GPCRdb

Ligand source activities (1 row/activity)

Affinity
Potency

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	Ligands				Receptor	Activity									Chemical information
	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

Ligands				Receptor	Activity									Chemical information
Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

CHEMBL107238	5418	None	1	Mouse	Binding	EC50	=	1800.00	5.75	-	1	Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol	ChEMBL	414.2	3	2	4	0.95	NC(=O)[C@@H]1CC[C@H]2CC(C3CCCCC3)=C(N3CC[C@]4(CCC(=O)N4)C3=O)C(=O)N21	https://dx.doi.org/10.1016/s0960-894x(98)00567-8
CHEMBL107238	5418	None	1	Mouse	Binding	Ki	=	1500.00	5.82	-	1	Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.	ChEMBL	414.2	3	2	4	0.95	NC(=O)[C@@H]1CC[C@H]2CC(C3CCCCC3)=C(N3CC[C@]4(CCC(=O)N4)C3=O)C(=O)N21	https://dx.doi.org/10.1016/s0960-894x(98)00567-8
CHEMBL197149	211564	None	0	Rat	Binding	Ki	=	320.00	6.50	-	1	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 uM	ChEMBL	-	-	-	-	-	CCCc1nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	https://dx.doi.org/10.1021/jm0505462
CHEMBL197149	211564	None	0	Rat	Binding	EC50	=	290.00	6.54	-	1	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 uM	ChEMBL	-	-	-	-	-	CCCc1nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	https://dx.doi.org/10.1021/jm0505462
CHEMBL223972	211906	None	0	Human	Binding	Ki	=	3.20	8.49	-	1	Displacement of [3H]N(1)-Me-His-TRH from TRHR1	ChEMBL	-	-	-	-	-	Cn1cnc(C[C@H](NC(=O)[C@@H]2CCCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1	https://dx.doi.org/10.1016/j.bmc.2006.09.045
CHEMBL224525	211907	None	0	Human	Binding	Ki	=	400.00	6.40	-	1	Displacement of [3H]N(1)-Me-His-TRH from TRHR1	ChEMBL	-	-	-	-	-	CCCc1nc(C[C@H](NC(=O)[C@@H]2CCCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	https://dx.doi.org/10.1016/j.bmc.2006.09.045
CHEMBL224730	85146	None	0	Human	Binding	Ki	=	3.00	8.52	-	1	Displacement of [3H]N(1)-Me-His-TRH from TRHR1	ChEMBL	514.3	9	5	7	-2.85	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	https://dx.doi.org/10.1016/j.bmc.2006.09.045
CHEMBL2370383	212302	None	2	Mouse	Binding	Ki	=	6500.00	5.19	-	1	Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.	ChEMBL	-	-	-	-	-	NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H]1CCC(=O)N1	https://dx.doi.org/10.1016/s0960-894x(98)00567-8
CHEMBL2370383	212302	None	2	Mouse	Binding	EC50	=	430.00	6.37	-	1	Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol	ChEMBL	-	-	-	-	-	NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC1CCCCC1)NC(=O)[C@@H]1CCC(=O)N1	https://dx.doi.org/10.1016/s0960-894x(98)00567-8
CHEMBL319910	108509	None	1	Mouse	Binding	Ki	=	36000.00	4.44	-	1	Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.	ChEMBL	414.2	3	2	4	0.95	NC(=O)[C@@H]1CC[C@@H]2CC(C3CCCCC3)=C(N3CC[C@]4(CCC(=O)N4)C3=O)C(=O)N12	https://dx.doi.org/10.1016/s0960-894x(98)00567-8
CHEMBL319910	108509	None	1	Mouse	Binding	EC50	=	18000.00	4.75	-	1	Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol	ChEMBL	414.2	3	2	4	0.95	NC(=O)[C@@H]1CC[C@@H]2CC(C3CCCCC3)=C(N3CC[C@]4(CCC(=O)N4)C3=O)C(=O)N12	https://dx.doi.org/10.1016/s0960-894x(98)00567-8
CHEMBL365775	127291	None	0	Rat	Binding	Ki	=	3.00	8.52	-	1	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	ChEMBL	513.2	9	4	9	-2.27	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	https://dx.doi.org/10.1021/jm0505462
CHEMBL365775	127291	None	0	Rat	Binding	EC50	=	0.50	9.30	-	1	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	ChEMBL	513.2	9	4	9	-2.27	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	https://dx.doi.org/10.1021/jm0505462
CHEMBL36631	214508	None	11	Mouse	Binding	Ki	=	1500.00	5.82	-	1	Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL	-	-	-	-	-	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1	https://dx.doi.org/10.1021/jm960053k
CHEMBL36631	214508	None	11	Mouse	Binding	EC50	=	110.00	6.96	-	1	Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells	ChEMBL	-	-	-	-	-	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1	https://dx.doi.org/10.1021/jm960053k
CHEMBL3779931	138806	None	0	Mouse	Binding	IC50	=	18600.00	4.73	-	1	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	468.1	7	3	6	-0.55	CCn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br	https://dx.doi.org/10.1016/j.ejmech.2016.01.038
CHEMBL3780248	138827	None	0	Mouse	Binding	IC50	=	20400.00	4.69	-	1	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	486.2	8	3	6	0.37	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1cn(Cc2ccccc2)c(Cl)n1)NC(=O)[C@@H]1CCC(=O)N1	https://dx.doi.org/10.1016/j.ejmech.2016.01.038
CHEMBL3780633	138857	None	0	Mouse	Binding	IC50	=	48030.00	4.32	-	1	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	628.0	6	3	6	-0.59	Cn1c(I)nc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1I	https://dx.doi.org/10.1016/j.ejmech.2016.01.038
CHEMBL3780645	138859	None	0	Mouse	Binding	IC50	=	324.00	6.49	-	1	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	502.1	6	3	6	-1.19	Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1I	https://dx.doi.org/10.1016/j.ejmech.2016.01.038
CHEMBL3780746	138870	None	0	Mouse	Binding	IC50	=	170.00	6.77	-	1	Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs	ChEMBL	454.1	6	3	6	-1.03	Cn1cc(C[C@H](NC(=O)[C@@H]2CCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)nc1Br	https://dx.doi.org/10.1016/j.ejmech.2016.01.038

