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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

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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

(+)-aceclidine	251	None	0	Human	Functional	pEC50	None	-	5.70	-3	5	Unclassified	Guide to Pharmacology	170.1	1	1	2	-0.77	CC(=O)O[C@@H]1C[NH+]2CCC1CC2	https://pubmed.ncbi.nlm.nih.gov/8968358
(-)-aceclidine	252	None	0	Human	Functional	pEC50	None	-	5.10	-3	5	Unclassified	Guide to Pharmacology	170.1	1	1	2	-0.77	CC(=O)O[C@H]1C[NH+]2CCC1CC2	https://pubmed.ncbi.nlm.nih.gov/8968358
AC-260584	236	None	29	Human	Functional	EC50	=	5900.00	5.23	-144	4	Agonist activity at human muscarinic M3 receptor by calcium mobilization assay	ChEMBL	348.2	7	0	3	3.84	CCCCC1CCN(CCCN2C(=O)COc3cc(F)ccc32)CC1	https://dx.doi.org/10.1016/j.bmcl.2012.03.088
ACECLIDINE	77355	None	47	Human	Functional	pEC50	=	5.10	8.29	-1	9	None	Drug Central	169.1	1	0	3	0.64	CC(=O)OC1CN2CCC1CC2	-
ACECLIDINE	77355	None	47	Mouse	Functional	EC50	=	10000.00	5.00	-2089	9	Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line	ChEMBL	169.1	1	0	3	0.64	CC(=O)OC1CN2CCC1CC2	https://dx.doi.org/10.1021/jm960467d
acetylcholine	255	None	24	Human	Functional	EC50	=	3.20	8.49	-1	12	Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay	ChEMBL	146.1	3	0	2	0.26	CC(=O)OCC[N+](C)(C)C	https://dx.doi.org/10.1021/jm100697g
acetylcholine	255	None	24	Human	Functional	pEC50	=	6.66	8.18	-1	12	Activation of M3-ACh receptor-FLASH/CFP expressed in HEK293 cells assessed as FRET signal	Drug Central	146.1	3	0	2	0.26	CC(=O)OCC[N+](C)(C)C	-
acetylcholine	255	None	24	Human	Functional	EC50	=	205.00	6.69	-1	12	Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay	ChEMBL	146.1	3	0	2	0.26	CC(=O)OCC[N+](C)(C)C	https://dx.doi.org/10.1016/j.bmcl.2015.08.011
acetylcholine	255	None	24	Human	Functional	EC50	=	3.20	8.49	-1	12	Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining	ChEMBL	146.1	3	0	2	0.26	CC(=O)OCC[N+](C)(C)C	https://dx.doi.org/10.1016/j.bmcl.2012.05.048
arecoline	465	None	43	Mouse	Functional	EC50	=	12000.00	4.92	-17	11	Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line	ChEMBL	155.1	1	0	3	0.42	COC(=O)C1=CCCN(C)C1	https://dx.doi.org/10.1021/jm960467d
benzatropine	597	None	17	Human	Functional	IC50	=	19.95	7.70	-4	27	Antagonist activity at human recombinant muscarinic receptor M3 expressed in CHO-K1 cells assessed as EC80 acetylcholine-induced calcium flux incubated for 30 mins	ChEMBL	307.2	4	0	2	4.42	CN1[C@H]2CC[C@@H]1C[C@H](OC(c1ccccc1)c1ccccc1)C2	https://dx.doi.org/10.1021/acsmedchemlett.0c00626
carbachol	794	None	13	Human	Functional	ED50	=	100.00	7.00	-4	14	Amplification of transfected NIH3T3 cells was measured in Muscarinic acetylcholine receptor M3 required to produce half maximal effect	ChEMBL	147.1	3	1	2	-0.21	C[N+](C)(C)CCOC(N)=O	https://dx.doi.org/10.1021/jm960683m
carbachol	794	None	13	Human	Functional	EC50	=	15000.00	4.82	-4	14	Agonist activity at human M3 receptor in HEK293 cells assessed as induction of calcium response by fluorescence assay	ChEMBL	147.1	3	1	2	-0.21	C[N+](C)(C)CCOC(N)=O	https://dx.doi.org/10.1021/jm201348t
CARBACHOL	218453	None	0	Human	Functional	pEC50	=	8.70	8.06	-1	12	None	Drug Central	182.1	3	1	2	-3.21	C[N+](C)(C)CCOC(N)=O.[Cl-]	-
carbachol	794	None	13	Human	Functional	EC50	=	10600.00	4.97	-4	14	Effective concentration for MIPA (muscarinic-stimulated inositol phosphate accumulation) activity in SK-N-SH neuroblastoma cells expressing human muscarinic M3 receptor	ChEMBL	147.1	3	1	2	-0.21	C[N+](C)(C)CCOC(N)=O	https://dx.doi.org/10.1016/S0960-894X(00)80538-7
carbachol	794	None	13	Human	Functional	EC50	=	5011.87	5.30	-4	14	Agonist activity at human M3 receptor expressed in A9 L cells assessed as stimulation of phosphoinositide hydrolysis	ChEMBL	147.1	3	1	2	-0.21	C[N+](C)(C)CCOC(N)=O	https://dx.doi.org/10.1021/jm0606995
carbachol	794	None	13	Human	Functional	EC50	=	1819.70	5.74	-4	14	Agonist activity at human muscarinic M3 receptor expressed in CHO cells	ChEMBL	147.1	3	1	2	-0.21	C[N+](C)(C)CCOC(N)=O	https://dx.doi.org/10.1016/j.bmc.2006.10.040
carbachol	794	None	13	Human	Functional	EC50	=	25.00	7.60	-4	14	Agonist activity at human muscarinic M3 receptor expressed in HEK293 cells assessed as increase in IP1 accumulation incubated for 90 min by TR-HTRF assay	ChEMBL	147.1	3	1	2	-0.21	C[N+](C)(C)CCOC(N)=O	https://dx.doi.org/10.1021/acs.jmedchem.0c00297
carbachol	794	None	13	Mouse	Functional	EC50	=	9900.00	5.00	-93	14	Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line	ChEMBL	147.1	3	1	2	-0.21	C[N+](C)(C)CCOC(N)=O	https://dx.doi.org/10.1021/jm960467d
carbachol	794	None	13	Rat	Functional	EC50	=	130.00	6.89	2	14	Agonist activity at rat M3'(3C)-Xa receptor V94C/R551C mutant expressed in african green monkey COS7 cells assessed as increase in myo-[3H]inositol hydrolysis	ChEMBL	147.1	3	1	2	-0.21	C[N+](C)(C)CCOC(N)=O	https://dx.doi.org/10.1074/jbc.m704875200

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Ligand source activities (1 row/activity)