	ChEMBL	158	2	3	5	-0.5	N[C@H](C(=O)O)c1cc(O)no1	10.1021/jm00009a001
	CHEMBL30285	101731	17	None	-	0	Rat	4.2	pEC50	=	4.2	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat	ChEMBL	158	2	3	5	-0.5	N[C@H](C(=O)O)c1cc(O)no1	10.1021/jm00009a001
	45082292	114752	2	None	3	3	Human	5.2	pEC50	=	5.2	Binding	Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells	ChEMBL	159	3	3	3	-0.7	N[C@@]1(C(=O)O)C[C@@H]1CC(=O)O	10.1039/C1MD00186H
	CHEMBL3347670	114752	2	None	3	3	Human	5.2	pEC50	=	5.2	Binding	Agonist activity at human mGluR1 receptor expressed in HEK cellsAgonist activity at human mGluR1 receptor expressed in HEK cells	ChEMBL	159	3	3	3	-0.7	N[C@@]1(C(=O)O)C[C@@H]1CC(=O)O	10.1039/C1MD00186H
	52949785	17115	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	457	8	2	6	3.4	CCN(CC)Cc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	CHEMBL1257181	17115	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	457	8	2	6	3.4	CCN(CC)Cc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	52946415	17641	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	441	7	3	6	2.8	NC(=O)c1c(NC(=O)Cn2cc(CNC3CC3)c(C(F)(F)F)n2)sc2c1CCCC2	10.1016/j.bmcl.2010.08.063
	CHEMBL1258914	17641	0	None	-	0	Human	6.2	pEC50	=	6.2	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	441	7	3	6	2.8	NC(=O)c1c(NC(=O)Cn2cc(CNC3CC3)c(C(F)(F)F)n2)sc2c1CCCC2	10.1016/j.bmcl.2010.08.063
	1366	2049	39	None	-	0	Human	4.2	pEC50	=	4.2	Binding	Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)	ChEMBL	167	2	3	3	0.5	OC(=O)[C@H](c1cccc(c1)O)N	10.1021/jm9601718
	40428795	2049	39	None	-	0	Human	4.2	pEC50	=	4.2	Binding	Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)	ChEMBL	167	2	3	3	0.5	OC(=O)[C@H](c1cccc(c1)O)N	10.1021/jm9601718
	6604712	2049	39	None	-	0	Human	4.2	pEC50	=	4.2	Binding	Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)	ChEMBL	167	2	3	3	0.5	OC(=O)[C@H](c1cccc(c1)O)N	10.1021/jm9601718
	CHEMBL442347	2049	39	None	-	0	Human	4.2	pEC50	=	4.2	Binding	Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)Effective concentration for half maximal stimulation of PI hydrolysis (mGluR1a)	ChEMBL	167	2	3	3	0.5	OC(=O)[C@H](c1cccc(c1)O)N	10.1021/jm9601718
	1370	3212	62	None	44	8	Rat	6.2	pEC50	=	6.2	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	1372	3212	62	None	44	8	Rat	6.2	pEC50	=	6.2	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	40539	3212	62	None	44	8	Rat	6.2	pEC50	=	6.2	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	6971145	3212	62	None	44	8	Rat	6.2	pEC50	=	6.2	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	CHEMBL279956	3212	62	None	44	8	Rat	6.2	pEC50	=	6.2	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	DB02999	3212	62	None	44	8	Rat	6.2	pEC50	=	6.2	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	1370	3212	62	None	44	8	Rat	6.1	pEC50	=	6.1	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	1372	3212	62	None	44	8	Rat	6.1	pEC50	=	6.1	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	40539	3212	62	None	44	8	Rat	6.1	pEC50	=	6.1	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	6971145	3212	62	None	44	8	Rat	6.1	pEC50	=	6.1	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	CHEMBL279956	3212	62	None	44	8	Rat	6.1	pEC50	=	6.1	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	DB02999	3212	62	None	44	8	Rat	6.1	pEC50	=	6.1	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1c in ratConcentration for half maximal activation of metabotropic glutamate mGluR1c in rat	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm00009a001
	24967783	16302	0	None	-	0	Human	6.1	pEC50	=	6.1	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	429	7	3	6	2.7	CCNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	CHEMBL1234887	16302	0	None	-	0	Human	6.1	pEC50	=	6.1	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	429	7	3	6	2.7	CCNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	52943768	17182	0	None	-	0	Human	6.1	pEC50	=	6.1	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	417	7	3	6	3.0	CCNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(C)(C)C	10.1016/j.bmcl.2010.08.063
	CHEMBL1257415	17182	0	None	-	0	Human	6.1	pEC50	=	6.1	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	417	7	3	6	3.0	CCNCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(C)(C)C	10.1016/j.bmcl.2010.08.063
	52941496	17537	0	None	-	0	Human	6.1	pEC50	=	6.1	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	401	5	3	6	2.0	NCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	CHEMBL1258571	17537	0	None	-	0	Human	6.1	pEC50	=	6.1	Binding	Positive modulation of GluR1Positive modulation of GluR1	ChEMBL	401	5	3	6	2.0	NCc1cn(CC(=O)Nc2sc3c(c2C(N)=O)CCCC3)nc1C(F)(F)F	10.1016/j.bmcl.2010.08.063
	1310	2286	108	None	-4	18	Rat	5.1	pEC50	=	5.1	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	1369	2286	108	None	-4	18	Rat	5.1	pEC50	=	5.1	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	33032	2286	108	None	-4	18	Rat	5.1	pEC50	=	5.1	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	44272391	2286	108	None	-4	18	Rat	5.1	pEC50	=	5.1	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	88747398	2286	108	None	-4	18	Rat	5.1	pEC50	=	5.1	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	CHEMBL575060	2286	108	None	-4	18	Rat	5.1	pEC50	=	5.1	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	DB00142	2286	108	None	-4	18	Rat	5.1	pEC50	=	5.1	Binding	Concentration for half maximal activation of metabotropic glutamate mGluR1a in ratConcentration for half maximal activation of metabotropic glutamate mGluR1a in rat	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm00009a001
	22708855	145841	1	None	-	0	Human	5.0	pEC50	=	5.0	Binding	Compound was tested for inhibitory binding activity towards metabotropic glutamate receptor (mGluRla) expressed in LLC-PK1 cellsCompound was tested for inhibitory binding activity towards metabotropic glutamate receptor (mGluRla) expressed in LLC-PK1 cells	ChEMBL	199	2	3	3	-0.1	NC1(C(=O)O)CC2CCC1C2C(=O)O	10.1016/0960-894X(95)00457-5
	CHEMBL39215	145841	1	None	-	0	Human	5.0	pEC50	=	5.0	Binding	Compound was tested for inhibitory binding activity towards metabotropic glutamate receptor (mGluRla) expressed in LLC-PK1 cellsCompound was tested for inhibitory binding activity towards metabotropic glutamate receptor (mGluRla) expressed in LLC-PK1 cells	ChEMBL	199	2	3	3	-0.1	NC1(C(=O)O)CC2CCC1C2C(=O)O	10.1016/0960-894X(95)00457-5
	11313361	2103	54	None	-	1	Human	9.3	pIC50	=	9.3	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm049499o
	1385	2103	54	None	-	1	Human	9.3	pIC50	=	9.3	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm049499o
	CHEMBL174588	2103	54	None	-	1	Human	9.3	pIC50	=	9.3	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm049499o
	CHEMBL254574	2103	54	None	-	1	Human	9.3	pIC50	=	9.3	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm049499o
	11483690	62677	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	309	3	0	3	4.1	CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCC4)CC1	10.1021/jm049499o
	CHEMBL178690	62677	0	None	-	0	Human	9.3	pIC50	=	9.3	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	309	3	0	3	4.1	CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCC4)CC1	10.1021/jm049499o
	11537456	207	9	None	-	1	Rat	9.0	pIC50	=	9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	342	2	0	6	4.0	CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C	10.1016/j.ejmech.2007.06.024
	6354	207	9	None	-	1	Rat	9.0	pIC50	=	9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	342	2	0	6	4.0	CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C	10.1016/j.ejmech.2007.06.024
	CHEMBL225032	207	9	None	-	1	Rat	9.0	pIC50	=	9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	342	2	0	6	4.0	CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C	10.1016/j.ejmech.2007.06.024
	11461116	78518	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	312	4	1	4	3.8	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1N	10.1021/jm049499o
	CHEMBL2112967	78518	0	None	-	0	Human	9.0	pIC50	=	9	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	312	4	1	4	3.8	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1N	10.1021/jm049499o
	11301185	1653	24	None	-	1	Mouse	8.9	pIC50	=	8.9	Binding	Binding affinity to mouse mGluR1Binding affinity to mouse mGluR1	ChEMBL	305	2	0	5	3.3	Cc1c(nnn1c1cccnc1F)c1ccc2c(c1)cccn2	10.1016/j.bmc.2010.11.048
	6353	1653	24	None	-	1	Mouse	8.9	pIC50	=	8.9	Binding	Binding affinity to mouse mGluR1Binding affinity to mouse mGluR1	ChEMBL	305	2	0	5	3.3	Cc1c(nnn1c1cccnc1F)c1ccc2c(c1)cccn2	10.1016/j.bmc.2010.11.048
	CHEMBL1645352	1653	24	None	-	1	Mouse	8.9	pIC50	=	8.9	Binding	Binding affinity to mouse mGluR1Binding affinity to mouse mGluR1	ChEMBL	305	2	0	5	3.3	Cc1c(nnn1c1cccnc1F)c1ccc2c(c1)cccn2	10.1016/j.bmc.2010.11.048
	11559235	209	37	None	-	0	Rat	8.0	pIC50	=	8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	343	2	0	7	2.6	CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C	10.1016/j.ejmech.2007.06.024
	3953	209	37	None	-	0	Rat	8.0	pIC50	=	8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	343	2	0	7	2.6	CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C	10.1016/j.ejmech.2007.06.024
	CHEMBL386565	209	37	None	-	0	Rat	8.0	pIC50	=	8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	343	2	0	7	2.6	CN(c1ccnc2c1c1ncn(c(=O)c1s2)N1CCCCCC1)C	10.1016/j.ejmech.2007.06.024
	10085578	61781	1	None	-	0	Rat	8.0	pIC50	=	8	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	289	4	0	2	4.5	CCc1cc2cc(C(=O)Cc3ccccc3)ccc2nc1C	10.1021/jm049499o
	CHEMBL177586	61781	1	None	-	0	Rat	8.0	pIC50	=	8	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	289	4	0	2	4.5	CCc1cc2cc(C(=O)Cc3ccccc3)ccc2nc1C	10.1021/jm049499o
	44306937	100561	3	None	-	0	Rat	7.0	pIC50	=	7	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	281	2	1	4	3.2	Cc1c(C(=O)OC(C)(C)C)c[nH]c1C(=O)OC(C)(C)C	10.1016/s0960-894x(03)00396-2
	CHEMBL294550	100561	3	None	-	0	Rat	7.0	pIC50	=	7	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	281	2	1	4	3.2	Cc1c(C(=O)OC(C)(C)C)c[nH]c1C(=O)OC(C)(C)C	10.1016/s0960-894x(03)00396-2
	44430067	151370	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells	ChEMBL	305	4	1	4	3.2	CCOC(=O)c1[nH]c(C)c(C(=O)OC2CC3CCC2C3)c1C	10.1016/j.bmcl.2006.11.039
	CHEMBL396594	151370	0	None	-	0	Human	7.0	pIC50	=	7	Binding	Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells	ChEMBL	305	4	1	4	3.2	CCOC(=O)c1[nH]c(C)c(C(=O)OC2CC3CCC2C3)c1C	10.1016/j.bmcl.2006.11.039
	11654379	141539	0	None	-	0	Rat	7.0	pIC50	=	7	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	406	6	0	6	5.0	CCCCc1nc2c(sc3nccc(N(C)C)c32)c(=O)n1-c1ccc(CC)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL387976	141539	0	None	-	0	Rat	7.0	pIC50	=	7	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	406	6	0	6	5.0	CCCCc1nc2c(sc3nccc(N(C)C)c32)c(=O)n1-c1ccc(CC)cc1	10.1016/j.ejmech.2007.06.024
	44306721	201884	0	None	-	0	Rat	6.0	pIC50	=	6	Binding	In vitro inhibitory concentration required against rat mGluR1a in CHO cells using the CDP-DAG accumulation methodIn vitro inhibitory concentration required against rat mGluR1a in CHO cells using the CDP-DAG accumulation method	ChEMBL	295	4	0	5	3.2	CCCOC(=O)c1c(C)c(C(=O)OC(C)(C)C)c(C)n1C	10.1016/s0960-894x(03)00396-2
	CHEMBL66794	201884	0	None	-	0	Rat	6.0	pIC50	=	6	Binding	In vitro inhibitory concentration required against rat mGluR1a in CHO cells using the CDP-DAG accumulation methodIn vitro inhibitory concentration required against rat mGluR1a in CHO cells using the CDP-DAG accumulation method	ChEMBL	295	4	0	5	3.2	CCCOC(=O)c1c(C)c(C(=O)OC(C)(C)C)c(C)n1C	10.1016/s0960-894x(03)00396-2
	44430068	87499	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells	ChEMBL	389	8	3	4	2.6	CC(=O)NCCCCNC(=O)c1[nH]c(C)c(C(=O)OC2CC3CCC2C3)c1C	10.1016/j.bmcl.2006.11.039
	CHEMBL233914	87499	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells	ChEMBL	389	8	3	4	2.6	CC(=O)NCCCCNC(=O)c1[nH]c(C)c(C(=O)OC2CC3CCC2C3)c1C	10.1016/j.bmcl.2006.11.039
	10018131	57180	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.	ChEMBL	308	2	1	4	2.7	CN(C(=O)C12CC1/C(=N\O)c1ccccc1O2)c1ccccc1	10.1016/0960-894X(96)00104-7
	CHEMBL165828	57180	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.	ChEMBL	308	2	1	4	2.7	CN(C(=O)C12CC1/C(=N\O)c1ccccc1O2)c1ccccc1	10.1016/0960-894X(96)00104-7
	11654379	141539	0	None	-	0	Rat	7.0	pIC50	=	7	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	406	6	0	6	5.0	CCCCc1nc2c(sc3nccc(N(C)C)c32)c(=O)n1-c1ccc(CC)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL387976	141539	0	None	-	0	Rat	7.0	pIC50	=	7	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	406	6	0	6	5.0	CCCCc1nc2c(sc3nccc(N(C)C)c32)c(=O)n1-c1ccc(CC)cc1	10.1016/j.ejmech.2007.06.024
	11485531	128954	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	370	8	1	5	4.2	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1NCCOC	10.1021/jm049499o
	CHEMBL367227	128954	0	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	370	8	1	5	4.2	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1NCCOC	10.1021/jm049499o
	11313361	2103	54	None	-	1	Human	7.0	pIC50	=	7.0	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm049499o
	1385	2103	54	None	-	1	Human	7.0	pIC50	=	7.0	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm049499o
	CHEMBL174588	2103	54	None	-	1	Human	7.0	pIC50	=	7.0	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm049499o
	CHEMBL254574	2103	54	None	-	1	Human	7.0	pIC50	=	7.0	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm049499o
	11347844	78514	1	None	-	0	Rat	8.0	pIC50	=	8.0	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	322	4	0	4	4.1	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C#N	10.1021/jm049499o
	CHEMBL2112963	78514	1	None	-	0	Rat	8.0	pIC50	=	8.0	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	322	4	0	4	4.1	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C#N	10.1021/jm049499o
	11682046	84730	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	362	3	0	6	3.8	CCc1ccc(-n2cnc3c(sc4nccc(N5CCC5)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL225126	84730	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	362	3	0	6	3.8	CCc1ccc(-n2cnc3c(sc4nccc(N5CCC5)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11682046	84730	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	362	3	0	6	3.8	CCc1ccc(-n2cnc3c(sc4nccc(N5CCC5)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL225126	84730	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	362	3	0	6	3.8	CCc1ccc(-n2cnc3c(sc4nccc(N5CCC5)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11461691	61976	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	331	3	0	3	4.5	CCc1cc2cc(C(=O)C3COc4ccccc4C3)ccc2nc1C	10.1021/jm049499o
	CHEMBL177866	61976	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	331	3	0	3	4.5	CCc1cc2cc(C(=O)C3COc4ccccc4C3)ccc2nc1C	10.1021/jm049499o
	44387723	127298	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	315	3	0	2	4.7	CCc1cc2cc(C(=O)C3Cc4ccccc4C3)ccc2nc1C	10.1021/jm049499o
	CHEMBL366448	127298	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	315	3	0	2	4.7	CCc1cc2cc(C(=O)C3Cc4ccccc4C3)ccc2nc1C	10.1021/jm049499o
	44307323	201309	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	305	4	1	5	3.2	Cc1c(C(=O)OC(C)(C)C)c[nH]c1C(=O)OCc1ccco1	10.1016/s0960-894x(03)00396-2
	CHEMBL63161	201309	0	None	-	0	Rat	5.9	pIC50	=	5.9	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	305	4	1	5	3.2	Cc1c(C(=O)OC(C)(C)C)c[nH]c1C(=O)OCc1ccco1	10.1016/s0960-894x(03)00396-2
	2733519	106430	27	None	-	0	Rat	4.9	pIC50	=	4.9	Binding	Compound was tested in vitro for binding affinity against mGluR1a metabotropic glutamate receptor, using [3H]glutamate as the radioligand.Compound was tested in vitro for binding affinity against mGluR1a metabotropic glutamate receptor, using [3H]glutamate as the radioligand.	ChEMBL	159	3	3	3	-0.9	O=C(O)C[C@H]1CN[C@@H]1C(=O)O	10.1016/0960-894X(96)00464-7
	CHEMBL314690	106430	27	None	-	0	Rat	4.9	pIC50	=	4.9	Binding	Compound was tested in vitro for binding affinity against mGluR1a metabotropic glutamate receptor, using [3H]glutamate as the radioligand.Compound was tested in vitro for binding affinity against mGluR1a metabotropic glutamate receptor, using [3H]glutamate as the radioligand.	ChEMBL	159	3	3	3	-0.9	O=C(O)C[C@H]1CN[C@@H]1C(=O)O	10.1016/0960-894X(96)00464-7
	44562546	173895	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	361	2	1	6	3.5	CN(C)c1ccnc2sc3c(=O)n(-c4ccc5cc[nH]c5c4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL455415	173895	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	361	2	1	6	3.5	CN(C)c1ccnc2sc3c(=O)n(-c4ccc5cc[nH]c5c4)cnc3c12	10.1016/j.ejmech.2007.06.024
	44562546	173895	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	361	2	1	6	3.5	CN(C)c1ccnc2sc3c(=O)n(-c4ccc5cc[nH]c5c4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL455415	173895	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	361	2	1	6	3.5	CN(C)c1ccnc2sc3c(=O)n(-c4ccc5cc[nH]c5c4)cnc3c12	10.1016/j.ejmech.2007.06.024
	11220954	78125	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	321	2	0	2	5.5	C[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCCC4)CC1	10.1021/jm049499o
	CHEMBL2112048	78125	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	321	2	0	2	5.5	C[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCCC4)CC1	10.1021/jm049499o
	11174991	63181	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	333	3	0	2	5.5	CCc1cc2cc(C(=O)C34CC5CC(CC(C5)C3)C4)ccc2nc1C	10.1021/jm049499o
	CHEMBL180011	63181	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	333	3	0	2	5.5	CCc1cc2cc(C(=O)C34CC5CC(CC(C5)C3)C4)ccc2nc1C	10.1021/jm049499o
	44307362	201919	0	None	-	0	Rat	4.9	pIC50	=	4.9	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	379	8	0	7	3.4	C=CCOC(=O)Cn1c(C)c(C(=O)OC(C)(C)C)c(C)c1C(=O)OCCC	10.1016/s0960-894x(03)00396-2
	CHEMBL67071	201919	0	None	-	0	Rat	4.9	pIC50	=	4.9	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	379	8	0	7	3.4	C=CCOC(=O)Cn1c(C)c(C(=O)OC(C)(C)C)c(C)c1C(=O)OCCC	10.1016/s0960-894x(03)00396-2
	11515957	84385	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	356	2	0	6	4.4	CN(C)c1ccnc2sc3c(=O)n(C4CCCCCCC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL223399	84385	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	356	2	0	6	4.4	CN(C)c1ccnc2sc3c(=O)n(C4CCCCCCC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	44387711	59964	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	293	3	0	2	4.7	CCc1cc2cc(C(=O)C3CC4CCC3C4)ccc2nc1C	10.1021/jm049499o
	CHEMBL174218	59964	0	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	293	3	0	2	4.7	CCc1cc2cc(C(=O)C3CC4CCC3C4)ccc2nc1C	10.1021/jm049499o
	11177701	61138	1	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	423	4	0	3	4.8	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1I	10.1021/jm049499o
	CHEMBL177043	61138	1	None	-	0	Rat	7.9	pIC50	=	7.9	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	423	4	0	3	4.8	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1I	10.1021/jm049499o
	16660135	1612	30	None	-	1	Rat	7.9	pIC50	=	7.9	Binding	Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr	ChEMBL	371	5	1	6	3.8	CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C	10.1021/jm201590g
	8767	1612	30	None	-	1	Rat	7.9	pIC50	=	7.9	Binding	Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr	ChEMBL	371	5	1	6	3.8	CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C	10.1021/jm201590g
	CHEMBL566581	1612	30	None	-	1	Rat	7.9	pIC50	=	7.9	Binding	Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr	ChEMBL	371	5	1	6	3.8	CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C	10.1021/jm201590g
	11515679	84678	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	342	2	0	6	3.8	CC1CCCCC1n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1016/j.ejmech.2007.06.024
	CHEMBL224672	84678	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	342	2	0	6	3.8	CC1CCCCC1n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1016/j.ejmech.2007.06.024
	11515679	84678	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	342	2	0	6	3.8	CC1CCCCC1n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1016/j.ejmech.2007.06.024
	CHEMBL224672	84678	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	342	2	0	6	3.8	CC1CCCCC1n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1016/j.ejmech.2007.06.024
	11681681	84584	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	342	3	0	6	3.7	CN(C)c1ccnc2sc3c(=O)n(CC4CCCCC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL223868	84584	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	342	3	0	6	3.7	CN(C)c1ccnc2sc3c(=O)n(CC4CCCCC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	11493897	84639	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	342	2	0	6	3.8	CC1CCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)CC1	10.1016/j.ejmech.2007.06.024
	CHEMBL224315	84639	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	342	2	0	6	3.8	CC1CCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)CC1	10.1016/j.ejmech.2007.06.024
	10470232	3218	18	None	1	2	Human	7.9	pIC50	=	7.9	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	10.1021/jm049499o
	1391	3218	18	None	1	2	Human	7.9	pIC50	=	7.9	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	10.1021/jm049499o
	6336	3218	18	None	1	2	Human	7.9	pIC50	=	7.9	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	10.1021/jm049499o
	CHEMBL369459	3218	18	None	1	2	Human	7.9	pIC50	=	7.9	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	10.1021/jm049499o
	11493897	84639	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	342	2	0	6	3.8	CC1CCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)CC1	10.1016/j.ejmech.2007.06.024
	CHEMBL224315	84639	0	None	-	0	Rat	6.9	pIC50	=	6.9	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	342	2	0	6	3.8	CC1CCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)CC1	10.1016/j.ejmech.2007.06.024
