GPCRdb

Ligand source activities (1 row/activity)

Potency
Affinity

Get vendors

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	6861	48	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	6861	48	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	6861	48	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	199608	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	199608	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	131018	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	131018	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	145802	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	145802	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	145802	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	145802	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	144473	2	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	144473	2	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	78664	38	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	78664	38	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	78664	38	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	130709	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	130709	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	130712	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	130712	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	130709	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	130709	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	130712	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	130712	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	145817	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	145817	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	144473	2	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	144473	2	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	145817	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	145817	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	131035	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	131035	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	131016	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	131016	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	144570	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	144570	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	194416	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	194416	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	144570	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	144570	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	145868	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	145868	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	145868	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	145868	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	145732	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	145732	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	145732	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	145732	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	144607	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	144607	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	145747	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	145747	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	131035	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	131035	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	194415	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	194415	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	144607	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	144607	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	145747	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	145747	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	145820	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	145820	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	188534	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	188534	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	145761	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	145761	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	144475	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	144475	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	144475	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	144475	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	194416	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	194416	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	146870	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	146870	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	144547	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	144547	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	144547	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	144547	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	146870	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	146870	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	131022	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	131022	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	145761	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	145761	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	144540	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	144540	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	144540	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	144540	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	131037	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	131037	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	6822	42	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	6822	42	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	6822	42	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	144543	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	144543	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	144543	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	144543	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	145861	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	145861	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	131019	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	131019	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	145861	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	145861	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	131005	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	131005	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	131032	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	131032	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	194419	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	194419	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	194383	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	194383	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	186865	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	186865	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	146709	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	146709	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	144588	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	144588	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	144609	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	144609	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	146709	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	146709	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	144588	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	144588	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	145822	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	145822	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	145751	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	145751	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	145822	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	145822	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	130853	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	130853	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	146429	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	146429	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	144519	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	144519	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	146429	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	146429	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	144519	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	144519	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	144515	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	144515	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	199608	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	199608	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	144438	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	144438	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	144572	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	144572	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	144515	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	144515	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	144572	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	144572	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	144438	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	144438	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	131026	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	131026	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	187234	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	187234	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	199913	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	199913	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	131031	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	131031	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	131034	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	131034	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	10113	26	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	10113	26	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	10113	26	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	131029	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	131029	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	145762	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	145762	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	194415	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	194415	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	131013	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	131013	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	144508	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	144508	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	145751	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	145751	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	145762	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	145762	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	189409	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	189409	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	144508	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	144508	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	131008	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	131008	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	144473	2	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	144473	2	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	144440	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	144440	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	144506	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	144506	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	7868	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	7868	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	7868	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	189300	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	189300	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	144440	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	144440	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	145741	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	145741	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	144626	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	144626	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	131033	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	131033	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	130711	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	130711	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	9070	37	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	9070	37	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	9070	37	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	144626	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	144626	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	146719	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	146719	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	130711	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	130711	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	130706	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	130706	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	130706	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	130706	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	146719	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	146719	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	144609	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	144609	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	145741	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	145741	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	145892	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	145892	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	10113	26	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	10113	26	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	10113	26	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	145892	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	145892	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	10113	26	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	10113	26	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	10113	26	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	145820	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	145820	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	194383	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	194383	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	144420	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	144420	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	144473	2	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	144473	2	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	144568	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	144568	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	144568	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	144568	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	144420	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	144420	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	131009	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	131009	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	194083	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	194083	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	145891	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	145891	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	144582	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	144582	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	145891	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	145891	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	144582	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	144582	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	146532	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	146532	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	146532	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	146532	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	10113	26	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	10113	26	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	10113	26	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	10113	26	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	10113	26	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	10113	26	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	131010	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	131010	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	131006	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	131006	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	131036	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	131036	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	130716	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	130716	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	190361	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	190361	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	130710	6	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	130710	6	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	130710	6	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	130710	6	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	130710	6	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	130710	6	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	8860	42	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	8860	42	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	8860	42	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	130708	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	130708	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	130708	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	130708	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	131038	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	131038	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	144630	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	144630	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	144630	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	144630	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	131011	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	131011	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	131025	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	131025	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	145742	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	145742	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	145764	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	145764	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	144427	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	144427	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	145764	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	145764	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	10821	40	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	10821	40	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	10821	40	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	146870	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	146870	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	145801	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	145801	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	145742	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	145742	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	145801	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	145801	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	146870	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	146870	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	145966	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	145966	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	145966	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	145966	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	144427	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	144427	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	194418	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	194418	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	131023	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	131023	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	145759	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	145759	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	10821	40	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	10821	40	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	10821	40	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	10821	40	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	10821	40	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	10821	40	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	145759	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	145759	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	194418	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	194418	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	194016	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	194016	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	194083	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	194083	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	130710	6	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	130710	6	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	130710	6	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	130710	6	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	144453	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	144453	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	144453	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	144453	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	190308	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	190308	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	6822	42	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	6822	42	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	6822	42	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	108978	23	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	108978	23	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	108978	23	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	8751	64	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	8751	64	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	8751	64	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	8751	64	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	144561	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	144561	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	194452	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	194452	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	131007	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	131007	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	130704	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	130704	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	130704	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	130704	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	131020	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	131020	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	131027	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	131027	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	144551	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	144551	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	145942	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	145942	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	194419	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	194419	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	144551	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	144551	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	47475	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	47475	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	145942	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	145942	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	131004	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	131004	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	47475	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	47475	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	145852	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	145852	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	145852	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	145852	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	131014	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	131014	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	131015	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	131015	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	131021	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	131021	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	144561	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	144561	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	144612	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	144612	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	144411	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	144411	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	188757	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	188757	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	144411	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	144411	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	7868	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	7868	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	7868	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	144497	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	144497	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	144497	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	144497	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	131017	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	131017	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	144612	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	144612	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	131030	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	131030	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	144536	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	144536	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	130707	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	130707	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	144536	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	144536	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	130707	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	130707	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	130703	4	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	130703	4	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	130703	4	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	130703	4	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	144585	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	144585	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	10113	26	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	10113	26	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	10113	26	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	144463	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	144463	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	189292	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	189292	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	144585	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	144585	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	145738	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	145738	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	145738	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	145738	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	189674	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	189674	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	190169	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	190169	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	144463	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	144463	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	186359	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	186359	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	144506	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	144506	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	144499	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	144499	