GproteinDb

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Ligand source activities (1 row/activity)

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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	3H-DHA	60	Human	Binding	pKi	=	10000.00	5.00	-1995	14	-	PDSP KiDatabase	183.1	3	4	4	0.35	CNCC(O)c1ccc(O)c(O)c1	-
(+)-adrenaline	290	None	26	Dog	Binding	Ki	=	3700.00	5.43	-3	5	Binding of [3H]dihydroalprenolol to beta-2 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
(+)-sulpiride	3703	3H-DHA	66	Rat	Binding	pKi	=	10000.00	5.00	-549	23	-	PDSP KiDatabase	341.1	6	2	5	0.56	CCN1CCC[C@@H]1CNC(=O)c1cc(S(N)(=O)=O)ccc1OC	-
(-)-adrenaline	291	None	40	Human	Binding	pKi	=	-	6.10	-89	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	=	-	6.10	-89	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/9295336
(-)-adrenaline	291	None	40	Human	Binding	pKi	=	-	6.10	-89	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	=	-	6.10	-89	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	Kd	=	630.00	6.20	-89	35	Binding affinity to human adrenergic beta2 receptor	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1016/j.ejmech.2008.12.016
(-)-adrenaline	291	3H-DHA	40	Human	Binding	pKi	=	1100.00	5.96	-89	35	-	PDSP KiDatabase	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-adrenaline	291	125I-CYP	40	Human	Binding	pKi	=	735.00	6.13	-89	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	pKd	=	6.20	8.21	-89	35	Binding affinity to human adrenergic beta2 receptor	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	=	284.00	6.55	-89	35	DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-adrenaline	291	None	40	Human	Binding	Ki	=	196.00	6.71	-89	35	DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-adrenaline	291	None	40	Human	Binding	Kd	=	630.96	6.20	-89	35	Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1016/j.bmcl.2013.07.052
(-)-adrenaline	291	None	40	Human	Binding	Ki	=	360.00	6.44	-89	35	Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1016/j.bmc.2016.04.028
(-)-adrenaline	291	125I-ICYP	40	Human	Binding	pKi	=	3467.36	5.46	-89	35	-	PDSP KiDatabase	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-adrenaline	291	3H-CGP-12177	40	Human	Binding	pKi	=	1995.26	5.70	-89	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	=	720.00	6.14	-12	35	Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar 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	pKi	=	6.14	8.21	-12	35	Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes	Drug Central	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-adrenaline	291	None	40	Dog	Binding	Ki	=	660.00	6.18	-30	35	Binding of [3H]dihydroalprenolol to beta-2 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

Showing 1 to 20 of 2,550 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	3139	None	60	Human	Functional	EC50	=	2620.00	5.58	1	14	PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]	ChEMBL	183.1	3	4	4	0.35	CNCC(O)c1ccc(O)c(O)c1	-
(+)-HIGENAMINE	188503	None	8	Rat	Functional	EC50	=	4500.00	5.35	-	1	Agonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to control	ChEMBL	271.1	2	4	4	2.23	Oc1ccc(C[C@H]2NCCc3cc(O)c(O)cc32)cc1	https://dx.doi.org/10.1016/j.bmc.2017.10.011
(-)-adrenaline	291	None	40	Human	Functional	pEC50	=	-	7.90	-7	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	EC50	=	1380.00	5.86	-7	35	PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	-
(-)-adrenaline	291	None	40	Human	Functional	EC50	=	615.46	6.21	-7	35	GPCR PRESTO-Tango dose-response in agonist mode with target: ADRB2	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	AC50	=	22.00	7.66	-7	35	Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer 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	Guinea pig	Functional	EC50	=	15.00	7.82	-4	35	Effective dose for relaxation of guinea pig trachea.	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	-4	35	Effective dose for relaxation of guinea pig trachea.	ChEMBL	183.1	3	4	4	0.35	CNC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm00019a001
(-)-HIGENAMINE	179060	None	19	Rat	Functional	EC50	=	600.00	6.22	-	1	Agonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to control	ChEMBL	271.1	2	4	4	2.23	Oc1ccc(C[C@@H]2NCCc3cc(O)c(O)cc32)cc1	https://dx.doi.org/10.1016/j.bmc.2017.10.011
(-)-noradrenaline	2857	None	46	Human	Functional	pEC50	=	-	6.40	-154	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	Human	Functional	EC50	=	9380.02	5.03	-154	32	GPCR PRESTO-Tango dose-response in agonist mode with target: ADRB2	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	Guinea pig	Functional	EC50	=	213.00	6.67	-204	32	Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.	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	=	30000.00	4.52	-204	32	Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.	ChEMBL	169.1	2	4	4	0.09	NC[C@H](O)c1ccc(O)c(O)c1	https://dx.doi.org/10.1021/jm00019a001
(-)-propranolol	3187	None	44	Human	Functional	Kd	=	0.24	9.62	6	34	Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-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	=	50.12	7.30	6	34	Antagonist activity at human beta2 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	IC50	=	0.55	9.26	6	34	Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under dark conditions by FRET assay	ChEMBL	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	https://dx.doi.org/10.1021/acs.jmedchem.0c00831
(-)-propranolol	3187	None	44	Human	Functional	IC50	=	2.26	8.65	6	34	GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2	ChEMBL	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	https://dx.doi.org/10.6019/CHEMBL5442687
(-)-propranolol	3187	None	44	Human	Functional	IC50	=	0.48	9.32	6	34	Antagonist activity at ADRB2 endogenously expressed in HEK293 cells transfected with cAMP FRET biosensor assessed as inhibition of cimaterol-induced response pre-incubated for 45 mins under constant violet light conditions by FRET assay	ChEMBL	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	https://dx.doi.org/10.1021/acs.jmedchem.0c00831
(-)-propranolol	3187	None	44	Guinea pig	Functional	Kd	=	3.39	8.47	-18	34	Antagonism of isoprenaline-induced relaxation of guinea pig tracheal chains, contracted with carbachol	ChEMBL	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	https://dx.doi.org/10.1021/jm00119a011
(-)-propranolol	3187	None	44	Guinea pig	Functional	Kd	=	3.39	8.47	-18	34	The apparent pA2 value was measured for beta-2 adrenergic blocking activity on the trachea of guinea pig	ChEMBL	259.2	6	2	3	2.58	CC(C)NC[C@H](O)COc1cccc2ccccc12	https://dx.doi.org/10.1021/jm00180a007

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Ligand source activities (1 row/activity)