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
	2139	10627	56	None	1	3	Mouse	9.0	pEC50	=	9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.01.038
	2316	10627	56	None	1	3	Mouse	9.0	pEC50	=	9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.01.038
	3836	10627	56	None	1	3	Mouse	9.0	pEC50	=	9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.01.038
	638678	10627	56	None	1	3	Mouse	9.0	pEC50	=	9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.01.038
	CHEMBL1472	10627	56	None	1	3	Mouse	9.0	pEC50	=	9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.01.038
	DB09421	10627	56	None	1	3	Mouse	9.0	pEC50	=	9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.01.038
	2139	10627	56	None	1	3	Mouse	9.0	pEC50	=	9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL		None	None	None		None	10.1016/j.bmc.2015.07.022
	2316	10627	56	None	1	3	Mouse	9.0	pEC50	=	9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL		None	None	None		None	10.1016/j.bmc.2015.07.022
	3836	10627	56	None	1	3	Mouse	9.0	pEC50	=	9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL		None	None	None		None	10.1016/j.bmc.2015.07.022
	638678	10627	56	None	1	3	Mouse	9.0	pEC50	=	9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL		None	None	None		None	10.1016/j.bmc.2015.07.022
	CHEMBL1472	10627	56	None	1	3	Mouse	9.0	pEC50	=	9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL		None	None	None		None	10.1016/j.bmc.2015.07.022
	DB09421	10627	56	None	1	3	Mouse	9.0	pEC50	=	9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL		None	None	None		None	10.1016/j.bmc.2015.07.022
	CHEMBL3600450	218590	0	None	-	1	Mouse	6.0	pEC50	=	6	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL		None	None	None		CC(C)c1nc(C[C@H](NC(=O)[C@H]2CCCCN2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	10.1016/j.bmc.2015.07.022
	122185156	129350	0	None	-	1	Mouse	5.0	pEC50	=	5.0	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	609	6	3	6	0.2	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)[nH]c1I)NC(=O)c1cnccn1	10.1016/j.bmc.2015.07.022
	CHEMBL3601784	129350	0	None	-	1	Mouse	5.0	pEC50	=	5.0	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	609	6	3	6	0.2	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)[nH]c1I)NC(=O)c1cnccn1	10.1016/j.bmc.2015.07.022
	127032260	145497	0	None	-	1	Mouse	7.9	pEC50	=	7.9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	468	7	3	6	-0.6	CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br	10.1016/j.ejmech.2016.01.038
	CHEMBL3779931	145497	0	None	-	1	Mouse	7.9	pEC50	=	7.9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	468	7	3	6	-0.6	CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br	10.1016/j.ejmech.2016.01.038
	127032877	145571	0	None	-	1	Mouse	4.9	pEC50	=	4.9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	430	6	4	5	-0.5	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Cl)[nH]c1Cl)NC(=O)[C@@H]1CCC(=O)N1	10.1016/j.ejmech.2016.01.038
	CHEMBL3780836	145571	0	None	-	1	Mouse	4.9	pEC50	=	4.9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	430	6	4	5	-0.5	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Cl)[nH]c1Cl)NC(=O)[C@@H]1CCC(=O)N1	10.1016/j.ejmech.2016.01.038
	127032875	145657	0	None	-	1	Mouse	7.9	pEC50	=	7.9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	516	7	3	6	-0.7	CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I	10.1016/j.ejmech.2016.01.038
	CHEMBL3782037	145657	0	None	-	1	Mouse	7.9	pEC50	=	7.9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	516	7	3	6	-0.7	CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I	10.1016/j.ejmech.2016.01.038
	CHEMBL390942	219227	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activityAgonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity	ChEMBL		None	None	None		CCn1cnc(C[C@H](NC(=O)[C@@H]2CCCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1	10.1016/j.bmc.2006.09.045
	122185155	129349	0	None	-	1	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	528	6	4	7	0.1	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Br)[nH]c1Br)NC(=O)c1nccnc1N	10.1016/j.bmc.2015.07.022
	CHEMBL3601783	129349	0	None	-	1	Mouse	5.9	pEC50	=	5.9	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	528	6	4	7	0.1	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Br)[nH]c1Br)NC(=O)c1nccnc1N	10.1016/j.bmc.2015.07.022
	127033489	145545	0	None	-	1	Mouse	7.8	pEC50	=	7.8	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	704	8	3	6	0.9	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)n(Cc2ccccc2)c1I)NC(=O)[C@@H]1CCC(=O)N1	10.1016/j.ejmech.2016.01.038
	CHEMBL3780549	145545	0	None	-	1	Mouse	7.8	pEC50	=	7.8	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	704	8	3	6	0.9	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)n(Cc2ccccc2)c1I)NC(=O)[C@@H]1CCC(=O)N1	10.1016/j.ejmech.2016.01.038
	122184246	129158	0	None	-	1	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	399	8	3	6	-0.0	CCCc1nc(C[C@H](NC(=O)c2cnccn2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	10.1016/j.bmc.2015.07.022
	CHEMBL3600446	129158	0	None	-	1	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	399	8	3	6	-0.0	CCCc1nc(C[C@H](NC(=O)c2cnccn2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	10.1016/j.bmc.2015.07.022
	122184248	129160	0	None	-	1	Mouse	5.8	pEC50	=	5.8	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	414	8	4	7	-0.4	CCCc1nc(C[C@H](NC(=O)c2nccnc2N)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	10.1016/j.bmc.2015.07.022
	CHEMBL3600448	129160	0	None	-	1	Mouse	5.8	pEC50	=	5.8	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	414	8	4	7	-0.4	CCCc1nc(C[C@H](NC(=O)c2nccnc2N)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	10.1016/j.bmc.2015.07.022
	127032258	145518	0	None	-	1	Mouse	4.8	pEC50	=	4.8	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	486	8	3	6	0.4	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(Cl)n1)NC(=O)[C@@H]1CCC(=O)N1	10.1016/j.ejmech.2016.01.038
	CHEMBL3780248	145518	0	None	-	1	Mouse	4.8	pEC50	=	4.8	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	486	8	3	6	0.4	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(Cl)n1)NC(=O)[C@@H]1CCC(=O)N1	10.1016/j.ejmech.2016.01.038
	122184247	129159	0	None	-	1	Mouse	7.8	pEC50	=	7.8	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	413	8	3	6	0.3	CCCc1nc(C[C@H](NC(=O)c2cnc(C)cn2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	10.1016/j.bmc.2015.07.022
	CHEMBL3600447	129159	0	None	-	1	Mouse	7.8	pEC50	=	7.8	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	413	8	3	6	0.3	CCCc1nc(C[C@H](NC(=O)c2cnc(C)cn2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	10.1016/j.bmc.2015.07.022
	127033191	145567	0	None	-	1	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	642	7	3	6	-0.1	CCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I	10.1016/j.ejmech.2016.01.038
	CHEMBL3780802	145567	0	None	-	1	Mouse	6.8	pEC50	=	6.8	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	642	7	3	6	-0.1	CCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I	10.1016/j.ejmech.2016.01.038
