ArrestinDb

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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

[Ac-His¹]PACAP-27	257	None	0	Human	Binding	IC50	=	13.00	7.89	-	4	Displacement of [125I]PACAP27 from human VPAC2 receptor expressed in CHO cells	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm0609059
[Ala^11,22,28]VIP	328	None	0	Human	Binding	pKi	=	-	5.60	-316	3	inhibition of [125I]-VIP binding to membranes from CHO cells stably expressing the recombinant receptor	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/10801840
[Arg¹⁶]chicken secretin	468	None	0	Human	Binding	pIC50	=	-	5.30	-	7	Inhibition of [125I]VIP binding in membranes from CHO cells expressing recombinant receptor	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9437714
[Arg¹⁶]chicken secretin	468	None	0	Rat	Binding	pIC50	=	-	5.00	-	7	Inhibition of [125I]VIP binding in membranes from CHO cells expressing recombinant receptor	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9437714
[Lys¹⁵,Arg¹⁶,Leu²⁷]VIP-(1-7)/GRF-(8-27)-NH₂	2436	None	0	Human	Binding	pIC50	>	-	6.00	-	5	inhibition of [125I]-VIP binding to membranes from CHO cells stably expressing the recombinant receptor	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11931347
[Lys¹⁵,Arg¹⁶,Leu²⁷]VIP-(1-7)/GRF-(8-27)-NH₂	2436	None	0	Human	Binding	pIC50	>	-	4.50	-	5	Inhibition of [125I]VIP binding in membranes from CHO cells expressing recombinant receptor	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9437714
[Lys¹⁵,Arg¹⁶,Leu²⁷]VIP-(1-7)/GRF-(8-27)-NH₂	2436	None	0	Rat	Binding	pIC50	=	-	4.50	-	5	Inhibition of [125I]VIP binding in membranes from CHO cells expressing recombinant receptor	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9437714
BAY 55-9837	583	None	0	Human	Binding	pIC50	=	-	7.20	-	3	inhibition of [125I]-PACAP-27 binding to membranes from CHO cells stably expressing the recombinant receptor	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11978642
BAY 55-9837	583	None	0	Human	Binding	pKd	=	-	9.20	-	3	binding to membranes from CHO cells stably expressing the recombinant receptor	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11978642
CHEMBL3736134	136572	None	0	Human	Binding	IC50	=	36.31	7.44	-	3	Displacement of Ac-[125I]-PACAP27 from recombinant human VPAC2 expressed in CHO cells after 90 mins by gamma counting analysis	ChEMBL	3263.7	105	48	45	-10.62	CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(C#Cc2ccc(F)cc2)cc1)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)C(C)C)[C@@H](C)O	https://dx.doi.org/10.1016/j.ejmech.2015.09.017
CHEMBL3736134	136572	None	0	Human	Binding	IC50	=	36.00	7.44	-	3	Displacement of Ac-[125I]-PACAP27 from recombinant human VPAC2 expressed in CHO cells after 90 mins by gamma counting analysis	ChEMBL	3263.7	105	48	45	-10.62	CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(C#Cc2ccc(F)cc2)cc1)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)C(C)C)[C@@H](C)O	https://dx.doi.org/10.1016/j.ejmech.2015.09.017
CHEMBL3736230	136590	None	0	Human	Binding	IC50	=	53.70	7.27	-	3	Displacement of Ac-[125I]-PACAP27 from recombinant human VPAC2 expressed in CHO cells after 90 mins by gamma counting analysis	ChEMBL	3245.7	105	48	45	-10.76	CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(C#Cc2ccccc2)cc1)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)C(C)C)[C@@H](C)O	https://dx.doi.org/10.1016/j.ejmech.2015.09.017
CHEMBL3736230	136590	None	0	Human	Binding	IC50	=	53.00	7.28	-	3	Displacement of Ac-[125I]-PACAP27 from recombinant human VPAC2 expressed in CHO cells after 90 mins by gamma counting analysis	ChEMBL	3245.7	105	48	45	-10.76	CC[C@H](C)[C@H](NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(C#Cc2ccccc2)cc1)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)C(C)C)[C@@H](C)O	https://dx.doi.org/10.1016/j.ejmech.2015.09.017
