GPCRdb

Ligand source activities (1 row/activity)

Potency
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Ligands					Receptor			Assay information							Chemical information
Sel. page	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity (Potency)	# tested GPCRs (Potency)	Species	p-value (-log)	Type	Activity Relation	Activity Value	Assay Type	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	168294449	192416	0	None	50	2	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5204599	192416	0	None	50	2	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222793	192416	0	None	50	2	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5093461	213777	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095884	213777	0	None	-	1	Human	7.0	pEC50	=	7	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	164611342	184505	0	None	-1	3	Human	7.0	pEC50	=	7	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	346	6	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4856005	184505	0	None	-1	3	Human	7.0	pEC50	=	7	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	346	6	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1016/j.ejmech.2021.113190
	155559319	174291	0	None	13	2	Human	7.0	pEC50	=	7	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	239	1	1	3	3.2	CC1CCCc2c(-c3ccccc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4563363	174291	0	None	13	2	Human	7.0	pEC50	=	7	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	239	1	1	3	3.2	CC1CCCc2c(-c3ccccc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	168290815	192371	0	None	10	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5200771	192371	0	None	10	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222529	192371	0	None	10	2	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5083588	213758	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095633	213758	0	None	-	1	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	1204	1901	114	None	-61	10	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1247	1901	114	None	-61	10	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1375	1901	114	None	-61	10	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	774	1901	114	None	-61	10	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	CHEMBL90	1901	114	None	-61	10	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	DB05381	1901	114	None	-61	10	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	CHEMBL5075713	213753	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095559	213753	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	1204	1901	114	None	-61	10	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	1247	1901	114	None	-61	10	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	1375	1901	114	None	-61	10	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	774	1901	114	None	-61	10	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	CHEMBL90	1901	114	None	-61	10	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	DB05381	1901	114	None	-61	10	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	168268853	192183	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5180504	192183	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221353	192183	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	46887041	8672	0	None	-5	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	313	7	4	3	2.2	C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1	10.1016/j.bmcl.2010.03.082
	CHEMBL1096428	8672	0	None	-5	4	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	313	7	4	3	2.2	C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1	10.1016/j.bmcl.2010.03.082
	CHEMBL5092267	213581	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C	10.1016/j.bmcl.2021.128388
	CHEMBL5075713	213753	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095559	213753	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	1204	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	1247	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	1375	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	774	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	CHEMBL90	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	DB05381	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm900526h
	1204	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
	1247	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
	1375	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
	774	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
	CHEMBL90	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
	DB05381	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
	44482302	5550	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	321	6	4	4	1.2	Cc1ccc(S(=O)(=O)NC(=N)NCCCc2c[nH]cn2)cc1	10.1021/jm900526h
	CHEMBL1077596	5550	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	321	6	4	4	1.2	Cc1ccc(S(=O)(=O)NC(=N)NCCCc2c[nH]cn2)cc1	10.1021/jm900526h
	44481217	5717	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	335	8	4	4	1.0	N=C(NCCCc1c[nH]cn1)NS(=O)(=O)CCc1ccccc1	10.1021/jm900526h
	CHEMBL1078747	5717	0	None	-	1	Human	4.9	pEC50	=	4.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	335	8	4	4	1.0	N=C(NCCCc1c[nH]cn1)NS(=O)(=O)CCc1ccccc1	10.1021/jm900526h
	CHEMBL5090859	213509	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C	10.1016/j.bmcl.2021.128388
	1204	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.03.082
	1247	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.03.082
	1375	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.03.082
	774	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.03.082
	CHEMBL90	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.03.082
	DB05381	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.03.082
	1204	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm201128q
	1247	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm201128q
	1375	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm201128q
	774	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm201128q
	CHEMBL90	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm201128q
	DB05381	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm201128q
	CHEMBL5083588	213758	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095633	213758	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	168268853	192183	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5180504	192183	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221353	192183	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5077939	213765	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095769	213765	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	13170764	174507	0	None	2	2	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	255	2	1	4	2.6	COc1ccc(-c2nc(N)nc3c2CCCC3)cc1	10.1021/acs.jmedchem.9b00241
	CHEMBL4568452	174507	0	None	2	2	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	255	2	1	4	2.6	COc1ccc(-c2nc(N)nc3c2CCCC3)cc1	10.1021/acs.jmedchem.9b00241
	168294449	192416	0	None	50	2	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5204599	192416	0	None	50	2	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222793	192416	0	None	50	2	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	56954513	81671	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	578	17	6	8	2.6	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/jm201128q
	CHEMBL2165645	81671	0	None	-	1	Human	7.9	pEC50	=	7.9	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	578	17	6	8	2.6	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/jm201128q
	CHEMBL5092102	213572	0	None	-	1	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		NCCCCCCCCNC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1016/j.bmcl.2021.128388
	164611757	184320	0	None	3	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	402	8	4	4	2.8	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
	CHEMBL4853107	184320	0	None	3	3	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	402	8	4	4	2.8	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
	168294449	192416	0	None	50	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5204599	192416	0	None	50	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222793	192416	0	None	50	2	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	168295528	192429	0	None	31	9	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5206565	192429	0	None	31	9	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222872	192429	0	None	31	9	Human	6.9	pEC50	=	6.9	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5085542	213199	0	None	-	1	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C	10.1016/j.bmcl.2021.128388
	13170764	174507	0	None	2	2	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	255	2	1	4	2.6	COc1ccc(-c2nc(N)nc3c2CCCC3)cc1	10.1021/acs.jmedchem.9b00241
	CHEMBL4568452	174507	0	None	2	2	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	255	2	1	4	2.6	COc1ccc(-c2nc(N)nc3c2CCCC3)cc1	10.1021/acs.jmedchem.9b00241
