GPCRdb

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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

α-ergocryptine	358	None	18	Human	Binding	Ki	=	2.98	8.53	-3	21	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: 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	=	7.95	8.10	-3	21	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: 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	=	8.53	8.07	-3	21	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: 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	-
(+)-chlorpheniramine	918	None	42	Human	Binding	Ki	=	7625.00	5.12	-416	27	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)	ChEMBL	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	-
(+)-chlorpheniramine	918	None	42	Human	Binding	IC50	=	20333.00	4.69	-416	27	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)	ChEMBL	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	-
(+)-chlorpheniramine	918	None	42	Human	Binding	pKi	=	5.12	8.29	-416	27	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)	Drug Central	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	-
(+)-sulpiride	3703	None	66	Human	Binding	IC50	=	2019.00	5.70	-3	23	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)	ChEMBL	341.1	6	2	5	0.56	CCN1CCC[C@@H]1CNC(=O)c1cc(S(N)(=O)=O)ccc1OC	-
(+)-sulpiride	3703	None	66	Human	Binding	Ki	=	757.00	6.12	-3	23	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)	ChEMBL	341.1	6	2	5	0.56	CCN1CCC[C@@H]1CNC(=O)c1cc(S(N)(=O)=O)ccc1OC	-
(+)-sulpiride	3703	None	66	Human	Binding	AC50	=	7517.10	5.12	-3	23	Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting	ChEMBL	341.1	6	2	5	0.56	CCN1CCC[C@@H]1CNC(=O)c1cc(S(N)(=O)=O)ccc1OC	https://dx.doi.org/10.1038/s41467-023-40064-9
(+)-sulpiride	3703	None	66	Human	Binding	pKi	=	6.12	8.21	-3	23	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)	Drug Central	341.1	6	2	5	0.56	CCN1CCC[C@@H]1CNC(=O)c1cc(S(N)(=O)=O)ccc1OC	-
(-)-adrenaline	291	35S-GTPGammaS	40	Human	Binding	pKi	=	1479.11	5.83	-48	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	=	6.56	8.18	-48	35	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: 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	pKi	=	-	5.55	-48	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/9824686
(-)-adrenaline	291	None	40	Human	Binding	pKi	=	-	5.55	-48	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	=	-	5.55	-48	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	None	40	Human	Binding	IC50	=	737.00	6.13	-48	35	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: 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	=	276.00	6.56	-48	35	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: 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	AC50	=	8500.00	5.07	-48	35	Binding affinity towards human ADRA2A in an in vitro assay with cellular components measured by scintillation counting	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	3H-Yohimbine	40	Pig	Binding	pKi	=	645.65	6.19	-120	35	-	PDSP KiDatabase	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-adrenaline	291	35S-GTPGammaS	40	Mouse	Binding	pKi	=	389.05	6.41	-72	35	-	PDSP KiDatabase	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-

Showing 1 to 20 of 2,357 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	pEC50	=	-	5.50	-7	35	increased cAMP generation	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	EC50	=	5.63	8.25	-7	35	GPCR PRESTO-Tango dose-response in agonist mode with target: ADRA2A	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.6019/CHEMBL5442687
(-)-adrenaline	291	None	40	Human	Functional	pIC50	=	-	6.50	-7	35	inhibition of forskolin stimulated cAMP generation	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	=	-	6.80	-7	35	GTPγs binding	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	Functional	pEC50	=	-	8.00	-7	35	increased 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	=	11.00	7.96	-7	35	Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader	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	=	84.00	7.08	-7	35	Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader	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	pEC50	=	-	6.70	-11	32	GTPγs binding	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	Functional	EC50	=	371.54	6.43	-11	32	Agonistic potency at human adrenergic alpha-2A 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	=	371.54	6.43	-11	32	Agonist activity at human alpha2A 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	EC50	=	110.00	6.96	-11	32	Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting	ChEMBL	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1016/j.bmc.2010.11.020
(-)-noradrenaline	2857	None	46	Human	Functional	AC50	=	27.00	7.57	-11	32	Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader	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	AC50	=	4147.30	5.38	-11	32	Agonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader	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	=	30.11	7.52	-11	32	GPCR PRESTO-Tango dose-response in agonist mode with target: ADRA2A	ChEMBL	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.6019/CHEMBL5442687
(-)-noradrenaline	2857	None	46	Human	Functional	EC50	=	128.82	6.89	-11	32	Agonist activity at human alpha2A adrenoceptor expressed in CHO-K1 cells after 30 mins by [35S]GTPgammaS binding assay	ChEMBL	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1016/j.ejmech.2014.09.083
(-)-noradrenaline	2857	None	46	Human	Functional	EC50	=	118.00	6.93	-11	32	Agonist activity at human adrenoceptor alpha2A expressed in CHOK1 cells assessed as stimulation of agonist-induced [35S]GTPgammaS binding by scintillation counting	ChEMBL	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1016/j.bmc.2011.11.025
(-)-noradrenaline	2857	None	46	Human	Functional	EC50	=	371.54	6.43	-11	32	Agonist activity at human recombinant adrenergic alpha2A 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	=	371.54	6.43	-11	32	Agonist activity at human adrenergic alpha-2A 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
(-)-noradrenaline	2857	None	46	Human	Functional	pEC50	=	-	5.30	-11	32	increased cAMP generation	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	=	-	6.60	-11	32	inhibition of forskolin stimulated cAMP generation	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

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Ligand source activities (1 row/activity)