ArrestinDb

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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

β-phenylethylamine	620	3H-Histamine	48	Human	Binding	pKi	=	10000.00	5.00	-3	7	-	PDSP KiDatabase	121.1	2	1	1	1.19	NCCc1ccccc1	-
β-phenylethylamine	620	3H-MEPYRAMINE	48	Human	Binding	pKi	=	158489.32	3.80	-3	7	-	PDSP KiDatabase	121.1	2	1	1	1.19	NCCc1ccccc1	-
(±)-cis-H₂-PAT	3141	None	0	Human	Binding	pKi	None	-	8.15	-	1	Unclassified	Guide to Pharmacology	251.2	2	0	1	3.69	CN(C)[C@@H]1Cc2ccccc2[C@H](c2ccccc2)C1	https://pubmed.ncbi.nlm.nih.gov/12065734
(±)-cis-H₂-PAT	3141	None	0	Human	Binding	pKi	None	-	7.85	-	1	Unclassified	Guide to Pharmacology	251.2	2	0	1	3.69	CN(C)[C@@H]1Cc2ccccc2[C@H](c2ccccc2)C1	https://pubmed.ncbi.nlm.nih.gov/12065734
(+)-butaclamol	746	3H-MEPYRAMINE	9	Human	Binding	pKi	=	405.00	6.39	-1174	25	-	PDSP KiDatabase	361.2	0	1	2	4.84	CC(C)(C)[C@]1(O)CCN2C[C@H]3c4ccccc4CCc4cccc(c43)[C@@H]2C1	-
(+)-butaclamol	746	3H-MEPYRAMINE	9	Human	Binding	pKi	=	2100.00	5.68	-1174	25	-	PDSP KiDatabase	361.2	0	1	2	4.84	CC(C)(C)[C@]1(O)CCN2C[C@H]3c4ccccc4CCc4cccc(c43)[C@@H]2C1	-
(+)-butaclamol	746	3H-MEPYRAMINE	9	Human	Binding	pKi	=	147.00	6.83	-1174	25	-	PDSP KiDatabase	361.2	0	1	2	4.84	CC(C)(C)[C@]1(O)CCN2C[C@H]3c4ccccc4CCc4cccc(c43)[C@@H]2C1	-
(+)-butaclamol	746	3H-MEPYRAMINE	9	Guinea pig	Binding	pKi	=	3100.00	5.51	-7244	25	-	PDSP KiDatabase	361.2	0	1	2	4.84	CC(C)(C)[C@]1(O)CCN2C[C@H]3c4ccccc4CCc4cccc(c43)[C@@H]2C1	-
(+)-butaclamol	746	3H-MEPYRAMINE	9	Rat	Binding	pKi	=	1300.00	5.89	-3019	25	-	PDSP KiDatabase	361.2	0	1	2	4.84	CC(C)(C)[C@]1(O)CCN2C[C@H]3c4ccccc4CCc4cccc(c43)[C@@H]2C1	-
(+)-butaclamol	746	3H-MEPYRAMINE	9	Rat	Binding	pKi	=	1300.00	5.89	-3019	25	-	PDSP KiDatabase	361.2	0	1	2	4.84	CC(C)(C)[C@]1(O)CCN2C[C@H]3c4ccccc4CCc4cccc(c43)[C@@H]2C1	-
(+)-chlorpheniramine	918	None	42	Human	Binding	pKi	=	-	8.15	-20	27	Unclassified	Guide to Pharmacology	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	https://pubmed.ncbi.nlm.nih.gov/21381763
(+)-chlorpheniramine	918	None	42	Human	Binding	IC50	=	66.00	7.18	-20	27	Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells	ChEMBL	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	https://dx.doi.org/10.1128/aac.00669-07
(+)-chlorpheniramine	918	None	42	Human	Binding	Ki	=	7.00	8.15	-20	27	Binding affinity to histamine H1 receptor	ChEMBL	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	https://dx.doi.org/10.1021/jm1013874
(+)-chlorpheniramine	918	None	42	Human	Binding	Ki	=	0.73	9.14	-20	27	DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)	ChEMBL	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	-
(+)-chlorpheniramine	918	None	42	Human	Binding	IC50	=	6.29	8.20	-20	27	DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)	ChEMBL	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	-
(+)-chlorpheniramine	918	None	42	Human	Binding	Ki	=	0.92	9.04	-20	27	Displacement of [3H]Pyrilamine from histamine H1 receptor (unknown origin)	ChEMBL	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	https://dx.doi.org/10.1016/j.bmcl.2013.12.024
(+)-chlorpheniramine	918	None	42	Human	Binding	AC50	=	33.00	7.48	-20	27	Binding affinity towards human HRH1 in an in vitro assay measured by filtration	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	AC50	=	20.00	7.70	-20	27	Binding affinity towards human HRH1 in an in vitro assay measured by filtration	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	3H-MEPYRAMINE	42	Human	Binding	pKi	=	2.51	8.60	-20	27	-	PDSP KiDatabase	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	-
(+)-chlorpheniramine	918	3H-MEPYRAMINE	42	Human	Binding	pKi	=	3.00	8.52	-20	27	-	PDSP KiDatabase	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	-