	1204	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1247	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1375	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	774	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	CHEMBL90	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	DB05381	1901	114	None	-61	10	Human	5.9	pEC50	=	5.9	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	44481489	5637	0	None	-18	2	Human	4.9	pEC50	=	4.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	310	8	3	3	2.0	N#C/N=C(\NCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	CHEMBL1078210	5637	0	None	-18	2	Human	4.9	pEC50	=	4.9	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	310	8	3	3	2.0	N#C/N=C(\NCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	CHEMBL5088914	213786	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095949	213786	0	None	-	1	Human	5.8	pEC50	=	5.8	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	164628701	185885	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	338	5	4	4	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1	10.1016/j.ejmech.2021.113190
	CHEMBL4876743	185885	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	338	5	4	4	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1	10.1016/j.ejmech.2021.113190
	164626370	185891	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	338	6	4	4	1.8	CCCCCCNC(=O)/N=C(\N)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	CHEMBL4876799	185891	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	338	6	4	4	1.8	CCCCCCNC(=O)/N=C(\N)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	56954517	81654	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	502	17	6	6	0.5	N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1ncn[nH]1)NCCCc1ncn[nH]1	10.1021/jm201128q
	CHEMBL2165629	81654	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	502	17	6	6	0.5	N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1ncn[nH]1)NCCCc1ncn[nH]1	10.1021/jm201128q
	164614645	184549	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	402	8	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C	10.1016/j.ejmech.2021.113190
	CHEMBL4856572	184549	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	402	8	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C	10.1016/j.ejmech.2021.113190
	1204	1901	114	None	-61	10	Human	5.8	pEC50	=	5.8	Functional	Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assayAntagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
	1247	1901	114	None	-61	10	Human	5.8	pEC50	=	5.8	Functional	Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assayAntagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
	1375	1901	114	None	-61	10	Human	5.8	pEC50	=	5.8	Functional	Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assayAntagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
	774	1901	114	None	-61	10	Human	5.8	pEC50	=	5.8	Functional	Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assayAntagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
	CHEMBL90	1901	114	None	-61	10	Human	5.8	pEC50	=	5.8	Functional	Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assayAntagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
	DB05381	1901	114	None	-61	10	Human	5.8	pEC50	=	5.8	Functional	Antagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assayAntagonist activity at Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins in presence of histamine by GTPgammaS binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
	56954002	81658	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	620	19	6	8	3.7	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	CHEMBL2165633	81658	0	None	-	1	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	620	19	6	8	3.7	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	44414337	79729	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human H2RAgonist activity at human H2R	ChEMBL	945	24	3	9	8.3	CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCC/N=C(\NC#N)NCCCOc3cccc(CN4CCCCC4)c3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2006.05.039
	CHEMBL213357	79729	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human H2RAgonist activity at human H2R	ChEMBL	945	24	3	9	8.3	CC1(C)C(/C=C/C=C/C=C2/N(CCCCCC(=O)NCC/N=C(\NC#N)NCCCOc3cccc(CN4CCCCC4)c3)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2006.05.039
	90667237	108987	0	None	-	1	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting	ChEMBL	356	9	3	4	2.8	Cc1nc(CCCCN/C(=N\C#N)NCCSc2ccccc2)c[nH]1	10.1039/C3MD00245D
	CHEMBL3220638	108987	0	None	-	1	Human	4.8	pEC50	=	4.8	Functional	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting	ChEMBL	356	9	3	4	2.8	Cc1nc(CCCCN/C(=N\C#N)NCCSc2ccccc2)c[nH]1	10.1039/C3MD00245D
	164622190	185034	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	360	7	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4864067	185034	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	360	7	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1	10.1016/j.ejmech.2021.113190
	119570	3110	90	None	-128	7	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	2233	3110	90	None	-128	7	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	953	3110	90	None	-128	7	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	CHEMBL301265	3110	90	None	-128	7	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	DB00413	3110	90	None	-128	7	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	164627189	185739	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	298	6	4	4	1.0	CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	CHEMBL4874758	185739	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	298	6	4	4	1.0	CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	164610892	184615	0	None	4	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	394	8	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1	10.1016/j.ejmech.2021.113190
	CHEMBL4857560	184615	0	None	4	3	Human	7.8	pEC50	=	7.8	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	394	8	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1	10.1016/j.ejmech.2021.113190
	164612037	184795	0	None	-11	11	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	326	8	4	4	1.8	CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	CHEMBL4860528	184795	0	None	-11	11	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	326	8	4	4	1.8	CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	164627189	185739	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	298	6	4	4	1.0	CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	CHEMBL4874758	185739	0	None	-	1	Human	6.8	pEC50	=	6.8	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	298	6	4	4	1.0	CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	46887042	8674	0	None	-6	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	319	7	4	3	2.6	C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	CHEMBL1096430	8674	0	None	-6	4	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	319	7	4	3	2.6	C[C@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	CHEMBL5094663	213730	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](C)c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	168273640	192203	0	None	4	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5176229	192203	0	None	4	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221444	192203	0	None	4	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	168295541	192438	0	None	14	2	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5208845	192438	0	None	14	2	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222926	192438	0	None	14	2	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5094663	213730	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](C)c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	126688	400	28	None	57	2	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1021/jm201128q
	4025	400	28	None	57	2	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1021/jm201128q
	CHEMBL293762	400	28	None	57	2	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1021/jm201128q
	CHEMBL5092102	213572	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		NCCCCCCCCNC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1016/j.bmcl.2021.128388
	44481214	5659	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	314	7	4	2	1.2	NC(=O)/N=C(/NCCCc1ccccc1)NCCc1c[nH]cn1	10.1021/jm900526h
	CHEMBL1078358	5659	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	314	7	4	2	1.2	NC(=O)/N=C(/NCCCc1ccccc1)NCCc1c[nH]cn1	10.1021/jm900526h
	46887080	8460	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	365	7	4	5	3.2	Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	CHEMBL1094452	8460	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	365	7	4	5	3.2	Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	71458814	81672	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	345	7	3	4	2.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCc1ccccc1	10.1021/jm201128q
	CHEMBL2165646	81672	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	345	7	3	4	2.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCc1ccccc1	10.1021/jm201128q
	CHEMBL5076746	213749	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(N)(=O)=O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095519	213749	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(N)(=O)=O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5075106	213751	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095549	213751	0	None	-	1	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	56954227	81662	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	564	17	6	8	2.3	N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1	10.1021/jm201128q
	CHEMBL2165637	81662	0	None	-	1	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	564	17	6	8	2.3	N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1	10.1021/jm201128q