	CHEMBL389037	219202	0	None	-	1	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activityAgonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity	ChEMBL		None	None	None		NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)cn1)NC(=O)[C@@H]1CCCC(=O)N1	10.1016/j.bmc.2006.09.045
	127032260	145497	0	None	-	1	Mouse	5.7	pEC50	=	5.7	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	468	7	3	6	-0.6	CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br	10.1016/j.ejmech.2016.01.038
	CHEMBL3779931	145497	0	None	-	1	Mouse	5.7	pEC50	=	5.7	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	468	7	3	6	-0.6	CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br	10.1016/j.ejmech.2016.01.038
	122184251	129161	0	None	-	1	Mouse	4.7	pEC50	=	4.7	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	391	6	3	6	-0.3	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc[nH]c1Cl)NC(=O)c1cnccn1	10.1016/j.bmc.2015.07.022
	CHEMBL3600451	129161	0	None	-	1	Mouse	4.7	pEC50	=	4.7	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	391	6	3	6	-0.3	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc[nH]c1Cl)NC(=O)c1cnccn1	10.1016/j.bmc.2015.07.022
	127033192	145514	0	None	-	1	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	656	8	3	6	0.3	CCCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I	10.1016/j.ejmech.2016.01.038
	CHEMBL3780191	145514	0	None	-	1	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	656	8	3	6	0.3	CCCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I	10.1016/j.ejmech.2016.01.038
	127033191	145567	0	None	-	1	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	642	7	3	6	-0.1	CCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I	10.1016/j.ejmech.2016.01.038
	CHEMBL3780802	145567	0	None	-	1	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	642	7	3	6	-0.1	CCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I	10.1016/j.ejmech.2016.01.038
	122184253	129163	0	None	-	1	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	513	6	3	6	0.5	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Br)[nH]c1Br)NC(=O)c1cnccn1	10.1016/j.bmc.2015.07.022
	CHEMBL3600453	129163	0	None	-	1	Mouse	5.6	pEC50	=	5.6	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	513	6	3	6	0.5	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Br)[nH]c1Br)NC(=O)c1cnccn1	10.1016/j.bmc.2015.07.022
	127032258	145518	0	None	-	1	Mouse	4.6	pEC50	=	4.6	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	486	8	3	6	0.4	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(Cl)n1)NC(=O)[C@@H]1CCC(=O)N1	10.1016/j.ejmech.2016.01.038
	CHEMBL3780248	145518	0	None	-	1	Mouse	4.6	pEC50	=	4.6	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	486	8	3	6	0.4	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(Cl)n1)NC(=O)[C@@H]1CCC(=O)N1	10.1016/j.ejmech.2016.01.038
	127032876	145639	0	None	-	1	Mouse	7.6	pEC50	=	7.6	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	578	8	3	6	0.3	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(I)n1)NC(=O)[C@@H]1CCC(=O)N1	10.1016/j.ejmech.2016.01.038
	CHEMBL3781773	145639	0	None	-	1	Mouse	7.6	pEC50	=	7.6	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	578	8	3	6	0.3	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(I)n1)NC(=O)[C@@H]1CCC(=O)N1	10.1016/j.ejmech.2016.01.038
	127032878	145548	0	None	-	1	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	628	6	3	6	-0.6	Cn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I	10.1016/j.ejmech.2016.01.038
	CHEMBL3780633	145548	0	None	-	1	Mouse	6.6	pEC50	=	6.6	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	628	6	3	6	-0.6	Cn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I	10.1016/j.ejmech.2016.01.038
	127032259	145561	0	None	-	1	Mouse	7.6	pEC50	=	7.6	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	454	6	3	6	-1.0	Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br	10.1016/j.ejmech.2016.01.038
	CHEMBL3780746	145561	0	None	-	1	Mouse	7.6	pEC50	=	7.6	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	454	6	3	6	-1.0	Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br	10.1016/j.ejmech.2016.01.038
	122185154	129348	0	None	-	1	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	450	6	4	7	-0.6	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc[nH]c1Br)NC(=O)c1nccnc1N	10.1016/j.bmc.2015.07.022
	CHEMBL3601782	129348	0	None	-	1	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	450	6	4	7	-0.6	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc[nH]c1Br)NC(=O)c1nccnc1N	10.1016/j.bmc.2015.07.022
	2139	10627	56	None	-1	3	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activityAgonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity	ChEMBL		None	None	None		None	10.1016/j.bmc.2006.09.045
	2316	10627	56	None	-1	3	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activityAgonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity	ChEMBL		None	None	None		None	10.1016/j.bmc.2006.09.045
	3836	10627	56	None	-1	3	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activityAgonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity	ChEMBL		None	None	None		None	10.1016/j.bmc.2006.09.045
	638678	10627	56	None	-1	3	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activityAgonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity	ChEMBL		None	None	None		None	10.1016/j.bmc.2006.09.045
	CHEMBL1472	10627	56	None	-1	3	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activityAgonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity	ChEMBL		None	None	None		None	10.1016/j.bmc.2006.09.045
	DB09421	10627	56	None	-1	3	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activityAgonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity	ChEMBL		None	None	None		None	10.1016/j.bmc.2006.09.045
	2139	10627	56	None	1	3	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.01.038
	2316	10627	56	None	1	3	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.01.038
	3836	10627	56	None	1	3	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.01.038
	638678	10627	56	None	1	3	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.01.038
	CHEMBL1472	10627	56	None	1	3	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.01.038
	DB09421	10627	56	None	1	3	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.01.038
	127032259	145561	0	None	-	1	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	454	6	3	6	-1.0	Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br	10.1016/j.ejmech.2016.01.038
	CHEMBL3780746	145561	0	None	-	1	Mouse	8.5	pEC50	=	8.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	454	6	3	6	-1.0	Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br	10.1016/j.ejmech.2016.01.038
	127032563	145550	0	None	-	1	Mouse	7.5	pEC50	=	7.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	502	6	3	6	-1.2	Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I	10.1016/j.ejmech.2016.01.038
	CHEMBL3780645	145550	0	None	-	1	Mouse	7.5	pEC50	=	7.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	502	6	3	6	-1.2	Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I	10.1016/j.ejmech.2016.01.038
	127032261	145529	0	None	-	1	Mouse	7.5	pEC50	=	7.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	482	8	3	6	-0.2	CCCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br	10.1016/j.ejmech.2016.01.038
