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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

(±)-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/2849109
(+)-adrenaline	290	None	26	Rat	Binding	Ki	=	13000.00	4.89	-12	5	Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes	ChEMBL	183.1	3	4	4	0.35	CNC[C@@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm990599h
(-)-adrenaline	291	None	40	Human	Binding	pKi	=	-	5.60	-70	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/2849109
(-)-adrenaline	291	None	40	Human	Binding	pKi	=	-	5.60	-70	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/14730417
(-)-adrenaline	291	None	40	Human	Binding	pKi	=	-	5.60	-70	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/20590599
(-)-adrenaline	291	None	40	Human	Binding	pKi	None	5.40	8.27	-70	35	None	Drug Central	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-adrenaline	291	125I-CYP	40	Human	Binding	pKi	=	3970.00	5.40	-70	35	-	PDSP KiDatabase	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-adrenaline	291	None	40	Rat	Binding	Ki	=	1100.00	5.96	-66	35	Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm990599h
(-)-adrenaline	291	None	40	Rat	Binding	pKi	=	5.96	8.22	-66	35	Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes	Drug Central	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-adrenaline	291	None	40	Rat	Binding	Ki	=	1200.00	5.92	-66	35	Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm00076a024
(-)-adrenaline	291	None	40	Rat	Binding	Ki	=	2100.00	5.68	-66	35	Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm990599h
(-)-adrenaline	291	None	40	Guinea pig	Binding	pKi	=	5.52	8.26	-23	35	Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol	Drug Central	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-adrenaline	291	None	40	Guinea pig	Binding	Ki	=	3000.00	5.52	-23	35	Binding affinity against beta-1 adrenergic receptor in guinea pig cerebral cortical membranes by displacement of Dihydro-[3H]-alprenolol	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm00118a019
(-)-noradrenaline	2857	None	46	Human	Binding	Ki	=	413.90	6.38	-33	32	PDSP Secondary Binding target: ADRB1 - 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	=	6.00	8.22	-33	32	None	Drug Central	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	-
(-)-noradrenaline	2857	None	46	Human	Binding	pKi	=	-	5.75	-33	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/2849109
(-)-noradrenaline	2857	None	46	Human	Binding	pKi	=	-	5.75	-33	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/14730417
(-)-noradrenaline	2857	None	46	Human	Binding	pKi	=	-	5.75	-33	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/20590599
(-)-noradrenaline	2857	None	46	Rat	Binding	Ki	=	1300.00	5.89	-144	32	Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes	ChEMBL	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm990599h
(-)-noradrenaline	2857	None	46	Rat	Binding	Ki	=	26000.00	4.58	-144	32	Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes	ChEMBL	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm990599h

Showing 1 to 20 of 1,968 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	=	-	7.60	-10	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/20590599
(-)-adrenaline	291	None	40	Human	Functional	AC50	=	970.00	6.01	-10	35	Compound was evaluated for inhibition of human ADRB1 in an in vitro assay measured by radioactivity method	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	EC50	=	290.00	6.54	-10	35	Agonist activity at human beta1 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/acs.jnatprod.9b00418
(-)-adrenaline	291	None	40	Guinea pig	Functional	EC50	=	15.00	7.82	-6	35	Effective dose required to stimulate contractions in isolated guinea pig atrium.	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm00019a001
(-)-adrenaline	291	None	40	Guinea pig	Functional	EC50	=	436.00	6.36	-6	35	Effective dose required to stimulate contractions in isolated guinea pig atrium.	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm00019a001
(-)-adrenaline	291	None	40	Guinea pig	Functional	EC50	=	260.00	6.58	-6	35	Agonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atria	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm00118a019
(-)-noradrenaline	2857	None	46	Human	Functional	pEC50	=	-	7.90	1	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/20590599
(-)-noradrenaline	2857	None	46	Guinea pig	Functional	EC50	=	10000.00	5.00	-37	32	Effective dose required to stimulate contractions in isolated guinea pig atrium.	ChEMBL	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm00019a001
(-)-noradrenaline	2857	None	46	Guinea pig	Functional	EC50	=	30.00	7.52	-37	32	Effective concentration for Beta-1 adrenergic receptor mediated inhibition of neurotransmission in field-stimulated reserpine pretreated guinea pig ileum.	ChEMBL	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm00019a001
(-)-noradrenaline	2857	None	46	Guinea pig	Functional	EC50	=	350.00	6.46	-37	32	Agonistic potency at beta-1 adrenergic receptor for the percent maximal increase in contraction rate of isolated guinea pig atria	ChEMBL	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm00118a019
(-)-propranolol	3187	None	44	Human	Functional	Kd	=	199.53	6.70	-6	34	Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis	ChEMBL	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	https://dx.doi.org/10.1021/jm2008562
(-)-propranolol	3187	None	44	Human	Functional	Kd	=	1.82	8.74	-6	34	Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis	ChEMBL	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	https://dx.doi.org/10.1021/jm2008562
(-)-propranolol	3187	None	44	Human	Functional	IC50	=	251.19	6.60	-6	34	Antagonist activity at human beta1 receptor expressed in CHO-K1 cells assessed as isoproterenol-induced cAMP level by HTRF assay	ChEMBL	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	https://dx.doi.org/10.1021/acs.jmedchem.5b01088
(-)-propranolol	3187	None	44	Human	Functional	AC50	=	21.00	7.68	-6	34	Compound was evaluated for inhibition of human ADRB1 in an in vitro assay measured by radioactivity method	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
(-)-propranolol	3187	None	44	Rat	Functional	Kd	=	2.40	8.62	-	34	Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for R-enantiomer)	ChEMBL	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	https://dx.doi.org/10.1021/jm970338c
(-)-propranolol	3187	None	44	Rat	Functional	Kd	=	2630.27	5.58	-	34	Beta-1 adrenergic receptor-Antagonism in isolated rat heart ventricle. ( for S-enantiomer)	ChEMBL	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	https://dx.doi.org/10.1021/jm970338c
(-)-propranolol	3187	None	44	Rat	Functional	Kd	=	4.37	8.36	-	34	Antagonist activity was determined against beta-1 adrenergic receptor in spontaneously beating rat atria	ChEMBL	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	https://dx.doi.org/10.1021/jm00389a008
(-)-propranolol	3187	None	44	Rat	Functional	Kd	=	4.37	8.36	-	34	Cardioselectivity for the beta-1 adrenergic receptor was determined against isoprenaline (antagonism) in isolated rat atria	ChEMBL	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	https://dx.doi.org/10.1021/jm00389a008
(-)-propranolol	3187	None	44	Rat	Functional	Ki	=	3.16	8.50	-	34	Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells	ChEMBL	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	https://dx.doi.org/10.1021/jm050624l
(-)-propranolol	3187	None	44	Rat	Functional	Ki	=	31.62	7.50	-	34	Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells	ChEMBL	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	https://dx.doi.org/10.1021/jm050624l

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Ligand source activities (1 row/activity)