	164608815	183872	0	None	3	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	380	7	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1016/j.ejmech.2021.113190
	CHEMBL4846638	183872	0	None	3	3	Human	7.7	pEC50	=	7.7	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	380	7	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1016/j.ejmech.2021.113190
	155544816	174461	0	None	2	2	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	269	2	1	4	2.9	COc1ccc(-c2nc(N)nc3c2CC(C)CC3)cc1	10.1021/acs.jmedchem.9b00241
	CHEMBL4567405	174461	0	None	2	2	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	269	2	1	4	2.9	COc1ccc(-c2nc(N)nc3c2CC(C)CC3)cc1	10.1021/acs.jmedchem.9b00241
	56954318	81666	0	None	-2	2	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	444	13	6	4	0.1	N/C(=N\C(=O)CCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1	10.1021/jm201128q
	CHEMBL2165640	81666	0	None	-2	2	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	444	13	6	4	0.1	N/C(=N\C(=O)CCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1	10.1021/jm201128q
	164627774	185983	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	344	3	4	4	1.4	N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	CHEMBL4878215	185983	0	None	-	1	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	344	3	4	4	1.4	N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	155544816	174461	0	None	2	2	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	269	2	1	4	2.9	COc1ccc(-c2nc(N)nc3c2CC(C)CC3)cc1	10.1021/acs.jmedchem.9b00241
	CHEMBL4567405	174461	0	None	2	2	Human	5.7	pEC50	=	5.7	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	269	2	1	4	2.9	COc1ccc(-c2nc(N)nc3c2CC(C)CC3)cc1	10.1021/acs.jmedchem.9b00241
	164608815	183872	0	None	3	3	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	380	7	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1016/j.ejmech.2021.113190
	CHEMBL4846638	183872	0	None	3	3	Human	6.7	pEC50	=	6.7	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	380	7	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1016/j.ejmech.2021.113190
	168286426	192324	0	None	5	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5198795	192324	0	None	5	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222241	192324	0	None	5	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	164609493	183854	0	None	-2	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	350	6	4	5	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1	10.1016/j.ejmech.2021.113190
	CHEMBL4846380	183854	0	None	-2	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	350	6	4	5	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1	10.1016/j.ejmech.2021.113190
	168292954	192395	0	None	7	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5202592	192395	0	None	7	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222660	192395	0	None	7	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	168294767	192417	0	None	40	10	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5207281	192417	0	None	40	10	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222802	192417	0	None	40	10	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5075106	213751	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095549	213751	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	56954425	81669	0	None	13	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	584	23	6	4	4.0	N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1	10.1021/jm201128q
	CHEMBL2165643	81669	0	None	13	2	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	584	23	6	4	4.0	N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1	10.1021/jm201128q
	155523256	170179	0	None	-3	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	269	2	1	4	3.2	COc1cccc(-c2nc(N)nc3c2CCCC3C)c1	10.1021/acs.jmedchem.9b00241
	CHEMBL4452406	170179	0	None	-3	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	269	2	1	4	3.2	COc1cccc(-c2nc(N)nc3c2CCCC3C)c1	10.1021/acs.jmedchem.9b00241
	56954125	81659	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	676	23	6	8	5.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	CHEMBL2165634	81659	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	676	23	6	8	5.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	168290235	192366	0	None	9	9	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5201074	192366	0	None	9	9	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222491	192366	0	None	9	9	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	168294767	192417	0	None	40	10	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5207281	192417	0	None	40	10	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222802	192417	0	None	40	10	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	155523256	170179	0	None	-3	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	269	2	1	4	3.2	COc1cccc(-c2nc(N)nc3c2CCCC3C)c1	10.1021/acs.jmedchem.9b00241
	CHEMBL4452406	170179	0	None	-3	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	269	2	1	4	3.2	COc1cccc(-c2nc(N)nc3c2CCCC3C)c1	10.1021/acs.jmedchem.9b00241
	CHEMBL5092267	213581	0	None	-	1	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C	10.1016/j.bmcl.2021.128388
	164609017	183843	0	None	-6	3	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	416	10	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4846201	183843	0	None	-6	3	Human	5.6	pEC50	=	5.6	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	416	10	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL5093461	213777	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095884	213777	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	164617783	184007	0	None	-2	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	388	8	4	4	2.8	CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4848815	184007	0	None	-2	3	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	388	8	4	4	2.8	CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1	10.1016/j.ejmech.2021.113190
	46887078	8916	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	359	7	4	5	2.8	Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)c1ccccc1	10.1016/j.bmcl.2010.03.082
	CHEMBL1098442	8916	0	None	-	1	Human	7.6	pEC50	=	7.6	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	359	7	4	5	2.8	Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)c1ccccc1	10.1016/j.bmcl.2010.03.082
	46887115	8426	0	None	47	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	365	7	4	5	3.2	Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	CHEMBL1094144	8426	0	None	47	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	365	7	4	5	3.2	Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@H](C)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	164617783	184007	0	None	-2	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	388	8	4	4	2.8	CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4848815	184007	0	None	-2	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	388	8	4	4	2.8	CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1	10.1016/j.ejmech.2021.113190
	164611342	184505	0	None	-1	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	346	6	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4856005	184505	0	None	-1	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	346	6	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1016/j.ejmech.2021.113190
	164620704	185501	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	416	8	4	4	3.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1	10.1016/j.ejmech.2021.113190
	CHEMBL4871482	185501	0	None	-	1	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	416	8	4	4	3.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1	10.1016/j.ejmech.2021.113190
	168295541	192438	0	None	14	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5208845	192438	0	None	14	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222926	192438	0	None	14	2	Human	6.6	pEC50	=	6.6	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	168286426	192324	0	None	5	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5198795	192324	0	None	5	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222241	192324	0	None	5	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	1269	121	33	None	-67	6	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1021/jm900526h
	37463	121	33	None	-67	6	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1021/jm900526h
	CHEMBL275443	121	33	None	-67	6	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1021/jm900526h
	164624107	185140	0	None	8	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	402	9	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4865765	185140	0	None	8	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	402	9	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1	10.1016/j.ejmech.2021.113190
	168295528	192429	0	None	31	9	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5206565	192429	0	None	31	9	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222872	192429	0	None	31	9	Human	8.5	pEC50	=	8.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	56954129	81661	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	536	15	6	8	1.5	N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1	10.1021/jm201128q
	CHEMBL2165636	81661	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	536	15	6	8	1.5	N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1	10.1021/jm201128q
