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Ligand source activities (1 row/activity)

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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

α-ergocryptine	358	None	18	Human	Binding	Ki	=	5.48	8.26	-5	21	DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)	ChEMBL	575.3	5	3	6	2.43	CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12	-
α-ergocryptine	358	None	18	Human	Binding	IC50	=	38.00	7.42	-5	21	DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)	ChEMBL	575.3	5	3	6	2.43	CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12	-
α-ergocryptine	358	None	18	Human	Binding	pKi	=	8.26	8.08	-5	21	DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)	Drug Central	575.3	5	3	6	2.43	CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12	-
(±)-adrenaline	3139	None	60	Human	Binding	pKi	=	-	6.00	-199	14	Unclassified	Guide to Pharmacology	183.1	3	4	4	0.35	CNCC(O)c1ccc(O)c(O)c1	https://pubmed.ncbi.nlm.nih.gov/9605427
(-)-adrenaline	291	None	40	Human	Binding	pKi	=	-	5.35	-85	35	Unclassified	Guide to Pharmacology	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://pubmed.ncbi.nlm.nih.gov/9605427
(-)-adrenaline	291	None	40	Human	Binding	pKi	=	-	5.35	-85	35	Unclassified	Guide to Pharmacology	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://pubmed.ncbi.nlm.nih.gov/36101495
(-)-adrenaline	291	35S-GTPGammaS	40	Human	Binding	pKi	=	1698.24	5.77	-85	35	-	PDSP KiDatabase	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-adrenaline	291	None	40	Human	Binding	pKi	=	6.45	8.19	-85	35	DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)	Drug Central	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-adrenaline	291	None	40	Human	Binding	IC50	=	2449.00	5.61	-85	35	DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-adrenaline	291	None	40	Human	Binding	Ki	=	356.00	6.45	-85	35	DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-adrenaline	291	None	40	Human	Binding	Ki	=	1150.67	5.94	-85	35	PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.6019/CHEMBL5442175
(-)-noradrenaline	2857	None	46	Human	Binding	pKi	=	-	5.65	-28	32	Unclassified	Guide to Pharmacology	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://pubmed.ncbi.nlm.nih.gov/9824686
(-)-noradrenaline	2857	None	46	Human	Binding	pKi	=	-	5.65	-28	32	Unclassified	Guide to Pharmacology	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://pubmed.ncbi.nlm.nih.gov/9605427
(-)-noradrenaline	2857	None	46	Human	Binding	pKi	=	-	5.65	-28	32	Unclassified	Guide to Pharmacology	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://pubmed.ncbi.nlm.nih.gov/36101495
(-)-noradrenaline	2857	None	46	Human	Binding	pKi	=	-	5.65	-28	32	Unclassified	Guide to Pharmacology	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://pubmed.ncbi.nlm.nih.gov/25080296
(-)-noradrenaline	2857	None	46	Human	Binding	Ki	=	63.00	7.20	-28	32	Binding affinity for human Alpha-2C adrenergic receptor	ChEMBL	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm960012o
(-)-noradrenaline	2857	None	46	Human	Binding	Ki	=	385.65	6.41	-28	32	PDSP Secondary Binding target: ADRA2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.6019/CHEMBL5442175
(-)-noradrenaline	2857	None	46	Human	Binding	pKi	=	7.20	8.14	-28	32	Binding affinity for human Alpha-2C adrenergic receptor	Drug Central	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	-
(-)-noradrenaline	2857	None	46	Mouse	Binding	Ki	=	650.00	6.19	-12	32	Binding affinity to mouse alpha-2C receptor expressed in COS7 cells	ChEMBL	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	-
(-)-noradrenaline	2857	None	46	Mouse	Binding	pKi	=	6.19	8.21	-12	32	Binding affinity to mouse alpha-2C receptor expressed in COS7 cells	Drug Central	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	-