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	186731	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	186731	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	144499	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	144499	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	144546	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	144546	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	144546	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	144546	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	145970	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	145970	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	153230	53	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	153230	53	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	153230	53	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	145970	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	145970	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	199913	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	199913	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	144504	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	144504	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	144504	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	144504	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	145913	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	145913	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	145913	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	145913	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	146429	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	146429	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	146429	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	146429	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	186683	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	186683	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	131028	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	131028	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	188213	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	188213	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	145743	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	145743	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	190061	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	190061	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	145743	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	145743	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	130709	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	130709	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	130709	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	130709	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	102861	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	102861	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	144523	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	144523	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	144523	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	144523	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	145831	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	145831	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	131012	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	131012	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	145831	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	145831	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	194452	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	194452	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	146719	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	146719	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	146719	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	146719	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	145876	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	145876	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	6822	42	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	6822	42	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	6822	42	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	145876	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	145876	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	131024	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	131024	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	145771	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	145771	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	145771	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	145771	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	145730	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	145730	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	145730	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	145730	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	130705	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	130705	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	130705	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	130705	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	130712	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	130712	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	130712	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	130712	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	188954	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	188954	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	96731	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	96731	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	77747	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	77747	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	155112	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	155112	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	77799	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	77799	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	7763	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	7763	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	7763	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	79987	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	79987	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	90597	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	90597	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	90598	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	90598	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	90599	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	90599	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	6997	12	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	6997	12	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	6997	12	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	6999	42	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	6999	42	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	6999	42	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	69434	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	69434	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	8915	62	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	8915	62	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	8915	62	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	8915	62	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	7825	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	7825	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	7825	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	69444	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	69444	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	181849	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	181849	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	69518	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	69518	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	204157	2	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	204157	2	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	69522	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	69522	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	6999	42	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	6999	42	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	6999	42	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	204126	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	204126	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	77749	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	77749	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	69439	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	69439	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	69437	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	69437	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	69530	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	69530	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	69521	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	69521	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	79992	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	79992	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	205427	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	205427	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	161838	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	161838	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	182330	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	182330	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	98808	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	98808	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	10222	53	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	10222	53	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	10222	53	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	131900	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	131900	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	148849	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	148849	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	93527	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	93527	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	94292	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	94292	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	69441	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	69441	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	99128	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	99128	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	131018	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	131018	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	149121	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	149121	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	101528	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	101528	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	24893	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	24893	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	139882	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	139882	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	69517	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	69517	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	201964	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	201964	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	125688	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	125688	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	25087	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	25087	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	15004	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	15004	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	69429	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	69429	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	195981	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	195981	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	204037	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	204037	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	79988	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	79988	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	161723	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	161723	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	161352	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	161352	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	131878	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	131878	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	131914	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	131914	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	121116	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	121116	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	121116	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	121116	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	91929	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	91929	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	97823	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	97823	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	98796	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	98796	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	77757	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	77757	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	97823	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	97823	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	98796	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	98796	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	131887	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	131887	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	139898	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	139898	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	90590	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	90590	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	155391	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	155391	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	7765	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	7765	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	7765	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	77817	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	77817	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	180088	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	180088	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	69524	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	69524	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	69519	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	69519	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	131035	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	131035	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	69431	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	69431	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	183612	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	183612	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	95248	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	95248	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	139859	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	139859	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	35821	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	35821	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	101440	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	101440	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	91969	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	91969	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	125684	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	125684	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	131016	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	131016	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	77767	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	77767	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	125693	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	125693	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	100705	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	100705	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	121119	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	121119	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	69538	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	69538	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	91584	1	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	91584	1	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	91877	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	91877	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	203884	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	203884	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	101529	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	101529	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	131856	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	131856	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	139803	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	139803	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	139820	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	139820	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	94291	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	94291	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	161623	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	161623	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	97824	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	97824	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	77769	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	77769	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	97824	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	97824	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	128984	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	128984	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	121108	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	121108	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	69543	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	69543	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	79997	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	79997	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	97811	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	97811	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	91783	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	91783	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	90601	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	90601	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	77753	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	77753	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	69526	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	69526	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	91838	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	91838	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	130717	6	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	130717	6	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	139819	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	139819	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	139821	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	139821	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	139852	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	139852	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	175076	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	175076	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	97811	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	97811	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	112380	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	112380	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	7843	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	7843	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	7843	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	125687	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	125687	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	98804	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	98804	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	131022	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	131022	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	98804	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	98804	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	91843	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	91843	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	145926	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	145926	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	145926	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	145926	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	131895	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	131895	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	90481	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	90481	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	77765	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	77765	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	77813	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	77813	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	77816	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	77816	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	139797	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	139797	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	139823	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	139823	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	131037	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	131037	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	148041	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	148041	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	131032	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	131032	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	182328	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	182328	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	139796	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	139796	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	205109	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	205109	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	204015	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	204015	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	205413	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	205413	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	101492	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	101492	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	131911	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	131911	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	139850	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	139850	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	139887	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	139887	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	139890	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	139890	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	85298	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	85298	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	173957	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	173957	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	145734	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	145734	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	145734	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	145734	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	202555	13	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	202555	13	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	90592	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	90592	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	131019	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	131019	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
	67424813	95850	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	95850	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	95850	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	14693	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	14693	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	69532	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	69532	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	90602	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	90602	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	91997	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	91997	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	183587	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	183587	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	101773	17	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	101773	17	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	183674	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	183674	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	8231	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	8231	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	8231	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	131005	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	131005	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	69438	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	69438	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	96994	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	96994	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	7368	30	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	7368	30	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	7368	30	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	183612	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	183612	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	101598	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	101598	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	183610	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	183610	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	139827	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	139827	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	139847	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	139847	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	139870	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	139870	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	97815	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	97815	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	145805	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	145805	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	145814	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	145814	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	121113	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	121113	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	97815	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	97815	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	145805	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	145805	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	145814	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	145814	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	131884	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	131884	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	97817	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	97817	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	97820	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	97820	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	97817	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	97817	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	148506	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	148506	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	148609	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	148609	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	7820	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	7820	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	7820	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	97820	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	97820	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	157049	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	157049	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	69533	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	