	164614645	184549	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	402	8	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C	10.1016/j.ejmech.2021.113190
	CHEMBL4856572	184549	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	402	8	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C	10.1016/j.ejmech.2021.113190
	164610892	184615	0	None	4	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	394	8	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1	10.1016/j.ejmech.2021.113190
	CHEMBL4857560	184615	0	None	4	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	394	8	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1	10.1016/j.ejmech.2021.113190
	155565842	175043	0	None	-5	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	317	1	1	3	3.9	CC1CCCc2c(-c3cccc(Br)c3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4580450	175043	0	None	-5	2	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	317	1	1	3	3.9	CC1CCCc2c(-c3cccc(Br)c3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	1269	121	33	None	-67	6	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1016/j.bmcl.2010.10.041
	37463	121	33	None	-67	6	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1016/j.bmcl.2010.10.041
	CHEMBL275443	121	33	None	-67	6	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1016/j.bmcl.2010.10.041
	168290235	192366	0	None	9	9	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5201074	192366	0	None	9	9	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222491	192366	0	None	9	9	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5094083	213692	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		C=C(/N=C(\C)NCCCc1nnc(N)s1)NCCCCCCCCN	10.1016/j.bmcl.2021.128388
	164627020	185826	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	422	7	4	4	3.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4876025	185826	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	422	7	4	4	3.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL5075713	213753	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095559	213753	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5093461	213777	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095884	213777	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5083588	213758	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095633	213758	0	None	-	1	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	164610421	184678	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	332	5	4	4	2.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4858567	184678	0	None	-	1	Human	5.5	pEC50	=	5.5	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	332	5	4	4	2.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1	10.1016/j.ejmech.2021.113190
	168273640	192203	0	None	4	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5176229	192203	0	None	4	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221444	192203	0	None	4	3	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting methodAgonist activity at human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 90 mins by [35S]GTPgammaS binding based liquid scintillation counting method	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	164620704	185501	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	416	8	4	4	3.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1	10.1016/j.ejmech.2021.113190
	CHEMBL4871482	185501	0	None	-	1	Human	7.5	pEC50	=	7.5	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	416	8	4	4	3.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1	10.1016/j.ejmech.2021.113190
	164624107	185140	0	None	8	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	402	9	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4865765	185140	0	None	8	3	Human	6.5	pEC50	=	6.5	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	402	9	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1	10.1016/j.ejmech.2021.113190
	155567151	175279	0	None	-1	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	245	1	1	3	3.5	CC1CCCc2c1nc(N)nc2C1CCCCC1	10.1021/acs.jmedchem.9b00241
	CHEMBL4585616	175279	0	None	-1	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	245	1	1	3	3.5	CC1CCCc2c1nc(N)nc2C1CCCCC1	10.1021/acs.jmedchem.9b00241
	155567151	175279	0	None	-1	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	245	1	1	3	3.5	CC1CCCc2c1nc(N)nc2C1CCCCC1	10.1021/acs.jmedchem.9b00241
	CHEMBL4585616	175279	0	None	-1	2	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	245	1	1	3	3.5	CC1CCCc2c1nc(N)nc2C1CCCCC1	10.1021/acs.jmedchem.9b00241
	164616851	184367	0	None	-2	3	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	376	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4853772	184367	0	None	-2	3	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	376	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	164614549	184360	0	None	-2	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	340	9	4	4	2.2	CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	CHEMBL4853668	184360	0	None	-2	3	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	340	9	4	4	2.2	CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	44482300	5716	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	342	9	4	2	2.0	NC(=O)/N=C(/NCCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	CHEMBL1078746	5716	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	342	9	4	2	2.0	NC(=O)/N=C(/NCCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	1204	1901	114	None	-61	10	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1247	1901	114	None	-61	10	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1375	1901	114	None	-61	10	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	774	1901	114	None	-61	10	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	CHEMBL90	1901	114	None	-61	10	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	DB05381	1901	114	None	-61	10	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1204	1901	114	None	-61	10	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	1247	1901	114	None	-61	10	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	1375	1901	114	None	-61	10	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	774	1901	114	None	-61	10	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	CHEMBL90	1901	114	None	-61	10	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	DB05381	1901	114	None	-61	10	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	1204	1901	114	None	-61	10	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	1247	1901	114	None	-61	10	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	1375	1901	114	None	-61	10	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	774	1901	114	None	-61	10	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	CHEMBL90	1901	114	None	-61	10	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	DB05381	1901	114	None	-61	10	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	164628701	185885	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	338	5	4	4	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1	10.1016/j.ejmech.2021.113190
	CHEMBL4876743	185885	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	338	5	4	4	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1	10.1016/j.ejmech.2021.113190
	CHEMBL5087637	213779	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095891	213779	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	44481487	6030	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	302	7	3	3	2.3	N#C/N=C(/NCCCC1CCCCC1)NCCc1c[nH]cn1	10.1021/jm900526h
	CHEMBL1080772	6030	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	302	7	3	3	2.3	N#C/N=C(/NCCCC1CCCCC1)NCCc1c[nH]cn1	10.1021/jm900526h
	59868	93720	56	None	-	1	Human	4.4	pEC50	=	4.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	211	3	2	4	1.6	CCCN[C@@H]1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	CHEMBL249420	93720	56	None	-	1	Human	4.4	pEC50	=	4.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	211	3	2	4	1.6	CCCN[C@@H]1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	168273745	192206	0	None	4	3	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5178472	192206	0	None	4	3	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221451	192206	0	None	4	3	Human	8.3	pEC50	=	8.3	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	168273640	192203	0	None	4	3	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5176229	192203	0	None	4	3	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221444	192203	0	None	4	3	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5075713	213753	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095559	213753	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	44482299	5660	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	328	8	4	2	1.6	NC(=O)/N=C(/NCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	CHEMBL1078359	5660	0	None	-	1	Human	6.4	pEC50	=	6.4	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	328	8	4	2	1.6	NC(=O)/N=C(/NCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	164627774	185983	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	344	3	4	4	1.4	N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	CHEMBL4878215	185983	0	None	-	1	Human	5.4	pEC50	=	5.4	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	344	3	4	4	1.4	N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	56953998	81656	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	578	16	6	8	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	CHEMBL2165631	81656	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	578	16	6	8	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	164622190	185034	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	360	7	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4864067	185034	0	None	-	1	Human	7.4	pEC50	=	7.4	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	360	7	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1	10.1016/j.ejmech.2021.113190