	CHEMBL3780373	145529	0	None	-	1	Mouse	7.5	pEC50	=	7.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	482	8	3	6	-0.2	CCCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br	10.1016/j.ejmech.2016.01.038
	127032257	145624	0	None	-	1	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	410	6	3	6	-1.1	Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Cl	10.1016/j.ejmech.2016.01.038
	CHEMBL3781522	145624	0	None	-	1	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	410	6	3	6	-1.1	Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Cl	10.1016/j.ejmech.2016.01.038
	127032876	145639	0	None	-	1	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	578	8	3	6	0.3	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(I)n1)NC(=O)[C@@H]1CCC(=O)N1	10.1016/j.ejmech.2016.01.038
	CHEMBL3781773	145639	0	None	-	1	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	578	8	3	6	0.3	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(I)n1)NC(=O)[C@@H]1CCC(=O)N1	10.1016/j.ejmech.2016.01.038
	122185157	129351	0	None	-	1	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	449	6	2	7	-0.2	Cn1cnc(C[C@H](NC(=O)c2cnccn2)C(=O)N2CCC[C@H]2C(N)=O)c1Br	10.1016/j.bmc.2015.07.022
	CHEMBL3601785	129351	0	None	-	1	Mouse	6.5	pEC50	=	6.5	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	449	6	2	7	-0.2	Cn1cnc(C[C@H](NC(=O)c2cnccn2)C(=O)N2CCC[C@H]2C(N)=O)c1Br	10.1016/j.bmc.2015.07.022
	127032878	145548	0	None	-	1	Mouse	4.4	pEC50	=	4.4	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	628	6	3	6	-0.6	Cn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I	10.1016/j.ejmech.2016.01.038
	CHEMBL3780633	145548	0	None	-	1	Mouse	4.4	pEC50	=	4.4	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	628	6	3	6	-0.6	Cn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I	10.1016/j.ejmech.2016.01.038
	CHEMBL224525	216227	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activityAgonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity	ChEMBL		None	None	None		CCCc1nc(C[C@H](NC(=O)[C@@H]2CCCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	10.1016/j.bmc.2006.09.045
	122184252	129162	0	None	-	1	Mouse	5.4	pEC50	=	5.4	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	435	6	3	6	-0.2	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc[nH]c1Br)NC(=O)c1cnccn1	10.1016/j.bmc.2015.07.022
	CHEMBL3600452	129162	0	None	-	1	Mouse	5.4	pEC50	=	5.4	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	435	6	3	6	-0.2	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc[nH]c1Br)NC(=O)c1cnccn1	10.1016/j.bmc.2015.07.022
	CHEMBL223972	216226	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activityAgonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity	ChEMBL		None	None	None		Cn1cnc(C[C@H](NC(=O)[C@@H]2CCCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1	10.1016/j.bmc.2006.09.045
	127032875	145657	0	None	-	1	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	516	7	3	6	-0.7	CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I	10.1016/j.ejmech.2016.01.038
	CHEMBL3782037	145657	0	None	-	1	Mouse	8.3	pEC50	=	8.3	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	516	7	3	6	-0.7	CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I	10.1016/j.ejmech.2016.01.038
	122185153	129347	0	None	-	1	Mouse	6.3	pEC50	=	6.3	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	449	6	3	6	0.1	Cc1cnc(C(=O)N[C@@H](Cc2nc[nH]c2Br)C(=O)N2CCC[C@H]2C(N)=O)cn1	10.1016/j.bmc.2015.07.022
	CHEMBL3601781	129347	0	None	-	1	Mouse	6.3	pEC50	=	6.3	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	449	6	3	6	0.1	Cc1cnc(C(=O)N[C@@H](Cc2nc[nH]c2Br)C(=O)N2CCC[C@H]2C(N)=O)cn1	10.1016/j.bmc.2015.07.022
	44422122	91887	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activityAgonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity	ChEMBL	514	9	5	7	-2.8	C[n+]1c[nH]cc1C[C@H](N)C(=O)N1C(=O)CC[C@H]1C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N1CCC[C@H]1C(N)=O	10.1016/j.bmc.2006.09.045
	CHEMBL224730	91887	0	None	-	1	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activityAgonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity	ChEMBL	514	9	5	7	-2.8	C[n+]1c[nH]cc1C[C@H](N)C(=O)N1C(=O)CC[C@H]1C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N1CCC[C@H]1C(N)=O	10.1016/j.bmc.2006.09.045
	127032563	145550	0	None	-	1	Mouse	8.2	pEC50	=	8.2	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	502	6	3	6	-1.2	Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I	10.1016/j.ejmech.2016.01.038
	CHEMBL3780645	145550	0	None	-	1	Mouse	8.2	pEC50	=	8.2	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	502	6	3	6	-1.2	Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I	10.1016/j.ejmech.2016.01.038
	CHEMBL388528	219197	0	None	-	1	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activityAgonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity	ChEMBL		None	None	None		C=CCn1cnc(C[C@H](NC(=O)[C@@H]2CCCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1	10.1016/j.bmc.2006.09.045
	127033489	145545	0	None	-	1	Mouse	7.3	pEC50	=	7.3	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	704	8	3	6	0.9	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)n(Cc2ccccc2)c1I)NC(=O)[C@@H]1CCC(=O)N1	10.1016/j.ejmech.2016.01.038
	CHEMBL3780549	145545	0	None	-	1	Mouse	7.3	pEC50	=	7.3	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	704	8	3	6	0.9	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)n(Cc2ccccc2)c1I)NC(=O)[C@@H]1CCC(=O)N1	10.1016/j.ejmech.2016.01.038
	127032877	145571	0	None	-	1	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	430	6	4	5	-0.5	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Cl)[nH]c1Cl)NC(=O)[C@@H]1CCC(=O)N1	10.1016/j.ejmech.2016.01.038
	CHEMBL3780836	145571	0	None	-	1	Mouse	5.2	pEC50	=	5.2	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	430	6	4	5	-0.5	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Cl)[nH]c1Cl)NC(=O)[C@@H]1CCC(=O)N1	10.1016/j.ejmech.2016.01.038
	122185158	129352	0	None	-	1	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	637	7	2	7	0.7	CCn1c(I)nc(C[C@H](NC(=O)c2cnccn2)C(=O)N2CCC[C@H]2C(N)=O)c1I	10.1016/j.bmc.2015.07.022
	CHEMBL3601786	129352	0	None	-	1	Mouse	5.1	pEC50	=	5.1	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	637	7	2	7	0.7	CCn1c(I)nc(C[C@H](NC(=O)c2cnccn2)C(=O)N2CCC[C@H]2C(N)=O)c1I	10.1016/j.bmc.2015.07.022
	122184244	129156	0	None	-	1	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	713	8	2	7	2.1	Cc1cnc(C(=O)N[C@@H](Cc2nc(I)n(Cc3ccccc3)c2I)C(=O)N2CCC[C@H]2C(N)=O)cn1	10.1016/j.bmc.2015.07.022
	CHEMBL3600444	129156	0	None	-	1	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	713	8	2	7	2.1	Cc1cnc(C(=O)N[C@@H](Cc2nc(I)n(Cc3ccccc3)c2I)C(=O)N2CCC[C@H]2C(N)=O)cn1	10.1016/j.bmc.2015.07.022
	122184254	129164	0	None	-	1	Mouse	7.1	pEC50	=	7.1	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	527	6	3	6	0.9	Cc1cnc(C(=O)N[C@@H](Cc2nc(Br)[nH]c2Br)C(=O)N2CCC[C@H]2C(N)=O)cn1	10.1016/j.bmc.2015.07.022
	CHEMBL3600454	129164	0	None	-	1	Mouse	7.1	pEC50	=	7.1	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	527	6	3	6	0.9	Cc1cnc(C(=O)N[C@@H](Cc2nc(Br)[nH]c2Br)C(=O)N2CCC[C@H]2C(N)=O)cn1	10.1016/j.bmc.2015.07.022