Showing 1 to 20 of 60 entries

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	Ligands				Receptor	Activity									Chemical information
	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

Ligands				Receptor	Activity									Chemical information
Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

CHEMBL223972	211906	None	0	Human	Functional	EC50	=	4.90	8.31	-	1	Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity	ChEMBL	-	-	-	-	-	Cn1cnc(C[C@H](NC(=O)[C@@H]2CCCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c1	https://dx.doi.org/10.1016/j.bmc.2006.09.045
CHEMBL224525	211907	None	0	Human	Functional	EC50	=	380.00	6.42	-	1	Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity	ChEMBL	-	-	-	-	-	CCCc1nc(C[C@H](NC(=O)[C@@H]2CCCC(=O)N2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	https://dx.doi.org/10.1016/j.bmc.2006.09.045
CHEMBL224730	85146	None	0	Human	Functional	EC50	=	5.00	8.30	-	1	Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity	ChEMBL	514.3	9	5	7	-2.85	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	https://dx.doi.org/10.1016/j.bmc.2006.09.045
CHEMBL3600444	122444	None	0	Mouse	Functional	EC50	=	740.00	6.13	-	1	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	713.0	8	2	7	2.06	Cc1cnc(C(=O)N[C@@H](Cc2nc(I)n(Cc3ccccc3)c2I)C(=O)N2CCC[C@H]2C(N)=O)cn1	https://dx.doi.org/10.1016/j.bmc.2015.07.022
CHEMBL3600445	122445	None	0	Mouse	Functional	EC50	=	980.00	6.01	-	1	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	699.0	8	2	7	1.75	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)n(Cc2ccccc2)c1I)NC(=O)c1cnccn1	https://dx.doi.org/10.1016/j.bmc.2015.07.022
CHEMBL3600446	122446	None	0	Mouse	Functional	EC50	=	150.00	6.82	-	1	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	399.2	8	3	6	-0.03	CCCc1nc(C[C@H](NC(=O)c2cnccn2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	https://dx.doi.org/10.1016/j.bmc.2015.07.022
CHEMBL3600447	122447	None	0	Mouse	Functional	EC50	=	17.00	7.77	-	1	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	413.2	8	3	6	0.28	CCCc1nc(C[C@H](NC(=O)c2cnc(C)cn2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	https://dx.doi.org/10.1016/j.bmc.2015.07.022
CHEMBL3600448	122448	None	0	Mouse	Functional	EC50	=	1560.00	5.81	-	1	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	414.2	8	4	7	-0.45	CCCc1nc(C[C@H](NC(=O)c2nccnc2N)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	https://dx.doi.org/10.1016/j.bmc.2015.07.022
CHEMBL3600449	214270	None	0	Mouse	Functional	EC50	=	940.00	6.03	-	1	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	-	-	-	-	-	CCCc1nc(C[C@H](NC(=O)[C@H]2CCCCN2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	https://dx.doi.org/10.1016/j.bmc.2015.07.022
