GproteinDb

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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	=	12.00	7.92	-7	21	DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)	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	=	7.92	8.10	-7	21	DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)	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	-
α-ergocryptine	358	None	18	Human	Binding	IC50	=	26.00	7.58	-7	21	DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)	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	-
(±)-adrenaline	3139	None	60	Human	Binding	pKi	=	-	5.70	-398	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
(+)-chlorpheniramine	918	None	42	Human	Binding	Ki	=	2103.00	5.68	-234	27	DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)	ChEMBL	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	-
(+)-chlorpheniramine	918	None	42	Human	Binding	IC50	=	4607.00	5.34	-234	27	DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)	ChEMBL	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	-
(+)-chlorpheniramine	918	None	42	Human	Binding	AC50	=	9800.10	5.01	-234	27	Binding affinity towards human ADRA2B in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	https://dx.doi.org/10.1038/s41467-023-40064-9
(+)-chlorpheniramine	918	None	42	Human	Binding	pKi	=	5.68	8.25	-234	27	DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)	Drug Central	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	-
(+)-chlorpheniramine	918	None	42	Human	Binding	AC50	=	4900.00	5.31	-234	27	Binding affinity towards human ADRA2B in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	https://dx.doi.org/10.1038/s41467-023-40064-9
(-)-adrenaline	291	None	40	Human	Binding	pKi	=	-	4.40	-151	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	=	-	4.40	-151	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	3H-RAUWOLSCINE	40	Human	Binding	pKi	=	255.00	6.59	-151	35	-	PDSP KiDatabase	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-adrenaline	291	35S-GTPGammaS	40	Human	Binding	pKi	=	6309.57	5.20	-151	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	=	6.40	8.19	-151	35	DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)	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	=	869.00	6.06	-151	35	DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-adrenaline	291	None	40	Human	Binding	Ki	=	397.00	6.40	-151	35	DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-adrenaline	291	None	40	Human	Binding	AC50	=	7799.90	5.11	-151	35	Binding affinity towards human ADRA2B in an in vitro assay with cellular components measured by scintillation proximity assay	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	Binding	AC50	=	4000.00	5.40	-151	35	Binding affinity towards human ADRA2B in an in vitro assay with cellular components measured by scintillation proximity assay	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	Binding	Ki	=	1737.80	5.76	-151	35	PDSP Secondary Binding target: ADRA2B - 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	=	-	4.75	-61	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

Showing 1 to 20 of 1,639 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	=	-	7.50	-25	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	pIC50	=	-	7.60	-25	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	=	-	6.30	-25	35	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
(-)-noradrenaline	2857	None	46	Human	Functional	pEC50	=	-	6.90	-2	32	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	=	-	7.80	-2	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
(-)-noradrenaline	2857	None	46	Human	Functional	pEC50	=	-	7.80	-2	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	=	61.66	7.21	-2	32	Agonist activity at human recombinant adrenergic alpha2B receptor expressed in CHO cells	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	=	61.66	7.21	-2	32	Agonistic potency at human adrenergic alpha-2B 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	=	61.66	7.21	-2	32	Agonist activity at human adrenergic alpha-2B 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
A-1262543	193	None	0	Rat	Functional	pEC50	=	-	8.40	-	1	Unclassified	Guide to Pharmacology	306.1	2	2	4	3.14	FC(F)(F)c1ccc(NC2=NCCN2)c(-c2cccnc2)c1	https://pubmed.ncbi.nlm.nih.gov/25154730
amitriptyline	401	None	38	Human	Functional	pIC50	=	8.00	8.10	-56	51	None	Drug Central	277.2	3	0	1	4.17	CN(C)CCC=C1c2ccccc2CCc2ccccc21	-
ASCORBIC ACID	71449	None	60	Human	Functional	EC50	=	0.50	9.30	-	1	Agonist activity at human adrenergic alpha2B receptor expressed in HEK293 cells coexpressing Gqi5 protein by FLIPR assay	ChEMBL	176.0	2	4	6	-1.41	O=C1O[C@H]([C@@H](O)CO)C(O)=C1O	https://dx.doi.org/10.1016/j.bmc.2009.01.065
BIPHENYLINE	18863	None	0	Human	Functional	EC50	=	645.65	6.19	-11	3	Agonist activity at human adrenergic alpha-2B receptor expressed in CHO cells assessed as extracellular acidification by cytosensor microphysiometry	ChEMBL	266.1	4	1	3	3.12	CC(Oc1ccccc1-c1ccccc1)C1=NCCN1	https://dx.doi.org/10.1021/jm0408215
BIPHENYLINE	18863	None	0	Human	Functional	EC50	=	645.65	6.19	-11	3	Agonistic potency at human adrenergic alpha-2B receptor expressed in CHO cells assessed as forskolin-induced cAMP accumulation	ChEMBL	266.1	4	1	3	3.12	CC(Oc1ccccc1-c1ccccc1)C1=NCCN1	https://dx.doi.org/10.1021/jm061487a
BIPHENYLINE	18863	None	0	Human	Functional	EC50	=	645.65	6.19	-11	3	Agonist activity at human recombinant adrenergic alpha2B receptor expressed in CHO cells	ChEMBL	266.1	4	1	3	3.12	CC(Oc1ccccc1-c1ccccc1)C1=NCCN1	https://dx.doi.org/10.1021/jm800250z
BIPHENYLINE	18863	None	0	Human	Functional	EC50	=	645.65	6.19	-11	3	Agonist activity at human alpha2B adrenoceptor expressed in CHO cells assessed as induction of extracellular acidification by microphysiometry	ChEMBL	266.1	4	1	3	3.12	CC(Oc1ccccc1-c1ccccc1)C1=NCCN1	https://dx.doi.org/10.1021/jm100977d
brimonidine (UK14304)	722	None	63	Human	Functional	pIC50	=	-	8.40	-28	14	inhibition of forskolin stimulated cAMP generation	Guide to Pharmacology	291.0	1	2	5	1.76	Brc1c(NC2=NCCN2)ccc2nccnc12	https://pubmed.ncbi.nlm.nih.gov/36101495
brimonidine (UK14304)	722	None	63	Human	Functional	pEC50	=	-	7.80	-28	14	ERK1/2 phosphorylation	Guide to Pharmacology	291.0	1	2	5	1.76	Brc1c(NC2=NCCN2)ccc2nccnc12	https://pubmed.ncbi.nlm.nih.gov/36101495
brimonidine (UK14304)	722	None	63	Human	Functional	pEC50	=	7.26	8.14	-28	14	None	Drug Central	291.0	1	2	5	1.76	Brc1c(NC2=NCCN2)ccc2nccnc12	-
brimonidine (UK14304)	722	None	63	Human	Functional	EC50	=	281.84	6.55	-28	14	Alpha-2B adrenergic receptor agonistic potency as inhibition of forskolin-stimulated cyclic adenosine monophosphate synthesis	ChEMBL	291.0	1	2	5	1.76	Brc1c(NC2=NCCN2)ccc2nccnc12	https://dx.doi.org/10.1016/0960-894X(95)00391-6

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Ligand source activities (1 row/activity)