	11256015	62658	4	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	331	4	0	3	4.8	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1Cl	10.1021/jm049499o
	CHEMBL178592	62658	4	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	331	4	0	3	4.8	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1Cl	10.1021/jm049499o
	44307128	202037	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	331	4	1	6	2.9	Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)Oc1ccncn1	10.1016/s0960-894x(03)00396-2
	CHEMBL67769	202037	0	None	-	0	Rat	5.8	pIC50	=	5.8	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	331	4	1	6	2.9	Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)Oc1ccncn1	10.1016/s0960-894x(03)00396-2
	11186076	168769	1	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	313	4	1	4	3.9	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1O	10.1021/jm049499o
	CHEMBL441844	168769	1	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	313	4	1	4	3.9	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1O	10.1021/jm049499o
	44430066	87309	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells	ChEMBL	320	6	2	4	2.0	COCCNC(=O)c1[nH]cc(C(=O)OC2CC3CCC2C3)c1C	10.1016/j.bmcl.2006.11.039
	CHEMBL233710	87309	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells	ChEMBL	320	6	2	4	2.0	COCCNC(=O)c1[nH]cc(C(=O)OC2CC3CCC2C3)c1C	10.1016/j.bmcl.2006.11.039
	11722867	95	2	None	-	0	Rat	4.8	pIC50	=	4.8	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	309	5	1	4	3.8	CCCOC(=O)c1[nH]c(c(c1C)C(=O)OC(C(C)(C)C)C)C	10.1016/s0960-894x(03)00396-2
	3397	95	2	None	-	0	Rat	4.8	pIC50	=	4.8	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	309	5	1	4	3.8	CCCOC(=O)c1[nH]c(c(c1C)C(=O)OC(C(C)(C)C)C)C	10.1016/s0960-894x(03)00396-2
	CHEMBL304824	95	2	None	-	0	Rat	4.8	pIC50	=	4.8	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	309	5	1	4	3.8	CCCOC(=O)c1[nH]c(c(c1C)C(=O)OC(C(C)(C)C)C)C	10.1016/s0960-894x(03)00396-2
	1069776	84798	11	None	257	2	Rat	7.8	pIC50	=	7.8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	356	2	0	6	3.7	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL225589	84798	11	None	257	2	Rat	7.8	pIC50	=	7.8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	356	2	0	6	3.7	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	11220954	78125	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	321	2	0	2	5.5	C[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCCC4)CC1	10.1021/jm049499o
	CHEMBL2112048	78125	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	321	2	0	2	5.5	C[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCCC4)CC1	10.1021/jm049499o
	11324832	60192	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	325	5	0	3	4.9	CCc1cc2cc(C(=O)C[C@H]3CC[C@@H](OC)CC3)ccc2nc1C	10.1021/jm049499o
	CHEMBL175699	60192	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	325	5	0	3	4.9	CCc1cc2cc(C(=O)C[C@H]3CC[C@@H](OC)CC3)ccc2nc1C	10.1021/jm049499o
	11688880	84641	0	None	616	2	Rat	7.8	pIC50	=	7.8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	350	2	0	6	3.7	Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c(C)c1	10.1016/j.ejmech.2007.06.024
	CHEMBL224356	84641	0	None	616	2	Rat	7.8	pIC50	=	7.8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	350	2	0	6	3.7	Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c(C)c1	10.1016/j.ejmech.2007.06.024
	44307138	96357	1	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	419	4	1	4	4.8	Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)Oc1c(F)c(F)c(F)c(F)c1F	10.1016/s0960-894x(03)00396-2
	CHEMBL265023	96357	1	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	419	4	1	4	4.8	Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)Oc1c(F)c(F)c(F)c(F)c1F	10.1016/s0960-894x(03)00396-2
	44307429	201875	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	329	5	1	4	4.1	CCCOC(=O)c1[nH]c(Cl)c(C(=O)OC(C)C(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	CHEMBL66728	201875	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	329	5	1	4	4.1	CCCOC(=O)c1[nH]c(Cl)c(C(=O)OC(C)C(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	11347669	119895	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	317	4	0	3	4.4	O=C(CCc1ccccc1)c1ccc2nc3c(cc2c1)CCCO3	10.1021/jm049499o
	CHEMBL353547	119895	0	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	317	4	0	3	4.4	O=C(CCc1ccccc1)c1ccc2nc3c(cc2c1)CCCO3	10.1021/jm049499o
	11184404	60181	1	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	255	4	0	2	4.3	CCc1cc2cc(C(=O)CC(C)C)ccc2nc1C	10.1021/jm049499o
	CHEMBL175610	60181	1	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	255	4	0	2	4.3	CCc1cc2cc(C(=O)CC(C)C)ccc2nc1C	10.1021/jm049499o
	11666576	141196	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	300	2	0	6	2.8	CN(C)c1ccnc2sc3c(=O)n(C4CCC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL385776	141196	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	300	2	0	6	2.8	CN(C)c1ccnc2sc3c(=O)n(C4CCC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	44562406	176352	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	358	2	0	6	4.0	C[N+](C)([O-])c1ccnc2sc3c(=O)n(C4CCCCCC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL462007	176352	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	358	2	0	6	4.0	C[N+](C)([O-])c1ccnc2sc3c(=O)n(C4CCCCCC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	11666576	141196	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	300	2	0	6	2.8	CN(C)c1ccnc2sc3c(=O)n(C4CCC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL385776	141196	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	300	2	0	6	2.8	CN(C)c1ccnc2sc3c(=O)n(C4CCC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	44562406	176352	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	358	2	0	6	4.0	C[N+](C)([O-])c1ccnc2sc3c(=O)n(C4CCCCCC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL462007	176352	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	358	2	0	6	4.0	C[N+](C)([O-])c1ccnc2sc3c(=O)n(C4CCCCCC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	44307214	102246	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	309	3	1	4	3.9	Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)OC(C)(C)C	10.1016/s0960-894x(03)00396-2
	CHEMBL304866	102246	0	None	-	0	Rat	7.8	pIC50	=	7.8	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	309	3	1	4	3.9	Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)OC(C)(C)C	10.1016/s0960-894x(03)00396-2
	11688880	84641	0	None	616	2	Rat	7.8	pIC50	=	7.8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	350	2	0	6	3.7	Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c(C)c1	10.1016/j.ejmech.2007.06.024
	CHEMBL224356	84641	0	None	616	2	Rat	7.8	pIC50	=	7.8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	350	2	0	6	3.7	Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c(C)c1	10.1016/j.ejmech.2007.06.024
	11347844	78514	1	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	322	4	0	4	4.1	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C#N	10.1021/jm049499o
	CHEMBL2112963	78514	1	None	-	0	Human	6.8	pIC50	=	6.8	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	322	4	0	4	4.1	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C#N	10.1021/jm049499o
	11530673	165560	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	364	4	0	6	4.0	CCCc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL426018	165560	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	364	4	0	6	4.0	CCCc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11209923	62683	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	337	3	0	3	4.9	CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCCC4)CC1	10.1021/jm049499o
	CHEMBL178741	62683	0	None	-	0	Human	7.8	pIC50	=	7.8	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	337	3	0	3	4.9	CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCCC4)CC1	10.1021/jm049499o
	11530673	165560	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	364	4	0	6	4.0	CCCc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL426018	165560	0	None	-	0	Rat	6.8	pIC50	=	6.8	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	364	4	0	6	4.0	CCCc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	10245890	1951	7	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	327	5	0	4	4.2	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC	10.1021/jm049499o
	6474	1951	7	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	327	5	0	4	4.2	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC	10.1021/jm049499o
	CHEMBL175643	1951	7	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	327	5	0	4	4.2	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC	10.1021/jm049499o
	44430064	151368	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells	ChEMBL	291	4	1	4	2.8	CCOC(=O)c1[nH]cc(C(=O)OC2CC3CCC2C3)c1C	10.1016/j.bmcl.2006.11.039
	CHEMBL396593	151368	0	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells	ChEMBL	291	4	1	4	2.8	CCOC(=O)c1[nH]cc(C(=O)OC2CC3CCC2C3)c1C	10.1016/j.bmcl.2006.11.039
	11474450	78516	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	379	5	0	4	5.9	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1-c1ccsc1	10.1021/jm049499o
	CHEMBL2112965	78516	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	379	5	0	4	5.9	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1-c1ccsc1	10.1021/jm049499o
	44430065	87308	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells	ChEMBL	375	8	3	4	2.3	CC(=O)NCCCCNC(=O)c1[nH]cc(C(=O)OC2CC3CCC2C3)c1C	10.1016/j.bmcl.2006.11.039
	CHEMBL233709	87308	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells	ChEMBL	375	8	3	4	2.3	CC(=O)NCCCCNC(=O)c1[nH]cc(C(=O)OC2CC3CCC2C3)c1C	10.1016/j.bmcl.2006.11.039
	11232687	60155	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	327	3	0	4	4.3	CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCS4)CC1	10.1021/jm049499o
	CHEMBL175463	60155	0	None	-	0	Human	8.7	pIC50	=	8.7	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	327	3	0	4	4.3	CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCS4)CC1	10.1021/jm049499o
	11232687	60155	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	327	3	0	4	4.3	CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCS4)CC1	10.1021/jm049499o
	CHEMBL175463	60155	0	None	-	0	Rat	8.7	pIC50	=	8.7	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	327	3	0	4	4.3	CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCS4)CC1	10.1021/jm049499o
	11530404	208	11	None	38	2	Rat	8.5	pIC50	=	8.5	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1016/j.ejmech.2007.06.024
	6211	208	11	None	38	2	Rat	8.5	pIC50	=	8.5	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1016/j.ejmech.2007.06.024
	CHEMBL385336	208	11	None	38	2	Rat	8.5	pIC50	=	8.5	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1016/j.ejmech.2007.06.024
	699222	84668	11	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	322	2	0	6	3.1	CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL224615	84668	11	None	-	0	Rat	7.7	pIC50	=	7.7	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	322	2	0	6	3.1	CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	10245890	1951	7	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domainInhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domain	ChEMBL	327	5	0	4	4.2	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC	10.1021/jm049499o
	6474	1951	7	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domainInhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domain	ChEMBL	327	5	0	4	4.2	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC	10.1021/jm049499o
	CHEMBL175643	1951	7	None	-	0	Human	7.7	pIC50	=	7.7	Binding	Inhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domainInhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domain	ChEMBL	327	5	0	4	4.2	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC	10.1021/jm049499o
	44306971	201921	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	295	5	1	5	2.7	CCCOC(=O)c1[nH]c(C=O)c(C(=O)OC(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	CHEMBL67075	201921	0	None	-	0	Rat	5.7	pIC50	=	5.7	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	295	5	1	5	2.7	CCCOC(=O)c1[nH]c(C=O)c(C(=O)OC(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	1376	318	50	None	-	2	Human	3.7	pIC50	=	3.7	Binding	Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)	ChEMBL	221	2	3	3	0.6	OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O	10.1021/jm9601718
	2071	318	50	None	-	2	Human	3.7	pIC50	=	3.7	Binding	Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)	ChEMBL	221	2	3	3	0.6	OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O	10.1021/jm9601718
	CHEMBL313938	318	50	None	-	2	Human	3.7	pIC50	=	3.7	Binding	Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)	ChEMBL	221	2	3	3	0.6	OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O	10.1021/jm9601718
	11667270	84728	0	None	-	1	Rat	7.6	pIC50	=	7.6	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	340	2	0	6	3.2	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL225124	84728	0	None	-	1	Rat	7.6	pIC50	=	7.6	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	340	2	0	6	3.2	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	11667270	84728	0	None	-	1	Rat	7.6	pIC50	=	7.6	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	340	2	0	6	3.2	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL225124	84728	0	None	-	1	Rat	7.6	pIC50	=	7.6	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	340	2	0	6	3.2	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	11483517	59986	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	303	5	0	2	4.9	CCc1cc2cc(C(=O)CCc3ccccc3)ccc2nc1C	10.1021/jm049499o
	CHEMBL174382	59986	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	303	5	0	2	4.9	CCc1cc2cc(C(=O)CCc3ccccc3)ccc2nc1C	10.1021/jm049499o
	44306730	202093	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	In vitro inhibitory concentration required against rat mGluR1a in CHO cells using the CDP-DAG accumulation methodIn vitro inhibitory concentration required against rat mGluR1a in CHO cells using the CDP-DAG accumulation method	ChEMBL	381	4	0	7	4.4	CCCOC(=O)c1c(C)c(C(=O)OC(C)(C)C)c(C)n1C(=O)OC(C)(C)C	10.1016/s0960-894x(03)00396-2
	CHEMBL68250	202093	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	In vitro inhibitory concentration required against rat mGluR1a in CHO cells using the CDP-DAG accumulation methodIn vitro inhibitory concentration required against rat mGluR1a in CHO cells using the CDP-DAG accumulation method	ChEMBL	381	4	0	7	4.4	CCCOC(=O)c1c(C)c(C(=O)OC(C)(C)C)c(C)n1C(=O)OC(C)(C)C	10.1016/s0960-894x(03)00396-2
	1382	1167	29	None	-1	2	Human	4.6	pIC50	=	4.6	Binding	Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.	ChEMBL	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	10.1016/0960-894X(96)00104-7
	6278000	1167	29	None	-1	2	Human	4.6	pIC50	=	4.6	Binding	Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.	ChEMBL	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	10.1016/0960-894X(96)00104-7
	CHEMBL327783	1167	29	None	-1	2	Human	4.6	pIC50	=	4.6	Binding	Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.	ChEMBL	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	10.1016/0960-894X(96)00104-7
	10245890	1951	7	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	327	5	0	4	4.2	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC	10.1021/jm049499o
	6474	1951	7	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	327	5	0	4	4.2	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC	10.1021/jm049499o
	CHEMBL175643	1951	7	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	327	5	0	4	4.2	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC	10.1021/jm049499o
	44307328	103116	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	364	7	2	5	3.0	CCCOC(=O)c1[nH]c(C(=O)NCC2CC2)c(C(=O)OC(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	CHEMBL308641	103116	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	364	7	2	5	3.0	CCCOC(=O)c1[nH]c(C(=O)NCC2CC2)c(C(=O)OC(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	3421	3488	35	None	-	1	Human	4.6	pIC50	=	4.6	Binding	Inhibition of mGluR1a receptorInhibition of mGluR1a receptor	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1021/jm1013693
	5311040	3488	35	None	-	1	Human	4.6	pIC50	=	4.6	Binding	Inhibition of mGluR1a receptorInhibition of mGluR1a receptor	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1021/jm1013693
	CHEMBL43412	3488	35	None	-	1	Human	4.6	pIC50	=	4.6	Binding	Inhibition of mGluR1a receptorInhibition of mGluR1a receptor	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1021/jm1013693
	3421	3488	35	None	-	1	Rat	4.6	pIC50	=	4.6	Binding	Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells.Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells.	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1021/jm980571q
	5311040	3488	35	None	-	1	Rat	4.6	pIC50	=	4.6	Binding	Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells.Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells.	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1021/jm980571q
	CHEMBL43412	3488	35	None	-	1	Rat	4.6	pIC50	=	4.6	Binding	Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells.Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells.	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1021/jm980571q
	11501188	137018	0	None	-	1	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	350	3	0	6	3.6	CCc1ccccc1-n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1016/j.ejmech.2007.06.024
	CHEMBL375439	137018	0	None	-	1	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	350	3	0	6	3.6	CCc1ccccc1-n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1016/j.ejmech.2007.06.024
	11501188	137018	0	None	-	1	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	350	3	0	6	3.6	CCc1ccccc1-n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1016/j.ejmech.2007.06.024
	CHEMBL375439	137018	0	None	-	1	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	350	3	0	6	3.6	CCc1ccccc1-n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1016/j.ejmech.2007.06.024
	11631279	141379	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	328	3	0	6	3.3	CN(C)c1ccnc2sc3c(=O)n(CC4CCCC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL386935	141379	0	None	-	0	Rat	7.6	pIC50	=	7.6	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	328	3	0	6	3.3	CN(C)c1ccnc2sc3c(=O)n(CC4CCCC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	71459305	82619	0	None	-	1	Rat	7.6	pIC50	=	7.6	Binding	Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting	ChEMBL	367	5	1	6	4.0	Cc1ccc(C(=O)N(C)c2nc(-c3cc(NC(C)C)ncn3)cs2)cc1	10.1021/jm301597s
	CHEMBL2181520	82619	0	None	-	1	Rat	7.6	pIC50	=	7.6	Binding	Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting	ChEMBL	367	5	1	6	4.0	Cc1ccc(C(=O)N(C)c2nc(-c3cc(NC(C)C)ncn3)cs2)cc1	10.1021/jm301597s
	44307139	201933	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	350	5	1	5	3.2	CCN1CCC(OC(=O)c2[nH]cc(C(=O)OC(C)C(C)(C)C)c2C)C1	10.1016/s0960-894x(03)00396-2
	CHEMBL67143	201933	0	None	-	0	Rat	6.6	pIC50	=	6.6	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	350	5	1	5	3.2	CCN1CCC(OC(=O)c2[nH]cc(C(=O)OC(C)C(C)(C)C)c2C)C1	10.1016/s0960-894x(03)00396-2
	11461525	60193	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	325	5	0	3	5.0	C=C(c1ccc2nc(OC)c(CC)cc2c1)[C@H]1CC[C@@H](OC)CC1	10.1021/jm049499o
	CHEMBL175700	60193	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	325	5	0	3	5.0	C=C(c1ccc2nc(OC)c(CC)cc2c1)[C@H]1CC[C@@H](OC)CC1	10.1021/jm049499o
	44307263	201344	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	339	6	1	6	2.9	CCCOC(=O)c1[nH]c(COC(C)=O)c(C(=O)OC(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	CHEMBL63393	201344	0	None	-	0	Rat	5.6	pIC50	=	5.6	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	339	6	1	6	2.9	CCCOC(=O)c1[nH]c(COC(C)=O)c(C(=O)OC(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	657896	141550	10	None	-	1	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	336	3	0	6	3.1	CN(C)c1ccnc2sc3c(=O)n(Cc4ccccc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL388087	141550	10	None	-	1	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	336	3	0	6	3.1	CN(C)c1ccnc2sc3c(=O)n(Cc4ccccc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	657896	141550	10	None	-	1	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	336	3	0	6	3.1	CN(C)c1ccnc2sc3c(=O)n(Cc4ccccc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL388087	141550	10	None	-	1	Rat	6.6	pIC50	=	6.6	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	336	3	0	6	3.1	CN(C)c1ccnc2sc3c(=O)n(Cc4ccccc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	11450605	59963	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	338	3	0	4	4.0	CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCN4C)CC1	10.1021/jm049499o
	CHEMBL174216	59963	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	338	3	0	4	4.0	CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCN4C)CC1	10.1021/jm049499o
	11530404	208	11	None	38	2	Rat	8.5	pIC50	=	8.5	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1016/j.ejmech.2007.06.024
	6211	208	11	None	38	2	Rat	8.5	pIC50	=	8.5	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1016/j.ejmech.2007.06.024
	CHEMBL385336	208	11	None	38	2	Rat	8.5	pIC50	=	8.5	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1016/j.ejmech.2007.06.024
	11255377	60701	1	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	311	5	0	3	4.6	CCCc1ccc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2n1	10.1021/jm049499o
	CHEMBL176279	60701	1	None	-	0	Human	8.5	pIC50	=	8.5	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	311	5	0	3	4.6	CCCc1ccc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2n1	10.1021/jm049499o