	127033192	145514	0	None	-	1	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	656	8	3	6	0.3	CCCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I	10.1016/j.ejmech.2016.01.038
	CHEMBL3780191	145514	0	None	-	1	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISAAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA	ChEMBL	656	8	3	6	0.3	CCCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I	10.1016/j.ejmech.2016.01.038
	127032257	145624	0	None	-	1	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	410	6	3	6	-1.1	Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Cl	10.1016/j.ejmech.2016.01.038
	CHEMBL3781522	145624	0	None	-	1	Mouse	6.1	pEC50	=	6.1	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assayAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay	ChEMBL	410	6	3	6	-1.1	Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Cl	10.1016/j.ejmech.2016.01.038
	CHEMBL3600449	218589	0	None	-	1	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL		None	None	None		CCCc1nc(C[C@H](NC(=O)[C@H]2CCCCN2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	10.1016/j.bmc.2015.07.022
	122184245	129157	0	None	-	1	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	699	8	2	7	1.7	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)n(Cc2ccccc2)c1I)NC(=O)c1cnccn1	10.1016/j.bmc.2015.07.022
	CHEMBL3600445	129157	0	None	-	1	Mouse	6.0	pEC50	=	6.0	Functional	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR methodAgonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	699	8	2	7	1.7	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)n(Cc2ccccc2)c1I)NC(=O)c1cnccn1	10.1016/j.bmc.2015.07.022

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
	2139	10627	56	None	-1	4	Mouse	9.3	pEC50	=	9.3	Binding	Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol	ChEMBL		None	None	None		None	10.1016/s0960-894x(98)00567-8
	2316	10627	56	None	-1	4	Mouse	9.3	pEC50	=	9.3	Binding	Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol	ChEMBL		None	None	None		None	10.1016/s0960-894x(98)00567-8
	3836	10627	56	None	-1	4	Mouse	9.3	pEC50	=	9.3	Binding	Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol	ChEMBL		None	None	None		None	10.1016/s0960-894x(98)00567-8
	638678	10627	56	None	-1	4	Mouse	9.3	pEC50	=	9.3	Binding	Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol	ChEMBL		None	None	None		None	10.1016/s0960-894x(98)00567-8
	CHEMBL1472	10627	56	None	-1	4	Mouse	9.3	pEC50	=	9.3	Binding	Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol	ChEMBL		None	None	None		None	10.1016/s0960-894x(98)00567-8
	DB09421	10627	56	None	-1	4	Mouse	9.3	pEC50	=	9.3	Binding	Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol	ChEMBL		None	None	None		None	10.1016/s0960-894x(98)00567-8
	44403976	134002	0	None	-	1	Rat	9.3	pEC50	=	9.3	Binding	Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8	ChEMBL	513	9	4	9	-2.3	Cn1cncc1C[C@H](N)C(=O)N1C(=O)CC[C@H]1C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N1CCC[C@H]1C(N)=O	10.1021/jm0505462
	CHEMBL365775	134002	0	None	-	1	Rat	9.3	pEC50	=	9.3	Binding	Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8	ChEMBL	513	9	4	9	-2.3	Cn1cncc1C[C@H](N)C(=O)N1C(=O)CC[C@H]1C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N1CCC[C@H]1C(N)=O	10.1021/jm0505462
	2139	10627	56	None	-1	4	Mouse	9.2	pEC50	=	9.2	Binding	Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL		None	None	None		None	10.1021/jm960053k
	2316	10627	56	None	-1	4	Mouse	9.2	pEC50	=	9.2	Binding	Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL		None	None	None		None	10.1021/jm960053k
	3836	10627	56	None	-1	4	Mouse	9.2	pEC50	=	9.2	Binding	Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL		None	None	None		None	10.1021/jm960053k
	638678	10627	56	None	-1	4	Mouse	9.2	pEC50	=	9.2	Binding	Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL		None	None	None		None	10.1021/jm960053k
	CHEMBL1472	10627	56	None	-1	4	Mouse	9.2	pEC50	=	9.2	Binding	Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL		None	None	None		None	10.1021/jm960053k
	DB09421	10627	56	None	-1	4	Mouse	9.2	pEC50	=	9.2	Binding	Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL		None	None	None		None	10.1021/jm960053k
	CHEMBL36631	218827	14	None	-	1	Mouse	7.0	pEC50	=	7.0	Binding	Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL		None	None	None		NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1	10.1021/jm960053k
	9979181	12188	1	None	-	1	Mouse	5.8	pEC50	=	5.8	Binding	Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol	ChEMBL	414	3	2	4	1.0	NC(=O)[C@@H]1CC[C@H]2CC(C3CCCCC3)=C(N3CC[C@]4(CCC(=O)N4)C3=O)C(=O)N21	10.1016/s0960-894x(98)00567-8
	CHEMBL107238	12188	1	None	-	1	Mouse	5.8	pEC50	=	5.8	Binding	Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol	ChEMBL	414	3	2	4	1.0	NC(=O)[C@@H]1CC[C@H]2CC(C3CCCCC3)=C(N3CC[C@]4(CCC(=O)N4)C3=O)C(=O)N21	10.1016/s0960-894x(98)00567-8
	9979180	115230	1	None	-	1	Mouse	4.8	pEC50	=	4.8	Binding	Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol	ChEMBL	414	3	2	4	1.0	NC(=O)[C@@H]1CC[C@@H]2CC(C3CCCCC3)=C(N3CC[C@]4(CCC(=O)N4)C3=O)C(=O)N12	10.1016/s0960-894x(98)00567-8
	CHEMBL319910	115230	1	None	-	1	Mouse	4.8	pEC50	=	4.8	Binding	Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol	ChEMBL	414	3	2	4	1.0	NC(=O)[C@@H]1CC[C@@H]2CC(C3CCCCC3)=C(N3CC[C@]4(CCC(=O)N4)C3=O)C(=O)N12	10.1016/s0960-894x(98)00567-8
	11795153	208637	0	None	-	1	Mouse	6.5	pEC50	=	6.5	Binding	Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL	398	5	2	4	-0.0	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)N1CC[C@]2(CCC(=O)N2)C1=O	10.1021/jm960053k
	CHEMBL607173	208637	0	None	-	1	Mouse	6.5	pEC50	=	6.5	Binding	Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cellsEffective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL	398	5	2	4	-0.0	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)N1CC[C@]2(CCC(=O)N2)C1=O	10.1021/jm960053k
	CHEMBL197149	215884	0	None	-	1	Rat	6.5	pEC50	=	6.5	Binding	Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.16-0.51 uMSignaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.16-0.51 uM	ChEMBL		None	None	None		CCCc1nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	10.1021/jm0505462
	2139	10627	56	None	-2	4	Rat	8.5	pEC50	=	8.5	Binding	Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uMSignaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uM	ChEMBL		None	None	None		None	10.1021/jm0505462
	2316	10627	56	None	-2	4	Rat	8.5	pEC50	=	8.5	Binding	Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uMSignaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uM	ChEMBL		None	None	None		None	10.1021/jm0505462
	3836	10627	56	None	-2	4	Rat	8.5	pEC50	=	8.5	Binding	Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uMSignaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uM	ChEMBL		None	None	None		None	10.1021/jm0505462
	638678	10627	56	None	-2	4	Rat	8.5	pEC50	=	8.5	Binding	Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uMSignaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uM	ChEMBL		None	None	None		None	10.1021/jm0505462
