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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

(+)-3-(4-Chlorophenyl)-N'-[(4-cyanophenyl)sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamidine	219565	UNDEFINED	0	Human	Binding	pKi	=	10000.00	5.00	-3467	5	-	PDSP KiDatabase	463.1	4	1	4	3.72	N#Cc1ccc(S(=O)(=O)N=C(N)N2CC(c3ccccc3)C(c3ccc(Cl)cc3)=N2)cc1	-
(+)-chlorpheniramine	918	None	42	Human	Binding	pKi	=	5.08	8.29	-446	27	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	-
(+)-chlorpheniramine	918	None	42	Human	Binding	AC50	=	412.30	6.38	-446	27	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane 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	Ki	=	8228.00	5.08	-446	27	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	-
(+)-chlorpheniramine	918	None	42	Human	Binding	IC50	=	8368.00	5.08	-446	27	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274.1	5	0	2	3.82	CN(C)CC[C@@H](c1ccc(Cl)cc1)c1ccccn1	-
(-)-stepholidine	3691	3H-TIOTIDINE	40	Human	Binding	pKi	=	10000.00	5.00	-2290	35	-	PDSP KiDatabase	327.1	2	2	5	2.77	COc1cc2c(cc1O)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2	-
(1R,2S)-PHENYLPROPANOLAMINE	27120	3H-TIOTIDINE	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	-
4-methylhistamine	121	None	34	Human	Binding	Ki	=	7943.28	5.10	-269	7	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	125.1	2	2	2	0.22	Cc1[nH]cnc1CCN	https://dx.doi.org/10.1016/j.bmcl.2010.10.041
4-methylhistamine	121	3H-TIOTIDINE	34	Guinea pig	Binding	pKi	=	10000.00	5.00	-338	7	-	PDSP KiDatabase	125.1	2	2	2	0.22	Cc1[nH]cnc1CCN	-
A-304121	196	None	15	Human	Binding	Ki	=	70794.58	4.15	-35481	5	Binding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359.2	8	1	5	1.54	C[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	https://dx.doi.org/10.1016/s0960-894x(02)00310-4
A-349,821	99024	None	0	Human	Binding	Ki	=	10000.00	5.00	-9120	10	Binding affinity towards human histaminergic (H2) receptor	ChEMBL	422.3	7	0	4	4.47	C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1	https://dx.doi.org/10.1016/s0960-894x(03)00118-5
A331440	198	None	23	Human	Binding	Ki	=	10000.00	5.00	-3467	4	Binding affinity to the human cortical histamine H2 receptor	ChEMBL	349.2	7	0	4	3.63	CN(C)[C@@H]1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1	https://dx.doi.org/10.1016/s0960-894x(02)00648-0
ABT-239	229	None	35	Human	Binding	pKi	None	-	5.20	-3548	4	Unclassified	Guide to Pharmacology	330.2	4	0	3	5.00	C[C@@H]1CCCN1CCc1cc2cc(-c3ccc(C#N)cc3)ccc2o1	https://pubmed.ncbi.nlm.nih.gov/15608078
Alpha-Dimethylhistane-alpha	218639	3H-Histamine	0	Guinea pig	Binding	pKi	=	0.20	9.70	-6	3	-	PDSP KiDatabase	139.1	3	2	2	0.56	CNC(C)Cc1cnc[nH]1	-
AMBROXOL	46238	None	57	Human	Binding	AC50	=	6361.40	5.20	-	4	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	376.0	3	3	3	3.19	Nc1c(Br)cc(Br)cc1CN[C@H]1CC[C@H](O)CC1	https://dx.doi.org/10.1038/s41467-023-40064-9
amiodarone	398	None	47	Human	Binding	IC50	=	10555.00	4.98	-6	40	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645.0	11	0	4	6.94	CCCCc1oc2ccccc2c1C(=O)c1cc(I)c(OCCN(CC)CC)c(I)c1	-
amiodarone	398	None	47	Human	Binding	Ki	=	10379.00	4.98	-6	40	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645.0	11	0	4	6.94	CCCCc1oc2ccccc2c1C(=O)c1cc(I)c(OCCN(CC)CC)c(I)c1	-
amiodarone	398	None	47	Human	Binding	pKi	=	4.98	8.30	-6	40	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	645.0	11	0	4	6.94	CCCCc1oc2ccccc2c1C(=O)c1cc(I)c(OCCN(CC)CC)c(I)c1	-
amiodarone	398	None	47	Human	Binding	AC50	=	2822.20	5.55	-6	40	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	645.0	11	0	4	6.94	CCCCc1oc2ccccc2c1C(=O)c1cc(I)c(OCCN(CC)CC)c(I)c1	https://dx.doi.org/10.1038/s41467-023-40064-9
amisulpride	400	3H-TIOTIDINE	72	Human	Binding	pKi	=	10000.00	5.00	-4365	53	-	PDSP KiDatabase	369.2	7	2	6	1.28	CCN1CCCC1CNC(=O)c1cc(S(=O)(=O)CC)c(N)cc1OC	-