69533	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	91840	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	91840	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	77770	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	77770	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	205372	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	205372	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	139860	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	139860	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	202691	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	202691	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	101526	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	101526	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	69549	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	69549	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	145870	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	145870	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	183540	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	183540	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	203885	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	203885	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	130853	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	130853	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	172892	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	172892	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	161588	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	161588	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	180345	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	180345	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	181944	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	181944	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	205707	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	205707	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	131906	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	131906	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	145870	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	145870	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	119321	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	119321	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	125697	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	125697	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	139899	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	139899	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	91894	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	91894	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	121115	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	121115	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	98809	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	98809	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	139884	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	139884	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	98809	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	98809	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	15002	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	15002	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	90479	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	90479	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	90587	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	90587	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	143620	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	143620	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	131034	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	131034	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	82481	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	82481	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	145294	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	145294	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	176885	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	176885	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	94293	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	94293	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	101491	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	101491	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	9198	44	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	9198	44	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	9198	44	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	98801	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	98801	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	98801	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	98801	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	131864	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	131864	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	90474	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	90474	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	77768	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	77768	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	139880	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	139880	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	69442	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	69442	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	159321	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	159321	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	131026	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	131026	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	69428	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	69428	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	90596	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	90596	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	77774	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	77774	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	77808	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	77808	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	7764	2	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	7764	2	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	7764	2	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	7830	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	7830	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	7830	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	7824	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	7824	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	7824	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	95461	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	95461	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	77809	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	77809	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	205274	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	205274	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	95517	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	95517	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	7822	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	7822	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	7822	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	180088	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	180088	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	203638	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	203638	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	7823	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	7823	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	7823	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	90606	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	90606	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	91867	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	91867	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	131031	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	131031	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	204593	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	204593	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	77800	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	77800	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	125690	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	125690	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	90605	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	90605	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	202429	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	202429	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	128979	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	128979	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	131890	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	131890	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	131847	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	131847	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	131029	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	131029	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	69545	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	69545	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	25088	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	25088	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	69546	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	69546	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	87614	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	87614	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	131013	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	131013	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	203639	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	203639	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	203634	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	203634	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	139799	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	139799	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	94617	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	94617	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	101718	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	101718	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	101460	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	101460	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	101460	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	69540	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	69540	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	145830	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	145830	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	145830	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	145830	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	69547	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	69547	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	204067	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	204067	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	139826	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	139826	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	131008	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	131008	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	131033	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	131033	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	182330	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	182330	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	161403	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	161403	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	139888	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	139888	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	131898	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	131898	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	139834	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	139834	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	121121	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	121121	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	121123	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	121123	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	95862	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	95862	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	95862	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	145967	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	145967	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	145790	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	145790	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	145790	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	145790	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	145967	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	145967	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	203369	2	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	203369	2	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	99127	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	99127	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	131882	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	131882	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	61483	16	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	61483	16	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	91927	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	91927	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	161353	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	161353	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	204537	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	204537	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	101493	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	101493	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	131907	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	131907	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	139835	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	139835	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	101717	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	101717	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	145833	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	145833	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	145901	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	145901	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	145833	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	145833	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	145901	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	145901	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	131881	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	131881	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	95869	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	95869	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	95869	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	125700	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	125700	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	173286	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	173286	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	202561	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	202561	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	202812	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	202812	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	97814	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	97814	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	90588	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	90588	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	195982	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	195982	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	95519	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	95519	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	100376	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	100376	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	100700	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	100700	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	203995	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	203995	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	139893	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	139893	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	69443	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	69443	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	100545	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	100545	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	97814	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	97814	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	145809	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	145809	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	125689	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	125689	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	97826	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	97826	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	97826	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	97826	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	145809	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	145809	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	147116	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	147116	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	205148	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	205148	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	101412	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	101412	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	10317	41	None	1	3	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	10317	41	None	1	3	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	10317	41	None	1	3	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	101436	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	101436	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	161542	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	161542	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	53087	10	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	53087	10	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	10317	41	None	1	3	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	10317	41	None	1	3	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	10317	41	None	1	3	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	144321	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	144321	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	82202	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	82202	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	82337	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	82337	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	97807	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	97807	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	121126	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	121126	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	97807	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	97807	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	148689	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	148689	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	131009	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	131009	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	10791	24	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	10791	24	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	10791	24	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	161142	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	161142	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	131875	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	131875	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	97825	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	97825	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	97825	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	97825	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	145908	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	145908	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	7836	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	7836	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	7836	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	77764	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	77764	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	139794	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	139794	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	131010	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	131010	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	128974	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	128974	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	145908	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	145908	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	90595	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	90595	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	95851	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	95851	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	95851	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	9201	9	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	9201	9	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	9201	9	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	131006	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	131006	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	131036	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	131036	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	139810	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	139810	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	148860	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	148860	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	125691	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	125691	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	202628	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	202628	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	159084	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	159084	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	131903	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	131903	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	183611	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	183611	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	125694	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	125694	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	98797	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	98797	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	98797	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	98797	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	202412	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	202412	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	112382	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	112382	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	69536	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	69536	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	90476	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	90476	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	90585	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	90585	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	6998	14	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	6998	14	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	6998	14	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	6998	14	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	6998	14	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	6998	14	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	77806	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	77806	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	6998	14	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	6998	14	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	6998	14	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	7821	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	7821	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	7821	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	8916	6	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	8916	6	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	8916	6	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	8916	6	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	15246	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	15246	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	77755	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	77755	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	8478	34	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	8478	34	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	8478	34	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	205293	1	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	205293	1	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	181571	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	181571	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	77771	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	77771	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	7672	40	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	7672	40	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	7672	40	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	204034	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	204034	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	204034	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	9336	33	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	9336	33	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	9336	33	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	203718	1	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	203718	1	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	69520	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	69520	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	69537	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	69537	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	77752	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	77752	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	90480	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	90480	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	157383	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	157383	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	203873	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	203873	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	194857	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	194857	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	101462	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	101462	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	202610	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	202610	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	101411	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	101411	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	139798	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	139798	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	112369	13	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	112369	13	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	150927	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	150927	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	125702	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	125702	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	77815	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	77815	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	183587	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	183587	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	139846	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	139846	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	95868	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	95868	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	95868	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	100079	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	100079	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	69548	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	69548	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	125696	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	125696	