CHEMBL3600450	214271	None	0	Mouse	Functional	EC50	=	1000.00	6.00	-	1	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	-	-	-	-	-	CC(C)c1nc(C[C@H](NC(=O)[C@H]2CCCCN2)C(=O)N2CCC[C@H]2C(N)=O)c[nH]1	https://dx.doi.org/10.1016/j.bmc.2015.07.022
CHEMBL3600451	122449	None	0	Mouse	Functional	EC50	=	19350.00	4.71	-	1	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	391.1	6	3	6	-0.33	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc[nH]c1Cl)NC(=O)c1cnccn1	https://dx.doi.org/10.1016/j.bmc.2015.07.022
CHEMBL3600452	122450	None	0	Mouse	Functional	EC50	=	3980.00	5.40	-	1	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	435.1	6	3	6	-0.22	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc[nH]c1Br)NC(=O)c1cnccn1	https://dx.doi.org/10.1016/j.bmc.2015.07.022
CHEMBL3600453	122451	None	0	Mouse	Functional	EC50	=	2540.00	5.59	-	1	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	513.0	6	3	6	0.54	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Br)[nH]c1Br)NC(=O)c1cnccn1	https://dx.doi.org/10.1016/j.bmc.2015.07.022
CHEMBL3600454	122452	None	0	Mouse	Functional	EC50	=	77.00	7.11	-	1	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	527.0	6	3	6	0.85	Cc1cnc(C(=O)N[C@@H](Cc2nc(Br)[nH]c2Br)C(=O)N2CCC[C@H]2C(N)=O)cn1	https://dx.doi.org/10.1016/j.bmc.2015.07.022
CHEMBL3601781	122635	None	0	Mouse	Functional	EC50	=	498.00	6.30	-	1	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	449.1	6	3	6	0.09	Cc1cnc(C(=O)N[C@@H](Cc2nc[nH]c2Br)C(=O)N2CCC[C@H]2C(N)=O)cn1	https://dx.doi.org/10.1016/j.bmc.2015.07.022
CHEMBL3601782	122636	None	0	Mouse	Functional	EC50	=	287.00	6.54	-	1	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	450.1	6	4	7	-0.64	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc[nH]c1Br)NC(=O)c1nccnc1N	https://dx.doi.org/10.1016/j.bmc.2015.07.022
CHEMBL3601783	122637	None	0	Mouse	Functional	EC50	=	1410.00	5.85	-	1	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	528.0	6	4	7	0.12	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(Br)[nH]c1Br)NC(=O)c1nccnc1N	https://dx.doi.org/10.1016/j.bmc.2015.07.022
CHEMBL3601784	122638	None	0	Mouse	Functional	EC50	=	11280.00	4.95	-	1	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	608.9	6	3	6	0.23	NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1nc(I)[nH]c1I)NC(=O)c1cnccn1	https://dx.doi.org/10.1016/j.bmc.2015.07.022
CHEMBL3601785	122639	None	0	Mouse	Functional	EC50	=	340.00	6.47	-	1	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	449.1	6	2	7	-0.21	Cn1cnc(C[C@H](NC(=O)c2cnccn2)C(=O)N2CCC[C@H]2C(N)=O)c1Br	https://dx.doi.org/10.1016/j.bmc.2015.07.022
CHEMBL3601786	122640	None	0	Mouse	Functional	EC50	=	7210.00	5.14	-	1	Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method	ChEMBL	637.0	7	2	7	0.72	CCn1c(I)nc(C[C@H](NC(=O)c2cnccn2)C(=O)N2CCC[C@H]2C(N)=O)c1I	https://dx.doi.org/10.1016/j.bmc.2015.07.022

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