ArrestinDb

Ligand source activities (1 row/activity)

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Ligands (move mouse cursor over ligand name to see structure)					Receptor			Assay information							Chemical information
Sel. page	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity	# Tested GPCRs	Species	p-value (-log)	Activity Type	Activity Relation	Activity Value	AssayType	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	68344426	175696	0	None	-4	3	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R44 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as effect on intracellular calcium level by FLIPR assayAgonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R44 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as effect on intracellular calcium level by FLIPR assay	ChEMBL	250	0	1	3	2.6	C/C1=C\C[C@H](O)/C(C)=C/[C@H]2OC(=O)[C@@H](C)C2CC1	nan
	CHEMBL4582048	175696	0	None	-4	3	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R44 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as effect on intracellular calcium level by FLIPR assayAgonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R44 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as effect on intracellular calcium level by FLIPR assay	ChEMBL	250	0	1	3	2.6	C/C1=C\C[C@H](O)/C(C)=C/[C@H]2OC(=O)[C@@H](C)C2CC1	nan
	23259348	169913	0	None	-3	3	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R44 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R44 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as increase in intracellular calcium level by FLIPR assay	ChEMBL	250	0	1	3	2.6	C/C1=C\C[C@H](O)/C(C)=C/[C@H]2OC(=O)[C@@H](C)[C@@H]2CC1	nan
	CHEMBL4440983	169913	0	None	-3	3	Human	4.5	pEC50	=	4.5	Functional	Agonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R44 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as increase in intracellular calcium level by FLIPR assayAgonist activity at recombinant human N-terminal rat ST3 receptor-fused TAS2R44 expressed in HEK293T cells co-expressing Galpha16gust44 assessed as increase in intracellular calcium level by FLIPR assay	ChEMBL	250	0	1	3	2.6	C/C1=C\C[C@H](O)/C(C)=C/[C@H]2OC(=O)[C@@H](C)[C@@H]2CC1	nan
	1499	2091	47	None	-63	38	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay	ChEMBL	211	4	4	4	1.1	CC(NCC(c1ccc(c(c1)O)O)O)C	nan
	3779	2091	47	None	-63	38	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay	ChEMBL	211	4	4	4	1.1	CC(NCC(c1ccc(c(c1)O)O)O)C	nan
	536	2091	47	None	-63	38	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay	ChEMBL	211	4	4	4	1.1	CC(NCC(c1ccc(c(c1)O)O)O)C	nan
	CHEMBL434	2091	47	None	-63	38	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay	ChEMBL	211	4	4	4	1.1	CC(NCC(c1ccc(c(c1)O)O)O)C	nan
	DB01064	2091	47	None	-63	38	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay	ChEMBL	211	4	4	4	1.1	CC(NCC(c1ccc(c(c1)O)O)O)C	nan
	1499	2091	47	None	-63	38	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay	Drug Central	211	4	4	4	1.1	CC(NCC(c1ccc(c(c1)O)O)O)C	None
	3779	2091	47	None	-63	38	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay	Drug Central	211	4	4	4	1.1	CC(NCC(c1ccc(c(c1)O)O)O)C	None
	536	2091	47	None	-63	38	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay	Drug Central	211	4	4	4	1.1	CC(NCC(c1ccc(c(c1)O)O)O)C	None
	CHEMBL434	2091	47	None	-63	38	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay	Drug Central	211	4	4	4	1.1	CC(NCC(c1ccc(c(c1)O)O)O)C	None
	DB01064	2091	47	None	-63	38	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assayAgonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay	Drug Central	211	4	4	4	1.1	CC(NCC(c1ccc(c(c1)O)O)O)C	None
	12460	253	0	None	1	2	Human	2.6	pEC50	=	2.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	163	0	1	4	-0.7	CC1=CC(=O)NS(=O)(=O)O1	15537898
	36573	253	0	None	1	2	Human	2.6	pEC50	=	2.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	163	0	1	4	-0.7	CC1=CC(=O)NS(=O)(=O)O1	15537898
	CHEMBL176687	253	0	None	1	2	Human	2.6	pEC50	=	2.6	Functional	UnclassifiedUnclassified	Guide to Pharmacology	163	0	1	4	-0.7	CC1=CC(=O)NS(=O)(=O)O1	15537898
	5143	3457	0	None	1	2	Human	3.0	pEC50	=	3.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	183	0	1	3	0.1	O=C1NS(=O)(=O)c2c1cccc2	15537898
	5432	3457	0	None	1	2	Human	3.0	pEC50	=	3.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	183	0	1	3	0.1	O=C1NS(=O)(=O)c2c1cccc2	15537898
	CHEMBL310671	3457	0	None	1	2	Human	3.0	pEC50	=	3.0	Functional	UnclassifiedUnclassified	Guide to Pharmacology	183	0	1	3	0.1	O=C1NS(=O)(=O)c2c1cccc2	15537898
	12438	471	0	None	-5	3	Human	6.4	pEC50	=	6.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	341	3	1	6	3.3	COC1=CC=CC2=C3C(=C(C=C21)[N+](=O)[O-])C(=CC4=C3OCO4)C(=O)O	15537898
	2236	471	0	None	-5	3	Human	6.4	pEC50	=	6.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	341	3	1	6	3.3	COC1=CC=CC2=C3C(=C(C=C21)[N+](=O)[O-])C(=CC4=C3OCO4)C(=O)O	15537898
	CHEMBL93353	471	0	None	-5	3	Human	6.4	pEC50	=	6.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	341	3	1	6	3.3	COC1=CC=CC2=C3C(=C(C=C21)[N+](=O)[O-])C(=CC4=C3OCO4)C(=O)O	15537898
	12470	1276	0	None	-3	2	Human	1.8	pIC50	=	1.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	179	2	2	2	0.7	C1CCC(CC1)NS(=O)(=O)O	28919036
	7533	1276	0	None	-3	2	Human	1.8	pIC50	=	1.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	179	2	2	2	0.7	C1CCC(CC1)NS(=O)(=O)O	28919036
	CHEMBL1206440	1276	0	None	-3	2	Human	1.8	pIC50	=	1.8	Functional	UnclassifiedUnclassified	Guide to Pharmacology	179	2	2	2	0.7	C1CCC(CC1)NS(=O)(=O)O	28919036
	412	3460	46	None	-	1	Human	5.3	pIC50	=	5.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	286	2	2	5	2.8	COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O	22059530
	73571	3460	46	None	-	1	Human	5.3	pIC50	=	5.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	286	2	2	5	2.8	COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O	22059530
	CHEMBL448297	3460	46	None	-	1	Human	5.3	pIC50	=	5.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	286	2	2	5	2.8	COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O	22059530
	DB08517	3460	46	None	-	1	Human	5.3	pIC50	=	5.3	Functional	UnclassifiedUnclassified	Guide to Pharmacology	286	2	2	5	2.8	COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O	22059530
	25099817	1802	0	None	1	3	Human	5.5	pIC50	=	5.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	198	4	1	1	3.3	CC1CCC(C1(C)C)CCCC(=O)O	20537538
	9112	1802	0	None	1	3	Human	5.5	pIC50	=	5.5	Functional	UnclassifiedUnclassified	Guide to Pharmacology	198	4	1	1	3.3	CC1CCC(C1(C)C)CCCC(=O)O	20537538