	11313361	2103	54	None	-	1	Rat	8.5	pIC50	=	8.5	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm049499o
	1385	2103	54	None	-	1	Rat	8.5	pIC50	=	8.5	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm049499o
	CHEMBL174588	2103	54	None	-	1	Rat	8.5	pIC50	=	8.5	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm049499o
	CHEMBL254574	2103	54	None	-	1	Rat	8.5	pIC50	=	8.5	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm049499o
	44387697	60145	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	325	5	0	3	4.7	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1CC	10.1021/jm049499o
	CHEMBL175377	60145	0	None	-	0	Rat	8.5	pIC50	=	8.5	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	325	5	0	3	4.7	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1CC	10.1021/jm049499o
	11301185	1653	24	None	-	1	Human	8.4	pIC50	=	8.4	Binding	Binding affinity to human mGluR1Binding affinity to human mGluR1	ChEMBL	305	2	0	5	3.3	Cc1c(nnn1c1cccnc1F)c1ccc2c(c1)cccn2	10.1016/j.bmc.2010.11.048
	6353	1653	24	None	-	1	Human	8.4	pIC50	=	8.4	Binding	Binding affinity to human mGluR1Binding affinity to human mGluR1	ChEMBL	305	2	0	5	3.3	Cc1c(nnn1c1cccnc1F)c1ccc2c(c1)cccn2	10.1016/j.bmc.2010.11.048
	CHEMBL1645352	1653	24	None	-	1	Human	8.4	pIC50	=	8.4	Binding	Binding affinity to human mGluR1Binding affinity to human mGluR1	ChEMBL	305	2	0	5	3.3	Cc1c(nnn1c1cccnc1F)c1ccc2c(c1)cccn2	10.1016/j.bmc.2010.11.048
	44430062	88054	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells	ChEMBL	295	5	1	4	3.5	CCCOC(=O)c1[nH]cc(C(=O)O[C@@H](C)C(C)(C)C)c1C	10.1016/j.bmcl.2006.11.039
	CHEMBL234972	88054	0	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells	ChEMBL	295	5	1	4	3.5	CCCOC(=O)c1[nH]cc(C(=O)O[C@@H](C)C(C)(C)C)c1C	10.1016/j.bmcl.2006.11.039
	11574901	84800	0	None	-	1	Rat	8.4	pIC50	=	8.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	400	2	0	6	3.8	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL225590	84800	0	None	-	1	Rat	8.4	pIC50	=	8.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	400	2	0	6	3.8	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	1416	3044	37	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.	ChEMBL	294	2	2	4	2.7	O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccc1	10.1016/0960-894X(96)00104-7
	5866327	3044	37	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.	ChEMBL	294	2	2	4	2.7	O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccc1	10.1016/0960-894X(96)00104-7
	CHEMBL164770	3044	37	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.Compound was tested for inhibition of glutamate-evoked (10 uM) [Ca2+] mobilization in mGluR1-alpha expressed-CHO cells.	ChEMBL	294	2	2	4	2.7	O/N=C\1/c2ccccc2OC2(C1C2)C(=O)Nc1ccccc1	10.1016/0960-894X(96)00104-7
	44307322	201358	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	318	3	1	5	3.6	Cc1c(C(=O)OC(C)(C)C)c[nH]c1C(=O)Sc1ccccn1	10.1016/s0960-894x(03)00396-2
	CHEMBL63539	201358	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	318	3	1	5	3.6	Cc1c(C(=O)OC(C)(C)C)c[nH]c1C(=O)Sc1ccccn1	10.1016/s0960-894x(03)00396-2
	11639210	143617	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	366	3	0	6	3.6	CCc1ccc(-n2cnc3c(sc4nccc([N+](C)(C)[O-])c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL390391	143617	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	366	3	0	6	3.6	CCc1ccc(-n2cnc3c(sc4nccc([N+](C)(C)[O-])c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11639210	143617	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	366	3	0	6	3.6	CCc1ccc(-n2cnc3c(sc4nccc([N+](C)(C)[O-])c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL390391	143617	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	366	3	0	6	3.6	CCc1ccc(-n2cnc3c(sc4nccc([N+](C)(C)[O-])c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	44430063	87307	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells	ChEMBL	310	6	2	4	2.3	COCCNC(=O)c1[nH]cc(C(=O)O[C@@H](C)C(C)(C)C)c1C	10.1016/j.bmcl.2006.11.039
	CHEMBL233708	87307	0	None	-	0	Human	7.5	pIC50	=	7.5	Binding	Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells	ChEMBL	310	6	2	4	2.3	COCCNC(=O)c1[nH]cc(C(=O)O[C@@H](C)C(C)(C)C)c1C	10.1016/j.bmcl.2006.11.039
	11560185	84643	0	None	-	1	Rat	7.5	pIC50	=	7.5	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	390	2	0	6	4.1	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL224375	84643	0	None	-	1	Rat	7.5	pIC50	=	7.5	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	390	2	0	6	4.1	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	44430069	166471	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells	ChEMBL	334	6	2	4	2.4	COCCNC(=O)c1[nH]c(C)c(C(=O)OC2CC3CCC2C3)c1C	10.1016/j.bmcl.2006.11.039
	CHEMBL428850	166471	0	None	-	0	Human	6.5	pIC50	=	6.5	Binding	Inhibition of recombinant mGluR1a receptor expressed in CHO cellsInhibition of recombinant mGluR1a receptor expressed in CHO cells	ChEMBL	334	6	2	4	2.4	COCCNC(=O)c1[nH]c(C)c(C(=O)OC2CC3CCC2C3)c1C	10.1016/j.bmcl.2006.11.039
	11560185	84643	0	None	-	1	Rat	7.5	pIC50	=	7.5	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	390	2	0	6	4.1	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL224375	84643	0	None	-	1	Rat	7.5	pIC50	=	7.5	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	390	2	0	6	4.1	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	16660470	76276	0	None	-	1	Rat	7.5	pIC50	=	7.5	Binding	Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr	ChEMBL	383	6	1	7	3.7	COc1ccc(C(=O)N(C)c2nc(-c3cc(NC(C)C)ncn3)cs2)cc1	10.1021/jm201590g
	CHEMBL2063722	76276	0	None	-	1	Rat	7.5	pIC50	=	7.5	Binding	Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr	ChEMBL	383	6	1	7	3.7	COc1ccc(C(=O)N(C)c2nc(-c3cc(NC(C)C)ncn3)cs2)cc1	10.1021/jm201590g
	CHEMBL177736	61803	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	341	5	1	5	3.7	CCc1cc2cc(/C(=N\N)[C@H]3CC[C@@H](OC)CC3)ccc2nc1OC	10.1021/jm049499o
	44307059	101614	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	404	6	1	7	4.2	CCCOC(=O)c1[nH]c(C(=O)Sc2ccccn2)c(C(=O)OC(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	CHEMBL302153	101614	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	404	6	1	7	4.2	CCCOC(=O)c1[nH]c(C(=O)Sc2ccccn2)c(C(=O)OC(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	44307336	201990	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	325	5	1	6	2.6	CCCOC(=O)c1[nH]c(C(=O)OC)c(C(=O)OC(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	CHEMBL67472	201990	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	325	5	1	6	2.6	CCCOC(=O)c1[nH]c(C(=O)OC)c(C(=O)OC(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	3421	3488	35	None	-	1	Human	4.5	pIC50	=	4.5	Binding	Inhibitory activity against mGluR1 receptorInhibitory activity against mGluR1 receptor	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1016/s0960-894x(98)00265-0
	5311040	3488	35	None	-	1	Human	4.5	pIC50	=	4.5	Binding	Inhibitory activity against mGluR1 receptorInhibitory activity against mGluR1 receptor	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1016/s0960-894x(98)00265-0
	CHEMBL43412	3488	35	None	-	1	Human	4.5	pIC50	=	4.5	Binding	Inhibitory activity against mGluR1 receptorInhibitory activity against mGluR1 receptor	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1016/s0960-894x(98)00265-0
	11222713	60481	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	379	5	0	4	5.9	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1-c1cccs1	10.1021/jm049499o
	CHEMBL176174	60481	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	379	5	0	4	5.9	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1-c1cccs1	10.1021/jm049499o
	11594849	84574	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	316	4	0	6	3.4	CCC(CC)n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1016/j.ejmech.2007.06.024
	CHEMBL223819	84574	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	316	4	0	6	3.4	CCC(CC)n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1016/j.ejmech.2007.06.024
	11594849	84574	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	316	4	0	6	3.4	CCC(CC)n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1016/j.ejmech.2007.06.024
	CHEMBL223819	84574	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	316	4	0	6	3.4	CCC(CC)n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1016/j.ejmech.2007.06.024
	72163432	91595	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Negative allosteric modulation of rat mGlu1 receptorNegative allosteric modulation of rat mGlu1 receptor	ChEMBL	351	2	0	3	3.2	O=C(N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	CHEMBL2418364	91595	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Negative allosteric modulation of rat mGlu1 receptorNegative allosteric modulation of rat mGlu1 receptor	ChEMBL	351	2	0	3	3.2	O=C(N1C[C@@H]2CN(c3ccccn3)C[C@@H]2C1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmcl.2013.07.029
	44306948	101763	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	253	3	1	4	2.5	CCOC(=O)c1[nH]cc(C(=O)OC(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	CHEMBL303018	101763	0	None	-	0	Rat	6.5	pIC50	=	6.5	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	253	3	1	4	2.5	CCOC(=O)c1[nH]cc(C(=O)OC(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	11383509	78517	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	383	6	0	5	4.8	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C(=O)OC(C)C	10.1021/jm049499o
	CHEMBL2112966	78517	0	None	-	0	Rat	5.5	pIC50	=	5.5	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	383	6	0	5	4.8	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C(=O)OC(C)C	10.1021/jm049499o
	11639176	84423	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	364	4	0	6	4.0	CCc1ccc(-n2cnc3c(sc4nccc(N(C)CC)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL223543	84423	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	364	4	0	6	4.0	CCc1ccc(-n2cnc3c(sc4nccc(N(C)CC)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11639176	84423	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	364	4	0	6	4.0	CCc1ccc(-n2cnc3c(sc4nccc(N(C)CC)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL223543	84423	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	364	4	0	6	4.0	CCc1ccc(-n2cnc3c(sc4nccc(N(C)CC)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11717319	142962	0	None	-	1	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	353	3	0	8	2.5	COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cn1	10.1016/j.ejmech.2007.06.024
	CHEMBL389870	142962	0	None	-	1	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	353	3	0	8	2.5	COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cn1	10.1016/j.ejmech.2007.06.024
	11717319	142962	0	None	-	1	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	353	3	0	8	2.5	COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cn1	10.1016/j.ejmech.2007.06.024
	CHEMBL389870	142962	0	None	-	1	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	353	3	0	8	2.5	COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cn1	10.1016/j.ejmech.2007.06.024
	44307245	201944	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	338	6	1	5	3.0	Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)OC(C)CN(C)C	10.1016/s0960-894x(03)00396-2
	CHEMBL67197	201944	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	338	6	1	5	3.0	Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)OC(C)CN(C)C	10.1016/s0960-894x(03)00396-2
	70688666	76277	0	None	-	1	Rat	6.4	pIC50	=	6.4	Binding	Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr	ChEMBL	415	8	1	7	4.0	CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(OCCF)cc3)n2)ncn1	10.1021/jm201590g
	CHEMBL2063723	76277	0	None	-	1	Rat	6.4	pIC50	=	6.4	Binding	Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr	ChEMBL	415	8	1	7	4.0	CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(OCCF)cc3)n2)ncn1	10.1021/jm201590g
	44307069	100414	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	295	5	1	4	3.5	CCCOC(=O)c1[nH]cc(C(=O)OC(C)C(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	CHEMBL293665	100414	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	295	5	1	4	3.5	CCCOC(=O)c1[nH]cc(C(=O)OC(C)C(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	11574901	84800	0	None	-	1	Rat	8.4	pIC50	=	8.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	400	2	0	6	3.8	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL225590	84800	0	None	-	1	Rat	8.4	pIC50	=	8.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	400	2	0	6	3.8	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	11256015	62658	4	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	331	4	0	3	4.8	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1Cl	10.1021/jm049499o
	CHEMBL178592	62658	4	None	-	0	Human	8.4	pIC50	=	8.4	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	331	4	0	3	4.8	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1Cl	10.1021/jm049499o
	11483690	62677	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	309	3	0	3	4.1	CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCC4)CC1	10.1021/jm049499o
	CHEMBL178690	62677	0	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	309	3	0	3	4.1	CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCC4)CC1	10.1021/jm049499o
	11220222	63211	1	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	297	4	0	3	4.2	CCc1cnc2ccc(C(=O)C3CCC(OC)CC3)cc2c1	10.1021/jm049499o
	CHEMBL180021	63211	1	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	297	4	0	3	4.2	CCc1cnc2ccc(C(=O)C3CCC(OC)CC3)cc2c1	10.1021/jm049499o
	11174504	78515	4	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	315	4	0	3	4.3	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1F	10.1021/jm049499o
	CHEMBL2112964	78515	4	None	-	0	Rat	8.4	pIC50	=	8.4	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	315	4	0	3	4.3	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1F	10.1021/jm049499o
	1374	2050	31	None	-	2	Rat	4.4	pIC50	=	4.4	Binding	Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cellsInhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells	ChEMBL	211	3	4	4	0.2	N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O	10.1021/jm980571q
	5311455	2050	31	None	-	2	Rat	4.4	pIC50	=	4.4	Binding	Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cellsInhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells	ChEMBL	211	3	4	4	0.2	N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O	10.1021/jm980571q
	CHEMBL39372	2050	31	None	-	2	Rat	4.4	pIC50	=	4.4	Binding	Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cellsInhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells	ChEMBL	211	3	4	4	0.2	N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O	10.1021/jm980571q
	1374	2050	31	None	12	2	Human	4.4	pIC50	=	4.4	Binding	Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)	ChEMBL	211	3	4	4	0.2	N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O	10.1021/jm9601718
	5311455	2050	31	None	12	2	Human	4.4	pIC50	=	4.4	Binding	Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)	ChEMBL	211	3	4	4	0.2	N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O	10.1021/jm9601718
	CHEMBL39372	2050	31	None	12	2	Human	4.4	pIC50	=	4.4	Binding	Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)	ChEMBL	211	3	4	4	0.2	N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O	10.1021/jm9601718
	11552320	136304	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	364	3	0	6	4.2	CC(C)c1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL374167	136304	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	364	3	0	6	4.2	CC(C)c1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11552320	136304	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	364	3	0	6	4.2	CC(C)c1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL374167	136304	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	364	3	0	6	4.2	CC(C)c1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11660540	84615	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	362	4	1	6	4.1	CCc1ccc(-n2cnc3c(sc4nccc(NC5CC5)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL224088	84615	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	362	4	1	6	4.1	CCc1ccc(-n2cnc3c(sc4nccc(NC5CC5)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11660540	84615	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	362	4	1	6	4.1	CCc1ccc(-n2cnc3c(sc4nccc(NC5CC5)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL224088	84615	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	362	4	1	6	4.1	CCc1ccc(-n2cnc3c(sc4nccc(NC5CC5)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11660511	165590	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	361	4	1	7	3.5	CCc1ccc(-n2cnc3c(sc4nccc(NCC#N)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL426190	165590	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	361	4	1	7	3.5	CCc1ccc(-n2cnc3c(sc4nccc(NCC#N)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11501465	84679	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	364	3	0	6	3.9	CCc1ccc(-n2c(C)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL224673	84679	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	364	3	0	6	3.9	CCc1ccc(-n2c(C)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11232413	60153	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	319	5	0	3	4.5	CCc1cc2cc(C(=O)Cc3cccc(OC)c3)ccc2nc1C	10.1021/jm049499o
	CHEMBL175446	60153	0	None	-	0	Rat	6.4	pIC50	=	6.4	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	319	5	0	3	4.5	CCc1cc2cc(C(=O)Cc3cccc(OC)c3)ccc2nc1C	10.1021/jm049499o
	CHEMBL177736	61803	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	341	5	1	5	3.7	CCc1cc2cc(/C(=N\N)[C@H]3CC[C@@H](OC)CC3)ccc2nc1OC	10.1021/jm049499o
	11501465	84679	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	364	3	0	6	3.9	CCc1ccc(-n2c(C)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL224673	84679	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	364	3	0	6	3.9	CCc1ccc(-n2c(C)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11661106	84709	0	None	208	2	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	390	2	0	6	4.4	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4Cl)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL224898	84709	0	None	208	2	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	390	2	0	6	4.4	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4Cl)cnc3c12	10.1016/j.ejmech.2007.06.024
	11661106	84709	0	None	208	2	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	390	2	0	6	4.4	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4Cl)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL224898	84709	0	None	208	2	Rat	7.4	pIC50	=	7.4	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	390	2	0	6	4.4	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4Cl)cnc3c12	10.1016/j.ejmech.2007.06.024
	11313361	2103	54	None	-	1	Rat	7.4	pIC50	=	7.4	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm049499o
	1385	2103	54	None	-	1	Rat	7.4	pIC50	=	7.4	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm049499o
	CHEMBL174588	2103	54	None	-	1	Rat	7.4	pIC50	=	7.4	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm049499o
	CHEMBL254574	2103	54	None	-	1	Rat	7.4	pIC50	=	7.4	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1021/jm049499o
	11382171	60391	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	338	4	0	6	3.2	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2n2nnnc12	10.1021/jm049499o
	CHEMBL176068	60391	0	None	-	0	Rat	7.4	pIC50	=	7.4	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	338	4	0	6	3.2	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2n2nnnc12	10.1021/jm049499o
	11382171	60391	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	338	4	0	6	3.2	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2n2nnnc12	10.1021/jm049499o
	CHEMBL176068	60391	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	338	4	0	6	3.2	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2n2nnnc12	10.1021/jm049499o
	71452099	82620	0	None	-	1	Rat	7.3	pIC50	=	7.3	Binding	Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting	ChEMBL	387	5	1	6	4.4	CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(Cl)cc3)n2)ncn1	10.1021/jm301597s
	CHEMBL2181521	82620	0	None	-	1	Rat	7.3	pIC50	=	7.3	Binding	Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting	ChEMBL	387	5	1	6	4.4	CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(Cl)cc3)n2)ncn1	10.1021/jm301597s
	44307299	101714	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	279	4	1	4	2.8	Cc1c(C(=O)OC(C)(C)C)c[nH]c1C(=O)OCC1CC1	10.1016/s0960-894x(03)00396-2
	CHEMBL302781	101714	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	279	4	1	4	2.8	Cc1c(C(=O)OC(C)(C)C)c[nH]c1C(=O)OCC1CC1	10.1016/s0960-894x(03)00396-2
	11681680	141824	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	342	2	0	6	3.8	CC1CCCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)C1	10.1016/j.ejmech.2007.06.024
	CHEMBL388827	141824	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	342	2	0	6	3.8	CC1CCCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)C1	10.1016/j.ejmech.2007.06.024
	11681680	141824	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	342	2	0	6	3.8	CC1CCCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)C1	10.1016/j.ejmech.2007.06.024
	CHEMBL388827	141824	0	None	-	0	Rat	6.3	pIC50	=	6.3	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	342	2	0	6	3.8	CC1CCCC(n2cnc3c(sc4nccc(N(C)C)c43)c2=O)C1	10.1016/j.ejmech.2007.06.024
