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

(+)-chlorpheniramine	918	None	42	Human	Binding	AC50	=	20000.00	4.70	-125	27	Binding affinity towards human CHRM3 in an in vitro assay with cellular components measured by scintillation proximity assay	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	pKi	=	6.26	8.20	-125	27	DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)	Drug Central	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	-
(+)-chlorpheniramine	918	None	42	Human	Binding	Ki	=	547.00	6.26	-125	27	DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)	ChEMBL	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	-
(+)-chlorpheniramine	918	None	42	Human	Binding	IC50	=	2579.00	5.59	-125	27	DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)	ChEMBL	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	-
(1R,2S)-PHENYLPROPANOLAMINE	27120	3H-QNB	13	Human	Binding	pKi	=	10000.00	5.00	-38	42	-	PDSP KiDatabase	151.1	2	2	2	1.07	C[C@H](N)[C@H](O)c1ccccc1	-
(R)-Hexbutinol	218743	3H-NMS	0	Human	Binding	pKi	=	45.71	7.34	-1	5	-	PDSP KiDatabase	311.2	3	1	2	3.94	OC(C#CCN1CCCCC1)(c1ccccc1)C1CCCCC1	-
(R)-Hexbutinol	218743	3H-NMS	0	Human	Binding	pKi	=	2.14	8.67	-1	5	-	PDSP KiDatabase	311.2	3	1	2	3.94	OC(C#CCN1CCCCC1)(c1ccccc1)C1CCCCC1	-
(S)-(+)-DIMETHINDENE	199081	None	3	Human	Binding	Ki	=	3388.44	5.47	-8128	6	Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine	ChEMBL	292.2	5	0	2	4.15	C[C@H](C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1	https://dx.doi.org/10.1021/jm020895l
(S)-dimetindene	3566	None	10	Human	Binding	pKi	=	-	6.86	-4	7	Binding to hM3 receptors expressed in CHO cells.	Guide to Pharmacology	292.2	5	0	2	4.15	C[C@@H](C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1	https://pubmed.ncbi.nlm.nih.gov/12593665
(S)-dimetindene	3566	None	10	Human	Binding	Ki	=	138.04	6.86	-4	7	Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine	ChEMBL	292.2	5	0	2	4.15	C[C@@H](C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1	https://dx.doi.org/10.1021/jm020895l
3-(azepan-1-yl)-N,5-dicyclopropyl-2-methylbenzenamine	219563	UNDEFINED	0	Human	Binding	pKi	=	3.20	8.49	-	1	-	PDSP KiDatabase	284.2	4	1	2	4.83	Cc1c(NC2CC2)cc(C2CC2)cc1N1CCCCCC1	-
3-quinuclidinyl-benzilate	112	None	21	Human	Binding	pKd	=	-	10.40	-1	7	Unclassified	Guide to Pharmacology	337.2	4	1	4	2.56	O=C(OC1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1	https://pubmed.ncbi.nlm.nih.gov/3443095
3-quinuclidinyl-benzilate	112	None	21	Human	Binding	pKd	=	-	10.40	-1	7	Unclassified	Guide to Pharmacology	337.2	4	1	4	2.56	O=C(OC1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1	https://pubmed.ncbi.nlm.nih.gov/7562472
3-quinuclidinyl-benzilate	112	3H-QNB	21	Human	Binding	pKi	=	0.09	10.06	-1	7	-	PDSP KiDatabase	337.2	4	1	4	2.56	O=C(OC1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1	-
3-quinuclidinyl-benzilate	112	3H-QNB	21	Human	Binding	pKi	=	0.08	10.10	-1	7	-	PDSP KiDatabase	337.2	4	1	4	2.56	O=C(OC1CN2CCC1CC2)C(O)(c1ccccc1)c1ccccc1	-
4-DAMP	116	3H-NMS	5	Human	Binding	pKi	=	0.52	9.28	1	12	-	PDSP KiDatabase	324.2	4	0	2	3.60	C[N+]1(C)CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1	-
4-DAMP	116	3H-4-DAMP	5	Human	Binding	pKi	=	0.50	9.30	1	12	-	PDSP KiDatabase	324.2	4	0	2	3.60	C[N+]1(C)CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1	-
4-DAMP	116	3H-QNB	5	Human	Binding	pKi	=	0.68	9.17	1	12	-	PDSP KiDatabase	324.2	4	0	2	3.60	C[N+]1(C)CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1	-
4-DAMP	116	None	5	Human	Binding	Ki	=	0.22	9.66	1	12	Displacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	324.2	4	0	2	3.60	C[N+]1(C)CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1	https://dx.doi.org/10.1021/acs.jmedchem.6b01422
4-DAMP	116	None	5	Human	Binding	IC50	=	0.31	9.51	1	12	Displacement of [3H]4-DAMP from human recombinant Muscarinic acetylcholine receptor M3 expressed in CHO cells after 60 mins by scintillation counting	ChEMBL	324.2	4	0	2	3.60	C[N+]1(C)CCC(OC(=O)C(c2ccccc2)c2ccccc2)CC1	https://dx.doi.org/10.1021/acs.jmedchem.6b01422

Showing 1 to 20 of 3,401 entries

	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)