	CHEMBL1472	10627	56	None	-2	4	Rat	8.5	pEC50	=	8.5	Binding	Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uMSignaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uM	ChEMBL		None	None	None		None	10.1021/jm0505462
	DB09421	10627	56	None	-2	4	Rat	8.5	pEC50	=	8.5	Binding	Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uMSignaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uM	ChEMBL		None	None	None		None	10.1021/jm0505462
	CHEMBL2370383	216622	3	None	-	1	Mouse	6.4	pEC50	=	6.4	Binding	Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositolAbility to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol	ChEMBL		None	None	None		NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H]1CCC(=O)N1	10.1016/s0960-894x(98)00567-8
	127032875	145657	0	None	-	0	Mouse	5.9	pIC50	=	5.9	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	516	7	3	6	-0.7	CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I	10.1016/j.ejmech.2016.01.038
	CHEMBL3782037	145657	0	None	-	0	Mouse	5.9	pIC50	=	5.9	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	516	7	3	6	-0.7	CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I	10.1016/j.ejmech.2016.01.038
	127032259	145561	0	None	-	0	Mouse	6.8	pIC50	=	6.8	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	454	6	3	6	-1.0	Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br	10.1016/j.ejmech.2016.01.038
	CHEMBL3780746	145561	0	None	-	0	Mouse	6.8	pIC50	=	6.8	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	454	6	3	6	-1.0	Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br	10.1016/j.ejmech.2016.01.038
	127032260	145497	0	None	-	0	Mouse	4.7	pIC50	=	4.7	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	468	7	3	6	-0.6	CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br	10.1016/j.ejmech.2016.01.038
	CHEMBL3779931	145497	0	None	-	0	Mouse	4.7	pIC50	=	4.7	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	468	7	3	6	-0.6	CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br	10.1016/j.ejmech.2016.01.038
	2139	10627	56	None	-1	4	Mouse	8.6	pIC50	=	8.6	Binding	Displacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting methodDisplacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2015.07.022
	2316	10627	56	None	-1	4	Mouse	8.6	pIC50	=	8.6	Binding	Displacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting methodDisplacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2015.07.022
	3836	10627	56	None	-1	4	Mouse	8.6	pIC50	=	8.6	Binding	Displacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting methodDisplacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2015.07.022
	638678	10627	56	None	-1	4	Mouse	8.6	pIC50	=	8.6	Binding	Displacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting methodDisplacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2015.07.022
	CHEMBL1472	10627	56	None	-1	4	Mouse	8.6	pIC50	=	8.6	Binding	Displacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting methodDisplacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2015.07.022
	DB09421	10627	56	None	-1	4	Mouse	8.6	pIC50	=	8.6	Binding	Displacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting methodDisplacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method	ChEMBL		None	None	None		None	10.1016/j.bmc.2015.07.022
	127032258	145518	0	None	-	0	Mouse	4.7	pIC50	=	4.7	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	486	8	3	6	0.4	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(Cl)n1)NC(=O)[C@@H]1CCC(=O)N1	10.1016/j.ejmech.2016.01.038
	CHEMBL3780248	145518	0	None	-	0	Mouse	4.7	pIC50	=	4.7	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	486	8	3	6	0.4	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(Cl)n1)NC(=O)[C@@H]1CCC(=O)N1	10.1016/j.ejmech.2016.01.038
	2139	10627	56	None	-1	4	Mouse	7.6	pIC50	=	7.6	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.01.038
	2316	10627	56	None	-1	4	Mouse	7.6	pIC50	=	7.6	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.01.038
	3836	10627	56	None	-1	4	Mouse	7.6	pIC50	=	7.6	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.01.038
	638678	10627	56	None	-1	4	Mouse	7.6	pIC50	=	7.6	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.01.038
	CHEMBL1472	10627	56	None	-1	4	Mouse	7.6	pIC50	=	7.6	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.01.038
	DB09421	10627	56	None	-1	4	Mouse	7.6	pIC50	=	7.6	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL		None	None	None		None	10.1016/j.ejmech.2016.01.038
	127033191	145567	0	None	-	0	Mouse	4.5	pIC50	=	4.5	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	642	7	3	6	-0.1	CCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I	10.1016/j.ejmech.2016.01.038
	CHEMBL3780802	145567	0	None	-	0	Mouse	4.5	pIC50	=	4.5	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	642	7	3	6	-0.1	CCn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I	10.1016/j.ejmech.2016.01.038
	127032563	145550	0	None	-	0	Mouse	6.5	pIC50	=	6.5	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	502	6	3	6	-1.2	Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I	10.1016/j.ejmech.2016.01.038
	CHEMBL3780645	145550	0	None	-	0	Mouse	6.5	pIC50	=	6.5	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	502	6	3	6	-1.2	Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I	10.1016/j.ejmech.2016.01.038
	127032878	145548	0	None	-	0	Mouse	4.3	pIC50	=	4.3	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	628	6	3	6	-0.6	Cn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I	10.1016/j.ejmech.2016.01.038
	CHEMBL3780633	145548	0	None	-	0	Mouse	4.3	pIC50	=	4.3	Binding	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrsDisplacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	628	6	3	6	-0.6	Cn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I	10.1016/j.ejmech.2016.01.038
	CHEMBL39363	219247	0	None	-	1	Mouse	8.9	pKi	=	8.9	Binding	Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL		None	None	None		Cn1cnc(C[C@H](NC(=O)[C@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1	10.1021/jm960053k
	2139	10627	56	None	-1	4	Mouse	8.0	pKi	=	8	Binding	Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL		None	None	None		None	10.1021/jm960053k
	2316	10627	56	None	-1	4	Mouse	8.0	pKi	=	8	Binding	Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL		None	None	None		None	10.1021/jm960053k
	3836	10627	56	None	-1	4	Mouse	8.0	pKi	=	8	Binding	Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL		None	None	None		None	10.1021/jm960053k
	638678	10627	56	None	-1	4	Mouse	8.0	pKi	=	8	Binding	Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL		None	None	None		None	10.1021/jm960053k
	CHEMBL1472	10627	56	None	-1	4	Mouse	8.0	pKi	=	8	Binding	Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL		None	None	None		None	10.1021/jm960053k
	DB09421	10627	56	None	-1	4	Mouse	8.0	pKi	=	8	Binding	Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL		None	None	None		None	10.1021/jm960053k
	CHEMBL390942	219227	0	None	-	1	Human	8.0	pKi	=	8.0	Binding	Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1	ChEMBL		None	None	None		CCn1cnc(C[C@H](NC(=O)[C@@H]2CCCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1	10.1016/j.bmc.2006.09.045