	11660511	165590	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	361	4	1	7	3.5	CCc1ccc(-n2cnc3c(sc4nccc(NCC#N)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL426190	165590	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	361	4	1	7	3.5	CCc1ccc(-n2cnc3c(sc4nccc(NCC#N)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	744275	84420	13	None	251	2	Rat	8.3	pIC50	=	8.3	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	336	2	0	6	3.4	Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL223496	84420	13	None	251	2	Rat	8.3	pIC50	=	8.3	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	336	2	0	6	3.4	Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11609353	84669	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	314	2	0	6	3.2	CN(C)c1ccnc2sc3c(=O)n(C4CCCC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL224617	84669	0	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	314	2	0	6	3.2	CN(C)c1ccnc2sc3c(=O)n(C4CCCC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	11255377	60701	1	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	311	5	0	3	4.6	CCCc1ccc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2n1	10.1021/jm049499o
	CHEMBL176279	60701	1	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	311	5	0	3	4.6	CCCc1ccc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2n1	10.1021/jm049499o
	11256015	62658	4	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	331	4	0	3	4.8	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1Cl	10.1021/jm049499o
	CHEMBL178592	62658	4	None	-	0	Rat	8.3	pIC50	=	8.3	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	331	4	0	3	4.8	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1Cl	10.1021/jm049499o
	11695588	142707	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	328	2	0	6	3.6	CN(C)c1ccnc2sc3c(=O)n(C4CCCCC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL389655	142707	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	328	2	0	6	3.6	CN(C)c1ccnc2sc3c(=O)n(C4CCCCC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	11695769	143006	0	None	-	1	Rat	7.3	pIC50	=	7.3	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	338	2	1	7	2.8	CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4O)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL389897	143006	0	None	-	1	Rat	7.3	pIC50	=	7.3	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	338	2	1	7	2.8	CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4O)cnc3c12	10.1016/j.ejmech.2007.06.024
	11403753	61780	1	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	297	3	1	3	3.8	CCc1cc2cc(C(=O)C3CCC(O)CC3)ccc2nc1C	10.1021/jm049499o
	CHEMBL177585	61780	1	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	297	3	1	3	3.8	CCc1cc2cc(C(=O)C3CCC(O)CC3)ccc2nc1C	10.1021/jm049499o
	44387705	62067	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Inhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domainInhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domain	ChEMBL	288	2	1	3	4.1	Cc1cc2cc(C(C)(C#N)c3ccccc3)ccc2nc1O	10.1021/jm049499o
	CHEMBL177962	62067	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Inhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domainInhibitory concentration against human metabotropic glutamate receptor 1 transmembrane domain	ChEMBL	288	2	1	3	4.1	Cc1cc2cc(C(C)(C#N)c3ccccc3)ccc2nc1O	10.1021/jm049499o
	11462007	78124	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	342	5	1	5	4.2	CCc1cc2cc(/C(=N/O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1OC	10.1021/jm049499o
	CHEMBL2112047	78124	0	None	-	0	Rat	5.3	pIC50	=	5.3	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	342	5	1	5	4.2	CCc1cc2cc(/C(=N/O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1OC	10.1021/jm049499o
	10085578	61781	1	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	289	4	0	2	4.5	CCc1cc2cc(C(=O)Cc3ccccc3)ccc2nc1C	10.1021/jm049499o
	CHEMBL177586	61781	1	None	-	0	Human	7.3	pIC50	=	7.3	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	289	4	0	2	4.5	CCc1cc2cc(C(=O)Cc3ccccc3)ccc2nc1C	10.1021/jm049499o
	44416780	79821	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	441	6	0	7	4.6	CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCc5ccccn5)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL213760	79821	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	441	6	0	7	4.6	CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCc5ccccn5)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	44387723	127298	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	315	3	0	2	4.7	CCc1cc2cc(C(=O)C3Cc4ccccc4C3)ccc2nc1C	10.1021/jm049499o
	CHEMBL366448	127298	0	None	-	0	Rat	7.3	pIC50	=	7.3	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	315	3	0	2	4.7	CCc1cc2cc(C(=O)C3Cc4ccccc4C3)ccc2nc1C	10.1021/jm049499o
	44307338	202102	0	None	-	0	Rat	5.2	pIC50	=	5.2	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	339	7	1	6	3.0	CCCOC(=O)c1c(C)c(C(=O)OC(C)(C)C)c(C)n1CCCO	10.1016/s0960-894x(03)00396-2
	CHEMBL68305	202102	0	None	-	0	Rat	5.2	pIC50	=	5.2	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	339	7	1	6	3.0	CCCOC(=O)c1c(C)c(C(=O)OC(C)(C)C)c(C)n1CCCO	10.1016/s0960-894x(03)00396-2
	11232604	122434	1	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	325	5	0	3	4.9	CCCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C	10.1021/jm049499o
	CHEMBL360728	122434	1	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	325	5	0	3	4.9	CCCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C	10.1021/jm049499o
	10470232	3218	18	None	-1	2	Rat	8.2	pIC50	=	8.2	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	10.1021/jm049499o
	1391	3218	18	None	-1	2	Rat	8.2	pIC50	=	8.2	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	10.1021/jm049499o
	6336	3218	18	None	-1	2	Rat	8.2	pIC50	=	8.2	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	10.1021/jm049499o
	CHEMBL369459	3218	18	None	-1	2	Rat	8.2	pIC50	=	8.2	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	10.1021/jm049499o
	11177701	61138	1	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	423	4	0	3	4.8	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1I	10.1021/jm049499o
	CHEMBL177043	61138	1	None	-	0	Human	7.2	pIC50	=	7.2	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	423	4	0	3	4.8	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1I	10.1021/jm049499o
	11383509	78517	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	383	6	0	5	4.8	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C(=O)OC(C)C	10.1021/jm049499o
	CHEMBL2112966	78517	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	383	6	0	5	4.8	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C(=O)OC(C)C	10.1021/jm049499o
	11565466	84622	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	286	2	0	6	2.4	CN(C)c1ccnc2sc3c(=O)n(C4CC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL224135	84622	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	286	2	0	6	2.4	CN(C)c1ccnc2sc3c(=O)n(C4CC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	11565466	84622	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	286	2	0	6	2.4	CN(C)c1ccnc2sc3c(=O)n(C4CC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL224135	84622	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	286	2	0	6	2.4	CN(C)c1ccnc2sc3c(=O)n(C4CC4)cnc3c12	10.1016/j.ejmech.2007.06.024
	71457446	82617	0	None	-	1	Rat	7.2	pIC50	=	7.2	Binding	Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting	ChEMBL	378	5	1	7	3.6	CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(C#N)cc3)n2)ncn1	10.1021/jm301597s
	CHEMBL2181519	82617	0	None	-	1	Rat	7.2	pIC50	=	7.2	Binding	Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting	ChEMBL	378	5	1	7	3.6	CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(C#N)cc3)n2)ncn1	10.1021/jm301597s
	11186617	60247	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	332	5	0	3	4.6	CCc1cc2cc(C(=O)Cc3ccc(N(C)C)cc3)ccc2nc1C	10.1021/jm049499o
	CHEMBL175997	60247	0	None	-	0	Rat	6.2	pIC50	=	6.2	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	332	5	0	3	4.6	CCc1cc2cc(C(=O)Cc3ccc(N(C)C)cc3)ccc2nc1C	10.1021/jm049499o
	44387697	60145	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	325	5	0	3	4.7	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1CC	10.1021/jm049499o
	CHEMBL175377	60145	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	325	5	0	3	4.7	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1CC	10.1021/jm049499o
	1418	3393	48	None	-21	2	Human	4.2	pIC50	=	4.2	Binding	Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)	ChEMBL	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	10.1021/jm9601718
	5311459	3393	48	None	-21	2	Human	4.2	pIC50	=	4.2	Binding	Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)	ChEMBL	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	10.1021/jm9601718
	CHEMBL94990	3393	48	None	-21	2	Human	4.2	pIC50	=	4.2	Binding	Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a)	ChEMBL	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	10.1021/jm9601718
	10058919	3634	10	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Inhibition of mGluR1a receptorInhibition of mGluR1a receptor	ChEMBL	209	3	3	5	-1.0	OC(=O)[C@H](C12CC(C1)(C2)c1n[nH]nn1)N	10.1021/jm1013693
	3419	3634	10	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Inhibition of mGluR1a receptorInhibition of mGluR1a receptor	ChEMBL	209	3	3	5	-1.0	OC(=O)[C@H](C12CC(C1)(C2)c1n[nH]nn1)N	10.1021/jm1013693
	CHEMBL2204334	3634	10	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Inhibition of mGluR1a receptorInhibition of mGluR1a receptor	ChEMBL	209	3	3	5	-1.0	OC(=O)[C@H](C12CC(C1)(C2)c1n[nH]nn1)N	10.1021/jm1013693
	11232871	61769	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	333	3	0	4	4.1	CCc1cc2cc(C(=O)C3COc4ccccc4O3)ccc2nc1C	10.1021/jm049499o
	CHEMBL177519	61769	0	None	-	0	Human	8.2	pIC50	=	8.2	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	333	3	0	4	4.1	CCc1cc2cc(C(=O)C3COc4ccccc4O3)ccc2nc1C	10.1021/jm049499o
	11185961	62684	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	309	3	0	4	4.0	O=C(Cc1ccsc1)c1ccc2nc3c(cc2c1)CCCO3	10.1021/jm049499o
	CHEMBL178742	62684	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	309	3	0	4	4.0	O=C(Cc1ccsc1)c1ccc2nc3c(cc2c1)CCCO3	10.1021/jm049499o
	11461116	78518	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	312	4	1	4	3.8	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1N	10.1021/jm049499o
	CHEMBL2112967	78518	0	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	312	4	1	4	3.8	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1N	10.1021/jm049499o
	11232604	122434	1	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	325	5	0	3	4.9	CCCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C	10.1021/jm049499o
	CHEMBL360728	122434	1	None	-	0	Rat	8.2	pIC50	=	8.2	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	325	5	0	3	4.9	CCCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1C	10.1021/jm049499o
	11581985	84729	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	394	6	0	7	3.6	CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCOC)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL225125	84729	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	394	6	0	7	3.6	CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCOC)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11581985	84729	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	394	6	0	7	3.6	CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCOC)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL225125	84729	0	None	-	0	Rat	7.2	pIC50	=	7.2	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	394	6	0	7	3.6	CCc1ccc(-n2cnc3c(sc4nccc(N(C)CCOC)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	44307129	202128	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	330	4	1	5	3.5	Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)Oc1cccnc1	10.1016/s0960-894x(03)00396-2
	CHEMBL68471	202128	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	330	4	1	5	3.5	Cc1c(C(=O)OC(C)C(C)(C)C)c[nH]c1C(=O)Oc1cccnc1	10.1016/s0960-894x(03)00396-2
	11185961	62684	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	309	3	0	4	4.0	O=C(Cc1ccsc1)c1ccc2nc3c(cc2c1)CCCO3	10.1021/jm049499o
	CHEMBL178742	62684	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	309	3	0	4	4.0	O=C(Cc1ccsc1)c1ccc2nc3c(cc2c1)CCCO3	10.1021/jm049499o
	44306949	202049	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	267	4	1	4	2.8	CCCOC(=O)c1[nH]cc(C(=O)OC(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	CHEMBL67833	202049	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	267	4	1	4	2.8	CCCOC(=O)c1[nH]cc(C(=O)OC(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	11696595	84640	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	380	2	0	6	4.0	CN(C)c1ccnc2sc3c(=O)n(C45CC6CC(CC(C6)C4)C5)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL224322	84640	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	380	2	0	6	4.0	CN(C)c1ccnc2sc3c(=O)n(C45CC6CC(CC(C6)C4)C5)cnc3c12	10.1016/j.ejmech.2007.06.024
	11696595	84640	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	380	2	0	6	4.0	CN(C)c1ccnc2sc3c(=O)n(C45CC6CC(CC(C6)C4)C5)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL224322	84640	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	380	2	0	6	4.0	CN(C)c1ccnc2sc3c(=O)n(C45CC6CC(CC(C6)C4)C5)cnc3c12	10.1016/j.ejmech.2007.06.024
	10198359	73610	7	None	-	1	Human	4.1	pIC50	=	4.1	Binding	Inhibition of mGluR1b receptorInhibition of mGluR1b receptor	ChEMBL	221	3	3	3	-0.8	N[C@H](C(=O)O)C12C3C4C1C1C2C3C41C(=O)O	10.1021/jm1013693
	CHEMBL2021372	73610	7	None	-	1	Human	4.1	pIC50	=	4.1	Binding	Inhibition of mGluR1b receptorInhibition of mGluR1b receptor	ChEMBL	221	3	3	3	-0.8	N[C@H](C(=O)O)C12C3C4C1C1C2C3C41C(=O)O	10.1021/jm1013693
	11485531	128954	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	370	8	1	5	4.2	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1NCCOC	10.1021/jm049499o
	CHEMBL367227	128954	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	370	8	1	5	4.2	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1NCCOC	10.1021/jm049499o
	44307277	202032	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	297	5	2	5	2.3	CCCOC(=O)c1[nH]c(CO)c(C(=O)OC(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	CHEMBL67737	202032	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.In vitro inhibition of rat metabotropic glutamate receptor 1 in CHO cells using the CDP-DAG accumulation method.	ChEMBL	297	5	2	5	2.3	CCCOC(=O)c1[nH]c(CO)c(C(=O)OC(C)(C)C)c1C	10.1016/s0960-894x(03)00396-2
	44387697	60145	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	325	5	0	3	4.7	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1CC	10.1021/jm049499o
	CHEMBL175377	60145	0	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	325	5	0	3	4.7	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1CC	10.1021/jm049499o
	11450605	59963	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	338	3	0	4	4.0	CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCN4C)CC1	10.1021/jm049499o
	CHEMBL174216	59963	0	None	-	0	Rat	8.1	pIC50	=	8.1	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	338	3	0	4	4.0	CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCN4C)CC1	10.1021/jm049499o
	11717278	84614	0	None	102	2	Rat	8.1	pIC50	=	8.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	350	3	0	6	3.6	CCc1cccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c1	10.1016/j.ejmech.2007.06.024
	CHEMBL224084	84614	0	None	102	2	Rat	8.1	pIC50	=	8.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	350	3	0	6	3.6	CCc1cccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c1	10.1016/j.ejmech.2007.06.024
	11403753	61780	1	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	297	3	1	3	3.8	CCc1cc2cc(C(=O)C3CCC(O)CC3)ccc2nc1C	10.1021/jm049499o
	CHEMBL177585	61780	1	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	297	3	1	3	3.8	CCc1cc2cc(C(=O)C3CCC(O)CC3)ccc2nc1C	10.1021/jm049499o
	11209923	62683	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	337	3	0	3	4.9	CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCCC4)CC1	10.1021/jm049499o
	CHEMBL178741	62683	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	337	3	0	3	4.9	CO[C@H]1CC[C@@H](C(=O)c2ccc3nc4c(cc3c2)CCCCC4)CC1	10.1021/jm049499o
	1379	2387	36	None	-	1	Human	5.1	pIC50	=	5.1	Binding	Negative allosteric modulation of human mGluR1alpha expressed in syrian hamster AV-12 cells assessed as inhibition of quisqualate-induced phosphoinositide hydrolysisNegative allosteric modulation of human mGluR1alpha expressed in syrian hamster AV-12 cells assessed as inhibition of quisqualate-induced phosphoinositide hydrolysis	ChEMBL	209	3	3	3	0.8	OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N	10.1016/j.bmc.2014.12.034
	5311261	2387	36	None	-	1	Human	5.1	pIC50	=	5.1	Binding	Negative allosteric modulation of human mGluR1alpha expressed in syrian hamster AV-12 cells assessed as inhibition of quisqualate-induced phosphoinositide hydrolysisNegative allosteric modulation of human mGluR1alpha expressed in syrian hamster AV-12 cells assessed as inhibition of quisqualate-induced phosphoinositide hydrolysis	ChEMBL	209	3	3	3	0.8	OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N	10.1016/j.bmc.2014.12.034
	CHEMBL94631	2387	36	None	-	1	Human	5.1	pIC50	=	5.1	Binding	Negative allosteric modulation of human mGluR1alpha expressed in syrian hamster AV-12 cells assessed as inhibition of quisqualate-induced phosphoinositide hydrolysisNegative allosteric modulation of human mGluR1alpha expressed in syrian hamster AV-12 cells assessed as inhibition of quisqualate-induced phosphoinositide hydrolysis	ChEMBL	209	3	3	3	0.8	OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N	10.1016/j.bmc.2014.12.034
	11232871	61769	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	333	3	0	4	4.1	CCc1cc2cc(C(=O)C3COc4ccccc4O3)ccc2nc1C	10.1021/jm049499o
	CHEMBL177519	61769	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	333	3	0	4	4.1	CCc1cc2cc(C(=O)C3COc4ccccc4O3)ccc2nc1C	10.1021/jm049499o
	11530971	84736	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	378	4	0	6	4.2	CCc1ccc(-n2c(CC)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL225201	84736	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	378	4	0	6	4.2	CCc1ccc(-n2c(CC)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11438114	62159	1	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	303	3	0	3	4.0	O=C(Cc1ccccc1)c1ccc2cc3c(nc2c1)OCCC3	10.1021/jm049499o
	CHEMBL178022	62159	1	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	303	3	0	3	4.0	O=C(Cc1ccccc1)c1ccc2cc3c(nc2c1)OCCC3	10.1021/jm049499o
	11474450	78516	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	379	5	0	4	5.9	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1-c1ccsc1	10.1021/jm049499o
	CHEMBL2112965	78516	0	None	-	0	Rat	6.1	pIC50	=	6.1	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	379	5	0	4	5.9	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1-c1ccsc1	10.1021/jm049499o
	11530971	84736	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	378	4	0	6	4.2	CCc1ccc(-n2c(CC)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL225201	84736	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	378	4	0	6	4.2	CCc1ccc(-n2c(CC)nc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	44421618	84771	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	378	2	0	6	4.4	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(C)(C)C)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL225439	84771	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	378	2	0	6	4.4	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(C)(C)C)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	11324832	60192	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	325	5	0	3	4.9	CCc1cc2cc(C(=O)C[C@H]3CC[C@@H](OC)CC3)ccc2nc1C	10.1021/jm049499o
	CHEMBL175699	60192	0	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	325	5	0	3	4.9	CCc1cc2cc(C(=O)C[C@H]3CC[C@@H](OC)CC3)ccc2nc1C	10.1021/jm049499o
	11186076	168769	1	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	313	4	1	4	3.9	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1O	10.1021/jm049499o
	CHEMBL441844	168769	1	None	-	0	Human	7.1	pIC50	=	7.1	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	313	4	1	4	3.9	CCc1cc2cc(C(=O)C3CCC(OC)CC3)ccc2nc1O	10.1021/jm049499o
	11347669	119895	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	317	4	0	3	4.4	O=C(CCc1ccccc1)c1ccc2nc3c(cc2c1)CCCO3	10.1021/jm049499o
	CHEMBL353547	119895	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibitory concentration against rat metabotropic glutamate receptor 1Inhibitory concentration against rat metabotropic glutamate receptor 1	ChEMBL	317	4	0	3	4.4	O=C(CCc1ccccc1)c1ccc2nc3c(cc2c1)CCCO3	10.1021/jm049499o
	44421618	84771	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	378	2	0	6	4.4	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(C)(C)C)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL225439	84771	0	None	-	0	Rat	5.1	pIC50	=	5.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	378	2	0	6	4.4	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(C)(C)C)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	11588590	141503	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	362	3	0	6	3.9	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL387687	141503	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	362	3	0	6	3.9	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	11588590	141503	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	362	3	0	6	3.9	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	CHEMBL387687	141503	0	None	-	0	Rat	7.1	pIC50	=	7.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	362	3	0	6	3.9	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C5CC5)cc4)cnc3c12	10.1016/j.ejmech.2007.06.024
	1378	2384	48	None	-	10	Rat	5.1	pIC50	=	5.1	Binding	Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells	ChEMBL	353	5	3	4	2.8	OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N	10.1021/jm0400294
	1399	2384	48	None	-	10	Rat	5.1	pIC50	=	5.1	Binding	Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells	ChEMBL	353	5	3	4	2.8	OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N	10.1021/jm0400294