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	81808	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	81808	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	82699	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	82699	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	79987	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	79987	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	25073	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	25073	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	91842	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	91842	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	139848	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	139848	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	139902	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	139902	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	15257	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	15257	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	69535	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	69535	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	204035	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	204035	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	148609	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	148609	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	131886	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	131886	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	131905	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	131905	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	131038	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	131038	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	131889	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	131889	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	91773	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	91773	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	145818	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	145818	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	77812	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	77812	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	131011	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	131011	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	131025	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	131025	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	131899	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	131899	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	139830	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	139830	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	7973	33	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	7973	33	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	7973	33	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	145818	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	145818	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	97810	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	97810	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	97810	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	97810	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	77760	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	77760	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	139820	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	139820	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	100378	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	100378	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	139806	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	139806	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	112378	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	112378	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	69550	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	69550	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	97819	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	97819	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	98799	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	98799	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	97819	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	97819	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	98799	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	98799	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	91622	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	91622	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	96995	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	96995	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	121112	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	121112	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	173379	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	173379	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	139879	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	139879	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	131023	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	131023	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	79995	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	79995	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	150272	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	150272	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	181944	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	181944	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	183540	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	183540	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	128978	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	128978	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	172779	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	172779	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	204036	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	204036	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	202967	13	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	202967	13	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	95840	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	95840	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	95840	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	12635	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	12635	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	97812	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	97812	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	81207	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	81207	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	82026	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	82026	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	146586	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	146586	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	97812	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	97812	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	94610	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	94610	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	90600	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	90600	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	91999	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	91999	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	69433	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	69433	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	77807	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	77807	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	69528	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	69528	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	77745	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	77745	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	205602	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	205602	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	96732	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	96732	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	101490	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	101490	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	177031	36	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	177031	36	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	8862	35	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	8862	35	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	8862	35	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	25747	26	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	25747	26	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	131897	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	131897	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	143605	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	143605	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	121111	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	121111	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	120921	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	120921	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	156524	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	156524	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	7831	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	7831	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	7831	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	24892	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	24892	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	91814	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	91814	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	131888	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	131888	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	161774	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	161774	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	97808	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	97808	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	97808	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	97808	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	139861	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	139861	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	69440	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	69440	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	7000	9	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	7000	9	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	7000	9	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	131007	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	131007	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	85297	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	85297	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	9253	51	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	9253	51	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	9253	51	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	9253	51	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	9253	51	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	125686	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	125686	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	91878	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	91878	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	161378	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	161378	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	153167	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	153167	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	155734	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	155734	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	128980	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	128980	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	69544	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	69544	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	91908	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	91908	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	121122	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	121122	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	139843	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	139843	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	101461	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	101461	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	95876	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	95876	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	95876	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	131020	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	131020	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	145760	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	145760	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	100082	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	100082	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	145760	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	145760	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	131027	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	131027	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	77803	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	77803	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	131004	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	131004	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	203643	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	203643	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	125695	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	125695	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	98807	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	98807	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	98807	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	98807	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	145894	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	145894	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	131014	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	131014	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	131015	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	131015	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	131021	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	131021	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	101565	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	101565	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	139817	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	139817	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	149134	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	149134	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	145894	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	145894	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	172922	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	172922	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	182328	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	182328	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	204014	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	204014	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	205375	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	205375	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	131877	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	131877	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	139795	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	139795	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	121114	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	121114	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	90278	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	90278	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	90482	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	90482	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	90593	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	90593	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	91619	14	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	91619	14	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	91868	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	91868	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	77754	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	77754	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	6998	14	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	6998	14	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	6998	14	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	9655	59	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	9655	59	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	9655	59	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	8423	36	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	8423	36	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	8423	36	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	77746	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	77746	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	95462	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	95462	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	77762	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	77762	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	205683	1	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	205683	1	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	8478	34	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	8478	34	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	8478	34	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	77748	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	77748	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	8478	34	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	8478	34	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	8478	34	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	98763	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	98763	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	150017	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	150017	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	150316	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	150316	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	121117	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	121117	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	82632	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	82632	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	131883	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	131883	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	98800	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	98800	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	98803	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	98803	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	98803	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	98803	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	98800	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	98800	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	87006	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	87006	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	101563	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	101563	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	161544	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	161544	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	139811	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	139811	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	69531	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	69531	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	139804	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	139804	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	101413	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	101413	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	125699	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	125699	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	131017	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	131017	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	131030	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	131030	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	77759	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	77759	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	131902	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	131902	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	174192	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	174192	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	128983	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	128983	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	98795	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	98795	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	115051	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	115051	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	180345	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	180345	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	77766	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	77766	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	128982	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	128982	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	98795	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	98795	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	100083	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	100083	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	98810	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	98810	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	131904	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	131904	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	145851	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	145851	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	139903	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	139903	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	98810	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	98810	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	145851	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	145851	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	158936	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	158936	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	183611	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	183611	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	121120	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	121120	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	205254	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	205254	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	170300	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	170300	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	214533	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	214533	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	205496	11	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	205496	11	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	121109	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	121109	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	195981	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	195981	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	121112	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	121112	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	10222	53	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	10222	53	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	10222	53	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	139795	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	139795	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	139885	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	139885	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	112381	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	112381	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	183610	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	183610	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	139871	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	139871	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	139892	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	139892	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	97821	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	97821	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	7753	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	7753	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	7753	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	204590	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	204590	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	156654	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	156654	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	101747	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	101747	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	101525	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	101525	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	183674	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	183674	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	7932	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	7932	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	7932	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	77756	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	77756	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	77810	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	77810	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	77814	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	77814	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	7764	2	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	7764	2	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	7764	2	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	69432	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	69432	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	69539	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	69539	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	69435	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	69435	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	69430	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	69430	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	90594	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	90594	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	125692	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	125692	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	112762	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	112762	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	97821	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	97821	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	205194	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	205194	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	65593	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	65593	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	65593	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	65593	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	91821	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	91821	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	95420	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	95420	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	139889	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	139889	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	131898	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	131898	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	139856	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	139856	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	98473	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	98473	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	95873	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	95873	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	95873	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	79989	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	79989	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	139886	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	139886	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	139845	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	139845	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	118824	47	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	118824	47	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	