	164609729	184515	0	None	-2	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	360	6	4	4	2.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4856059	184515	0	None	-2	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	360	6	4	4	2.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	56953889	81655	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	564	15	6	8	2.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	CHEMBL2165630	81655	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	564	15	6	8	2.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	168273745	192206	0	None	4	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5178472	192206	0	None	4	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221451	192206	0	None	4	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	168294767	192417	0	None	40	10	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5207281	192417	0	None	40	10	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222802	192417	0	None	40	10	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	46887076	8870	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	359	7	4	5	2.8	Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)c1ccccc1	10.1016/j.bmcl.2010.03.082
	CHEMBL1098110	8870	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	359	7	4	5	2.8	Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)c1ccccc1	10.1016/j.bmcl.2010.03.082
	CHEMBL5094663	213730	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](C)c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5094663	213730	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](C)c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	155542256	172515	0	None	-1	2	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	257	5	1	4	3.1	CCCCc1cc(-c2ccc(OC)cc2)nc(N)n1	10.1021/acs.jmedchem.9b00241
	CHEMBL4519923	172515	0	None	-1	2	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	257	5	1	4	3.1	CCCCc1cc(-c2ccc(OC)cc2)nc(N)n1	10.1021/acs.jmedchem.9b00241
	168297879	191750	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at histamine H2 receptor (unknown origin)Agonist activity at histamine H2 receptor (unknown origin)	ChEMBL	640	18	5	9	4.9	CCOC(=O)C1=C(C)NC(CSCCCCCNC(=N)NCCCc2ccc[nH]2)=C(C(=O)OCC)C1c1cccc([N+](=O)[O-])c1	10.1016/j.bmc.2022.116706
	CHEMBL5207008	191750	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at histamine H2 receptor (unknown origin)Agonist activity at histamine H2 receptor (unknown origin)	ChEMBL	640	18	5	9	4.9	CCOC(=O)C1=C(C)NC(CSCCCCCNC(=N)NCCCc2ccc[nH]2)=C(C(=O)OCC)C1c1cccc([N+](=O)[O-])c1	10.1016/j.bmc.2022.116706
	164610421	184678	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	332	5	4	4	2.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4858567	184678	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	332	5	4	4	2.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1	10.1016/j.ejmech.2021.113190
	155542256	172515	0	None	-1	2	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	257	5	1	4	3.1	CCCCc1cc(-c2ccc(OC)cc2)nc(N)n1	10.1021/acs.jmedchem.9b00241
	CHEMBL4519923	172515	0	None	-1	2	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	257	5	1	4	3.1	CCCCc1cc(-c2ccc(OC)cc2)nc(N)n1	10.1021/acs.jmedchem.9b00241
	155544839	174371	0	None	2	2	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	284	2	1	5	3.1	CC1CCCc2c(-c3ccc([N+](=O)[O-])cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4565419	174371	0	None	2	2	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	284	2	1	5	3.1	CC1CCCc2c(-c3ccc([N+](=O)[O-])cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	46887077	8915	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	359	7	4	5	2.8	Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)c1ccccc1	10.1016/j.bmcl.2010.03.082
	CHEMBL1098441	8915	0	None	-	1	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	359	7	4	5	2.8	Cc1nc(N)sc1CCCNC(=N)NC(=O)C[C@@H](C)c1ccccc1	10.1016/j.bmcl.2010.03.082
	155544839	174371	0	None	2	2	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	284	2	1	5	3.1	CC1CCCc2c(-c3ccc([N+](=O)[O-])cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4565419	174371	0	None	2	2	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	284	2	1	5	3.1	CC1CCCc2c(-c3ccc([N+](=O)[O-])cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	1204	1901	114	None	-61	10	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1247	1901	114	None	-61	10	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1375	1901	114	None	-61	10	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	774	1901	114	None	-61	10	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	CHEMBL90	1901	114	None	-61	10	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	DB05381	1901	114	None	-61	10	Human	5.3	pEC50	=	5.3	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	56954320	81667	0	None	-13	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	472	15	6	4	0.9	N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1	10.1021/jm201128q
	CHEMBL2165641	81667	0	None	-13	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	472	15	6	4	0.9	N/C(=N\C(=O)CCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1	10.1021/jm201128q
	168278471	192246	0	None	2	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5183205	192246	0	None	2	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221757	192246	0	None	2	3	Human	7.3	pEC50	=	7.3	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5087637	213779	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095891	213779	0	None	-	1	Human	6.3	pEC50	=	6.3	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	56953887	81673	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	536	13	6	8	1.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	CHEMBL2165647	81673	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	536	13	6	8	1.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	168278471	192246	0	None	2	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5183205	192246	0	None	2	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221757	192246	0	None	2	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	168290815	192371	0	None	10	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5200771	192371	0	None	10	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222529	192371	0	None	10	2	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	56954322	81668	0	None	-3	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	500	17	6	4	1.7	N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1	10.1021/jm201128q
	CHEMBL2165642	81668	0	None	-3	3	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	500	17	6	4	1.7	N/C(=N\C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1)NCCCc1c[nH]cn1	10.1021/jm201128q
	46887043	8675	0	None	-1	4	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	319	7	4	3	2.6	C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	CHEMBL1096431	8675	0	None	-1	4	Human	8.2	pEC50	=	8.2	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	319	7	4	3	2.6	C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	164611757	184320	0	None	3	3	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	402	8	4	4	2.8	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
	CHEMBL4853107	184320	0	None	3	3	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	402	8	4	4	2.8	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
	168268853	192183	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5180504	192183	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221353	192183	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5083588	213758	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095633	213758	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB1 cells assessed as stimulation of beta-arrestin 1 recruitment	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	25149712	178408	0	None	-25	3	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	299	7	4	3	1.6	N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1	10.1016/j.bmcl.2010.10.041
	CHEMBL470790	178408	0	None	-25	3	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	299	7	4	3	1.6	N=C(NCCCc1c[nH]cn1)NC(=O)CCc1ccccc1	10.1016/j.bmcl.2010.10.041
	25149335	183643	0	None	-26	3	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1016/j.bmcl.2010.10.041
	CHEMBL483406	183643	0	None	-26	3	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1016/j.bmcl.2010.10.041
	CHEMBL5093461	213777	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095884	213777	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	164626153	185796	0	None	1	3	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	378	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1	10.1016/j.ejmech.2021.113190
	CHEMBL4875600	185796	0	None	1	3	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	378	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1	10.1016/j.ejmech.2021.113190