Showing 1 to 20 of 1,501 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

(-)-adrenaline	291	None	40	Human	Functional	pIC50	=	-	6.70	-44	35	inhibition of cAMP production	Guide to Pharmacology	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://pubmed.ncbi.nlm.nih.gov/36101495
(-)-adrenaline	291	None	40	Human	Functional	pEC50	=	-	7.60	-44	35	ERK1/2 phosphorylation	Guide to Pharmacology	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://pubmed.ncbi.nlm.nih.gov/36101495
(-)-adrenaline	291	None	40	Human	Functional	AC50	=	2700.00	5.57	-44	35	Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1038/s41467-023-40064-9
(-)-adrenaline	291	None	40	Human	Functional	AC50	=	10999.90	4.96	-44	35	Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1038/s41467-023-40064-9
(-)-noradrenaline	2857	None	46	Human	Functional	pIC50	=	-	7.55	-11	32	inhibition of cAMP production	Guide to Pharmacology	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://pubmed.ncbi.nlm.nih.gov/36101495
(-)-noradrenaline	2857	None	46	Human	Functional	pIC50	=	-	7.55	-11	32	inhibition of cAMP production	Guide to Pharmacology	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://pubmed.ncbi.nlm.nih.gov/25080296
(-)-noradrenaline	2857	None	46	Human	Functional	pEC50	=	-	6.31	-11	32	6.02 = value for β-arrestin recruitment and internalization	Guide to Pharmacology	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://pubmed.ncbi.nlm.nih.gov/25080296
(-)-noradrenaline	2857	None	46	Human	Functional	pEC50	=	-	7.70	-11	32	ERK1/2 phosphorylation	Guide to Pharmacology	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://pubmed.ncbi.nlm.nih.gov/36101495
(-)-noradrenaline	2857	None	46	Human	Functional	EC50	=	794.33	6.10	-11	32	Agonistic potency at human adrenergic Alpha-2C receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation	ChEMBL	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm061487a
(-)-noradrenaline	2857	None	46	Human	Functional	EC50	=	794.33	6.10	-11	32	Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification	ChEMBL	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm800250z
(-)-noradrenaline	2857	None	46	Human	Functional	EC50	=	794.33	6.10	-11	32	Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry	ChEMBL	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm901262f
(-)-noradrenaline	2857	None	46	Human	Functional	AC50	=	260.00	6.58	-11	32	Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1038/s41467-023-40064-9
(-)-noradrenaline	2857	None	46	Human	Functional	EC50	=	794.33	6.10	-11	32	Agonist activity at human adrenergic alpha-2C receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry	ChEMBL	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm0408215
(-)-propranolol	3187	None	44	Human	Functional	AC50	=	15000.00	4.82	-9549	34	Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	https://dx.doi.org/10.1038/s41467-023-40064-9
ACETOPHENAZINE	7074	None	25	Human	Functional	AC50	=	720.00	6.14	-165	16	Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	411.2	7	1	6	3.49	CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2	https://dx.doi.org/10.1038/s41467-023-40064-9
aclidinium	261	None	6	Human	Functional	AC50	=	2500.00	5.60	-13182	11	Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	484.2	9	1	6	4.67	O=C(O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)C(O)(c1cccs1)c1cccs1	https://dx.doi.org/10.1038/s41467-023-40064-9
AJMALINE	78241	None	0	Human	Functional	AC50	=	1400.00	5.85	3	4	Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	326.2	1	2	4	1.55	CCC1C2CC3C4N(C)c5ccccc5C45CC(C2[C@H]5O)N3C1O	https://dx.doi.org/10.1038/s41467-023-40064-9
alfuzosin	343	None	50	Human	Functional	AC50	=	810.00	6.09	-14	11	Compound was evaluated for inhibition of human ADRA2C in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	389.2	8	3	7	2.02	COc1cc2nc(N(C)CCCN=C(O)C3CCCO3)[nH]c(=N)c2cc1OC	https://dx.doi.org/10.1038/s41467-023-40064-9
ALLYPHENYLINE	187770	None	3	Human	Functional	EC50	=	50.12	7.30	-	4	Agonist activity at human recombinant adrenergic Alpha-2C receptor expressed in CHO cells assessed as stimulation of extracellular acidification	ChEMBL	230.1	5	1	3	2.18	C=CCc1ccccc1OC(C)C1=NCCN1	https://dx.doi.org/10.1021/jm800250z
ALLYPHENYLINE	187770	None	3	Human	Functional	EC50	=	50.12	7.30	-	4	Agonist activity at human Alpha-2C adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry	ChEMBL	230.1	5	1	3	2.18	C=CCc1ccccc1OC(C)C1=NCCN1	https://dx.doi.org/10.1021/jm100977d

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Ligand source activities (1 row/activity)