145811	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	145811	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	69436	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	69436	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	121110	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	121110	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	121113	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	121113	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	131874	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	131874	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	7973	33	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	7973	33	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	7973	33	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	97818	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	97818	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	145811	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	145811	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	121124	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	121124	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	97818	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	97818	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	98805	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	98805	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	79996	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	79996	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	131176	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	131176	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	98805	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	98805	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	120921	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	120921	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	15003	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	15003	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	77772	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	77772	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	93526	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	93526	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	139901	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	139901	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	95877	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	95877	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	95877	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	205303	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	205303	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	145938	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	145938	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	145938	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	145938	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	139802	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	139802	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	139824	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	139824	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	79991	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	79991	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	79994	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	79994	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	7936	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	7936	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	7936	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	90584	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	90584	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	90604	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	90604	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	181849	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	181849	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	181571	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	181571	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	69523	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	69523	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	77804	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	77804	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	90478	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	90478	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	7109	55	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	7109	55	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	7109	55	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	101564	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	101564	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	131879	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	131879	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	131846	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	131846	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	97809	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	97809	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	97822	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	97822	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	91928	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	91928	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	93498	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	93498	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	149122	0	None	-1	2	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	149122	0	None	-1	2	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	131910	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	131910	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	97809	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	97809	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	12275	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	12275	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	97822	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	97822	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	69527	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	69527	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	119299	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	119299	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	131860	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	131860	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	95833	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	95833	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	95833	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	121118	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	121118	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	121118	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	121118	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	202696	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	202696	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	161773	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	161773	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	121125	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	121125	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	77801	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	77801	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	145786	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	145786	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	131028	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	131028	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	145786	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	145786	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	91839	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	91839	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	100429	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	100429	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	161453	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	161453	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	139881	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	139881	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	98798	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	98798	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	205648	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	205648	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	98798	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	98798	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	100699	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	100699	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	161543	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	161543	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	9195	54	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	9195	54	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	9195	54	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	9195	54	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	77761	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	77761	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	101689	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	101689	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	90603	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	90603	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	139818	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	139818	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	77751	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	77751	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	69541	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	69541	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	77750	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	77750	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	69534	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	69534	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	205096	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	205096	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	157239	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	157239	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	100428	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	100428	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	139809	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	139809	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	203888	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	203888	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	131849	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	131849	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	90477	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	90477	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	91828	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	91828	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	139897	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	139897	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	205430	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	205430	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	145840	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	145840	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	98811	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	98811	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	98811	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	98811	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	91935	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	91935	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	145840	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	145840	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	69542	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	69542	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	77758	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	77758	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	98802	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	98802	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	98802	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	98802	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	202928	10	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	202928	10	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	91970	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	91970	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	90589	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	90589	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	24891	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	24891	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	148813	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	148813	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	77802	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	77802	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	77811	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	77811	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	205131	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	205131	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	9198	44	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	9198	44	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	9198	44	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	9198	44	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	9198	44	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	9198	44	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	145765	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	145765	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	131012	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	131012	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	131876	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	131876	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	139844	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	139844	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	94295	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	94295	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	145765	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	145765	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	79987	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	79987	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	79993	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	79993	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	90475	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	90475	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	90591	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	90591	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	91813	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	91813	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	79987	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	79987	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	173834	13	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	173834	13	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	173834	13	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	173834	13	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	173834	13	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	173834	13	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	69525	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	69525	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	195982	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	195982	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	96735	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	96735	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	77805	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	77805	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	100663	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	100663	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	79990	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	79990	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	93499	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	93499	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	139822	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	139822	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	98806	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	98806	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	145823	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	145823	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	98806	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	98806	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	145823	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	145823	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	145945	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	145945	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	85296	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	85296	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	131869	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	131869	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	105637	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	105637	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	145945	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	145945	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	139801	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	139801	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	150343	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	150343	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	131024	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	131024	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	94294	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	94294	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	69529	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	69529	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	12248	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	12248	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	9202	14	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	9202	14	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	9202	14	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	97813	12	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	97813	12	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	97816	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	97816	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	143955	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	143955	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	204594	6	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	204594	6	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	100512	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	100512	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	97816	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	97816	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	144705	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	144705	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	97813	12	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	97813	12	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	97813	12	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	97813	12	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	69438	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	69438	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	69439	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	69439	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	77748	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	77748	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	7763	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	7763	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	7763	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	69431	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	69431	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	69518	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	69518	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	69428	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	69428	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	69430	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	69430	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	69437	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	69437	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	69440	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	69440	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	69444	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	69444	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	77745	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	77745	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	77747	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	77747	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	185835	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	185835	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	69529	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	69529	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	168071	31	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	168071	31	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	185867	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	185867	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	185619	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	185619	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	69545	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	69545	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	77768	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	77768	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	100482	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	100482	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	100271	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	100271	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	185620	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	185620	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	77751	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	77751	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	77754	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	77754	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	10037	67	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	10037	67	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	10037	67	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	10037	67	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	10037	67	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	10037	67	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	196257	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	196257	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	77761	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	77761	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	77755	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	77755	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	77805	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	77805	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	100626	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	100626	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	159895	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	159895	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	177061	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	177061	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	196177	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	196177	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	69441	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	69441	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	69442	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	69442	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	77752	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	77752	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	77774	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	77774	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	77813	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	77813	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	7936	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	7936	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	7936	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	77767	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	77767	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	69432	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	69432	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	69443	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	69443	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	154525	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	154525	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	185989	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	185989	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	77762	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	77762	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	7753	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	7753	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	7753	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	194859	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	194859	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	100227	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	100227	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	148362	8	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	148362	8	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	77771	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	77771	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	69517	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	69517	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	178770	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	178770	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	213616	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	213616	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	185701	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	185701	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	176301	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	176301	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	7932	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	7932	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	7932	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	185621	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	185621	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	100552	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	100552	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	69520	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	69520	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	77750	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	77750	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	77764	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	77764	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	194713	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	194713	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	77753	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	77753	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	77810	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	77810	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	194858	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	194858	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	100226	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	100226	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	100270	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	100270	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	69523	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	69523	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	69534	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	69534	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	69429	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	69429	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	69524	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	69524	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	185893	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	185893	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	185834	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	185834	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	77758	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	77758	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	