	44482299	5660	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	328	8	4	2	1.6	NC(=O)/N=C(/NCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	CHEMBL1078359	5660	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	328	8	4	2	1.6	NC(=O)/N=C(/NCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	1204	1901	114	None	-61	10	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	1247	1901	114	None	-61	10	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	1375	1901	114	None	-61	10	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	774	1901	114	None	-61	10	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	CHEMBL90	1901	114	None	-61	10	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	DB05381	1901	114	None	-61	10	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H2 receptor expressed in 293-EBNA cells by luciferase reporter gene assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm0603318
	CHEMBL5076746	213749	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(N)(=O)=O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095519	213749	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(N)(=O)=O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5088914	213786	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095949	213786	0	None	-	1	Human	6.2	pEC50	=	6.2	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5085542	213199	0	None	-	1	Human	7.2	pEC50	=	7.2	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C	10.1016/j.bmcl.2021.128388
	CHEMBL5092102	213572	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL		None	None	None		NCCCCCCCCNC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1016/j.bmcl.2021.128388
	CHEMBL5094083	213692	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitmentAgonist activity at human H2 receptor expressed in HEK293T-ARRB2 cells assessed as stimulation of beta-arrestin 2 recruitment	ChEMBL		None	None	None		C=C(/N=C(\C)NCCCc1nnc(N)s1)NCCCCCCCCN	10.1016/j.bmcl.2021.128388
	56954515	81653	0	None	-2	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	546	17	6	6	2.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm201128q
	CHEMBL2165628	81653	0	None	-2	3	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	546	17	6	6	2.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm201128q
	56954000	81657	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	592	17	6	8	2.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	CHEMBL2165632	81657	0	None	-	1	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	592	17	6	8	2.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)CCCCCCCCC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1021/jm201128q
	CHEMBL5078202	213760	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1	10.1016/j.bmcl.2021.128388
	CHEMBL5095695	213760	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1	10.1016/j.bmcl.2021.128388
	44480707	5686	0	None	-5	2	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	328	8	3	4	2.2	N#C/N=C(/NCCCc1c[nH]cn1)NCCSc1ccccc1	10.1021/jm900526h
	CHEMBL1078529	5686	0	None	-5	2	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	328	8	3	4	2.2	N#C/N=C(/NCCCc1c[nH]cn1)NCCSc1ccccc1	10.1021/jm900526h
	168281746	192280	0	None	77	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5184911	192280	0	None	77	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221974	192280	0	None	77	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing ARRB2 incubated for 60 mins by beta-arrestin2 recruitment assay	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
	155525816	170487	0	None	7	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	257	1	1	3	3.3	CC1CCCc2c(-c3ccc(F)cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4456972	170487	0	None	7	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	257	1	1	3	3.3	CC1CCCc2c(-c3ccc(F)cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL5077939	213765	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095769	213765	0	None	-	1	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	168292954	192395	0	None	7	3	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5202592	192395	0	None	7	3	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222660	192395	0	None	7	3	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	155553964	174884	0	None	11	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	273	1	1	3	3.8	CC1CCCc2c(-c3ccc(Cl)cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4576986	174884	0	None	11	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	273	1	1	3	3.8	CC1CCCc2c(-c3ccc(Cl)cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	46830167	8673	0	None	-42	4	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	313	7	4	3	2.2	C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1	10.1016/j.bmcl.2010.03.082
	CHEMBL1096429	8673	0	None	-42	4	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	313	7	4	3	2.2	C[C@@H](CC(=O)NC(=N)NCCCc1c[nH]cn1)c1ccccc1	10.1016/j.bmcl.2010.03.082
	25149521	178474	0	None	-9	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	375	8	4	3	3.2	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1	10.1016/j.bmcl.2010.10.041
	CHEMBL471413	178474	0	None	-9	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing Gsalphas by steady-state GTPase activity assay	ChEMBL	375	8	4	3	3.2	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1	10.1016/j.bmcl.2010.10.041
	168281746	192280	0	None	77	2	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5184911	192280	0	None	77	2	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221974	192280	0	None	77	2	Human	8.1	pEC50	=	8.1	Functional	Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
	155525816	170487	0	None	7	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	257	1	1	3	3.3	CC1CCCc2c(-c3ccc(F)cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4456972	170487	0	None	7	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	257	1	1	3	3.3	CC1CCCc2c(-c3ccc(F)cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	155553964	174884	0	None	11	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	273	1	1	3	3.8	CC1CCCc2c(-c3ccc(Cl)cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4576986	174884	0	None	11	2	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	273	1	1	3	3.8	CC1CCCc2c(-c3ccc(Cl)cc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	155565842	175043	0	None	-5	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	317	1	1	3	3.9	CC1CCCc2c(-c3cccc(Br)c3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4580450	175043	0	None	-5	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	317	1	1	3	3.9	CC1CCCc2c(-c3cccc(Br)c3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	164614549	184360	0	None	-2	3	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	340	9	4	4	2.2	CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	CHEMBL4853668	184360	0	None	-2	3	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assayAgonist activity at human histamine H2 receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay	ChEMBL	340	9	4	4	2.2	CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	59868	93720	56	None	-	1	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@@H]1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	CHEMBL249420	93720	56	None	-	1	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@@H]1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	155532722	171219	0	None	3	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	253	1	1	3	3.5	Cc1ccc(-c2nc(N)nc3c2CCCC3C)cc1	10.1021/acs.jmedchem.9b00241
	CHEMBL4467878	171219	0	None	3	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	253	1	1	3	3.5	Cc1ccc(-c2nc(N)nc3c2CCCC3C)cc1	10.1021/acs.jmedchem.9b00241
	CHEMBL5090859	213509	0	None	-	1	Human	7.1	pEC50	=	7.1	Functional	Agonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysisAgonist activity at human H2 receptor expressed in Sf9 cell membranes co-exprssing GsalphaS assessed as stimulation of [35S]GTPgammaS binding incubated for 90 mins by scintillation counting analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C	10.1016/j.bmcl.2021.128388
	155532722	171219	0	None	3	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	253	1	1	3	3.5	Cc1ccc(-c2nc(N)nc3c2CCCC3C)cc1	10.1021/acs.jmedchem.9b00241
	CHEMBL4467878	171219	0	None	3	2	Human	6.1	pEC50	=	6.1	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	253	1	1	3	3.5	Cc1ccc(-c2nc(N)nc3c2CCCC3C)cc1	10.1021/acs.jmedchem.9b00241
	44481758	5638	0	None	-	1	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	324	9	3	3	2.4	N#C/N=C(\NCCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	CHEMBL1078212	5638	0	None	-	1	Human	5.1	pEC50	=	5.1	Functional	Agonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assayAgonist activity at human histamine H2 receptor expressed in Sf9 cells coexpressing GsalphaS protein by steady-state GTPase assay	ChEMBL	324	9	3	3	2.4	N#C/N=C(\NCCCCc1ccccc1)NCCCc1c[nH]cn1	10.1021/jm900526h
	46887079	8424	0	None	478	3	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	365	7	4	5	3.2	Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	CHEMBL1094142	8424	0	None	478	3	Human	8.0	pEC50	=	8.0	Functional	Agonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assayAgonist activity at GsalphaS-fused human histamine H2 receptor expressed in Sf9 cells by [35S]GTPgammaS binding assay	ChEMBL	365	7	4	5	3.2	Cc1nc(N)sc1CCCNC(=N)NC(=O)CC(C)C1CCCCC1	10.1016/j.bmcl.2010.03.082