	9819927	2384	48	None	-	10	Rat	5.1	pIC50	=	5.1	Binding	Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells	ChEMBL	353	5	3	4	2.8	OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N	10.1021/jm0400294
	CHEMBL432038	2384	48	None	-	10	Rat	5.1	pIC50	=	5.1	Binding	Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells	ChEMBL	353	5	3	4	2.8	OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N	10.1021/jm0400294
	11717278	84614	0	None	102	2	Rat	8.1	pIC50	=	8.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	350	3	0	6	3.6	CCc1cccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c1	10.1016/j.ejmech.2007.06.024
	CHEMBL224084	84614	0	None	102	2	Rat	8.1	pIC50	=	8.1	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	350	3	0	6	3.6	CCc1cccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c1	10.1016/j.ejmech.2007.06.024
	11174504	78515	4	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	315	4	0	3	4.3	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1F	10.1021/jm049499o
	CHEMBL2112964	78515	4	None	-	0	Human	8.1	pIC50	=	8.1	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	315	4	0	3	4.3	CCc1cc2cc(C(=O)[C@H]3CC[C@@H](OC)CC3)ccc2nc1F	10.1021/jm049499o
	1397	2493	11	None	-	5	Rat	4.0	pIC50	=	4.0	Binding	Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells	ChEMBL	377	5	3	4	2.1	OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O	10.1021/jm0400294
	9886034	2493	11	None	-	5	Rat	4.0	pIC50	=	4.0	Binding	Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells	ChEMBL	377	5	3	4	2.1	OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O	10.1021/jm0400294
	CHEMBL186453	2493	11	None	-	5	Rat	4.0	pIC50	=	4.0	Binding	Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cellsConcentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells	ChEMBL	377	5	3	4	2.1	OC(=O)[C@]1(N)[C@H](OCc2ccc(c(c2)Cl)Cl)C[C@@H]2[C@H]1[C@@]2(F)C(=O)O	10.1021/jm0400294
	10245890	1951	7	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	327	5	0	4	4.2	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC	10.1021/jm049499o
	6474	1951	7	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	327	5	0	4	4.2	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC	10.1021/jm049499o
	CHEMBL175643	1951	7	None	-	0	Human	7.0	pIC50	=	7.0	Binding	Inhibitory concentration against human metabotropic glutamate receptorInhibitory concentration against human metabotropic glutamate receptor	ChEMBL	327	5	0	4	4.2	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)OC)CC	10.1021/jm049499o
	11681575	136653	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	336	3	1	6	3.6	CCc1ccc(-n2cnc3c(sc4nccc(NC)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL374815	136653	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	336	3	1	6	3.6	CCc1ccc(-n2cnc3c(sc4nccc(NC)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11681575	136653	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	336	3	1	6	3.6	CCc1ccc(-n2cnc3c(sc4nccc(NC)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL374815	136653	0	None	-	0	Rat	7.0	pIC50	=	7.0	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	336	3	1	6	3.6	CCc1ccc(-n2cnc3c(sc4nccc(NC)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11582178	137400	0	None	-	0	Rat	7.0	pIC50	=	7	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	404	4	1	6	4.5	CCc1ccc(-n2cnc3c(sc4nccc(NCC(F)(F)F)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL376372	137400	0	None	-	0	Rat	7.0	pIC50	=	7	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	404	4	1	6	4.5	CCc1ccc(-n2cnc3c(sc4nccc(NCC(F)(F)F)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	11582178	137400	0	None	-	0	Rat	7.0	pIC50	=	7	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	404	4	1	6	4.5	CCc1ccc(-n2cnc3c(sc4nccc(NCC(F)(F)F)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	CHEMBL376372	137400	0	None	-	0	Rat	7.0	pIC50	=	7	Binding	Inhibition of rat mGluR1Inhibition of rat mGluR1	ChEMBL	404	4	1	6	4.5	CCc1ccc(-n2cnc3c(sc4nccc(NCC(F)(F)F)c43)c2=O)cc1	10.1016/j.ejmech.2007.06.024
	16659802	1023	0	None	-	1	Rat	9.7	pKi	=	9.7	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	384	1	1	7	3.8	C[C@@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	10.1021/jm070590c
	6348	1023	0	None	-	1	Rat	9.7	pKi	=	9.7	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	384	1	1	7	3.8	C[C@@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	10.1021/jm070590c
	CHEMBL241327	1023	0	None	-	1	Rat	9.7	pKi	=	9.7	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	384	1	1	7	3.8	C[C@@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	10.1021/jm070590c
	23657393	88314	0	None	-	1	Rat	9.5	pKi	=	9.5	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	380	2	1	8	3.2	COc1ccc(-n2cnc3c(sc4ncc5c(c43)NC[C@@H](C)O5)c2=O)cc1	10.1021/jm070590c
	CHEMBL236177	88314	0	None	-	1	Rat	9.5	pKi	=	9.5	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	380	2	1	8	3.2	COc1ccc(-n2cnc3c(sc4ncc5c(c43)NC[C@@H](C)O5)c2=O)cc1	10.1021/jm070590c
	11313361	2103	54	None	-	1	Human	9.5	pKi	=	9.5	Binding	Binding affinity to mGluR1Binding affinity to mGluR1	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1016/j.bmc.2010.11.048
	1385	2103	54	None	-	1	Human	9.5	pKi	=	9.5	Binding	Binding affinity to mGluR1Binding affinity to mGluR1	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1016/j.bmc.2010.11.048
	CHEMBL174588	2103	54	None	-	1	Human	9.5	pKi	=	9.5	Binding	Binding affinity to mGluR1Binding affinity to mGluR1	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1016/j.bmc.2010.11.048
	CHEMBL254574	2103	54	None	-	1	Human	9.5	pKi	=	9.5	Binding	Binding affinity to mGluR1Binding affinity to mGluR1	ChEMBL	325	3	0	4	3.9	COC1CCC(CC1)C(=O)c1ccc2c(c1)cc1c(n2)OCCC1	10.1016/j.bmc.2010.11.048
	15985249	195579	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Binding affinity to mGluR1Binding affinity to mGluR1	ChEMBL	351	4	0	5	3.1	CCCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O	10.1016/j.bmc.2010.11.048
	CHEMBL1645349	195579	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Binding affinity to mGluR1Binding affinity to mGluR1	ChEMBL	351	4	0	5	3.1	CCCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O	10.1016/j.bmc.2010.11.048
	CHEMBL568443	195579	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Binding affinity to mGluR1Binding affinity to mGluR1	ChEMBL	351	4	0	5	3.1	CCCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O	10.1016/j.bmc.2010.11.048
	15985249	195579	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis	ChEMBL	351	4	0	5	3.1	CCCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O	10.1016/j.bmcl.2011.03.046
	CHEMBL1645349	195579	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis	ChEMBL	351	4	0	5	3.1	CCCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O	10.1016/j.bmcl.2011.03.046
	CHEMBL568443	195579	0	None	-	1	Human	9.4	pKi	=	9.4	Binding	Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis	ChEMBL	351	4	0	5	3.1	CCCN1Cc2cc(-c3nnn(-c4cccnc4F)c3C)ccc2C1=O	10.1016/j.bmcl.2011.03.046
	16659801	1021	0	None	-	1	Rat	9.4	pKi	=	9.4	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	370	1	1	7	3.5	Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	10.1021/jm070590c
	6346	1021	0	None	-	1	Rat	9.4	pKi	=	9.4	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	370	1	1	7	3.5	Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	10.1021/jm070590c
	CHEMBL236994	1021	0	None	-	1	Rat	9.4	pKi	=	9.4	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	370	1	1	7	3.5	Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	10.1021/jm070590c
	16659966	88258	0	None	-	1	Rat	9.3	pKi	=	9.3	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	350	1	1	7	3.1	Cc1ccc(-n2cnc3c(sc4ncc5c(c43)NCCO5)c2=O)cc1	10.1021/jm070590c
	CHEMBL235975	88258	0	None	-	1	Rat	9.3	pKi	=	9.3	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	350	1	1	7	3.1	Cc1ccc(-n2cnc3c(sc4ncc5c(c43)NCCO5)c2=O)cc1	10.1021/jm070590c
	16659805	148080	0	None	-	1	Rat	9.3	pKi	=	9.3	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	384	1	1	7	3.8	C[C@H]1COc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c2N1	10.1021/jm070590c
	CHEMBL393923	148080	0	None	-	1	Rat	9.3	pKi	=	9.3	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	384	1	1	7	3.8	C[C@H]1COc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c2N1	10.1021/jm070590c
	16659968	88259	0	None	-	1	Rat	9.2	pKi	=	9.2	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	364	1	1	7	3.5	Cc1ccc(-n2cnc3c(sc4ncc5c(c43)NC[C@@H](C)O5)c2=O)cc1	10.1021/jm070590c
	CHEMBL235977	88259	0	None	-	1	Rat	9.2	pKi	=	9.2	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	364	1	1	7	3.5	Cc1ccc(-n2cnc3c(sc4ncc5c(c43)NC[C@@H](C)O5)c2=O)cc1	10.1021/jm070590c
	7442	2104	3	None	1	3	Human	9.1	pKi	=	9.1	Binding	Binding affinity to mGluR1Binding affinity to mGluR1	ChEMBL	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	10.1016/j.bmc.2010.11.048
	9948645	2104	3	None	1	3	Human	9.1	pKi	=	9.1	Binding	Binding affinity to mGluR1Binding affinity to mGluR1	ChEMBL	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	10.1016/j.bmc.2010.11.048
	CHEMBL188906	2104	3	None	1	3	Human	9.1	pKi	=	9.1	Binding	Binding affinity to mGluR1Binding affinity to mGluR1	ChEMBL	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	10.1016/j.bmc.2010.11.048
	CHEMBL253345	2104	3	None	1	3	Human	9.1	pKi	=	9.1	Binding	Binding affinity to mGluR1Binding affinity to mGluR1	ChEMBL	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	10.1016/j.bmc.2010.11.048
	7442	2104	3	None	1	3	Human	9.1	pKi	=	9.1	Binding	Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis	ChEMBL	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	10.1016/j.bmcl.2011.03.046
	9948645	2104	3	None	1	3	Human	9.1	pKi	=	9.1	Binding	Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis	ChEMBL	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	10.1016/j.bmcl.2011.03.046
	CHEMBL188906	2104	3	None	1	3	Human	9.1	pKi	=	9.1	Binding	Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis	ChEMBL	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	10.1016/j.bmcl.2011.03.046
	CHEMBL253345	2104	3	None	1	3	Human	9.1	pKi	=	9.1	Binding	Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis	ChEMBL	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	10.1016/j.bmcl.2011.03.046
	7442	2104	3	None	-1	3	Rat	9.1	pKi	=	9.1	Binding	In vitro affinity for cloned rat metabotropic glutamate 1 receptors stably expressed on CHO cells determined using [3H]-R214127 as radioligandIn vitro affinity for cloned rat metabotropic glutamate 1 receptors stably expressed on CHO cells determined using [3H]-R214127 as radioligand	ChEMBL	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	10.1021/jm050263+
	9948645	2104	3	None	-1	3	Rat	9.1	pKi	=	9.1	Binding	In vitro affinity for cloned rat metabotropic glutamate 1 receptors stably expressed on CHO cells determined using [3H]-R214127 as radioligandIn vitro affinity for cloned rat metabotropic glutamate 1 receptors stably expressed on CHO cells determined using [3H]-R214127 as radioligand	ChEMBL	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	10.1021/jm050263+
	CHEMBL188906	2104	3	None	-1	3	Rat	9.1	pKi	=	9.1	Binding	In vitro affinity for cloned rat metabotropic glutamate 1 receptors stably expressed on CHO cells determined using [3H]-R214127 as radioligandIn vitro affinity for cloned rat metabotropic glutamate 1 receptors stably expressed on CHO cells determined using [3H]-R214127 as radioligand	ChEMBL	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	10.1021/jm050263+
	CHEMBL253345	2104	3	None	-1	3	Rat	9.1	pKi	=	9.1	Binding	In vitro affinity for cloned rat metabotropic glutamate 1 receptors stably expressed on CHO cells determined using [3H]-R214127 as radioligandIn vitro affinity for cloned rat metabotropic glutamate 1 receptors stably expressed on CHO cells determined using [3H]-R214127 as radioligand	ChEMBL	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	10.1021/jm050263+
	16659967	1020	0	None	-	1	Rat	9.0	pKi	=	9	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	366	2	1	8	2.8	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	10.1021/jm070590c
	6345	1020	0	None	-	1	Rat	9.0	pKi	=	9	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	366	2	1	8	2.8	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	10.1021/jm070590c
	CHEMBL393922	1020	0	None	-	1	Rat	9.0	pKi	=	9	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	366	2	1	8	2.8	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	10.1021/jm070590c
	11574901	84800	0	None	-	1	Rat	9.0	pKi	=	9	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	400	2	0	6	3.8	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1021/jm0504407
	CHEMBL225590	84800	0	None	-	1	Rat	9.0	pKi	=	9	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	400	2	0	6	3.8	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Br)cc4)cnc3c12	10.1021/jm0504407
	16659803	1022	0	None	-	1	Rat	8.8	pKi	=	8.8	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	384	1	1	7	3.8	C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	10.1021/jm070590c
	6338	1022	0	None	-	1	Rat	8.8	pKi	=	8.8	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	384	1	1	7	3.8	C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	10.1021/jm070590c
	CHEMBL236180	1022	0	None	-	1	Rat	8.8	pKi	=	8.8	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	384	1	1	7	3.8	C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	10.1021/jm070590c
	1370	3212	62	None	44	8	Rat	8.0	pKi	=	8	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm010323l
	1372	3212	62	None	44	8	Rat	8.0	pKi	=	8	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm010323l
	40539	3212	62	None	44	8	Rat	8.0	pKi	=	8	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm010323l
	6971145	3212	62	None	44	8	Rat	8.0	pKi	=	8	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm010323l
	CHEMBL279956	3212	62	None	44	8	Rat	8.0	pKi	=	8	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm010323l
	DB02999	3212	62	None	44	8	Rat	8.0	pKi	=	8	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	10.1021/jm010323l
	16659963	149343	0	None	-	1	Rat	8.0	pKi	=	8.0	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	353	1	1	6	3.5	O=c1c2sc3ncc4nc[nH]c4c3c2ncn1-c1ccc(Cl)cc1	10.1021/jm070590c
	CHEMBL394914	149343	0	None	-	1	Rat	8.0	pKi	=	8.0	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	353	1	1	6	3.5	O=c1c2sc3ncc4nc[nH]c4c3c2ncn1-c1ccc(Cl)cc1	10.1021/jm070590c
	16659799	145856	0	None	-	1	Rat	6.0	pKi	=	6	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	366	1	1	7	3.2	Cc1ccc(-n2cnc3c(sc4ncc5sc(=O)[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	CHEMBL392164	145856	0	None	-	1	Rat	6.0	pKi	=	6	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	366	1	1	7	3.2	Cc1ccc(-n2cnc3c(sc4ncc5sc(=O)[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	16659647	166859	0	None	-	1	Rat	6.0	pKi	=	6	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	382	1	1	7	4.6	Cc1ccc(-n2cnc3c(sc4ncc5sc(=S)[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	CHEMBL429635	166859	0	None	-	1	Rat	6.0	pKi	=	6	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	382	1	1	7	4.6	Cc1ccc(-n2cnc3c(sc4ncc5sc(=S)[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	16659964	89529	0	None	-	1	Rat	7.0	pKi	=	7.0	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	367	1	0	7	3.5	Cn1cnc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c21	10.1021/jm070590c
	CHEMBL238090	89529	0	None	-	1	Rat	7.0	pKi	=	7.0	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	367	1	0	7	3.5	Cn1cnc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c21	10.1021/jm070590c
	11661106	84709	0	None	208	2	Rat	8.0	pKi	=	8.0	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	390	2	0	6	4.4	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4Cl)cnc3c12	10.1021/jm0504407
	CHEMBL224898	84709	0	None	208	2	Rat	8.0	pKi	=	8.0	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	390	2	0	6	4.4	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4Cl)cnc3c12	10.1021/jm0504407
	25067015	193940	0	None	-4	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human GluR1 by FLIPR assayBinding affinity to human GluR1 by FLIPR assay	ChEMBL	366	4	0	4	3.8	O=C(C1CC1c1ccc(N2CCOCC2)nc1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmc.2009.05.072
	CHEMBL556070	193940	0	None	-4	3	Human	7.0	pKi	=	7.0	Binding	Binding affinity to human GluR1 by FLIPR assayBinding affinity to human GluR1 by FLIPR assay	ChEMBL	366	4	0	4	3.8	O=C(C1CC1c1ccc(N2CCOCC2)nc1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmc.2009.05.072
	16660470	76276	0	None	-	1	Rat	7.9	pKi	=	7.9	Binding	Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr	ChEMBL	383	6	1	7	3.7	COc1ccc(C(=O)N(C)c2nc(-c3cc(NC(C)C)ncn3)cs2)cc1	10.1021/jm201590g
	CHEMBL2063722	76276	0	None	-	1	Rat	7.9	pKi	=	7.9	Binding	Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr	ChEMBL	383	6	1	7	3.7	COc1ccc(C(=O)N(C)c2nc(-c3cc(NC(C)C)ncn3)cs2)cc1	10.1021/jm201590g
	71459305	82619	0	None	-	1	Rat	7.9	pKi	=	7.9	Binding	Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting	ChEMBL	367	5	1	6	4.0	Cc1ccc(C(=O)N(C)c2nc(-c3cc(NC(C)C)ncn3)cs2)cc1	10.1021/jm301597s
	CHEMBL2181520	82619	0	None	-	1	Rat	7.9	pKi	=	7.9	Binding	Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting	ChEMBL	367	5	1	6	4.0	Cc1ccc(C(=O)N(C)c2nc(-c3cc(NC(C)C)ncn3)cs2)cc1	10.1021/jm301597s
	24759782	194965	0	None	-	1	Rat	6.9	pKi	=	6.9	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	331	3	0	2	5.1	O=C(C1CC1c1cnc2ccccc2c1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmc.2009.05.072
	CHEMBL564327	194965	0	None	-	1	Rat	6.9	pKi	=	6.9	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	331	3	0	2	5.1	O=C(C1CC1c1cnc2ccccc2c1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmc.2009.05.072
	11501188	137018	0	None	-	1	Rat	6.9	pKi	=	6.9	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	350	3	0	6	3.6	CCc1ccccc1-n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1021/jm0504407
	CHEMBL375439	137018	0	None	-	1	Rat	6.9	pKi	=	6.9	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	350	3	0	6	3.6	CCc1ccccc1-n1cnc2c(sc3nccc(N(C)C)c32)c1=O	10.1021/jm0504407
	70688666	76277	0	None	-	1	Rat	6.8	pKi	=	6.8	Binding	Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr	ChEMBL	415	8	1	7	4.0	CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(OCCF)cc3)n2)ncn1	10.1021/jm201590g
	CHEMBL2063723	76277	0	None	-	1	Rat	6.8	pKi	=	6.8	Binding	Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr	ChEMBL	415	8	1	7	4.0	CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(OCCF)cc3)n2)ncn1	10.1021/jm201590g
	1310	2286	108	None	-1	18	Human	5.8	pKi	=	5.8	Binding	Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1039/C1MD00186H
	1369	2286	108	None	-1	18	Human	5.8	pKi	=	5.8	Binding	Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1039/C1MD00186H
	33032	2286	108	None	-1	18	Human	5.8	pKi	=	5.8	Binding	Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1039/C1MD00186H
	44272391	2286	108	None	-1	18	Human	5.8	pKi	=	5.8	Binding	Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1039/C1MD00186H
	88747398	2286	108	None	-1	18	Human	5.8	pKi	=	5.8	Binding	Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1039/C1MD00186H
	CHEMBL575060	2286	108	None	-1	18	Human	5.8	pKi	=	5.8	Binding	Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1039/C1MD00186H
	DB00142	2286	108	None	-1	18	Human	5.8	pKi	=	5.8	Binding	Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1039/C1MD00186H
	16659645	147801	0	None	-	1	Rat	7.8	pKi	=	7.8	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	332	1	1	5	3.8	Cc1ccc(-n2cnc3c(sc4ncc5cc[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	CHEMBL393705	147801	0	None	-	1	Rat	7.8	pKi	=	7.8	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	332	1	1	5	3.8	Cc1ccc(-n2cnc3c(sc4ncc5cc[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	16038352	89788	0	None	-	1	Rat	7.8	pKi	=	7.8	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	333	1	1	6	3.2	Cc1ccc(-n2cnc3c(sc4ncc5cn[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	CHEMBL238262	89788	0	None	-	1	Rat	7.8	pKi	=	7.8	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	333	1	1	6	3.2	Cc1ccc(-n2cnc3c(sc4ncc5cn[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	5766228	193960	20	None	-	1	Rat	4.8	pKi	=	4.8	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	313	3	0	3	5.2	Cc1ccc2cc(/C=C/C(=O)c3cccs3)c(Cl)nc2c1	10.1016/j.bmc.2009.05.072
	CHEMBL556293	193960	20	None	-	1	Rat	4.8	pKi	=	4.8	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	313	3	0	3	5.2	Cc1ccc2cc(/C=C/C(=O)c3cccs3)c(Cl)nc2c1	10.1016/j.bmc.2009.05.072
	87549991	121691	0	None	-61	3	Rat	7.7	pKi	=	7.7	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	333	2	0	4	3.9	Cc1cccc(C#CC=C2CCN(c3ncccc3[N+](=O)[O-])CC2)c1	10.1016/j.bmc.2015.05.008
	CHEMBL3597597	121691	0	None	-61	3	Rat	7.7	pKi	=	7.7	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	333	2	0	4	3.9	Cc1cccc(C#CC=C2CCN(c3ncccc3[N+](=O)[O-])CC2)c1	10.1016/j.bmc.2015.05.008
	87550873	121692	0	None	-46	3	Rat	7.7	pKi	=	7.7	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	353	2	0	4	4.2	O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2cccc(Cl)c2)CC1	10.1016/j.bmc.2015.05.008
	CHEMBL3597598	121692	0	None	-46	3	Rat	7.7	pKi	=	7.7	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	353	2	0	4	4.2	O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2cccc(Cl)c2)CC1	10.1016/j.bmc.2015.05.008
	25183668	121688	0	None	-6025	3	Rat	6.7	pKi	=	6.7	Binding	Displacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysis	ChEMBL	334	2	0	5	3.3	Cc1cccc(C#CC=C2CCN(c3ncccc3[N+](=O)[O-])CC2)n1	10.1021/acs.jmedchem.8b01226
	CHEMBL3597594	121688	0	None	-6025	3	Rat	6.7	pKi	=	6.7	Binding	Displacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysis	ChEMBL	334	2	0	5	3.3	Cc1cccc(C#CC=C2CCN(c3ncccc3[N+](=O)[O-])CC2)n1	10.1021/acs.jmedchem.8b01226