185635	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	185635	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	98781	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	98781	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	77817	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	77817	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	195800	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	195800	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	77766	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	77766	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	69528	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	69528	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	69538	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	69538	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	10317	41	None	1	3	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	10317	41	None	1	3	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	10317	41	None	1	3	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	69521	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	69521	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	100334	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	100334	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	100335	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	100335	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	196173	17	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	196173	17	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	77772	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	77772	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	69519	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	69519	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	77814	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	77814	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	69539	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	69539	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	77746	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	77746	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	100186	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	100186	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	100273	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	100273	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	7821	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	7821	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	7821	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	69436	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	69436	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	77809	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	77809	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	7764	2	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	7764	2	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	7764	2	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	69526	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	69526	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	159896	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	159896	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	196047	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	196047	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	9391	67	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	9391	67	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	9391	67	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	177031	36	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	177031	36	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	77800	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	77800	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	196174	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	196174	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	100551	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	100551	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	69542	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	69542	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	77759	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	77759	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	77802	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	77802	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	77812	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	77812	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	196077	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	196077	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	185808	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	185808	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	100336	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	100336	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	213905	13	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	213905	13	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	9391	67	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	9391	67	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	9391	67	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	69530	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	69530	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	69541	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	69541	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	69435	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	69435	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	69536	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	69536	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	100228	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	100228	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	100554	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	100554	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	155079	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	155079	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	77801	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	77801	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	100438	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	100438	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	196118	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	196118	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	77760	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	77760	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	6822	42	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	6822	42	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	6822	42	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	69532	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	69532	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	100555	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	100555	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	8751	64	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	8751	64	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	8751	64	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	8751	64	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	154242	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	154242	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	69533	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	69533	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	195970	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	195970	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	7765	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	7765	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	7765	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	69434	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	69434	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	9070	37	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	9070	37	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	9070	37	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	154867	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	154867	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	77816	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	77816	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	185988	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	185988	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	100272	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	100272	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	77749	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	77749	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	77757	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	77757	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	213895	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	213895	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	7856	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	7856	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	7856	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	77799	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	77799	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	77756	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	77756	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	8408	60	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	8408	60	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	8408	60	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	8408	60	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	8408	60	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	8408	60	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	8408	60	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	8408	60	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	112762	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	112762	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	195893	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	195893	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	179421	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	179421	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	69531	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	69531	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	69546	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	69546	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	77770	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	77770	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	69535	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	69535	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	69544	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	69544	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	152816	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	152816	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	100229	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	100229	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	153230	53	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	153230	53	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	153230	53	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	69527	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	69527	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	9195	54	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	9195	54	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	9195	54	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	9195	54	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	69547	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	69547	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	100187	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	100187	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	185891	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	185891	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	77807	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	77807	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	77808	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	77808	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	69525	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	69525	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	69433	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	69433	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	173834	13	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	173834	13	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	77803	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	77803	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	69540	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	69540	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	77811	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	77811	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	77763	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	77763	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	69522	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	69522	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	100274	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	100274	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	69537	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	69537	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	77765	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	77765	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	10222	53	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	10222	53	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	10222	53	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	200172	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	200172	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	77769	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	77769	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	113829	27	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	113829	27	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	100275	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	100275	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	77806	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	77806	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	77804	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	77804	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	77815	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	77815	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	7973	33	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	7973	33	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	7973	33	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	69543	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	69543	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	7109	55	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	7109	55	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	7109	55	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	7973	33	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	7973	33	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	7973	33	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	10829	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	10829	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	10829	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	10821	40	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	10821	40	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	10821	40	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	7868	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	7868	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	7868	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	7891	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	7891	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	10113	26	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	10113	26	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	10113	26	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	10317	41	None	-1	3	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	10317	41	None	-1	3	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	10317	41	None	-1	3	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	10462	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	10462	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	10462	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	9198	44	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	9198	44	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	9198	44	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	6893	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	6893	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	6893	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	7973	33	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	7973	33	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	7973	33	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	7820	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	7820	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	7820	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	8337	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	8337	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	8337	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	9202	14	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	9202	14	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	9202	14	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	10890	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	10890	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	10890	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	10890	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	10820	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	10820	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	8763	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	8763	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	8763	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	7671	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	7671	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	7000	9	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	7000	9	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	7000	9	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	7000	9	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	7000	9	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	7000	9	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	7368	30	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	7368	30	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	7368	30	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	7368	30	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	7368	30	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	7368	30	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	9201	9	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	9201	9	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	9201	9	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	7836	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	7836	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	7836	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	6883	3	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	6883	3	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	6883	3	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	7874	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	7874	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	10890	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	10890	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	10890	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	10890	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	7765	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	7765	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	7765	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	10043	23	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	10043	23	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	10043	23	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	10043	23	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	6997	12	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	6997	12	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	6997	12	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	6999	42	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	6999	42	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	6999	42	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	7841	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	7841	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	10888	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	10888	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	7936	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	7936	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	7936	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	7932	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	7932	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	7932	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	7753	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	7753	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	7753	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	7856	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	7856	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	7856	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	8478	34	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	8478	34	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	8478	34	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	7758	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	7758	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	8478	34	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	8478	34	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	8478	34	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	6998	14	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	6998	14	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	6998	14	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	9336	33	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	9336	33	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	9336	33	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	6998	14	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	6998	14	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	6998	14	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	7821	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	7821	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	7821	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	7823	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	7823	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	7823	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	7672	40	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	7672	40	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	7672	40	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	7822	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	7822	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	7822	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	7824	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	7824	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	7824	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	7764	2	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	7764	2	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	7764	2	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	7830	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	7830	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	7830	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	7825	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	7825	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	7825	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	8915	62	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	8915	62	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	8915	62	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	8915	62	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	6999	42	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	6999	42	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	6999	42	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	6999	42	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	6999	42	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	6999	42	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	7763	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	7763	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	7763	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	8861	45	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	8861	45	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	8861	45	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	8861	45	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	8231	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	8231	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	8231	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	10821	40	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	10821	40	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	10821	40	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

Get vendors