Showing 1 to 20 of 3,491 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

(+)-chlorpheniramine	918	None	42	Human	Functional	AC50	=	56.00	7.25	-2	27	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	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	Guinea pig	Functional	IC50	=	12.00	7.92	2	27	In vitro inhibition of histamine-induced contractions in guinea pig ileum	ChEMBL	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	https://dx.doi.org/10.1021/jm00157a010
2-(3-bromophenyl)histamine	45	None	1	Human	Functional	EC50	=	199.53	6.70	50	4	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	265.0	3	2	2	2.34	NCCc1cnc(-c2cccc(Br)c2)[nH]1	https://dx.doi.org/10.1016/j.bmcl.2010.10.041
2-(3-bromophenyl)histamine	45	None	1	Guinea pig	Functional	Kd	=	1.26	8.90	-	4	Compound was tested for the contractile effects antagonized by mepyramine (1-1000 nM) against Histamine H1 receptor of guinea pig aorta.	ChEMBL	265.0	3	2	2	2.34	NCCc1cnc(-c2cccc(Br)c2)[nH]1	https://dx.doi.org/10.1016/s0960-894x(98)00461-2
2-(3-bromophenyl)histamine	45	None	1	Guinea pig	Functional	Kd	=	0.74	9.13	-	4	Contractile effects antagonized by mepyramine (0.3-100 nM) against Histamine H1 receptor in guinea pig ileum	ChEMBL	265.0	3	2	2	2.34	NCCc1cnc(-c2cccc(Br)c2)[nH]1	https://dx.doi.org/10.1016/s0960-894x(98)00461-2
2-[(2-METHYLAMINOETHYL)(P-METHOXYBENZYL)AMINO]PYRIDINE	205285	None	19	Guinea pig	Functional	Kd	=	6.61	8.18	-	1	Histamine H1 receptor antagonistic activity in guinea pig ileum using fluorescence-labeled H1 as radioligand	ChEMBL	271.2	7	1	4	2.32	CNCCN(Cc1ccc(OC)cc1)c1ccccn1	https://dx.doi.org/10.1016/s0960-894x(03)00113-6
2-METHYLHISTAMINE	17994	None	20	Human	Functional	EC50	=	794.33	6.10	5	2	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	125.1	2	2	2	0.22	Cc1ncc(CCN)[nH]1	https://dx.doi.org/10.1016/j.bmcl.2010.10.041
4-methylhistamine	121	None	34	Human	Functional	EC50	=	15848.93	4.80	-354	7	Agonist activity at human histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase assay	ChEMBL	125.1	2	2	2	0.22	Cc1[nH]cnc1CCN	https://dx.doi.org/10.1021/jm900526h
ACRIVASTINE	16162	None	49	Human	Functional	pIC50	=	7.16	8.15	5	4	None	Drug Central	348.2	6	1	3	4.01	Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1	-
ACRIVASTINE	16162	None	49	Guinea pig	Functional	pIC50	=	5.21	8.28	-5	4	Inhibition of H1 receptor in Cavia porcellus Hartley (guinea pig) ileum assessed as inhibition of histamine-induced spasms incubated 2 min prior histamine-challenge	Drug Central	348.2	6	1	3	4.01	Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1	-