	25183668	121688	0	None	-6025	3	Rat	6.7	pKi	=	6.7	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	334	2	0	5	3.3	Cc1cccc(C#CC=C2CCN(c3ncccc3[N+](=O)[O-])CC2)n1	10.1016/j.bmc.2015.05.008
	CHEMBL3597594	121688	0	None	-6025	3	Rat	6.7	pKi	=	6.7	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	334	2	0	5	3.3	Cc1cccc(C#CC=C2CCN(c3ncccc3[N+](=O)[O-])CC2)n1	10.1016/j.bmc.2015.05.008
	122183738	121694	0	None	-630	3	Rat	6.7	pKi	=	6.7	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	359	2	0	6	3.1	Cc1ccc([N+](=O)[O-])c(N2CCC(=CC#Cc3ccc(C#N)cn3)CC2)n1	10.1016/j.bmc.2015.05.008
	CHEMBL3597600	121694	0	None	-630	3	Rat	6.7	pKi	=	6.7	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	359	2	0	6	3.1	Cc1ccc([N+](=O)[O-])c(N2CCC(=CC#Cc3ccc(C#N)cn3)CC2)n1	10.1016/j.bmc.2015.05.008
	16659642	89789	0	None	-	1	Rat	7.7	pKi	=	7.7	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	353	1	1	6	3.5	O=c1c2sc3ncc4cn[nH]c4c3c2ncn1-c1ccc(Cl)cc1	10.1021/jm070590c
	CHEMBL238263	89789	0	None	-	1	Rat	7.7	pKi	=	7.7	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	353	1	1	6	3.5	O=c1c2sc3ncc4cn[nH]c4c3c2ncn1-c1ccc(Cl)cc1	10.1021/jm070590c
	11245287	1667	29	None	-	1	Human	8.7	pKi	=	8.7	Binding	Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis	ChEMBL	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	10.1016/j.bmcl.2011.03.046
	6363	1667	29	None	-	1	Human	8.7	pKi	=	8.7	Binding	Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis	ChEMBL	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	10.1016/j.bmcl.2011.03.046
	CHEMBL502882	1667	29	None	-	1	Human	8.7	pKi	=	8.7	Binding	Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis	ChEMBL	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	10.1016/j.bmcl.2011.03.046
	744275	84420	13	None	251	2	Rat	8.7	pKi	=	8.7	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	336	2	0	6	3.4	Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1021/jm0504407
	CHEMBL223496	84420	13	None	251	2	Rat	8.7	pKi	=	8.7	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	336	2	0	6	3.4	Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1021/jm0504407
	16659643	89525	0	None	-	1	Rat	8.6	pKi	=	8.6	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	352	1	1	5	4.1	O=c1c2sc3ncc4cc[nH]c4c3c2ncn1-c1ccc(Cl)cc1	10.1021/jm070590c
	CHEMBL238077	89525	0	None	-	1	Rat	8.6	pKi	=	8.6	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	352	1	1	5	4.1	O=c1c2sc3ncc4cc[nH]c4c3c2ncn1-c1ccc(Cl)cc1	10.1021/jm070590c
	44517772	193883	0	None	38	2	Rat	7.7	pKi	=	7.7	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	317	3	0	2	5.0	O=C(/C=C/c1cnc2ccccc2c1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmc.2009.05.072
	CHEMBL554700	193883	0	None	38	2	Rat	7.7	pKi	=	7.7	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	317	3	0	2	5.0	O=C(/C=C/c1cnc2ccccc2c1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmc.2009.05.072
	71452099	82620	0	None	-	1	Rat	7.7	pKi	=	7.7	Binding	Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting	ChEMBL	387	5	1	6	4.4	CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(Cl)cc3)n2)ncn1	10.1021/jm301597s
	CHEMBL2181521	82620	0	None	-	1	Rat	7.7	pKi	=	7.7	Binding	Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting	ChEMBL	387	5	1	6	4.4	CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(Cl)cc3)n2)ncn1	10.1021/jm301597s
	25067015	193940	0	None	4	3	Rat	7.6	pKi	=	7.6	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	366	4	0	4	3.8	O=C(C1CC1c1ccc(N2CCOCC2)nc1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmc.2009.05.072
	CHEMBL556070	193940	0	None	4	3	Rat	7.6	pKi	=	7.6	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	366	4	0	4	3.8	O=C(C1CC1c1ccc(N2CCOCC2)nc1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmc.2009.05.072
	1310	2286	108	None	-1	18	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm070322e
	1369	2286	108	None	-1	18	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm070322e
	33032	2286	108	None	-1	18	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm070322e
	44272391	2286	108	None	-1	18	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm070322e
	88747398	2286	108	None	-1	18	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm070322e
	CHEMBL575060	2286	108	None	-1	18	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm070322e
	DB00142	2286	108	None	-1	18	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm070322e
	11717319	142962	0	None	-	1	Rat	6.6	pKi	=	6.6	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	353	3	0	8	2.5	COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cn1	10.1021/jm0504407
	CHEMBL389870	142962	0	None	-	1	Rat	6.6	pKi	=	6.6	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	353	3	0	8	2.5	COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cn1	10.1021/jm0504407
	71457446	82617	0	None	-	1	Rat	7.6	pKi	=	7.6	Binding	Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting	ChEMBL	378	5	1	7	3.6	CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(C#N)cc3)n2)ncn1	10.1021/jm301597s
	CHEMBL2181519	82617	0	None	-	1	Rat	7.6	pKi	=	7.6	Binding	Displacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma countingDisplacement of [18F]FITM from mGlu1 receptor in rat brain homogenates after 1 hr by gamma counting	ChEMBL	378	5	1	7	3.6	CC(C)Nc1cc(-c2csc(N(C)C(=O)c3ccc(C#N)cc3)n2)ncn1	10.1021/jm301597s
	44404948	70210	0	None	-	1	Rat	4.6	pKi	=	4.6	Binding	Binding affinity for mGluR1 receptor expressed in CHO cellsBinding affinity for mGluR1 receptor expressed in CHO cells	ChEMBL	214	2	3	5	-1.0	NC1(C(=O)O)CC2ON=C(C(=O)O)C2C1	10.1021/jm0504499
	CHEMBL194787	70210	0	None	-	1	Rat	4.6	pKi	=	4.6	Binding	Binding affinity for mGluR1 receptor expressed in CHO cellsBinding affinity for mGluR1 receptor expressed in CHO cells	ChEMBL	214	2	3	5	-1.0	NC1(C(=O)O)CC2ON=C(C(=O)O)C2C1	10.1021/jm0504499
	10976811	109225	0	None	-	1	Rat	4.6	pKi	=	4.6	Binding	Inhibitory constant against cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cellsInhibitory constant against cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cells	ChEMBL	214	2	3	5	-1.0	N[C@]1(C(=O)O)C[C@@H]2ON=C(C(=O)O)[C@@H]2C1	10.1021/jm0308085
	CHEMBL322887	109225	0	None	-	1	Rat	4.6	pKi	=	4.6	Binding	Inhibitory constant against cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cellsInhibitory constant against cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cells	ChEMBL	214	2	3	5	-1.0	N[C@]1(C(=O)O)C[C@@H]2ON=C(C(=O)O)[C@@H]2C1	10.1021/jm0308085
	16659646	89526	0	None	-	1	Rat	7.5	pKi	=	7.5	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	348	2	1	6	3.5	COc1ccc(-n2cnc3c(sc4ncc5cc[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	CHEMBL238079	89526	0	None	-	1	Rat	7.5	pKi	=	7.5	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	348	2	1	6	3.5	COc1ccc(-n2cnc3c(sc4ncc5cc[nH]c5c43)c2=O)cc1	10.1021/jm070590c
	45273580	194928	0	None	17	2	Rat	6.5	pKi	=	6.5	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	311	4	0	3	4.2	COc1ncc(/C=C/C(=O)C23CC4CC(CC(C4)C2)C3)cc1C	10.1016/j.bmc.2009.05.072
	CHEMBL564089	194928	0	None	17	2	Rat	6.5	pKi	=	6.5	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	311	4	0	3	4.2	COc1ncc(/C=C/C(=O)C23CC4CC(CC(C4)C2)C3)cc1C	10.1016/j.bmc.2009.05.072
	11245287	1667	29	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity to mGluR1Binding affinity to mGluR1	ChEMBL	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	10.1016/j.bmc.2010.11.048
	6363	1667	29	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity to mGluR1Binding affinity to mGluR1	ChEMBL	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	10.1016/j.bmc.2010.11.048
	CHEMBL502882	1667	29	None	-	1	Human	8.4	pKi	=	8.4	Binding	Binding affinity to mGluR1Binding affinity to mGluR1	ChEMBL	358	3	0	5	2.7	CC(N(C(=O)N1CCC(=CC1)c1nnn(c1C)c1cccnc1F)C)C	10.1016/j.bmc.2010.11.048
	118718092	120084	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells	ChEMBL	215	3	3	6	-0.4	N[C@]1(C(=O)O)C[C@H]1Cc1nsnc1O	10.1039/C1MD00186H
	CHEMBL3347672	120084	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells	ChEMBL	215	3	3	6	-0.4	N[C@]1(C(=O)O)C[C@H]1Cc1nsnc1O	10.1039/C1MD00186H
	CHEMBL3545861	120084	0	None	-	1	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells	ChEMBL	215	3	3	6	-0.4	N[C@]1(C(=O)O)C[C@H]1Cc1nsnc1O	10.1039/C1MD00186H
	25066817	193637	0	None	60	2	Rat	6.5	pKi	=	6.5	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	311	4	0	3	4.0	COc1ccc(C2CC2C(=O)C23CC4CC(CC(C4)C2)C3)cn1	10.1016/j.bmc.2009.05.072
	CHEMBL551469	193637	0	None	60	2	Rat	6.5	pKi	=	6.5	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	311	4	0	3	4.0	COc1ccc(C2CC2C(=O)C23CC4CC(CC(C4)C2)C3)cn1	10.1016/j.bmc.2009.05.072
	12991435	71948	0	None	-	1	Rat	4.5	pKi	=	4.5	Binding	Binding affinity for mGluR1 receptor expressed in CHO cellsBinding affinity for mGluR1 receptor expressed in CHO cells	ChEMBL	214	2	3	5	-1.0	N[C@@]1(C(=O)O)C[C@H]2ON=C(C(=O)O)[C@H]2C1	10.1021/jm0504499
	CHEMBL198310	71948	0	None	-	1	Rat	4.5	pKi	=	4.5	Binding	Binding affinity for mGluR1 receptor expressed in CHO cellsBinding affinity for mGluR1 receptor expressed in CHO cells	ChEMBL	214	2	3	5	-1.0	N[C@@]1(C(=O)O)C[C@H]2ON=C(C(=O)O)[C@H]2C1	10.1021/jm0504499
	1310	2286	108	None	-4	18	Rat	6.5	pKi	=	6.5	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm010323l
	1369	2286	108	None	-4	18	Rat	6.5	pKi	=	6.5	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm010323l
	33032	2286	108	None	-4	18	Rat	6.5	pKi	=	6.5	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm010323l
	44272391	2286	108	None	-4	18	Rat	6.5	pKi	=	6.5	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm010323l
	88747398	2286	108	None	-4	18	Rat	6.5	pKi	=	6.5	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm010323l
	CHEMBL575060	2286	108	None	-4	18	Rat	6.5	pKi	=	6.5	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm010323l
	DB00142	2286	108	None	-4	18	Rat	6.5	pKi	=	6.5	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1021/jm010323l
	17758443	85713	2	None	1	2	Human	4.5	pKi	=	4.5	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	ChEMBL	195	3	3	4	-1.3	N[C@H](C(=O)O)[C@H]1C[C@@H]1S(=O)(=O)O	10.1021/jm070322e
	CHEMBL231157	85713	2	None	1	2	Human	4.5	pKi	=	4.5	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	ChEMBL	195	3	3	4	-1.3	N[C@H](C(=O)O)[C@H]1C[C@@H]1S(=O)(=O)O	10.1021/jm070322e
	3115037	193515	7	None	-	1	Rat	4.4	pKi	=	4.4	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	282	4	0	3	3.8	CC(CC(=O)c1ccc2c(c1)OCCO2)c1ccccc1	10.1016/j.bmc.2009.05.072
	CHEMBL550523	193515	7	None	-	1	Rat	4.4	pKi	=	4.4	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	282	4	0	3	3.8	CC(CC(=O)c1ccc2c(c1)OCCO2)c1ccccc1	10.1016/j.bmc.2009.05.072
	1418	3393	48	None	21	2	Rat	5.4	pKi	=	5.4	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	10.1021/jm010323l
	5311459	3393	48	None	21	2	Rat	5.4	pKi	=	5.4	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	10.1021/jm010323l
	CHEMBL94990	3393	48	None	21	2	Rat	5.4	pKi	=	5.4	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	10.1021/jm010323l
	86627336	121687	2	None	-389	3	Rat	7.4	pKi	=	7.4	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	320	2	0	5	3.0	O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2ccccn2)CC1	10.1016/j.bmc.2015.05.008
	CHEMBL3597593	121687	2	None	-389	3	Rat	7.4	pKi	=	7.4	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	320	2	0	5	3.0	O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2ccccn2)CC1	10.1016/j.bmc.2015.05.008
	11688880	84641	0	None	616	2	Rat	8.4	pKi	=	8.4	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	350	2	0	6	3.7	Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c(C)c1	10.1021/jm0504407
	CHEMBL224356	84641	0	None	616	2	Rat	8.4	pKi	=	8.4	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	350	2	0	6	3.7	Cc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c(C)c1	10.1021/jm0504407
	1069776	84798	11	None	257	2	Rat	8.4	pKi	=	8.4	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	356	2	0	6	3.7	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1021/jm0504407
	CHEMBL225589	84798	11	None	257	2	Rat	8.4	pKi	=	8.4	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	356	2	0	6	3.7	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(Cl)cc4)cnc3c12	10.1021/jm0504407
	18003010	76438	10	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity to mGluR1Binding affinity to mGluR1	ChEMBL	414	7	0	6	4.0	COCCN(C)Cc1ccc2nc3sc(C(=O)N(C)C4CCCCC4)cn3c2c1	10.1016/j.bmc.2010.11.048
	CHEMBL1645351	76438	10	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity to mGluR1Binding affinity to mGluR1	ChEMBL	414	7	0	6	4.0	COCCN(C)Cc1ccc2nc3sc(C(=O)N(C)C4CCCCC4)cn3c2c1	10.1016/j.bmc.2010.11.048
	CHEMBL1771388	76438	10	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity to mGluR1Binding affinity to mGluR1	ChEMBL	414	7	0	6	4.0	COCCN(C)Cc1ccc2nc3sc(C(=O)N(C)C4CCCCC4)cn3c2c1	10.1016/j.bmc.2010.11.048
	CHEMBL2068815	76438	10	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity to mGluR1Binding affinity to mGluR1	ChEMBL	414	7	0	6	4.0	COCCN(C)Cc1ccc2nc3sc(C(=O)N(C)C4CCCCC4)cn3c2c1	10.1016/j.bmc.2010.11.048
	18003010	76438	10	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis	ChEMBL	414	7	0	6	4.0	COCCN(C)Cc1ccc2nc3sc(C(=O)N(C)C4CCCCC4)cn3c2c1	10.1016/j.bmcl.2011.03.046
	CHEMBL1645351	76438	10	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis	ChEMBL	414	7	0	6	4.0	COCCN(C)Cc1ccc2nc3sc(C(=O)N(C)C4CCCCC4)cn3c2c1	10.1016/j.bmcl.2011.03.046
	CHEMBL1771388	76438	10	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis	ChEMBL	414	7	0	6	4.0	COCCN(C)Cc1ccc2nc3sc(C(=O)N(C)C4CCCCC4)cn3c2c1	10.1016/j.bmcl.2011.03.046
	CHEMBL2068815	76438	10	None	-	1	Human	8.3	pKi	=	8.3	Binding	Binding affinity to mGluR1 by PET analysisBinding affinity to mGluR1 by PET analysis	ChEMBL	414	7	0	6	4.0	COCCN(C)Cc1ccc2nc3sc(C(=O)N(C)C4CCCCC4)cn3c2c1	10.1016/j.bmcl.2011.03.046
	25183673	121686	0	None	-12	3	Rat	8.3	pKi	=	8.3	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	319	2	0	4	3.6	O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2ccccc2)CC1	10.1016/j.bmc.2015.05.008
	CHEMBL3597592	121686	0	None	-12	3	Rat	8.3	pKi	=	8.3	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	319	2	0	4	3.6	O=[N+]([O-])c1cccnc1N1CCC(=CC#Cc2ccccc2)CC1	10.1016/j.bmc.2015.05.008
	155549638	173276	0	None	-165	2	Rat	6.4	pKi	=	6.4	Binding	Displacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysis	ChEMBL	360	3	0	3	4.1	Cc1cccc(C#CC=C2CCN(C(=O)OCCc3ccccc3)CC2)n1	10.1021/acs.jmedchem.8b01226
	CHEMBL4539036	173276	0	None	-165	2	Rat	6.4	pKi	=	6.4	Binding	Displacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysisDisplacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysis	ChEMBL	360	3	0	3	4.1	Cc1cccc(C#CC=C2CCN(C(=O)OCCc3ccccc3)CC2)n1	10.1021/acs.jmedchem.8b01226
	10513894	79250	0	None	-	1	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards metabotropic glutamate receptor mGluR1Binding affinity towards metabotropic glutamate receptor mGluR1	ChEMBL	235	4	3	3	0.5	N[C@@H](C(=O)O)[C@@H]1[C@H](C(=O)O)[C@@H]1c1ccccc1	10.1021/jm960059+
	CHEMBL2115152	79250	0	None	-	1	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards metabotropic glutamate receptor mGluR1Binding affinity towards metabotropic glutamate receptor mGluR1	ChEMBL	235	4	3	3	0.5	N[C@@H](C(=O)O)[C@@H]1[C@H](C(=O)O)[C@@H]1c1ccccc1	10.1021/jm960059+
	87550659	121695	0	None	-891	3	Rat	6.4	pKi	=	6.4	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	390	2	0	4	4.9	Cc1cccc(C#CC=C2CCN(c3ncc(-c4ccccc4)cc3C#N)CC2)n1	10.1016/j.bmc.2015.05.008
	CHEMBL3597602	121695	0	None	-891	3	Rat	6.4	pKi	=	6.4	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	390	2	0	4	4.9	Cc1cccc(C#CC=C2CCN(c3ncc(-c4ccccc4)cc3C#N)CC2)n1	10.1016/j.bmc.2015.05.008
	11530404	208	11	None	38	2	Rat	8.3	pKi	=	8.3	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1021/jm0504407
	6211	208	11	None	38	2	Rat	8.3	pKi	=	8.3	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1021/jm0504407
	CHEMBL385336	208	11	None	38	2	Rat	8.3	pKi	=	8.3	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	350	3	0	6	3.6	CCc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(ccn1)N(C)C	10.1021/jm0504407
	16660135	1612	30	None	-	1	Rat	8.3	pKi	=	8.3	Binding	Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr	ChEMBL	371	5	1	6	3.8	CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C	10.1021/jm201590g
	8767	1612	30	None	-	1	Rat	8.3	pKi	=	8.3	Binding	Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr	ChEMBL	371	5	1	6	3.8	CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C	10.1021/jm201590g
	CHEMBL566581	1612	30	None	-	1	Rat	8.3	pKi	=	8.3	Binding	Displacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hrDisplacement of 4-[18F]fluoro-N-[4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide from mGluR1 in Sprague-Dawley rat brain homogenates after 1 hr	ChEMBL	371	5	1	6	3.8	CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C	10.1021/jm201590g
	1222	101267	56	None	-5	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards mGluR1a was determinedBinding affinity towards mGluR1a was determined	ChEMBL	209	3	3	3	0.6	CC(N)(C(=O)O)c1ccc(C(=O)O)cc1	10.1021/jm960059+
	CHEMBL299683	101267	56	None	-5	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards mGluR1a was determinedBinding affinity towards mGluR1a was determined	ChEMBL	209	3	3	3	0.6	CC(N)(C(=O)O)c1ccc(C(=O)O)cc1	10.1021/jm960059+
	11644388	196132	0	None	5	2	Rat	5.3	pKi	=	5.3	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	239	2	0	2	3.9	CC(C)(C)C(=O)/C=C/c1cnc2ccccc2c1	10.1016/j.bmc.2009.05.072
	CHEMBL572128	196132	0	None	5	2	Rat	5.3	pKi	=	5.3	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	239	2	0	2	3.9	CC(C)(C)C(=O)/C=C/c1cnc2ccccc2c1	10.1016/j.bmc.2009.05.072
	122183732	121684	0	None	-41	2	Rat	7.3	pKi	=	7.3	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	362	3	0	5	2.3	C=Cc1ccc([N+](=O)[O-])c(N2CCN(C(=O)C#Cc3ccccc3)CC2)n1	10.1016/j.bmc.2015.05.008
	CHEMBL3597586	121684	0	None	-41	2	Rat	7.3	pKi	=	7.3	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	362	3	0	5	2.3	C=Cc1ccc([N+](=O)[O-])c(N2CCN(C(=O)C#Cc3ccccc3)CC2)n1	10.1016/j.bmc.2015.05.008
	1310	2286	108	None	-1	18	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmc.2008.11.015
	1369	2286	108	None	-1	18	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmc.2008.11.015
	33032	2286	108	None	-1	18	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmc.2008.11.015
	44272391	2286	108	None	-1	18	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmc.2008.11.015
	88747398	2286	108	None	-1	18	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmc.2008.11.015
	CHEMBL575060	2286	108	None	-1	18	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmc.2008.11.015
	DB00142	2286	108	None	-1	18	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells	ChEMBL	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	10.1016/j.bmc.2008.11.015
	44569859	178009	0	None	-	1	Human	4.2	pKi	=	4.2	Binding	Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells	ChEMBL	213	5	3	3	0.4	N[C@@H](CC12CC(CC(=O)O)(C1)C2)C(=O)O	10.1016/j.bmc.2008.11.015
	CHEMBL467234	178009	0	None	-	1	Human	4.2	pKi	=	4.2	Binding	Displacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cellsDisplacement of [3H]Quisqualate from human mGluR1A receptor expressed in BHK cells	ChEMBL	213	5	3	3	0.4	N[C@@H](CC12CC(CC(=O)O)(C1)C2)C(=O)O	10.1016/j.bmc.2008.11.015
	11717278	84614	0	None	102	2	Rat	8.2	pKi	=	8.2	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	350	3	0	6	3.6	CCc1cccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c1	10.1021/jm0504407
	CHEMBL224084	84614	0	None	102	2	Rat	8.2	pKi	=	8.2	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	350	3	0	6	3.6	CCc1cccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)c1	10.1021/jm0504407
	10489913	79140	0	None	-	1	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards metabotropic glutamate receptor mGluR1Binding affinity towards metabotropic glutamate receptor mGluR1	ChEMBL	235	4	3	3	0.5	N[C@H](C(=O)O)[C@@H]1[C@H](c2ccccc2)[C@H]1C(=O)O	10.1021/jm960059+
	CHEMBL2114116	79140	0	None	-	1	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards metabotropic glutamate receptor mGluR1Binding affinity towards metabotropic glutamate receptor mGluR1	ChEMBL	235	4	3	3	0.5	N[C@H](C(=O)O)[C@@H]1[C@H](c2ccccc2)[C@H]1C(=O)O	10.1021/jm960059+
	45082292	114752	2	None	3	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells	ChEMBL	159	3	3	3	-0.7	N[C@@]1(C(=O)O)C[C@@H]1CC(=O)O	10.1039/C1MD00186H
	CHEMBL3347670	114752	2	None	3	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cellsDisplacement of [3H]-Quisqualate from human mGluR1 receptor expressed in HEK cells	ChEMBL	159	3	3	3	-0.7	N[C@@]1(C(=O)O)C[C@@H]1CC(=O)O	10.1039/C1MD00186H
	11537814	84770	0	None	19	2	Rat	7.2	pKi	=	7.2	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	362	2	1	7	2.9	CN(C)c1ccnc2sc3c(=O)n(-c4ccc5cn[nH]c5c4)cnc3c12	10.1021/jm0504407
	CHEMBL225438	84770	0	None	19	2	Rat	7.2	pKi	=	7.2	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	362	2	1	7	2.9	CN(C)c1ccnc2sc3c(=O)n(-c4ccc5cn[nH]c5c4)cnc3c12	10.1021/jm0504407
	45273579	194014	0	None	9	2	Rat	6.2	pKi	=	6.2	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	325	3	0	4	3.7	O=C(/C=C/c1cnc2c(c1)OCCO2)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmc.2009.05.072
	CHEMBL556707	194014	0	None	9	2	Rat	6.2	pKi	=	6.2	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	325	3	0	4	3.7	O=C(/C=C/c1cnc2c(c1)OCCO2)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmc.2009.05.072
	122183731	121683	0	None	-173	3	Rat	7.2	pKi	=	7.2	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	335	2	0	4	2.3	O=C(C#Cc1ccccc1)N1CCN(c2ccccc2[N+](=O)[O-])CC1	10.1016/j.bmc.2015.05.008
	CHEMBL3597585	121683	0	None	-173	3	Rat	7.2	pKi	=	7.2	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	335	2	0	4	2.3	O=C(C#Cc1ccccc1)N1CCN(c2ccccc2[N+](=O)[O-])CC1	10.1016/j.bmc.2015.05.008