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	24070	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	24070	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	24454	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	24454	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	211702	106	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	211702	106	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	211702	106	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	24525	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	24525	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	10113	26	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	10113	26	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	10113	26	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	10113	26	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	10113	26	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	10113	26	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	6822	42	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	6822	42	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	6822	42	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	24135	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	24135	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	24177	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	24177	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	24178	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	24178	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	24253	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	24253	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	24596	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	24596	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	108008	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	108008	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	146429	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	146429	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	146429	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	146429	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	24217	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	24217	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	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	10037	67	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	10037	67	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	10037	67	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	10037	67	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	10037	67	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	146719	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	146719	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	146719	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	146719	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	6822	42	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	6822	42	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	6822	42	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	6822	42	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	6822	42	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	6822	42	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	23253	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	23253	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	24490	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	24490	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	24216	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	24216	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	127373	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	127373	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	127373	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	23252	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	23252	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	24100	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	24100	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	24564	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	24564	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	108978	23	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	108978	23	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	108978	23	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	108978	23	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	108978	23	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	108978	23	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	6822	42	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	6822	42	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	6822	42	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	24563	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	24563	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	108978	23	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	108978	23	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	108978	23	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	108978	23	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	108978	23	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	108978	23	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	108978	23	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	108978	23	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	108978	23	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	122029	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	122029	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	24069	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	24069	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	24595	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	24595	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	8861	45	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	8861	45	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	8861	45	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	8861	45	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	23251	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	23251	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	24136	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	24136	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	24491	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	24491	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	153152	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	153152	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	8915	62	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	8915	62	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	8915	62	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	8915	62	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	69780	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	69780	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	6997	12	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	6997	12	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	6997	12	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	85703	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	85703	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	8464	32	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	8464	32	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	8464	32	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	6999	42	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	6999	42	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	6999	42	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	68884	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	68884	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	107807	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	107807	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	158681	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	158681	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	148849	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	148849	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	210357	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	210357	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	94702	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	94702	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	64256	2	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	64256	2	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	148849	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	148849	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	136254	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	136254	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	8915	62	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	8915	62	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	8915	62	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	8915	62	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	85699	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	85699	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	91929	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	91929	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	91929	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	91929	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	69079	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	69079	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	134598	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	134598	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	209777	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	209777	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	113690	29	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	113690	29	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	181246	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	181246	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	181246	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	181246	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	85309	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	85309	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	70285	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	70285	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	210392	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	210392	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	91584	1	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	91584	1	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	67054	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	67054	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	68241	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	68241	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	8423	36	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	8423	36	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	8423	36	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	91877	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	91877	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	91877	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	91877	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	91783	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	91783	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	91838	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	91838	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	10043	23	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	10043	23	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	10043	23	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	10043	23	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	91838	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	91838	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	69761	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	69761	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	210511	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	210511	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	176114	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	176114	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	94512	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	94512	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	6883	3	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	6883	3	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	6883	3	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	91997	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	91997	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	85309	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	85309	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	67290	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	67290	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	91840	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	91840	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	103580	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	103580	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	210348	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	210348	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	127179	1	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	127179	1	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	67279	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	67279	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	148506	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	148506	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	183705	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	183705	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	148506	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	148506	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	183705	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	183705	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	109496	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	109496	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	91840	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	91840	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	85699	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	85699	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	172892	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	172892	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	69786	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	69786	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	172892	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	172892	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	8763	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	8763	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	8763	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	158679	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	158679	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	85701	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	85701	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	94511	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	94511	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	67252	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	67252	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	67252	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	67252	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	6998	14	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	6998	14	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	6998	14	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	91867	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	91867	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	8763	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	8763	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	8763	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	210394	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	210394	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
	11667270	91927	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	91927	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	91927	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	91927	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	67079	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	67079	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	210569	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	210569	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	7973	33	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	7973	33	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	7973	33	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	8763	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	8763	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	8763	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	110368	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	110368	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	10317	41	None	-	1	Human	4.6	pIC50	=	4.6	Binding	Antagonist activity at mGluR1alpha (unknown origin)Antagonist activity at mGluR1alpha (unknown origin)	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1021/acs.jmedchem.1c01215
	5311040	10317	41	None	-	1	Human	4.6	pIC50	=	4.6	Binding	Antagonist activity at mGluR1alpha (unknown origin)Antagonist activity at mGluR1alpha (unknown origin)	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1021/acs.jmedchem.1c01215
	CHEMBL43412	10317	41	None	-	1	Human	4.6	pIC50	=	4.6	Binding	Antagonist activity at mGluR1alpha (unknown origin)Antagonist activity at mGluR1alpha (unknown origin)	ChEMBL	185	3	3	3	-0.3	OC(=O)[C@H](C12CC(C1)(C2)C(=O)O)N	10.1021/acs.jmedchem.1c01215
	3421	10317	41	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	10317	41	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	10317	41	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	10317	41	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	10317	41	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	10317	41	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	144321	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	144321	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	144321	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	144321	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	148689	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	148689	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	89807	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	89807	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	210407	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	210407	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	67291	1	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	67291	1	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	209812	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	209812	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	148860	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	148860	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	148860	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	148860	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	67053	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	67053	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	6998	14	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	6998	14	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	6998	14	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	67800	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	67800	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	8915	62	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	8915	62	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	8915	62	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	8915	62	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	67241	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	67241	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	8464	32	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	8464	32	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	8464	32	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	95257	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	95257	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	91999	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	91999	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	9867	41	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	9867	41	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	9867	41	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	209826	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	209826	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	150927	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	150927	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	150927	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	150927	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	94510	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	94510	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	91842	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	91842	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	173803	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	173803	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	91842	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	91842	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	83404	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	83404	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	68906	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	108861	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	108861	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	210464	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	210464	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	10317	41	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	10317	41	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	10317	41	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	67579	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	67579	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	91773	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	91773	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	91773	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	91773	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	98802	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	98802	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	109010	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	109010	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	85702	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	85702	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	91622	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	91622	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	91622	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	91622	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	150272	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	150272	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	150272	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	150272	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	210418	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	210418	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	83405	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	83405	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	107658	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	107658	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	91999	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	91999	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	69761	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	69761	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	69780	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	69780	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	70315	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	70315	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	85700	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	85700	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	8862	35	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	8862	35	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	8862	35	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	8862	35	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	8862	35	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	8862	35	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	143605	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	143605	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	143605	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	143605	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	91814	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	91814	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	91814	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	91814	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	172922	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	172922	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	91878	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	91878	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	67250	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	67250	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	68906	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	91878	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	91878	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	91908	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	91908	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	91908	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	91908	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	8915	62	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	8915	62	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	8915	62	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	8915	62	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	67489	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	67489	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	67489	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	67489	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	89808	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	89808	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	108961	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	108961	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	149134	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	149134	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	149134	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	149134	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	172922	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	172922	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	91619	14	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	91619	14	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	91868	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	91868	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	67800	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	67800	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	69761	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	69761	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	150017	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	150017	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	150316	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	150316	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	68883	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	68883	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	69170	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	69170	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	85308	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	85308	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	68884	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	68884	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	87006	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	87006	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	134598	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	134598	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	210578	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	210578	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	129727	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	129727	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	10043	23	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	10043	23	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	10043	23	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	10043	23	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	68241	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	68241	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	85702	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	85702	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	91821	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	91821	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	91821	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	91821	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	89805	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	89805	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	67345	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	67345	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	67241	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	67241	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	10222	53	None	-21	2	Human	4.2	pIC50	=	4.2	Binding	Antagonist activity at mGluR1alpha (unknown origin)Antagonist activity at mGluR1alpha (unknown origin)	ChEMBL	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	10.1021/acs.jmedchem.1c01215
	5311459	10222	53	None	-21	2	Human	4.2	pIC50	=	4.2	Binding	Antagonist activity at mGluR1alpha (unknown origin)Antagonist activity at mGluR1alpha (unknown origin)	ChEMBL	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	10.1021/acs.jmedchem.1c01215
	CHEMBL94990	10222	53	None	-21	2	Human	4.2	pIC50	=	4.2	Binding	Antagonist activity at mGluR1alpha (unknown origin)Antagonist activity at mGluR1alpha (unknown origin)	ChEMBL	195	3	3	3	0.5	N[C@@H](c1ccc(cc1)C(=O)O)C(=O)O	10.1021/acs.jmedchem.1c01215
	1418	10222	53	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	10222	53	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	10222	53	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	10462	10	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Antagonist activity at mGluR1alpha (unknown origin)Antagonist activity at mGluR1alpha (unknown origin)	ChEMBL	209	3	3	5	-1.0	OC(=O)[C@H](C12CC(C1)(C2)c1n[nH]nn1)N	10.1021/acs.jmedchem.1c01215
	3419	10462	10	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Antagonist activity at mGluR1alpha (unknown origin)Antagonist activity at mGluR1alpha (unknown origin)	ChEMBL	209	3	3	5	-1.0	OC(=O)[C@H](C12CC(C1)(C2)c1n[nH]nn1)N	10.1021/acs.jmedchem.1c01215
	CHEMBL2204334	10462	10	None	-	0	Human	4.2	pIC50	=	4.2	Binding	Antagonist activity at mGluR1alpha (unknown origin)Antagonist activity at mGluR1alpha (unknown origin)	ChEMBL	209	3	3	5	-1.0	OC(=O)[C@H](C12CC(C1)(C2)c1n[nH]nn1)N	10.1021/acs.jmedchem.1c01215