	56954229	81663	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	648	23	6	8	4.7	N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1	10.1021/jm201128q
	CHEMBL2165638	81663	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assayAgonist activity at human H2R-Gsalphas expressed in Sf9 cells at 0.1 nM to 10 uM by steady state GTPase activity assay	ChEMBL	648	23	6	8	4.7	N/C(=N\C(=O)CCCCCCCCCCCCCCC(=O)/N=C(\N)NCCCc1cnc(N)s1)NCCCc1cnc(N)s1	10.1021/jm201128q
	CHEMBL5094083	213692	0	None	-	1	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assayAgonist activity at NlucN/mini-Gi protein-fused human H2R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay	ChEMBL		None	None	None		C=C(/N=C(\C)NCCCc1nnc(N)s1)NCCCCCCCCN	10.1016/j.bmcl.2021.128388
	155559319	174291	0	None	13	2	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	239	1	1	3	3.2	CC1CCCc2c(-c3ccccc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	CHEMBL4563363	174291	0	None	13	2	Human	7.0	pEC50	=	7.0	Functional	Agonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assayAgonist activity at recombinant human Gs-coupled H2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by forskolin-stimulation by Glo-sensor assay	ChEMBL	239	1	1	3	3.2	CC1CCCc2c(-c3ccccc3)nc(N)nc21	10.1021/acs.jmedchem.9b00241
	1204	1901	114	None	-61	10	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	1247	1901	114	None	-61	10	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	1375	1901	114	None	-61	10	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	774	1901	114	None	-61	10	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	CHEMBL90	1901	114	None	-61	10	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	DB05381	1901	114	None	-61	10	Human	6.0	pEC50	=	6.0	Functional	Agonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysisAgonist activity at human histamine receptor expressed in sf9 insect cell membranes co-exprssing GsalphaS incubated for 90 mins [35S]GTPgammaS binding based microbeta scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	44281005	116231	0	None	-	3	Rat	6.0	pKd	=	6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	787	17	4	8	6.4	Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00249-1
	CHEMBL33743	116231	0	None	-	3	Rat	6.0	pKd	=	6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	787	17	4	8	6.4	Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00249-1
	CHEMBL432671	167532	0	None	-	3	Rat	6.0	pKd	=	6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	784	15	7	12	3.1	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCNC(=O)CC(=O)NCCSCc3csc(C=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	44280028	98720	0	None	-	3	Rat	6.0	pKd	=	6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	768	17	6	9	4.3	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	CHEMBL281318	98720	0	None	-	3	Rat	6.0	pKd	=	6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	768	17	6	9	4.3	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	9896825	102504	0	None	-	3	Rat	6.0	pKd	=	6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	742	14	6	10	2.9	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL30656	102504	0	None	-	3	Rat	6.0	pKd	=	6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	742	14	6	10	2.9	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44281078	99282	0	None	-	3	Rat	5.9	pKd	=	5.9	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	773	16	4	8	5.9	CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL284975	99282	0	None	-	3	Rat	5.9	pKd	=	5.9	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	773	16	4	8	5.9	CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	44280714	99571	0	None	-	3	Rat	5.9	pKd	=	5.9	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	726	14	6	9	3.2	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL286908	99571	0	None	-	3	Rat	5.9	pKd	=	5.9	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	726	14	6	9	3.2	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44281291	99364	0	None	-	0	Rat	7.8	pKd	=	7.8	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	433	11	2	5	3.9	CC(C)(C)OC(=O)NCCCC(=O)NCCCOc1cccc(CN2CCCCC2)c1	10.1016/S0960-894X(96)00249-1
	CHEMBL285556	99364	0	None	-	0	Rat	7.8	pKd	=	7.8	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	433	11	2	5	3.9	CC(C)(C)OC(=O)NCCCC(=O)NCCCOc1cccc(CN2CCCCC2)c1	10.1016/S0960-894X(96)00249-1
	44281292	114296	0	None	-	3	Rat	6.8	pKd	=	6.8	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	816	17	5	9	5.0	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCNC(=O)CC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL33398	114296	0	None	-	3	Rat	6.8	pKd	=	6.8	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	816	17	5	9	5.0	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCNC(=O)CC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL286835	99557	0	None	-	0	Rat	5.7	pKd	=	5.7	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	755	14	6	11	4.5	Cc1cccc(NC(=O)N[C@@H]2N=C(c3cccc(OC(=O)NCCCC(=O)NCCSCc4csc(C=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00249-1
	1231	924	112	None	-	3	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00249-1
	2756	924	112	None	-	3	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00249-1
	645	924	112	None	-	3	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00249-1
	CHEMBL30	924	112	None	-	3	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00249-1
	DB00501	924	112	None	-	3	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00249-1
	44281020	116144	0	None	-	3	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	773	16	4	8	6.2	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL33698	116144	0	None	-	3	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	773	16	4	8	6.2	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	1231	924	112	None	-	3	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00248-X
	2756	924	112	None	-	3	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00248-X
	645	924	112	None	-	3	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00248-X
	CHEMBL30	924	112	None	-	3	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00248-X
	DB00501	924	112	None	-	3	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/S0960-894X(96)00248-X
	44279811	96477	0	None	-	3	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	743	15	4	7	5.3	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	CHEMBL265987	96477	0	None	-	3	Rat	6.6	pKd	=	6.6	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	743	15	4	7	5.3	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	44281204	99388	0	None	-	3	Rat	6.5	pKd	=	6.5	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	871	18	4	10	5.5	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL285719	99388	0	None	-	3	Rat	6.5	pKd	=	6.5	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	871	18	4	10	5.5	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	44280741	156021	0	None	-	3	Rat	6.5	pKd	=	6.5	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	759	15	4	8	5.8	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL406844	156021	0	None	-	3	Rat	6.5	pKd	=	6.5	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	759	15	4	8	5.8	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	44280372	98928	0	None	-	3	Rat	6.5	pKd	=	6.5	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	787	17	4	8	5.8	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL282645	98928	0	None	-	3	Rat	6.5	pKd	=	6.5	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	787	17	4	8	5.8	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL282175	98863	0	None	-	3	Rat	5.5	pKd	=	5.5	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	769	16	6	11	4.6	Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(CCOC(=O)NCCCC(=O)NCCSCc3csc(C=C(N)N)n3)C2=O)c1	10.1016/S0960-894X(96)00249-1
	44280713	99570	0	None	-	3	Rat	5.5	pKd	=	5.5	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	740	15	6	9	3.6	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL286907	99570	0	None	-	3	Rat	5.5	pKd	=	5.5	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	740	15	6	9	3.6	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44280740	99941	0	None	-	3	Rat	6.4	pKd	=	6.4	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	787	17	4	8	6.3	CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL290122	99941	0	None	-	3	Rat	6.4	pKd	=	6.4	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	787	17	4	8	6.3	CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	44280200	100357	0	None	-	3	Rat	6.4	pKd	=	6.4	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	785	18	4	7	6.6	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL29331	100357	0	None	-	3	Rat	6.4	pKd	=	6.4	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	785	18	4	7	6.6	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44279861	102709	0	None	-	3	Rat	6.4	pKd	=	6.4	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	726	14	6	9	3.1	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	CHEMBL30821	102709	0	None	-	3	Rat	6.4	pKd	=	6.4	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	726	14	6	9	3.1	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	44279810	103367	0	None	-	3	Rat	6.4	pKd	=	6.4	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	757	16	4	7	5.7	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	CHEMBL30917	103367	0	None	-	3	Rat	6.4	pKd	=	6.4	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	757	16	4	7	5.7	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	44279808	98684	0	None	-	3	Rat	5.4	pKd	=	5.4	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	712	13	6	9	2.9	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL281082	98684	0	None	-	3	Rat	5.4	pKd	=	5.4	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	712	13	6	9	2.9	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCSCc3csc(N=C(N)N)n3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	135881774	99197	0	None	-	0	Rat	7.3	pKd	=	7.3	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	415	10	4	8	2.0	CC(C)(C)OC(=O)NCCCC(=O)NCCSCc1csc(C=C(N)N)n1	10.1016/S0960-894X(96)00249-1