Showing 1 to 20 of 1,038 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

4-methylhistamine	121	None	34	Human	Functional	EC50	=	3162.28	5.50	-67	7	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	125.1	2	2	2	0.22	Cc1[nH]cnc1CCN	https://dx.doi.org/10.1016/j.bmcl.2010.10.041
4-methylhistamine	121	None	34	Human	Functional	EC50	=	2884.03	5.54	-67	7	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	125.1	2	2	2	0.22	Cc1[nH]cnc1CCN	https://dx.doi.org/10.1021/jm900526h
amitriptyline	401	None	38	Human	Functional	pIC50	=	6.80	8.17	-100	51	None	Drug Central	277.2	3	0	1	4.17	CN(C)CCC=C1c2ccccc2CCc2ccccc21	-
amthamine	404	None	24	Human	Functional	pEC50	=	-	6.40	57	4	Unclassified	Guide to Pharmacology	157.1	2	2	4	0.54	Cc1nc(N)sc1CCN	https://pubmed.ncbi.nlm.nih.gov/19072936
amthamine	404	None	24	Human	Functional	EC50	=	190.55	6.72	57	4	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	157.1	2	2	4	0.54	Cc1nc(N)sc1CCN	https://dx.doi.org/10.1021/jm201128q
ASENAPINE	107587	None	16	Human	Functional	pIC50	=	8.21	8.09	-40	54	None	Drug Central	285.1	0	0	2	4.26	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	-
BETAZOLE	14503	None	47	Human	Functional	AC50	=	910.00	6.04	-	1	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	111.1	2	2	2	-0.09	NCCc1cc[nH]n1	https://dx.doi.org/10.1038/s41467-023-40064-9
bromocriptine	729	None	28	Human	Functional	AC50	=	2130.90	5.67	-676	45	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	653.2	5	3	6	3.19	CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]c(Br)c(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12	https://dx.doi.org/10.1038/s41467-023-40064-9
burimamide	743	None	0	Human	Functional	pEC50	None	-	5.65	-	7	Unclassified	Guide to Pharmacology	262.1	5	3	2	1.98	CNC(=S)NCCCCc1cccc2[nH]ncc12	https://pubmed.ncbi.nlm.nih.gov/9681472
cabergoline	778	None	41	Human	Functional	AC50	=	4230.00	5.37	-891	19	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	451.3	8	2	4	3.19	C=CCN1C[C@H](C(=O)N(CCCN(C)C)C(=O)NCC)C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]21	https://dx.doi.org/10.1038/s41467-023-40064-9
cefapirin	220190	None	0	Human	Functional	pIC50	=	5.24	8.28	-1	14	None	Drug Central	423.1	7	2	8	0.47	CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)CSc3ccncc3)[C@H]2SC1	-
CHEMBL1077596	5628	None	0	Human	Functional	EC50	=	12022.64	4.92	-	1	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	321.1	6	4	4	1.15	Cc1ccc(S(=O)(=O)NC(=N)NCCCc2c[nH]cn2)cc1	https://dx.doi.org/10.1021/jm900526h
CHEMBL1078210	5715	None	0	Human	Functional	EC50	=	14125.38	4.85	-18	2	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	310.2	8	3	3	1.99	N#C/N=C(\NCCCc1ccccc1)NCCCc1c[nH]cn1	https://dx.doi.org/10.1021/jm900526h
CHEMBL1078212	5716	None	0	Human	Functional	EC50	=	8912.51	5.05	-	1	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	324.2	9	3	3	2.38	N#C/N=C(\NCCCCc1ccccc1)NCCCc1c[nH]cn1	https://dx.doi.org/10.1021/jm900526h
CHEMBL1078358	5738	None	0	Human	Functional	EC50	=	1995.26	5.70	-	1	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	314.2	7	4	2	1.20	NC(=O)/N=C(/NCCCc1ccccc1)NCCc1c[nH]cn1	https://dx.doi.org/10.1021/jm900526h
CHEMBL1078359	5739	None	0	Human	Functional	EC50	=	436.52	6.36	-	1	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	328.2	8	4	2	1.59	NC(=O)/N=C(/NCCCc1ccccc1)NCCCc1c[nH]cn1	https://dx.doi.org/10.1021/jm900526h
CHEMBL1078359	5739	None	0	Human	Functional	EC50	=	645.65	6.19	-	1	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	328.2	8	4	2	1.59	NC(=O)/N=C(/NCCCc1ccccc1)NCCCc1c[nH]cn1	https://dx.doi.org/10.1021/jm900526h
CHEMBL1078529	5765	None	0	Human	Functional	EC50	=	7244.36	5.14	-5	2	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	328.1	8	3	4	2.15	N#C/N=C(/NCCCc1c[nH]cn1)NCCSc1ccccc1	https://dx.doi.org/10.1021/jm900526h
CHEMBL1078746	5795	None	0	Human	Functional	EC50	=	380.19	6.42	-	1	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	342.2	9	4	2	1.98	NC(=O)/N=C(/NCCCCc1ccccc1)NCCCc1c[nH]cn1	https://dx.doi.org/10.1021/jm900526h
CHEMBL1078747	5796	None	0	Human	Functional	EC50	=	12022.64	4.92	-	1	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	335.1	8	4	4	1.03	N=C(NCCCc1c[nH]cn1)NS(=O)(=O)CCc1ccccc1	https://dx.doi.org/10.1021/jm900526h

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Ligand source activities (1 row/activity)