	9979181	12188	1	None	-	1	Mouse	5.8	pKi	=	5.8	Binding	Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.	ChEMBL	414	3	2	4	1.0	NC(=O)[C@@H]1CC[C@H]2CC(C3CCCCC3)=C(N3CC[C@]4(CCC(=O)N4)C3=O)C(=O)N21	10.1016/s0960-894x(98)00567-8
	CHEMBL107238	12188	1	None	-	1	Mouse	5.8	pKi	=	5.8	Binding	Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.	ChEMBL	414	3	2	4	1.0	NC(=O)[C@@H]1CC[C@H]2CC(C3CCCCC3)=C(N3CC[C@]4(CCC(=O)N4)C3=O)C(=O)N21	10.1016/s0960-894x(98)00567-8
	CHEMBL36631	218827	14	None	-	1	Mouse	5.8	pKi	=	5.8	Binding	Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL		None	None	None		NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1	10.1021/jm960053k
	2139	10627	56	None	-1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1	ChEMBL		None	None	None		None	10.1016/j.bmc.2006.09.045
	2316	10627	56	None	-1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1	ChEMBL		None	None	None		None	10.1016/j.bmc.2006.09.045
	3836	10627	56	None	-1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1	ChEMBL		None	None	None		None	10.1016/j.bmc.2006.09.045
	638678	10627	56	None	-1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1	ChEMBL		None	None	None		None	10.1016/j.bmc.2006.09.045
	CHEMBL1472	10627	56	None	-1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1	ChEMBL		None	None	None		None	10.1016/j.bmc.2006.09.045
	DB09421	10627	56	None	-1	4	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1	ChEMBL		None	None	None		None	10.1016/j.bmc.2006.09.045
	2139	10627	56	None	-2	4	Rat	7.7	pKi	=	7.7	Binding	Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM	ChEMBL		None	None	None		None	10.1021/jm0505462
	2316	10627	56	None	-2	4	Rat	7.7	pKi	=	7.7	Binding	Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM	ChEMBL		None	None	None		None	10.1021/jm0505462
	3836	10627	56	None	-2	4	Rat	7.7	pKi	=	7.7	Binding	Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM	ChEMBL		None	None	None		None	10.1021/jm0505462
	638678	10627	56	None	-2	4	Rat	7.7	pKi	=	7.7	Binding	Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM	ChEMBL		None	None	None		None	10.1021/jm0505462
	CHEMBL1472	10627	56	None	-2	4	Rat	7.7	pKi	=	7.7	Binding	Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM	ChEMBL		None	None	None		None	10.1021/jm0505462
	DB09421	10627	56	None	-2	4	Rat	7.7	pKi	=	7.7	Binding	Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM	ChEMBL		None	None	None		None	10.1021/jm0505462
	134134558	150136	0	None	-	1	Rat	7.7	pKi	=	7.7	Binding	Displacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranesDisplacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranes	ChEMBL	518	11	3	5	4.9	O=C(O)C(Cc1ccccc1)N[C@@H](Cc1cn(Cc2ccccc2)cn1)C(=O)Nc1ccc2ccccc2c1	nan
	CHEMBL3897627	150136	0	None	-	1	Rat	7.7	pKi	=	7.7	Binding	Displacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranesDisplacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranes	ChEMBL	518	11	3	5	4.9	O=C(O)C(Cc1ccccc1)N[C@@H](Cc1cn(Cc2ccccc2)cn1)C(=O)Nc1ccc2ccccc2c1	nan
	2139	10627	56	None	-1	4	Mouse	7.6	pKi	=	7.6	Binding	Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.	ChEMBL		None	None	None		None	10.1016/s0960-894x(98)00567-8
	2316	10627	56	None	-1	4	Mouse	7.6	pKi	=	7.6	Binding	Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.	ChEMBL		None	None	None		None	10.1016/s0960-894x(98)00567-8
	3836	10627	56	None	-1	4	Mouse	7.6	pKi	=	7.6	Binding	Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.	ChEMBL		None	None	None		None	10.1016/s0960-894x(98)00567-8
	638678	10627	56	None	-1	4	Mouse	7.6	pKi	=	7.6	Binding	Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.	ChEMBL		None	None	None		None	10.1016/s0960-894x(98)00567-8
	CHEMBL1472	10627	56	None	-1	4	Mouse	7.6	pKi	=	7.6	Binding	Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.	ChEMBL		None	None	None		None	10.1016/s0960-894x(98)00567-8
	DB09421	10627	56	None	-1	4	Mouse	7.6	pKi	=	7.6	Binding	Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.	ChEMBL		None	None	None		None	10.1016/s0960-894x(98)00567-8
	44422122	91887	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1	ChEMBL	514	9	5	7	-2.8	C[n+]1c[nH]cc1C[C@H](N)C(=O)N1C(=O)CC[C@H]1C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N1CCC[C@H]1C(N)=O	10.1016/j.bmc.2006.09.045
	CHEMBL224730	91887	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1	ChEMBL	514	9	5	7	-2.8	C[n+]1c[nH]cc1C[C@H](N)C(=O)N1C(=O)CC[C@H]1C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N1CCC[C@H]1C(N)=O	10.1016/j.bmc.2006.09.045
	44403976	134002	0	None	-	1	Rat	8.5	pKi	=	8.5	Binding	Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRHInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH	ChEMBL	513	9	4	9	-2.3	Cn1cncc1C[C@H](N)C(=O)N1C(=O)CC[C@H]1C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N1CCC[C@H]1C(N)=O	10.1021/jm0505462
	CHEMBL365775	134002	0	None	-	1	Rat	8.5	pKi	=	8.5	Binding	Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRHInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH	ChEMBL	513	9	4	9	-2.3	Cn1cncc1C[C@H](N)C(=O)N1C(=O)CC[C@H]1C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N1CCC[C@H]1C(N)=O	10.1021/jm0505462
	CHEMBL223972	216226	0	None	-	1	Human	8.5	pKi	=	8.5	Binding	Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1	ChEMBL		None	None	None		Cn1cnc(C[C@H](NC(=O)[C@@H]2CCCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1	10.1016/j.bmc.2006.09.045
	CHEMBL197149	215884	0	None	-	1	Rat	6.5	pKi	=	6.5	Binding	Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.27-0.37 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.27-0.37 uM	ChEMBL		None	None	None		CCCc1nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	10.1021/jm0505462
	9979180	115230	1	None	-	1	Mouse	4.4	pKi	=	4.4	Binding	Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.	ChEMBL	414	3	2	4	1.0	NC(=O)[C@@H]1CC[C@@H]2CC(C3CCCCC3)=C(N3CC[C@]4(CCC(=O)N4)C3=O)C(=O)N12	10.1016/s0960-894x(98)00567-8
	CHEMBL319910	115230	1	None	-	1	Mouse	4.4	pKi	=	4.4	Binding	Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.	ChEMBL	414	3	2	4	1.0	NC(=O)[C@@H]1CC[C@@H]2CC(C3CCCCC3)=C(N3CC[C@]4(CCC(=O)N4)C3=O)C(=O)N12	10.1016/s0960-894x(98)00567-8
	CHEMBL224525	216227	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1	ChEMBL		None	None	None		CCCc1nc(C[C@H](NC(=O)[C@@H]2CCCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	10.1016/j.bmc.2006.09.045
	2139	10627	56	None	-2	4	Rat	7.4	pKi	=	7.4	Binding	Inhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrainInhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrain	ChEMBL		None	None	None		None	10.1021/jm020531t
	2316	10627	56	None	-2	4	Rat	7.4	pKi	=	7.4	Binding	Inhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrainInhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrain	ChEMBL		None	None	None		None	10.1021/jm020531t
	3836	10627	56	None	-2	4	Rat	7.4	pKi	=	7.4	Binding	Inhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrainInhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrain	ChEMBL		None	None	None		None	10.1021/jm020531t
	638678	10627	56	None	-2	4	Rat	7.4	pKi	=	7.4	Binding	Inhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrainInhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrain	ChEMBL		None	None	None		None	10.1021/jm020531t