AMINOPOTENTIDINE	207000	None	22	Guinea pig	Functional	Kd	=	26915.35	4.57	-	1	Histamine H1 receptor antagonistic activity on the isolated guinea pig ileum determined by Schild plot.	ChEMBL	477.3	11	4	6	2.47	N#CN/C(=N\CCNC(=O)c1ccc(N)cc1)NCCCOc1cccc(CN2CCCCC2)c1	https://dx.doi.org/10.1021/jm00090a013
amitriptyline	401	None	38	Rat	Functional	pIC50	=	10.70	7.97	3	51	Compound tested for its inhibitory activity against Histamine H1 receptor	Drug Central	277.2	3	0	1	4.17	CN(C)CCC=C1c2ccccc2CCc2ccccc21	-
amoxapine	403	None	60	Human	Functional	AC50	=	330.00	6.48	-21	42	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	313.1	0	1	4	3.43	Clc1ccc2c(c1)C(N1CCNCC1)=Nc1ccccc1O2	https://dx.doi.org/10.1038/s41467-023-40064-9
amthamine	404	None	24	Human	Functional	EC50	=	15848.93	4.80	-57	4	Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	ChEMBL	157.1	2	2	4	0.54	Cc1nc(N)sc1CCN	https://dx.doi.org/10.1016/j.bmcl.2010.10.041
ANTAZOLINE	20210	None	38	Guinea pig	Functional	Kd	=	72.44	7.14	-	14	Antagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhibition of histamine-induced contractions after 15 mins	ChEMBL	265.2	5	1	3	2.69	c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1	https://dx.doi.org/10.1016/j.bmc.2018.04.023
APRINDINE	15289	None	20	Human	Functional	AC50	=	8000.00	5.10	-3	12	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	322.2	8	0	2	4.39	CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1	https://dx.doi.org/10.1038/s41467-023-40064-9
aripiprazole	470	None	70	Human	Functional	AC50	=	2000.00	5.70	-97	60	Antagonist activity at human HRH1 in an in vitro cell-based assay measured by fluorescent imaging plate reader	ChEMBL	447.1	7	1	4	4.86	O=C1CCc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2N1	https://dx.doi.org/10.1038/s41467-023-40064-9
aripiprazole	470	None	70	Human	Functional	IC50	=	420.00	6.38	-97	60	Antagonistic activity at histamine 1 receptor (unknown origin) after 10 mins by FLIPR assay	ChEMBL	447.1	7	1	4	4.86	O=C1CCc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2N1	https://dx.doi.org/10.1016/j.bmcl.2018.01.038
aripiprazole	470	None	70	Human	Functional	IC50	=	420.00	6.38	-97	60	Antagonist activity at histamine H1 receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay	ChEMBL	447.1	7	1	4	4.86	O=C1CCc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2N1	https://dx.doi.org/10.1016/j.ejmech.2017.12.099
arpromidine	475	None	6	Guinea pig	Functional	Kd	=	22.39	7.65	-	3	Antagonist activity at histamine H1 receptor in guinea pig ileum assessed as inhibition of histamine-induced positive chronotropic activity	ChEMBL	380.2	9	3	3	3.00	NC(=NCCCc1cnc[nH]1)NCCC(c1ccc(F)cc1)c1ccccn1	https://dx.doi.org/10.1021/jm800841w

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Ligand source activities (1 row/activity)