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Ligands (move mouse cursor over ligand name to see structure)					Receptor			Assay information							Chemical information
Sel. page	Similar- ity	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity	# Tested GPCRs	Species	p-value (-log)	Activity Type	Activity Relation	Activity Value	Assay Type	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
		5379096	186407	93	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit	ChEMBL	330	3	3	7	2.6	COc1cc(-c2cc(=O)c3c(O)c(OC)c(O)cc3o2)ccc1O	10.1021/np200391c
		CHEMBL487601	186407	93	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit	ChEMBL	330	3	3	7	2.6	COc1cc(-c2cc(=O)c3c(O)c(OC)c(O)cc3o2)ccc1O	10.1021/np200391c
		44576022	186942	1	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit	ChEMBL	372	4	2	7	3.4	COc1cc([C@@H]2CC(=O)c3c(O)cc(O)cc3O2)ccc1OC(=O)C(C)C	10.1021/np200391c
		CHEMBL490162	186942	1	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit	ChEMBL	372	4	2	7	3.4	COc1cc([C@@H]2CC(=O)c3c(O)cc(O)cc3O2)ccc1OC(=O)C(C)C	10.1021/np200391c
		44412004	78261	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit	ChEMBL	316	3	2	6	2.8	COc1cc2c(c(O)c1OC)C(=O)C[C@@H](c1ccc(O)cc1)O2	10.1021/np200391c
		CHEMBL210692	78261	0	None	-	0	Human	5.6	pIC50	=	5.6	Binding	Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit	ChEMBL	316	3	2	6	2.8	COc1cc2c(c(O)c1OC)C(=O)C[C@@H](c1ccc(O)cc1)O2	10.1021/np200391c
		412	3460	46	None	-	3	Human	5.4	pIC50	=	5.4	Binding	Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit	ChEMBL	286	2	2	5	2.8	COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O	10.1021/np200391c
		73571	3460	46	None	-	3	Human	5.4	pIC50	=	5.4	Binding	Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit	ChEMBL	286	2	2	5	2.8	COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O	10.1021/np200391c
		CHEMBL448297	3460	46	None	-	3	Human	5.4	pIC50	=	5.4	Binding	Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit	ChEMBL	286	2	2	5	2.8	COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O	10.1021/np200391c
		DB08517	3460	46	None	-	3	Human	5.4	pIC50	=	5.4	Binding	Inhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunitInhibition of human TAS2R31 receptor expressed in HEK293T cells overexpressing chimeric G-protein alpha-subunit	ChEMBL	286	2	2	5	2.8	COc1cc2O[C@@H](CC(=O)c2c(c1)O)c1ccc(cc1)O	10.1021/np200391c
		13858192	113309	17	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Antagonist activity at human TAS2R31 expressed in HEK-293T cells stably expressing Galpha16gust44 assessed as inhibition receptor response to saccharin by fluorescence assayAntagonist activity at human TAS2R31 expressed in HEK-293T cells stably expressing Galpha16gust44 assessed as inhibition receptor response to saccharin by fluorescence assay	ChEMBL	362	5	1	3	5.1	C=C1CC[C@H]2C(C)(C)[C@@H](OC(C)=O)CC[C@]2(C)[C@H]1CC/C(C)=C/C(=O)O	10.1021/np5001413
		CHEMBL3315351	113309	17	None	-	0	Human	5.1	pIC50	=	5.1	Binding	Antagonist activity at human TAS2R31 expressed in HEK-293T cells stably expressing Galpha16gust44 assessed as inhibition receptor response to saccharin by fluorescence assayAntagonist activity at human TAS2R31 expressed in HEK-293T cells stably expressing Galpha16gust44 assessed as inhibition receptor response to saccharin by fluorescence assay	ChEMBL	362	5	1	3	5.1	C=C1CC[C@H]2C(C)(C)[C@@H](OC(C)=O)CC[C@]2(C)[C@H]1CC/C(C)=C/C(=O)O	10.1021/np5001413

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Ligand source activities (1 row/activity)