	CHEMBL1472	10627	56	None	-2	4	Rat	7.4	pKi	=	7.4	Binding	Inhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrainInhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrain	ChEMBL		None	None	None		None	10.1021/jm020531t
	DB09421	10627	56	None	-2	4	Rat	7.4	pKi	=	7.4	Binding	Inhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrainInhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrain	ChEMBL		None	None	None		None	10.1021/jm020531t
	11795153	208637	0	None	-	1	Mouse	5.4	pKi	=	5.4	Binding	Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL	398	5	2	4	-0.0	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)N1CC[C@]2(CCC(=O)N2)C1=O	10.1021/jm960053k
	CHEMBL607173	208637	0	None	-	1	Mouse	5.4	pKi	=	5.4	Binding	Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL	398	5	2	4	-0.0	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)N1CC[C@]2(CCC(=O)N2)C1=O	10.1021/jm960053k
	10255308	151213	0	None	-	1	Rat	4.3	pKi	=	4.3	Binding	Displacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranesDisplacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranes	ChEMBL	497	7	4	7	-0.3	Cc1cc(=O)oc2cc(NC(=O)[C@@H]3CCCN3C(=O)[C@H](CC(N)=O)NC(=O)[C@@H]3CCC(=O)N3)ccc12	nan
	CHEMBL3906398	151213	0	None	-	1	Rat	4.3	pKi	=	4.3	Binding	Displacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranesDisplacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranes	ChEMBL	497	7	4	7	-0.3	Cc1cc(=O)oc2cc(NC(=O)[C@@H]3CCCN3C(=O)[C@H](CC(N)=O)NC(=O)[C@@H]3CCC(=O)N3)ccc12	nan
	CHEMBL2370383	216622	3	None	-	1	Mouse	5.2	pKi	=	5.2	Binding	Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.	ChEMBL		None	None	None		NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H]1CCC(=O)N1	10.1016/s0960-894x(98)00567-8
	CHEMBL3954284	219265	0	None	-	1	Rat	5.2	pKi	=	5.2	Binding	Displacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranesDisplacement of [3H]-3MeHis-TRH from TRH receptor in Sprague-Dawley rat cortical membranes	ChEMBL		None	None	None		NC(=O)C[C@H](NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(N)=O	nan
	CHEMBL388528	219197	0	None	-	1	Human	5.1	pKi	=	5.1	Binding	Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1	ChEMBL		None	None	None		C=CCn1cnc(C[C@H](NC(=O)[C@@H]2CCCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1	10.1016/j.bmc.2006.09.045
	2137	9299	0	None	-1	2	Rat	8.5	pKd	=	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	376	6	3	5	-1.5	O=C(N1CCC[C@H]1C(=O)N)[C@@H](NC(=O)[C@@H]1CCC(=O)N1C)Cc1[nH]cnc1	6264336
	2141	9299	0	None	-1	2	Rat	8.5	pKd	=	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	376	6	3	5	-1.5	O=C(N1CCC[C@H]1C(=O)N)[C@@H](NC(=O)[C@@H]1CCC(=O)N1C)Cc1[nH]cnc1	6264336
	5311291	9299	0	None	-1	2	Rat	8.5	pKd	=	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	376	6	3	5	-1.5	O=C(N1CCC[C@H]1C(=O)N)[C@@H](NC(=O)[C@@H]1CCC(=O)N1C)Cc1[nH]cnc1	6264336
	None	223116	0	3H-MeTRH	1	2	Mouse	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	362	6	4	5	-1.8	C1CC(N(C1)C(=O)C(CC2=CN=CN2)NC(=O)C3CCC(=O)N3)C(=O)N	None
	None	223116	0	3H-MeTRH	-1	2	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	362	6	4	5	-1.8	C1CC(N(C1)C(=O)C(CC2=CN=CN2)NC(=O)C3CCC(=O)N3)C(=O)N	None
	None	223116	0	3H-N tau (1)-Me-His-TRH	-1	2	Human	7.7	pKi	=	7.7	Binding	NoneNone	PDSP KiDatabase	362	6	4	5	-1.8	C1CC(N(C1)C(=O)C(CC2=CN=CN2)NC(=O)C3CCC(=O)N3)C(=O)N	None
	2712	7703	34	None	-45	4	Mouse	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	None
	3370	7703	34	None	-45	4	Mouse	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	None
	594	7703	34	None	-45	4	Mouse	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	None
	CHEMBL451	7703	34	None	-45	4	Mouse	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	None
	DB00475	7703	34	None	-45	4	Mouse	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	None
	2712	7703	34	None	-40	4	Rat	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	None
	3370	7703	34	None	-40	4	Rat	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	None
	594	7703	34	None	-40	4	Rat	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	None
	CHEMBL451	7703	34	None	-40	4	Rat	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	None
	DB00475	7703	34	None	-40	4	Rat	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	None
	3016	8194	48	None	-46	5	Rat	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	284	1	0	2	3.2	Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1	None
	3364	8194	48	None	-46	5	Rat	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	284	1	0	2	3.2	Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1	None
	852	8194	48	None	-46	5	Rat	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	284	1	0	2	3.2	Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1	None
	CHEMBL12	8194	48	None	-46	5	Rat	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	284	1	0	2	3.2	Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1	None
	DB00829	8194	48	None	-46	5	Rat	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	284	1	0	2	3.2	Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1	None
	1802	9311	33	None	1513	2	Rat	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	325	1	0	3	4.3	Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F	None
	3342	9311	33	None	1513	2	Rat	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	325	1	0	3	4.3	Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F	None
	4192	9311	33	None	1513	2	Rat	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	325	1	0	3	4.3	Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F	None
	CHEMBL655	9311	33	None	1513	2	Rat	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	325	1	0	3	4.3	Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F	None
	DB00683	9311	33	None	1513	2	Rat	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	325	1	0	3	4.3	Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F	None
	114750	10518	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	405	6	4	6	-2.1	CN1C(=O)C[C@H](NC1=O)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N)Cc1[nH]cnc1	None
	2143	10518	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	405	6	4	6	-2.1	CN1C(=O)C[C@H](NC1=O)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N)Cc1[nH]cnc1	None
	CHEMBL2107016	10518	0	None	-	1	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	405	6	4	6	-2.1	CN1C(=O)C[C@H](NC1=O)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N)Cc1[nH]cnc1	None
	2712	7703	34	None	5	4	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	None
	3370	7703	34	None	5	4	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	None
	594	7703	34	None	5	4	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	None
	CHEMBL451	7703	34	None	5	4	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	None
	DB00475	7703	34	None	5	4	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	None
	2139	10627	56	None	-1	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1	Drug Central		None	None	None		None	None
	2316	10627	56	None	-1	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1	Drug Central		None	None	None		None	None
	3836	10627	56	None	-1	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1	Drug Central		None	None	None		None	None