	1208332	166502	12	None	-	1	Rat	8.1	pKi	=	8.1	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	352	3	0	7	3.1	COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1021/jm070590c
	CHEMBL428909	166502	12	None	-	1	Rat	8.1	pKi	=	8.1	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	352	3	0	7	3.1	COc1ccc(-n2cnc3c(sc4nccc(N(C)C)c43)c2=O)cc1	10.1021/jm070590c
	25183670	121690	0	None	-354	3	Rat	7.2	pKi	=	7.2	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	333	2	0	4	3.9	Cc1cccc(C#CC=C2CCN(c3ccccc3[N+](=O)[O-])CC2)n1	10.1016/j.bmc.2015.05.008
	CHEMBL3597596	121690	0	None	-354	3	Rat	7.2	pKi	=	7.2	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	333	2	0	4	3.9	Cc1cccc(C#CC=C2CCN(c3ccccc3[N+](=O)[O-])CC2)n1	10.1016/j.bmc.2015.05.008
	25066816	193108	0	None	3	2	Rat	5.2	pKi	=	5.2	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	281	3	0	2	4.0	O=C(C1CC1c1cccnc1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmc.2009.05.072
	CHEMBL538307	193108	0	None	3	2	Rat	5.2	pKi	=	5.2	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	281	3	0	2	4.0	O=C(C1CC1c1cccnc1)C12CC3CC(CC(C3)C1)C2	10.1016/j.bmc.2009.05.072
	44385546	128503	0	None	-1	2	Rat	4.2	pKi	=	4.2	Binding	The compound was tested for the receptor binding affinity at Metabotropic glutamate receptor 1 using established second messenger assay systems.The compound was tested for the receptor binding affinity at Metabotropic glutamate receptor 1 using established second messenger assay systems.	ChEMBL	264	4	4	6	0.7	N[C@@H](Cc1onc(O)c1-c1ccc(O)cc1)C(=O)O	10.1021/jm010443t
	CHEMBL367027	128503	0	None	-1	2	Rat	4.2	pKi	=	4.2	Binding	The compound was tested for the receptor binding affinity at Metabotropic glutamate receptor 1 using established second messenger assay systems.The compound was tested for the receptor binding affinity at Metabotropic glutamate receptor 1 using established second messenger assay systems.	ChEMBL	264	4	4	6	0.7	N[C@@H](Cc1onc(O)c1-c1ccc(O)cc1)C(=O)O	10.1021/jm010443t
	17758554	142582	2	None	1	2	Human	4.1	pKi	=	4.1	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	ChEMBL	195	3	3	4	-1.3	N[C@H](C(=O)O)[C@@H]1C[C@H]1S(=O)(=O)O	10.1021/jm070322e
	CHEMBL389555	142582	2	None	1	2	Human	4.1	pKi	=	4.1	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	ChEMBL	195	3	3	4	-1.3	N[C@H](C(=O)O)[C@@H]1C[C@H]1S(=O)(=O)O	10.1021/jm070322e
	1377	1313	19	None	-1230	6	Rat	4.1	pKi	=	4.1	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	203	4	4	4	-1.6	N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O	10.1021/jm010323l
	5310979	1313	19	None	-1230	6	Rat	4.1	pKi	=	4.1	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	203	4	4	4	-1.6	N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O	10.1021/jm010323l
	CHEMBL284193	1313	19	None	-1230	6	Rat	4.1	pKi	=	4.1	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	203	4	4	4	-1.6	N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O	10.1021/jm010323l
	16659798	88217	0	None	-	1	Rat	6.1	pKi	=	6.1	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	396	2	0	8	4.6	CSc1nc2c(cnc3sc4c(=O)n(-c5ccc(C)cc5)cnc4c32)s1	10.1021/jm070590c
	CHEMBL235767	88217	0	None	-	1	Rat	6.1	pKi	=	6.1	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	396	2	0	8	4.6	CSc1nc2c(cnc3sc4c(=O)n(-c5ccc(C)cc5)cnc4c32)s1	10.1021/jm070590c
	11560185	84643	0	None	-	1	Rat	8.1	pKi	=	8.1	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	390	2	0	6	4.1	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12	10.1021/jm0504407
	CHEMBL224375	84643	0	None	-	1	Rat	8.1	pKi	=	8.1	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	390	2	0	6	4.1	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(C(F)(F)F)cc4)cnc3c12	10.1021/jm0504407
	11667270	84728	0	None	-	1	Rat	8.1	pKi	=	8.1	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	340	2	0	6	3.2	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1021/jm0504407
	CHEMBL225124	84728	0	None	-	1	Rat	8.1	pKi	=	8.1	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	340	2	0	6	3.2	CN(C)c1ccnc2sc3c(=O)n(-c4ccc(F)cc4)cnc3c12	10.1021/jm0504407
	657896	141550	10	None	-	1	Rat	7.1	pKi	=	7.1	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	336	3	0	6	3.1	CN(C)c1ccnc2sc3c(=O)n(Cc4ccccc4)cnc3c12	10.1021/jm0504407
	CHEMBL388087	141550	10	None	-	1	Rat	7.1	pKi	=	7.1	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	336	3	0	6	3.1	CN(C)c1ccnc2sc3c(=O)n(Cc4ccccc4)cnc3c12	10.1021/jm0504407
	177491	85662	37	None	-1	3	Human	4.1	pKi	=	4.1	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	ChEMBL	183	4	3	4	-1.3	N[C@@H](CCS(=O)(=O)O)C(=O)O	10.1021/jm070322e
	CHEMBL230951	85662	37	None	-1	3	Human	4.1	pKi	=	4.1	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	ChEMBL	183	4	3	4	-1.3	N[C@@H](CCS(=O)(=O)O)C(=O)O	10.1021/jm070322e
	16659804	88316	0	None	-	1	Rat	8.0	pKi	=	8.0	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	384	1	1	7	3.8	C[C@@H]1COc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c2N1	10.1021/jm070590c
	CHEMBL236178	88316	0	None	-	1	Rat	8.0	pKi	=	8.0	Binding	Displacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membraneDisplacement of [3H]9-Dimethylamino-3-(4-methoxy-phenyl)-3H-pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-one from mGluR1 in rat cerebellum membrane	ChEMBL	384	1	1	7	3.8	C[C@@H]1COc2cnc3sc4c(=O)n(-c5ccc(Cl)cc5)cnc4c3c2N1	10.1021/jm070590c
	443586	145919	47	None	2	3	Rat	6.1	pKi	=	6.1	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	183	2	4	4	0.2	N[C@H](C(=O)O)c1cc(O)cc(O)c1	10.1021/jm010323l
	71668376	145919	47	None	2	3	Rat	6.1	pKi	=	6.1	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	183	2	4	4	0.2	N[C@H](C(=O)O)c1cc(O)cc(O)c1	10.1021/jm010323l
	CHEMBL39221	145919	47	None	2	3	Rat	6.1	pKi	=	6.1	Binding	Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cellsInhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells	ChEMBL	183	2	4	4	0.2	N[C@H](C(=O)O)c1cc(O)cc(O)c1	10.1021/jm010323l
	5766222	194238	17	None	-	1	Rat	5.0	pKi	=	5.0	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	307	3	0	2	5.1	Cc1ccc2nc(Cl)c(/C=C/C(=O)c3ccccc3)cc2c1	10.1016/j.bmc.2009.05.072
	CHEMBL559243	194238	17	None	-	1	Rat	5.0	pKi	=	5.0	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	307	3	0	2	5.1	Cc1ccc2nc(Cl)c(/C=C/C(=O)c3ccccc3)cc2c1	10.1016/j.bmc.2009.05.072
	44386146	128950	0	None	-1	2	Rat	4.0	pKi	=	4.0	Binding	The compound was tested for the receptor binding affinity at Metabotropic glutamate receptor 1 using established second messenger assay systems.The compound was tested for the receptor binding affinity at Metabotropic glutamate receptor 1 using established second messenger assay systems.	ChEMBL	276	6	3	5	1.1	N[C@@H](Cc1onc(O)c1CCc1ccccc1)C(=O)O	10.1021/jm010443t
	CHEMBL367189	128950	0	None	-1	2	Rat	4.0	pKi	=	4.0	Binding	The compound was tested for the receptor binding affinity at Metabotropic glutamate receptor 1 using established second messenger assay systems.The compound was tested for the receptor binding affinity at Metabotropic glutamate receptor 1 using established second messenger assay systems.	ChEMBL	276	6	3	5	1.1	N[C@@H](Cc1onc(O)c1CCc1ccccc1)C(=O)O	10.1021/jm010443t
	44404948	70210	0	None	-	1	Rat	4.0	pKi	=	4.0	Binding	Binding affinity for mGluR1 receptor expressed in CHO cellsBinding affinity for mGluR1 receptor expressed in CHO cells	ChEMBL	214	2	3	5	-1.0	NC1(C(=O)O)CC2ON=C(C(=O)O)C2C1	10.1021/jm0504499
	CHEMBL194787	70210	0	None	-	1	Rat	4.0	pKi	=	4.0	Binding	Binding affinity for mGluR1 receptor expressed in CHO cellsBinding affinity for mGluR1 receptor expressed in CHO cells	ChEMBL	214	2	3	5	-1.0	NC1(C(=O)O)CC2ON=C(C(=O)O)C2C1	10.1021/jm0504499
	10353177	163907	0	None	-	1	Rat	4.0	pKi	=	4.0	Binding	Inhibitory constant against cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cellsInhibitory constant against cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cells	ChEMBL	214	2	3	5	-1.0	N[C@@]1(C(=O)O)C[C@@H]2ON=C(C(=O)O)[C@@H]2C1	10.1021/jm0308085
	CHEMBL421402	163907	0	None	-	1	Rat	4.0	pKi	=	4.0	Binding	Inhibitory constant against cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cellsInhibitory constant against cloned rat Metabotropic glutamate receptor 1 expressed in Chinese Hamster Ovary (CHO) cells	ChEMBL	214	2	3	5	-1.0	N[C@@]1(C(=O)O)C[C@@H]2ON=C(C(=O)O)[C@@H]2C1	10.1021/jm0308085
	10353177	163907	0	None	-	1	Rat	4.0	pKi	=	4.0	Binding	Binding affinity for mGluR1 receptor expressed in CHO cellsBinding affinity for mGluR1 receptor expressed in CHO cells	ChEMBL	214	2	3	5	-1.0	N[C@@]1(C(=O)O)C[C@@H]2ON=C(C(=O)O)[C@@H]2C1	10.1021/jm0504499
	CHEMBL421402	163907	0	None	-	1	Rat	4.0	pKi	=	4.0	Binding	Binding affinity for mGluR1 receptor expressed in CHO cellsBinding affinity for mGluR1 receptor expressed in CHO cells	ChEMBL	214	2	3	5	-1.0	N[C@@]1(C(=O)O)C[C@@H]2ON=C(C(=O)O)[C@@H]2C1	10.1021/jm0504499
	10382361	121682	0	None	-194	3	Rat	7.0	pKi	=	7.0	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	336	2	0	5	1.7	O=C(C#Cc1ccccc1)N1CCN(c2ncccc2[N+](=O)[O-])CC1	10.1016/j.bmc.2015.05.008
	CHEMBL3597584	121682	0	None	-194	3	Rat	7.0	pKi	=	7.0	Binding	Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometryDisplacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry	ChEMBL	336	2	0	5	1.7	O=C(C#Cc1ccccc1)N1CCN(c2ncccc2[N+](=O)[O-])CC1	10.1016/j.bmc.2015.05.008
	11695769	143006	0	None	-	1	Rat	7.0	pKi	=	7	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	338	2	1	7	2.8	CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4O)cnc3c12	10.1021/jm0504407
	CHEMBL389897	143006	0	None	-	1	Rat	7.0	pKi	=	7	Binding	Displacement of [3H]R214127 from mGluR1 in rat cerebellum membranesDisplacement of [3H]R214127 from mGluR1 in rat cerebellum membranes	ChEMBL	338	2	1	7	2.8	CN(C)c1ccnc2sc3c(=O)n(-c4ccccc4O)cnc3c12	10.1021/jm0504407
	5766229	194243	6	None	-	1	Rat	5.0	pKi	=	5	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	313	3	0	3	5.2	Cc1ccc2nc(Cl)c(/C=C/C(=O)c3cccs3)cc2c1	10.1016/j.bmc.2009.05.072
	CHEMBL559310	194243	6	None	-	1	Rat	5.0	pKi	=	5	Binding	Displacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation countingDisplacement of [3H]E-3-(2-chloro-8-methylquinolin-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one from mGluR1 in rat cerebellar membrane after 14 to 16 hrs by scintillation counting	ChEMBL	313	3	0	3	5.2	Cc1ccc2nc(Cl)c(/C=C/C(=O)c3cccs3)cc2c1	10.1016/j.bmc.2009.05.072
	1389	4055	0	None	-	1	Rat	7.5	pKd	=	7.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	342	2	1	5	3.8	CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1	15976016
	5392	4055	0	None	-	1	Rat	7.5	pKd	=	7.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	342	2	1	5	3.8	CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1	15976016
	9819432	4055	0	None	-	1	Rat	7.5	pKd	=	7.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	342	2	1	5	3.8	CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1	15976016
	CHEMBL1517556	4055	0	None	-	1	Rat	7.5	pKd	=	7.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	342	2	1	5	3.8	CN(C(=O)c1sc2n(c1C)c1c(n2)ccc(c1)N)C1CCCCC1	15976016
	1370	3212	62	None	44	8	Rat	7.6	pKd	None	7.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	12509432
	1370	3212	62	None	44	8	Rat	7.6	pKd	None	7.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	12695537
	1372	3212	62	None	44	8	Rat	7.6	pKd	None	7.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	12509432
	1372	3212	62	None	44	8	Rat	7.6	pKd	None	7.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	12695537
	40539	3212	62	None	44	8	Rat	7.6	pKd	None	7.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	12509432
	40539	3212	62	None	44	8	Rat	7.6	pKd	None	7.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	12695537
	6971145	3212	62	None	44	8	Rat	7.6	pKd	None	7.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	12509432
	6971145	3212	62	None	44	8	Rat	7.6	pKd	None	7.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	12695537
	CHEMBL279956	3212	62	None	44	8	Rat	7.6	pKd	None	7.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	12509432
	CHEMBL279956	3212	62	None	44	8	Rat	7.6	pKd	None	7.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	12695537
	DB02999	3212	62	None	44	8	Rat	7.6	pKd	None	7.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	12509432
	DB02999	3212	62	None	44	8	Rat	7.6	pKd	None	7.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	12695537
	1390	1526	0	None	-	1	Rat	8.2	pKd	None	8.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	308	2	0	5	2.0	CCn1c(C)nc(c(c1=O)C#N)N1CCc2c(CC1)cccc2	12509432
	3363	1526	0	None	-	1	Rat	8.2	pKd	None	8.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	308	2	0	5	2.0	CCn1c(C)nc(c(c1=O)C#N)N1CCc2c(CC1)cccc2	12509432
	9904703	1526	0	None	-	1	Rat	8.2	pKd	None	8.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	308	2	0	5	2.0	CCn1c(C)nc(c(c1=O)C#N)N1CCc2c(CC1)cccc2	12509432
	10470232	3218	18	None	1	2	Human	9.0	pKd	None	9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	12695537
	1391	3218	18	None	1	2	Human	9.0	pKd	None	9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	12695537
	6336	3218	18	None	1	2	Human	9.0	pKd	None	9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	12695537
	CHEMBL369459	3218	18	None	1	2	Human	9.0	pKd	None	9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	12695537
	1310	2286	108	Functional	-4	18	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	1369	2286	108	Functional	-4	18	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	33032	2286	108	Functional	-4	18	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	44272391	2286	108	Functional	-4	18	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	88747398	2286	108	Functional	-4	18	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	CHEMBL575060	2286	108	Functional	-4	18	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	DB00142	2286	108	Functional	-4	18	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	134	2478	19	Functional	-8511	67	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	None
	1775	2478	19	Functional	-8511	67	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	None
	9681	2478	19	Functional	-8511	67	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	None
	CHEMBL1065	2478	19	Functional	-8511	67	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	None
	DB00247	2478	19	Functional	-8511	67	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	None
	15897	2817	0	Functional	-354	36	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	203	2	1	1	2.6	CC(Cc1cccc(c1)C(F)(F)F)N	None
	215	2817	0	Functional	-354	36	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	203	2	1	1	2.6	CC(Cc1cccc(c1)C(F)(F)F)N	None
	CHEMBL1979333	2817	0	Functional	-354	36	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	203	2	1	1	2.6	CC(Cc1cccc(c1)C(F)(F)F)N	None
	128563	3408	28	Functional	-2398	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	432	3	0	8	3.0	COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1	None
	1666	3408	28	Functional	-2398	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	432	3	0	8	3.0	COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1	None
	CHEMBL445332	3408	28	Functional	-2398	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	432	3	0	8	3.0	COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1	None
	DB12327	3408	28	Functional	-2398	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	432	3	0	8	3.0	COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1	None
	10297	26905	29	Functional	-38	43	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	151	2	2	2	1.1	C[C@H](N)[C@H](O)c1ccccc1	None
	CHEMBL136560	26905	29	Functional	-38	43	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	151	2	2	2	1.1	C[C@H](N)[C@H](O)c1ccccc1	None
	446220	132998	13	Functional	-1778	45	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	303	3	0	5	1.9	COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C	None
	CHEMBL370805	132998	13	Functional	-1778	45	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	303	3	0	5	1.9	COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C	None
	1615	167228	22	Functional	-26	44	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	193	3	1	3	1.6	CNC(C)Cc1ccc2c(c1)OCO2	None
	CHEMBL43048	167228	22	Functional	-26	44	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	193	3	1	3	1.6	CNC(C)Cc1ccc2c(c1)OCO2	None
	162265	200587	19	Functional	-239	44	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	151	2	2	2	1.1	CC(N)C(O)c1ccccc1	None
	4786	200587	19	Functional	-239	44	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	151	2	2	2	1.1	CC(N)C(O)c1ccccc1	None
	CHEMBL61006	200587	19	Functional	-239	44	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	151	2	2	2	1.1	CC(N)C(O)c1ccccc1	None
	11954224	214174	0	Functional	-141253	59	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	581	4	3	6	2.0	CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C	None
	6971132	214235	0	3H-YM-298198	-2570	14	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	268	1	2	2	2.1	CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)O	None
	None	214412	0	Functional	-2	7	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	173	2	3	3	-0.3	C1CC(CC1C(=O)O)(C(=O)O)N	None
	25137849	214425	0	Functional	-4	40	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	165	3	2	2	1.3	CC(C(C1=CC=CC=C1)O)NC	None
	71290	214425	0	Functional	-4	40	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	165	3	2	2	1.3	CC(C(C1=CC=CC=C1)O)NC	None
	3337	214441	0	Functional	-1513	40	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)CC1=CC(=CC=C1)C(F)(F)F	None
	65801	214441	0	Functional	-1513	40	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)CC1=CC(=CC=C1)C(F)(F)F	None
	66264	214441	0	Functional	-1513	40	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)CC1=CC(=CC=C1)C(F)(F)F	None
	91452	214441	0	Functional	-1513	40	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)CC1=CC(=CC=C1)C(F)(F)F	None
	None	214565	0	Functional	-1	39	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	153	3	3	3	-1.4	C(C(C(=O)O)N)S(=O)O	None
	None	214566	0	Functional	-1	38	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	169	3	3	4	-1.7	C(C(C(=O)O)N)S(=O)(=O)O	None
	None	214574	0	Functional	-13	40	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	149	2	1	2	1.2	CC(C(=O)C1=CC=CC=C1)N	None
	1576	214575	0	Functional	-16	40	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	163	3	1	2	1.5	CC(C(=O)C1=CC=CC=C1)NC	None
	135398740	215983	0	None	-1	2	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	255	5	4	8	-2.0	NC1=NC2=C(N=CN2COC(CO)CO)C(=O)N1	None
	1310	2286	108	None	-1	18	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	Drug Central	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	1369	2286	108	None	-1	18	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	Drug Central	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	33032	2286	108	None	-1	18	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	Drug Central	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	44272391	2286	108	None	-1	18	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	Drug Central	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	88747398	2286	108	None	-1	18	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	Drug Central	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	CHEMBL575060	2286	108	None	-1	18	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	Drug Central	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	DB00142	2286	108	None	-1	18	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cellsDisplacement of [3H]quisqualate from mGluR1 receptor expressed in BHK cells	Drug Central	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	None
	16660135	1612	30	None	-	1	Rat	8.3	pKi	=	8.3	Binding	Measured using rat brain homogenate in a competition binding assay displacing [<sup>18</sup>F}-FITM.Measured using rat brain homogenate in a competition binding assay displacing [<sup>18</sup>F}-FITM.	Guide to Pharmacology	371	5	1	6	3.8	CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C	22316010
	8767	1612	30	None	-	1	Rat	8.3	pKi	=	8.3	Binding	Measured using rat brain homogenate in a competition binding assay displacing [<sup>18</sup>F}-FITM.Measured using rat brain homogenate in a competition binding assay displacing [<sup>18</sup>F}-FITM.	Guide to Pharmacology	371	5	1	6	3.8	CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C	22316010
	CHEMBL566581	1612	30	None	-	1	Rat	8.3	pKi	=	8.3	Binding	Measured using rat brain homogenate in a competition binding assay displacing [<sup>18</sup>F}-FITM.Measured using rat brain homogenate in a competition binding assay displacing [<sup>18</sup>F}-FITM.	Guide to Pharmacology	371	5	1	6	3.8	CC(Nc1ncnc(c1)c1csc(n1)N(C(=O)c1ccc(cc1)F)C)C	22316010
	1387	3311	0	None	-	1	Rat	5.1	pKi	=	5.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	325	4	1	4	4.0	CCCCOC(=O)NC(=O)C1c2ccccc2Oc2c1cccc2	11606768
	9949202	3311	0	None	-	1	Rat	5.1	pKi	=	5.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	325	4	1	4	4.0	CCCCOC(=O)NC(=O)C1c2ccccc2Oc2c1cccc2	11606768
	1379	2387	36	None	-	1	Rat	5.9	pKi	=	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	209	3	3	3	0.8	OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N	12695537
	5311261	2387	36	None	-	1	Rat	5.9	pKi	=	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	209	3	3	3	0.8	OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N	12695537
	CHEMBL94631	2387	36	None	-	1	Rat	5.9	pKi	=	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	209	3	3	3	0.8	OC(=O)c1ccc(c(c1)C)[C@@H](C(=O)O)N	12695537
	3347	2390	6	None	-	1	Rat	6.8	pKi	=	6.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	341	5	2	5	3.0	OCCSc1nc(NC2Cc3c(C2)cccc3)c2c(n1)CCCC2	19559036