CHEMBL3889643	142476	None	0	Human	Binding	IC50	=	5000.00	5.30	-	1	Antagonist activity at recombinant human N-terminal signal peptide/FLAG epitope-tagged Rluc8-fused VIPR2 expressed in HEK293 cells assessed as inhibition of VIP-induced human mVenus-beta-arrestin2 binding preincubated for 5 mins with luciferin, coelenterazine H followed by VIP addition measured after 5 mins by BRET assay	ChEMBL	550.2	12	3	6	3.21	CO[C@@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H](Cc1ccccc1)C[C@H](O)CNS(=O)(=O)c1ccc(C(C)=O)cc1	-
CHEMBL3890096	142529	None	0	Human	Binding	IC50	=	6000.00	5.22	-	1	Antagonist activity at recombinant human N-terminal signal peptide/FLAG epitope-tagged Rluc8-fused VIPR2 expressed in HEK293 cells assessed as inhibition of VIP-induced human mVenus-beta-arrestin2 binding preincubated for 5 mins with luciferin, coelenterazine H followed by VIP addition measured after 5 mins by BRET assay	ChEMBL	566.2	11	3	7	2.77	CO[C@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H](Cc1ccccc1)C[C@H](O)CNS(=O)(=O)c1ccc2c(c1)OCCO2	-
CHEMBL3905363	144404	None	0	Human	Binding	IC50	=	10000.00	5.00	-	1	Antagonist activity at recombinant human N-terminal signal peptide/FLAG epitope-tagged Rluc8-fused VIPR2 expressed in HEK293 cells assessed as inhibition of VIP-induced human mVenus-beta-arrestin2 binding preincubated for 5 mins with luciferin, coelenterazine H followed by VIP addition measured after 5 mins by BRET assay	ChEMBL	534.2	10	4	5	2.84	O=C(N[C@H]1c2ccccc2C[C@H]1O)[C@H](Cc1ccccc1)C[C@H](O)CNS(=O)(=O)c1ccc2c(c1)CCC2	-
CHEMBL3908152	144736	None	0	Human	Binding	IC50	=	40600.00	4.39	-	1	Antagonist activity at recombinant human N-terminal signal peptide/FLAG epitope-tagged Rluc8-fused VIPR2 expressed in HEK293 cells assessed as inhibition of VIP-induced human mVenus-beta-arrestin2 binding preincubated for 5 mins with luciferin, coelenterazine H followed by VIP addition measured after 5 mins by BRET assay	ChEMBL	538.2	11	5	6	2.40	CC(O)c1ccc(S(=O)(=O)NC[C@@H](O)C[C@@H](Cc2ccccc2)C(=O)N[C@H]2c3ccccc3C[C@H]2O)cc1	-
CHEMBL3927475	147204	None	0	Human	Binding	IC50	=	206.00	6.69	-	1	Antagonist activity at recombinant human N-terminal signal peptide/FLAG epitope-tagged Rluc8-fused VIPR2 expressed in HEK293 cells assessed as inhibition of VIP-induced human mVenus-beta-arrestin2 binding preincubated for 5 mins with luciferin, coelenterazine H followed by VIP addition measured after 5 mins by BRET assay	ChEMBL	552.2	10	4	7	2.12	O=C(N[C@H]1c2ccccc2C[C@H]1O)[C@H](Cc1ccccc1)C[C@H](O)CNS(=O)(=O)c1ccc2c(c1)OCCO2	-
CHEMBL3927669	147225	None	0	Human	Binding	IC50	=	4000.00	5.40	-	1	Antagonist activity at recombinant human N-terminal signal peptide/FLAG epitope-tagged Rluc8-fused VIPR2 expressed in HEK293 cells assessed as inhibition of VIP-induced human mVenus-beta-arrestin2 binding preincubated for 5 mins with luciferin, coelenterazine H followed by VIP addition measured after 5 mins by BRET assay	ChEMBL	542.2	11	3	5	3.66	CO[C@@H]1Cc2ccccc2[C@@H]1NC(=O)[C@H](Cc1ccccc1)C[C@H](O)CNS(=O)(=O)c1ccc(Cl)cc1	-
CHEMBL3938565	148618	None	0	Human	Binding	IC50	=	1130.00	5.95	-	1	Antagonist activity at recombinant human N-terminal signal peptide/FLAG epitope-tagged Rluc8-fused VIPR2 expressed in HEK293 cells assessed as inhibition of VIP-induced human mVenus-beta-arrestin2 binding preincubated for 5 mins with luciferin, coelenterazine H followed by VIP addition measured after 5 mins by BRET assay	ChEMBL	522.2	11	4	5	2.91	CCc1ccc(S(=O)(=O)NC[C@@H](O)C[C@@H](Cc2ccccc2)C(=O)N[C@H]2c3ccccc3C[C@H]2O)cc1	-

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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

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Ligand source activities (1 row/activity)