	638678	10627	56	None	-1	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1	Drug Central		None	None	None		None	None
	CHEMBL1472	10627	56	None	-1	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1	Drug Central		None	None	None		None	None
	DB09421	10627	56	None	-1	4	Human	8.1	pKi	=	8.1	Binding	Displacement of [3H]N(1)-Me-His-TRH from TRHR1Displacement of [3H]N(1)-Me-His-TRH from TRHR1	Drug Central		None	None	None		None	None
	2139	10627	56	None	-2	4	Rat	8.1	pKi	=	8.1	Binding	Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM	Drug Central		None	None	None		None	None
	2316	10627	56	None	-2	4	Rat	8.1	pKi	=	8.1	Binding	Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM	Drug Central		None	None	None		None	None
	3836	10627	56	None	-2	4	Rat	8.1	pKi	=	8.1	Binding	Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM	Drug Central		None	None	None		None	None
	638678	10627	56	None	-2	4	Rat	8.1	pKi	=	8.1	Binding	Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM	Drug Central		None	None	None		None	None
	CHEMBL1472	10627	56	None	-2	4	Rat	8.1	pKi	=	8.1	Binding	Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM	Drug Central		None	None	None		None	None
	DB09421	10627	56	None	-2	4	Rat	8.1	pKi	=	8.1	Binding	Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uMInhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM	Drug Central		None	None	None		None	None
	2139	10627	56	None	-1	4	Mouse	8.1	pKi	=	8.1	Binding	Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells	Drug Central		None	None	None		None	None
	2316	10627	56	None	-1	4	Mouse	8.1	pKi	=	8.1	Binding	Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells	Drug Central		None	None	None		None	None
	3836	10627	56	None	-1	4	Mouse	8.1	pKi	=	8.1	Binding	Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells	Drug Central		None	None	None		None	None
	638678	10627	56	None	-1	4	Mouse	8.1	pKi	=	8.1	Binding	Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells	Drug Central		None	None	None		None	None
	CHEMBL1472	10627	56	None	-1	4	Mouse	8.1	pKi	=	8.1	Binding	Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells	Drug Central		None	None	None		None	None
	DB09421	10627	56	None	-1	4	Mouse	8.1	pKi	=	8.1	Binding	Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cellsBinding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells	Drug Central		None	None	None		None	None
	2712	7703	34	None	-45	4	Mouse	4.7	pKi	=	4.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	2175902
	3370	7703	34	None	-45	4	Mouse	4.7	pKi	=	4.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	2175902
	594	7703	34	None	-45	4	Mouse	4.7	pKi	=	4.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	2175902
	CHEMBL451	7703	34	None	-45	4	Mouse	4.7	pKi	=	4.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	2175902
	DB00475	7703	34	None	-45	4	Mouse	4.7	pKi	=	4.7	Binding	UnclassifiedUnclassified	Guide to Pharmacology	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	2175902
	2712	7703	34	None	-40	4	Rat	4.8	pKi	=	4.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	2566295
	3370	7703	34	None	-40	4	Rat	4.8	pKi	=	4.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	2566295
	594	7703	34	None	-40	4	Rat	4.8	pKi	=	4.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	2566295
	CHEMBL451	7703	34	None	-40	4	Rat	4.8	pKi	=	4.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	2566295
	DB00475	7703	34	None	-40	4	Rat	4.8	pKi	=	4.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	299	1	1	3	3.0	CNC1=Nc2ccc(cc2C(=[N+](C1)[O-])c1ccccc1)Cl	2566295
	3016	8194	48	None	-46	5	Rat	5.2	pKi	=	5.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	284	1	0	2	3.2	Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1	2566295
	3364	8194	48	None	-46	5	Rat	5.2	pKi	=	5.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	284	1	0	2	3.2	Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1	2566295
	852	8194	48	None	-46	5	Rat	5.2	pKi	=	5.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	284	1	0	2	3.2	Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1	2566295
	CHEMBL12	8194	48	None	-46	5	Rat	5.2	pKi	=	5.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	284	1	0	2	3.2	Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1	2566295
	DB00829	8194	48	None	-46	5	Rat	5.2	pKi	=	5.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	284	1	0	2	3.2	Clc1ccc2c(c1)C(=NCC(=O)N2C)c1ccccc1	2566295
	1802	9311	33	None	1513	2	Rat	5.5	pKi	=	5.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	325	1	0	3	4.3	Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F	2566295
	3342	9311	33	None	1513	2	Rat	5.5	pKi	=	5.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	325	1	0	3	4.3	Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F	2566295
	4192	9311	33	None	1513	2	Rat	5.5	pKi	=	5.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	325	1	0	3	4.3	Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F	2566295
	CHEMBL655	9311	33	None	1513	2	Rat	5.5	pKi	=	5.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	325	1	0	3	4.3	Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F	2566295
	DB00683	9311	33	None	1513	2	Rat	5.5	pKi	=	5.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	325	1	0	3	4.3	Clc1ccc2c(c1)C(=NCc1n2c(C)nc1)c1ccccc1F	2566295
	114750	10518	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	405	6	4	6	-2.1	CN1C(=O)C[C@H](NC1=O)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N)Cc1[nH]cnc1	23087672
	2143	10518	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	405	6	4	6	-2.1	CN1C(=O)C[C@H](NC1=O)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N)Cc1[nH]cnc1	23087672
	CHEMBL2107016	10518	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	405	6	4	6	-2.1	CN1C(=O)C[C@H](NC1=O)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N)Cc1[nH]cnc1	23087672
	2139	10627	56	None	-2	4	Rat	7.4	pKi	=	7.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8592728
	2316	10627	56	None	-2	4	Rat	7.4	pKi	=	7.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8592728
	3836	10627	56	None	-2	4	Rat	7.4	pKi	=	7.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8592728
	638678	10627	56	None	-2	4	Rat	7.4	pKi	=	7.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8592728
	CHEMBL1472	10627	56	None	-2	4	Rat	7.4	pKi	=	7.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8592728
	DB09421	10627	56	None	-2	4	Rat	7.4	pKi	=	7.4	Binding	UnclassifiedUnclassified	Guide to Pharmacology		None	None	None		None	8592728
	2137	9299	0	None	1	2	Human	8.5	pKi	=	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	376	6	3	5	-1.5	O=C(N1CCC[C@H]1C(=O)N)[C@@H](NC(=O)[C@@H]1CCC(=O)N1C)Cc1[nH]cnc1	5001013
	2141	9299	0	None	1	2	Human	8.5	pKi	=	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	376	6	3	5	-1.5	O=C(N1CCC[C@H]1C(=O)N)[C@@H](NC(=O)[C@@H]1CCC(=O)N1C)Cc1[nH]cnc1	5001013
	5311291	9299	0	None	1	2	Human	8.5	pKi	=	8.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	376	6	3	5	-1.5	O=C(N1CCC[C@H]1C(=O)N)[C@@H](NC(=O)[C@@H]1CCC(=O)N1C)Cc1[nH]cnc1	5001013

Join us

Cite us

Main reference

Ligand source activities (1 row/activity)