	10058919	10462	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	10462	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	10462	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	68872	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	68872	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	69787	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	69787	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	85703	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	85703	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	129727	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	129727	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	91928	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	91928	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	91928	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	91928	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	210604	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	210604	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	69787	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	69787	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	210523	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	210523	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	91839	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	91839	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	91839	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	91839	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	80733	9	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	80733	9	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	136254	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	136254	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	210506	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	210506	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	67241	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	67241	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	67053	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	67053	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	91813	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	91813	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	68883	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	68883	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	69786	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	69786	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	9198	44	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	9198	44	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	9198	44	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	68872	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	68872	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	91935	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	91935	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	69262	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	69262	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	85701	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	85701	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	91935	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	91935	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	91970	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	91970	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	67290	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	67290	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	176114	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	176114	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	127179	1	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	127179	1	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	91970	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	91970	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	148813	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	148813	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	148813	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	148813	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	9195	54	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	9195	54	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	9195	54	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	9195	54	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	91813	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	91813	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	85700	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	85700	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	9307	15	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	9307	15	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	9307	15	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	8763	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	8763	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	8763	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	143955	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	143955	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	143955	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	143955	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	144705	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	144705	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	144705	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	144705	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	7825	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	7825	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	7825	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	95517	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	95517	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	8915	62	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	8915	62	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	8915	62	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	8915	62	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	204034	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	204034	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	204034	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	204034	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	204034	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	204034	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	7823	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	7823	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	7823	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	95461	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	95461	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	155391	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	155391	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	95462	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	95462	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	8916	6	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	8916	6	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	8916	6	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	8916	6	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	8916	6	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	8916	6	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	8916	6	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	8916	6	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	8916	6	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	8916	6	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	8916	6	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	8916	6	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	7822	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	7822	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	7822	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	91999	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	91999	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	7824	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	7824	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	7824	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	156654	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	156654	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	153167	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	153167	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	174192	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	174192	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	96735	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	96735	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	91908	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	91908	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	202392	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	202392	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	83404	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	83404	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	89807	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	89807	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	203419	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	203419	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	144321	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	144321	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	83405	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	83405	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	155112	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	155112	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	96994	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	96994	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	202412	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	202412	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	128983	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	128983	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	128984	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	128984	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	128980	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	128980	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	128980	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	128980	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	128986	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	128986	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	96995	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	96995	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	8478	34	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	8478	34	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	8478	34	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	91619	14	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	91619	14	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	96731	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	96731	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	202335	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	202335	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	89808	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	89808	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	202392	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	202392	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	150272	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	150272	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	89805	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	89805	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	77329	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	77329	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	116490	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	116490	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	96732	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	96732	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	203382	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	203382	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	8478	34	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	8478	34	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	8478	34	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	127373	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	127373	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	127373	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	202086	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	202086	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	79067	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	79067	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	92915	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	92915	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	201964	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	201964	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	10222	53	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	10222	53	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	10222	53	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	128979	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	128979	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	91840	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	91840	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	91997	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	91997	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	83566	14	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	83566	14	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	83566	14	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	83566	14	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	83566	14	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	83566	14	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	83566	14	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	83566	14	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	128978	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	128978	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	180627	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	180627	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	86435	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	86435	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	128987	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	128987	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	6998	14	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	6998	14	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	6998	14	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	8423	36	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	8423	36	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	8423	36	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	108514	63	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	108514	63	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	204588	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	204588	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	128976	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	128976	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	185363	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	185363	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	91813	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	91813	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	86325	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	86325	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	122029	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	122029	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	91969	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	91969	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	202466	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	202466	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	128975	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	128975	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	173834	13	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	173834	13	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	128982	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	128982	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	201555	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	201555	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	135803	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	135803	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	149892	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	149892	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	8122	26	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	8122	26	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	8122	26	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	95420	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	95420	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	91842	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	91842	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	91927	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	91927	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	148860	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	148860	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	92864	42	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	92864	42	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	95519	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	95519	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	153230	53	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	153230	53	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	153230	53	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	202691	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	202691	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	136250	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	136250	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	77329	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	77329	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	171238	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	171238	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	171238	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	171238	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	128974	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	128974	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	150316	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	150316	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	202696	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	202696	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	10890	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	10890	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	10890	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	10890	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	8337	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	8337	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	8337	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	10043	23	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	10043	23	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	10043	23	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	10043	23	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9292	24	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	9292	24	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	9292	24	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	9292	24	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	9292	24	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	9637	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	9637	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	9637	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	10237	33	Functional	-2398	42	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	10237	33	Functional	-2398	42	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	10237	33	Functional	-2398	42	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	10237	33	Functional	-2398	42	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	33885	30	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	33885	30	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	140299	14	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	140299	14	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	174570	24	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	174570	24	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	209053	22	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	209053	22	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	209053	22	Functional	-239	44	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	151	2	2	2	1.1	CC(N)C(O)c1ccccc1	None
	3337	213146	27	Functional	-1513	40	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)Cc1cccc(C(F)(F)F)c1	None
	65801	213146	27	Functional	-1513	40	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)Cc1cccc(C(F)(F)F)c1	None
	66264	213146	27	Functional	-1513	40	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)Cc1cccc(C(F)(F)F)c1	None
	91452	213146	27	Functional	-1513	40	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)Cc1cccc(C(F)(F)F)c1	None
	CHEMBL87493	213146	27	Functional	-1513	40	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)Cc1cccc(C(F)(F)F)c1	None
	DB00574	213146	27	Functional	-1513	40	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)Cc1cccc(C(F)(F)F)c1	None
	11954224	222732	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	222788	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	222951	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	222958	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	222958	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
	None	223095	0	Functional	-1	40	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	223096	0	Functional	-1	39	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	223104	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	223105	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	224491	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	8423	36	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	8423	36	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	8423	36	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	10136	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	10136	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	9198	44	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	9198	44	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	9198	44	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	9201	9	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	9201	9	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	9201	9	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	7843	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	7843	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	7843	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	7830	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	7830	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	7830	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	7830	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	7830	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	7830	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	10111	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	10111	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	10137	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	10137	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	10888	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	10888	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	8337	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	8337	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	8337	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	8464	32	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	8464	32	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	8464	32	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	7841	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	7841	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	7836	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	7836	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	7836	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	6997	12	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	6997	12	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	6997	12	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	7765	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	7765	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	7765	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	7764	2	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	7764	2	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	7764	2	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	7820	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	7820	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	7820	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	7932	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	7932	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	7932	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	7763	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	7763	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	7763	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	7823	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	7823	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	7823	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	7824	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	7824	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	7824	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	8916	6	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	8916	6	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	8916	6	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	8916	6	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	10043	23	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	10043	23	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	10043	23	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	10043	23	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	7758	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	7758	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	7822	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	7822	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	7822	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	7368	30	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	7368	30	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	7368	30	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	9253	51	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	9253	51	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	9253	51	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	9253	51	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	9253	51	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	7109	55	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	7109	55	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	7109	55	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	8122	26	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	8122	26	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	8122	26	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	7973	33	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	7973	33	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	7973	33	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	10222	53	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	10222	53	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	10222	53	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	9070	37	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	9070	37	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	9070	37	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	6822	42	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	6822	42	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	6822	42	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	6822	42	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	6822	42	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	6822	42	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	6822	42	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	6822	42	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	6822	42	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	6881	0	None	-53	3	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	6881	0	None	-53	3	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	6881	0	None	-53	3	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	8862	35	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	8862	35	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	8862	35	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	8862	35	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	8862	35	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	8862	35	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	8751	64	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	8751	64	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	8751	64	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	8751	64	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	8751	64	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	8751	64	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	8751	64	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	8751	64	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	9095	110	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	10037	67	None	17	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	9195	54	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	9195	54	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	9195	54	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	9195	54	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	9655	59	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	9655	59	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	9655	59	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

Join us

Cite us

Main reference

Ligand source activities (1 row/activity)