	9840951	2390	6	None	-	1	Rat	6.8	pKi	=	6.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	341	5	2	5	3.0	OCCSc1nc(NC2Cc3c(C2)cccc3)c2c(n1)CCCC2	19559036
	CHEMBL3786530	2390	6	None	-	1	Rat	6.8	pKi	=	6.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	341	5	2	5	3.0	OCCSc1nc(NC2Cc3c(C2)cccc3)c2c(n1)CCCC2	19559036
	44442431	1040	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	415	3	1	7	2.2	Clc1ccc(cc1)n1c(C)nc2c(c1=O)cnn2c1ccc(cc1)S(=O)(=O)N	17532216
	6342	1040	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	415	3	1	7	2.2	Clc1ccc(cc1)n1c(C)nc2c(c1=O)cnn2c1ccc(cc1)S(=O)(=O)N	17532216
	CHEMBL245990	1040	0	None	-	1	Human	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	415	3	1	7	2.2	Clc1ccc(cc1)n1c(C)nc2c(c1=O)cnn2c1ccc(cc1)S(=O)(=O)N	17532216
	46866191	1028	0	None	-12	3	Human	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	324	1	2	8	1.9	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N	20346665
	46866191	1028	0	None	-12	3	Rat	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	324	1	2	8	1.9	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N	20346665
	6209	1028	0	None	-12	3	Human	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	324	1	2	8	1.9	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N	20346665
	6209	1028	0	None	-12	3	Rat	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	324	1	2	8	1.9	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N	20346665
	CHEMBL1093560	1028	0	None	-12	3	Human	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	324	1	2	8	1.9	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N	20346665
	CHEMBL1093560	1028	0	None	-12	3	Rat	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	324	1	2	8	1.9	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)N	20346665
	1386	3286	0	None	-	1	Rat	7.6	pKi	=	7.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	283	4	1	3	3.1	CCOC(=O)NC(=O)C(c1ccccc1)c1ccccc1	11606768
	9903898	3286	0	None	-	1	Rat	7.6	pKi	=	7.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	283	4	1	3	3.1	CCOC(=O)NC(=O)C(c1ccccc1)c1ccccc1	11606768
	1388	3312	0	None	-	1	Rat	7.7	pKi	=	7.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology	319	3	0	2	3.7	Cc1ccc(cc1)S(=O)(=O)N1CCCC1c1ccc(cc1)F	11606768
	17950211	3312	0	None	-	1	Rat	7.7	pKi	=	7.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology	319	3	0	2	3.7	Cc1ccc(cc1)S(=O)(=O)N1CCCC1c1ccc(cc1)F	11606768
	10409562	4053	0	None	-	1	Rat	7.7	pKi	=	7.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology	414	7	0	6	4.0	COCCN(Cc1ccc2c(c1)nc1n2cc(s1)C(=O)N(C1CCCCC1)C)C	18164695
	6361	4053	0	None	-	1	Rat	7.7	pKi	=	7.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology	414	7	0	6	4.0	COCCN(Cc1ccc2c(c1)nc1n2cc(s1)C(=O)N(C1CCCCC1)C)C	18164695
	1390	1526	0	None	-	1	Rat	7.8	pKi	=	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	308	2	0	5	2.0	CCn1c(C)nc(c(c1=O)C#N)N1CCc2c(CC1)cccc2	12509432
	3363	1526	0	None	-	1	Rat	7.8	pKi	=	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	308	2	0	5	2.0	CCn1c(C)nc(c(c1=O)C#N)N1CCc2c(CC1)cccc2	12509432
	9904703	1526	0	None	-	1	Rat	7.8	pKi	=	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	308	2	0	5	2.0	CCn1c(C)nc(c(c1=O)C#N)N1CCc2c(CC1)cccc2	12509432
	11301185	1653	24	None	-	1	Rat	7.9	pKi	=	7.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	305	2	0	5	3.3	Cc1c(nnn1c1cccnc1F)c1ccc2c(c1)cccn2	21172734
	6353	1653	24	None	-	1	Rat	7.9	pKi	=	7.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	305	2	0	5	3.3	Cc1c(nnn1c1cccnc1F)c1ccc2c(c1)cccn2	21172734
	CHEMBL1645352	1653	24	None	-	1	Rat	7.9	pKi	=	7.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	305	2	0	5	3.3	Cc1c(nnn1c1cccnc1F)c1ccc2c(c1)cccn2	21172734
	6208	1038	0	None	-	1	Rat	8.0	pKi	=	8.0	Binding	UnclassifiedUnclassified	Guide to Pharmacology	318	4	2	5	1.7	OCC1CCN(CC1)c1ncc(nc1)C(=O)NC1CCCCC1	17064898
	73755189	1038	0	None	-	1	Rat	8.0	pKi	=	8.0	Binding	UnclassifiedUnclassified	Guide to Pharmacology	318	4	2	5	1.7	OCC1CCN(CC1)c1ncc(nc1)C(=O)NC1CCCCC1	17064898
	46866192	1034	0	None	14	2	Rat	8.1	pKi	=	8.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	323	1	1	7	2.6	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)C	20346665
	6210	1034	0	None	14	2	Rat	8.1	pKi	=	8.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	323	1	1	7	2.6	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)C	20346665
	CHEMBL1093901	1034	0	None	14	2	Rat	8.1	pKi	=	8.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	323	1	1	7	2.6	Cc1ccc(cc1)n1cnc2c(c1=O)sc1c2c(N)nc(n1)C	20346665
	11537456	207	9	None	-	1	Rat	8.3	pKi	=	8.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology	342	2	0	6	4.0	CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C	18054908
	6354	207	9	None	-	1	Rat	8.3	pKi	=	8.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology	342	2	0	6	4.0	CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C	18054908
	CHEMBL225032	207	9	None	-	1	Rat	8.3	pKi	=	8.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology	342	2	0	6	4.0	CN(c1ccnc2c1c1ncn(c(=O)c1s2)C1CCCCCC1)C	18054908
	16118537	964	0	None	-	1	Rat	8.3	pKi	=	8.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology	363	4	1	6	4.2	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1	22266036
	6357	964	0	None	-	1	Rat	8.3	pKi	=	8.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology	363	4	1	6	4.2	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1	22266036
	CHEMBL1951683	964	0	None	-	1	Rat	8.3	pKi	=	8.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology	363	4	1	6	4.2	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)NC1CC1	22266036
	23634102	963	1	None	-	1	Rat	8.3	pKi	=	8.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology	362	4	1	7	3.0	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC	19433355
	6215	963	1	None	-	1	Rat	8.3	pKi	=	8.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology	362	4	1	7	3.0	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC	19433355
	CHEMBL1783876	963	1	None	-	1	Rat	8.3	pKi	=	8.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology	362	4	1	7	3.0	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)OC	19433355
	16739288	1018	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	306	3	2	2	3.3	Cc1cc2[nH]c3c(c2cc1OCc1ccccc1)CCNC3=O	17276684
	6358	1018	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	306	3	2	2	3.3	Cc1cc2[nH]c3c(c2cc1OCc1ccccc1)CCNC3=O	17276684
	CHEMBL396712	1018	0	None	-	1	Human	8.4	pKi	=	8.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	306	3	2	2	3.3	Cc1cc2[nH]c3c(c2cc1OCc1ccccc1)CCNC3=O	17276684
	16118119	1127	0	None	4	2	Human	8.4	pKi	=	8.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	351	3	0	6	3.7	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C	22266036
	6356	1127	0	None	4	2	Human	8.4	pKi	=	8.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	351	3	0	6	3.7	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C	22266036
	CHEMBL1951658	1127	0	None	4	2	Human	8.4	pKi	=	8.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	351	3	0	6	3.7	COc1ccc(cc1)n1ccc2c(c1=O)sc1c2c(ccn1)N(C)C	22266036
	23634171	962	1	None	-	1	Rat	8.5	pKi	=	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	366	3	1	6	3.7	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl	19433355
	6214	962	1	None	-	1	Rat	8.5	pKi	=	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	366	3	1	6	3.7	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl	19433355
	CHEMBL1783874	962	1	None	-	1	Rat	8.5	pKi	=	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	366	3	1	6	3.7	C#CCNc1ccnc2c1c1ncn(c(=O)c1s2)c1ccc(cc1)Cl	19433355
	16659801	1021	0	None	-	1	Rat	8.8	pKi	=	8.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	370	1	1	7	3.5	Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	17929793
	6346	1021	0	None	-	1	Rat	8.8	pKi	=	8.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	370	1	1	7	3.5	Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	17929793
	CHEMBL236994	1021	0	None	-	1	Rat	8.8	pKi	=	8.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	370	1	1	7	3.5	Clc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	17929793
	16659803	1022	0	None	-	1	Rat	8.8	pKi	=	8.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	384	1	1	7	3.8	C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	17929793
	6338	1022	0	None	-	1	Rat	8.8	pKi	=	8.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	384	1	1	7	3.8	C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	17929793
	CHEMBL236180	1022	0	None	-	1	Rat	8.8	pKi	=	8.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	384	1	1	7	3.8	C[C@H]1CNc2c(O1)cnc1c2c2ncn(c(=O)c2s1)c1ccc(cc1)Cl	17929793
	7442	2104	3	None	-1	3	Rat	8.9	pKi	=	8.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	16078827
	9948645	2104	3	None	-1	3	Rat	8.9	pKi	=	8.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	16078827
	CHEMBL188906	2104	3	None	-1	3	Rat	8.9	pKi	=	8.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	16078827
	CHEMBL253345	2104	3	None	-1	3	Rat	8.9	pKi	=	8.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	311	4	0	3	4.5	CO[C@@H]1CC[C@@H](CC1)C(=O)c1ccc2c(c1)cc(c(n2)C)CC	16078827
	10470232	3218	18	None	-1	2	Rat	8.9	pKi	=	8.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	12695537
	1391	3218	18	None	-1	2	Rat	8.9	pKi	=	8.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	12695537
	6336	3218	18	None	-1	2	Rat	8.9	pKi	=	8.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	12695537
	CHEMBL369459	3218	18	None	-1	2	Rat	8.9	pKi	=	8.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	303	3	0	3	4.0	O=C(c1ccc2c(c1)cc1c(n2)OCCC1)Cc1ccccc1	12695537
	6343	957	0	None	-	1	Rat	9.0	pKi	=	9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	352	2	1	6	2.6	COc1ccc(cc1)N1C=NC2C(C1=O)Sc1c2c2NCCc2cn1	17929793
	73755209	957	0	None	-	1	Rat	9.0	pKi	=	9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	352	2	1	6	2.6	COc1ccc(cc1)N1C=NC2C(C1=O)Sc1c2c2NCCc2cn1	17929793
	16659967	1020	0	None	-	1	Rat	9.4	pKi	=	9.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	366	2	1	8	2.8	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	17929793
	6345	1020	0	None	-	1	Rat	9.4	pKi	=	9.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	366	2	1	8	2.8	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	17929793
	CHEMBL393922	1020	0	None	-	1	Rat	9.4	pKi	=	9.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	366	2	1	8	2.8	COc1ccc(cc1)n1cnc2c(c1=O)sc1c2c2NCCOc2cn1	17929793
	1381	574	21	None	-	1	Rat	9.5	pKi	=	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	278	2	0	2	3.9	C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2	11306677
	9903757	574	21	None	-	1	Rat	9.5	pKi	=	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	278	2	0	2	3.9	C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2	11306677
	CHEMBL254372	574	21	None	-	1	Rat	9.5	pKi	=	9.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	278	2	0	2	3.9	C=C1C[C@H]2[C@](C1)(Cc1ccc3c(c1)cccc3)C(=O)OC2	11306677
	1373	2440	46	None	-6	5	Rat	3.8	pKi	None	3.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	209	3	3	3	0.6	OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C	12695537
	139055582	2440	46	None	-6	5	Rat	3.8	pKi	None	3.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	209	3	3	3	0.6	OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C	12695537
	446355	2440	46	None	-6	5	Rat	3.8	pKi	None	3.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	209	3	3	3	0.6	OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C	12695537
	CHEMBL257626	2440	46	None	-6	5	Rat	3.8	pKi	None	3.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	209	3	3	3	0.6	OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C	12695537
	DB04256	2440	46	None	-6	5	Rat	3.8	pKi	None	3.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	209	3	3	3	0.6	OC(=O)c1ccc(cc1)[C@@](C(=O)O)(N)C	12695537
	1376	318	50	None	-91	2	Rat	4.0	pKi	None	4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	221	2	3	3	0.6	OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O	12695537
	2071	318	50	None	-91	2	Rat	4.0	pKi	None	4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	221	2	3	3	0.6	OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O	12695537
	CHEMBL313938	318	50	None	-91	2	Rat	4.0	pKi	None	4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	221	2	3	3	0.6	OC(=O)c1ccc2c(c1)CCC2(N)C(=O)O	12695537
	1377	1313	19	None	-1230	6	Rat	4.1	pKi	None	4.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	203	4	4	4	-1.6	N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O	11080213
	5310979	1313	19	None	-1230	6	Rat	4.1	pKi	None	4.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	203	4	4	4	-1.6	N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O	11080213
	CHEMBL284193	1313	19	None	-1230	6	Rat	4.1	pKi	None	4.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	203	4	4	4	-1.6	N[C@@H](C1[C@H]([C@@H]1C(=O)O)C(=O)O)C(=O)O	11080213
	1382	1167	29	None	1	2	Rat	5.3	pKi	None	5.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	12695537
	6278000	1167	29	None	1	2	Rat	5.3	pKi	None	5.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	12695537
	CHEMBL327783	1167	29	None	1	2	Rat	5.3	pKi	None	5.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology	247	2	1	5	1.6	CCOC(=O)C12CC2/C(=N\O)/c2c(O1)cccc2	12695537
	1418	3393	48	None	21	2	Rat	5.4	pKi	None	5.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	12695537
	5311459	3393	48	None	21	2	Rat	5.4	pKi	None	5.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	12695537
	CHEMBL94990	3393	48	None	21	2	Rat	5.4	pKi	None	5.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	12695537
	1368	2258	31	None	-19	11	Rat	5.6	pKi	None	5.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	159	3	3	3	-0.9	N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O	11080213
	5310956	2258	31	None	-19	11	Rat	5.6	pKi	None	5.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	159	3	3	3	-0.9	N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O	11080213
	CHEMBL280563	2258	31	None	-19	11	Rat	5.6	pKi	None	5.6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	159	3	3	3	-0.9	N[C@@H]([C@H]1C[C@@H]1C(=O)O)C(=O)O	11080213
	104766	34	36	None	3	11	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	11080213
	104766	34	36	None	3	11	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	12695537
	104766	34	36	None	3	11	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	7690672
	1365	34	36	None	3	11	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	11080213
	1365	34	36	None	3	11	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	12695537
	1365	34	36	None	3	11	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	7690672
	CHEMBL34453	34	36	None	3	11	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	11080213
	CHEMBL34453	34	36	None	3	11	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	12695537
	CHEMBL34453	34	36	None	3	11	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	173	2	3	3	-0.3	OC(=O)[C@@H]1CC[C@@](C1)(N)C(=O)O	7690672
	108001	93	0	None	-	1	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	183	2	4	4	0.2	OC(=O)C(c1cc(O)cc(c1)O)N	12695537
	1367	93	0	None	-	1	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	183	2	4	4	0.2	OC(=O)C(c1cc(O)cc(c1)O)N	12695537
	CHEMBL66105	93	0	None	-	1	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	183	2	4	4	0.2	OC(=O)C(c1cc(O)cc(c1)O)N	12695537
	1374	2050	31	None	12	2	Human	5.9	pKi	None	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	211	3	4	4	0.2	N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O	11080213
	1374	2050	31	None	12	2	Human	5.9	pKi	None	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	211	3	4	4	0.2	N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O	12695537
	5311455	2050	31	None	12	2	Human	5.9	pKi	None	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	211	3	4	4	0.2	N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O	11080213
	5311455	2050	31	None	12	2	Human	5.9	pKi	None	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	211	3	4	4	0.2	N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O	12695537
	CHEMBL39372	2050	31	None	12	2	Human	5.9	pKi	None	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	211	3	4	4	0.2	N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O	11080213
	CHEMBL39372	2050	31	None	12	2	Human	5.9	pKi	None	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	211	3	4	4	0.2	N[C@@H](c1ccc(c(c1)O)C(=O)O)C(=O)O	12695537
	12310764	1939	59	None	14	8	Rat	6.2	pKi	None	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	158	2	3	4	-0.9	OC(=O)C(c1o[nH]c(=O)c1)N	11080213
	12310764	1939	59	None	14	8	Rat	6.2	pKi	None	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	158	2	3	4	-0.9	OC(=O)C(c1o[nH]c(=O)c1)N	7690672
	1233	1939	59	None	14	8	Rat	6.2	pKi	None	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	158	2	3	4	-0.9	OC(=O)C(c1o[nH]c(=O)c1)N	11080213
	1233	1939	59	None	14	8	Rat	6.2	pKi	None	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	158	2	3	4	-0.9	OC(=O)C(c1o[nH]c(=O)c1)N	7690672
	1371	1939	59	None	14	8	Rat	6.2	pKi	None	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	158	2	3	4	-0.9	OC(=O)C(c1o[nH]c(=O)c1)N	11080213
	1371	1939	59	None	14	8	Rat	6.2	pKi	None	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	158	2	3	4	-0.9	OC(=O)C(c1o[nH]c(=O)c1)N	7690672
	CHEMBL284895	1939	59	None	14	8	Rat	6.2	pKi	None	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	158	2	3	4	-0.9	OC(=O)C(c1o[nH]c(=O)c1)N	11080213
	CHEMBL284895	1939	59	None	14	8	Rat	6.2	pKi	None	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	158	2	3	4	-0.9	OC(=O)C(c1o[nH]c(=O)c1)N	7690672
	1310	2286	108	None	-4	18	Rat	6.5	pKi	None	6.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	11080213
	1310	2286	108	None	-4	18	Rat	6.5	pKi	None	6.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	12695537
	1369	2286	108	None	-4	18	Rat	6.5	pKi	None	6.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	11080213
	1369	2286	108	None	-4	18	Rat	6.5	pKi	None	6.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	12695537
	33032	2286	108	None	-4	18	Rat	6.5	pKi	None	6.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	11080213
	33032	2286	108	None	-4	18	Rat	6.5	pKi	None	6.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	12695537
	44272391	2286	108	None	-4	18	Rat	6.5	pKi	None	6.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	11080213
	44272391	2286	108	None	-4	18	Rat	6.5	pKi	None	6.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	12695537
	88747398	2286	108	None	-4	18	Rat	6.5	pKi	None	6.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	11080213
	88747398	2286	108	None	-4	18	Rat	6.5	pKi	None	6.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	12695537
	CHEMBL575060	2286	108	None	-4	18	Rat	6.5	pKi	None	6.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	11080213
	CHEMBL575060	2286	108	None	-4	18	Rat	6.5	pKi	None	6.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	12695537
	DB00142	2286	108	None	-4	18	Rat	6.5	pKi	None	6.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	11080213
	DB00142	2286	108	None	-4	18	Rat	6.5	pKi	None	6.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	147	4	3	3	-0.7	OC(=O)CC[C@@H](C(=O)O)N	12695537
	1370	3212	62	None	44	8	Rat	7.8	pKi	None	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	11080213
	1370	3212	62	None	44	8	Rat	7.8	pKi	None	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	12695537
	1372	3212	62	None	44	8	Rat	7.8	pKi	None	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	11080213
	1372	3212	62	None	44	8	Rat	7.8	pKi	None	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	12695537
	40539	3212	62	None	44	8	Rat	7.8	pKi	None	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	11080213
	40539	3212	62	None	44	8	Rat	7.8	pKi	None	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	12695537
	6971145	3212	62	None	44	8	Rat	7.8	pKi	None	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	11080213
	6971145	3212	62	None	44	8	Rat	7.8	pKi	None	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	12695537
	CHEMBL279956	3212	62	None	44	8	Rat	7.8	pKi	None	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	11080213
	CHEMBL279956	3212	62	None	44	8	Rat	7.8	pKi	None	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	12695537
	DB02999	3212	62	None	44	8	Rat	7.8	pKi	None	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	11080213
	DB02999	3212	62	None	44	8	Rat	7.8	pKi	None	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	189	3	3	6	-2.5	OC(=O)[C@H](Cn1oc(=O)[nH]c1=O)N	12695537
	1378	2384	48	None	-162	10	Human	7.8	pKi	None	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	353	5	3	4	2.8	OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N	9680254
	1399	2384	48	None	-162	10	Human	7.8	pKi	None	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	353	5	3	4	2.8	OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N	9680254
	9819927	2384	48	None	-162	10	Human	7.8	pKi	None	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	353	5	3	4	2.8	OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N	9680254
	CHEMBL432038	2384	48	None	-162	10	Human	7.8	pKi	None	7.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	353	5	3	4	2.8	OC(=O)[C@H]1C[C@@H]1[C@](C(=O)O)(CC1c2ccccc2Oc2c1cccc2)N	9680254
	1384	2836	54	None	-	1	Rat	8.9	pKi	None	8.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	307	2	1	3	3.3	O=C(c1cnc2c(n1)cccc2)NC12CC3CC(C2)CC(C1)C3	12695537
	7067728	2836	54	None	-	1	Rat	8.9	pKi	None	8.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	307	2	1	3	3.3	O=C(c1cnc2c(n1)cccc2)NC12CC3CC(C2)CC(C1)C3	12695537
	CHEMBL399160	2836	54	None	-	1	Rat	8.9	pKi	None	8.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	307	2	1	3	3.3	O=C(c1cnc2c(n1)cccc2)NC12CC3CC(C2)CC(C1)C3	12695537

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Ligand source activities (1 row/activity)