	CHEMBL284374	99197	0	None	-	0	Rat	7.3	pKd	=	7.3	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	415	10	4	8	2.0	CC(C)(C)OC(=O)NCCCC(=O)NCCSCc1csc(C=C(N)N)n1	10.1016/S0960-894X(96)00249-1
	44281004	99617	0	None	-	3	Rat	6.3	pKd	=	6.3	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	773	15	4	8	6.4	Cc1cccc(NC(=O)N[C@@H]2N=C(c3cccc(OC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00249-1
	CHEMBL287295	99617	0	None	-	3	Rat	6.3	pKd	=	6.3	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	773	15	4	8	6.4	Cc1cccc(NC(=O)N[C@@H]2N=C(c3cccc(OC(=O)NCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00249-1
	44280029	95994	0	None	-	3	Rat	6.3	pKd	=	6.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	740	15	6	9	3.5	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	CHEMBL262125	95994	0	None	-	3	Rat	6.3	pKd	=	6.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	740	15	6	9	3.5	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCC(=O)NCCSCc3csc(N=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	44280373	98929	0	None	-	3	Rat	6.3	pKd	=	6.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	773	16	4	8	5.4	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL282646	98929	0	None	-	3	Rat	6.3	pKd	=	6.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	773	16	4	8	5.4	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44280388	116369	0	None	-	3	Rat	6.3	pKd	=	6.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	759	15	4	8	5.0	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL33819	116369	0	None	-	3	Rat	6.3	pKd	=	6.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	759	15	4	8	5.0	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44279862	98673	0	None	-	3	Rat	5.3	pKd	=	5.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	702	13	3	7	5.9	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL281017	98673	0	None	-	3	Rat	5.3	pKd	=	5.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	702	13	3	7	5.9	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44280213	101147	0	None	-	3	Rat	5.3	pKd	=	5.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	685	12	5	9	3.7	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL29888	101147	0	None	-	3	Rat	5.3	pKd	=	5.3	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	685	12	5	9	3.7	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44281205	114320	0	None	-	3	Rat	6.2	pKd	=	6.2	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	857	17	4	10	5.1	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL33412	114320	0	None	-	3	Rat	6.2	pKd	=	6.2	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	857	17	4	10	5.1	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCCN3CCN(C(=O)CNCCCOc4cccc(CN5CCCCC5)c4)CC3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	44279809	98510	0	None	-	3	Rat	6.2	pKd	=	6.2	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	785	18	4	7	6.4	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	CHEMBL279778	98510	0	None	-	3	Rat	6.2	pKd	=	6.2	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	785	18	4	7	6.4	CN1C(=O)[C@H](NC(=O)Nc2cccc(CC(=O)NCCCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00248-X
	44280371	102554	0	None	-	3	Rat	6.2	pKd	=	6.2	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	815	19	4	8	6.6	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL30701	102554	0	None	-	3	Rat	6.2	pKd	=	6.2	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	815	19	4	8	6.6	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCCCC(=O)NCCCOc4cccc(CN5CCCCC5)c4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44280214	106818	0	None	-	3	Rat	6.2	pKd	=	6.2	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	770	16	6	10	3.6	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL31726	106818	0	None	-	3	Rat	6.2	pKd	=	6.2	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	770	16	6	10	3.6	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44280266	98322	0	None	-	3	Rat	5.2	pKd	=	5.2	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	729	14	4	7	5.0	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL278217	98322	0	None	-	3	Rat	5.2	pKd	=	5.2	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	729	14	4	7	5.0	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44280996	99283	0	None	-	3	Rat	6.1	pKd	=	6.1	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	745	14	4	8	5.4	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL284976	99283	0	None	-	3	Rat	6.1	pKd	=	6.1	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	745	14	4	8	5.4	CN1C(=O)[C@H](NC(=O)Nc2cccc(COC(=O)NCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	CHEMBL285995	99430	0	None	-	3	Rat	6.1	pKd	=	6.1	Functional	Antagonistic activity by inhibition histamine H2 receptor from rats.Antagonistic activity by inhibition histamine H2 receptor from rats.	ChEMBL	741	16	6	11	4.5	CN1C(=O)[C@H](NC(=O)Nc2cccc(CCOC(=O)NCCCNCCSCc3csc(C=C(N)N)n3)c2)N=C(c2ccccc2)c2ccccc21	10.1016/S0960-894X(96)00249-1
	44280215	99369	0	None	-	3	Rat	6.1	pKd	=	6.1	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	756	15	6	10	3.3	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL285586	99369	0	None	-	3	Rat	6.1	pKd	=	6.1	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	756	15	6	10	3.3	Cc1cccc(NC(=O)NC2N=C(c3cccc(OCC(=O)NCCC(=O)NCCSCc4csc(N=C(N)N)n4)c3)c3ccccc3N(C)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44280225	99501	0	None	-	3	Rat	6.1	pKd	=	6.1	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	743	15	4	7	5.4	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL286475	99501	0	None	-	3	Rat	6.1	pKd	=	6.1	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	743	15	4	7	5.4	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	44280224	104305	0	None	-	3	Rat	6.1	pKd	=	6.1	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	757	16	4	7	5.8	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	CHEMBL31090	104305	0	None	-	3	Rat	6.1	pKd	=	6.1	Functional	Antagonistic activity for inhibition of histamine H2 receptor from anesthetized ratsAntagonistic activity for inhibition of histamine H2 receptor from anesthetized rats	ChEMBL	757	16	4	7	5.8	Cc1cccc(NC(=O)NC2N=C(c3ccccc3)c3ccccc3N(CC(=O)NCCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)C2=O)c1	10.1016/S0960-894X(96)00248-X
	54754351	67875	0	None	-	0	Human	5.5	pKi	=	5.5	Functional	Antagonist activity at histamine H2 receptorAntagonist activity at histamine H2 receptor	ChEMBL	277	4	1	5	2.1	CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1	10.1016/j.bmcl.2011.07.114
	CHEMBL1915535	67875	0	None	-	0	Human	5.5	pKi	=	5.5	Functional	Antagonist activity at histamine H2 receptorAntagonist activity at histamine H2 receptor	ChEMBL	277	4	1	5	2.1	CN1CCN(c2cc(NCCC(C)(C)C)ncn2)CC1	10.1016/j.bmcl.2011.07.114
	57395620	67874	0	None	-	0	Human	5.1	pKi	=	5.1	Functional	Antagonist activity at histamine H2 receptorAntagonist activity at histamine H2 receptor	ChEMBL	263	5	3	5	2.1	CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1	10.1016/j.bmcl.2011.07.114
	CHEMBL1915534	67874	0	None	-	0	Human	5.1	pKi	=	5.1	Functional	Antagonist activity at histamine H2 receptorAntagonist activity at histamine H2 receptor	ChEMBL	263	5	3	5	2.1	CC(C)(C)CCNc1cc(N[C@H]2CCNC2)ncn1	10.1016/j.bmcl.2011.07.114
	126688	400	28	None	57	2	Human	6.4	pEC50	=	6.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	157	2	2	4	0.5	NCCc1sc(nc1C)N	19072936
	4025	400	28	None	57	2	Human	6.4	pEC50	=	6.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	157	2	2	4	0.5	NCCc1sc(nc1C)N	19072936
	CHEMBL293762	400	28	None	57	2	Human	6.4	pEC50	=	6.4	Functional	UnclassifiedUnclassified	Guide to Pharmacology	157	2	2	4	0.5	NCCc1sc(nc1C)N	19072936
	1229	732	0	None	-	1	Human	5.7	pEC50	None	5.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	262	5	3	2	2.0	CNC(=S)NCCCCc1cccc2c1cn[nH]2	9681472
	5311293	732	0	None	-	1	Human	5.7	pEC50	None	5.7	Functional	UnclassifiedUnclassified	Guide to Pharmacology	262	5	3	2	2.0	CNC(=S)NCCCCc1cccc2c1cn[nH]2	9681472
	18381	215975	0	None	1	4	Human	8.3	pIC50	=	8.3	Functional	NoneNone	Drug Central	469	4	2	6	3.2	CC1=C(C(=O)N[C@H]2[C@H]3SC(C)(C)[C@@H](N3C2=O)C(O)=O)C(=NO1)C1=C(Cl)C=CC=C1Cl	None
	30699	215969	0	None	-1	14	Human	8.3	pIC50	=	8.3	Functional	NoneNone	Drug Central	423	7	2	8	0.5	CC(=O)OCC1=C(N2[C@H](SC1)[C@H](NC(=O)CSC1=CC=NC=C1)C2=O)C(O)=O	None
	180	397	50	None	-151	26	Human	8.2	pIC50	=	8.2	Functional	NoneNone	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	200	397	50	None	-151	26	Human	8.2	pIC50	=	8.2	Functional	NoneNone	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	2160	397	50	None	-151	26	Human	8.2	pIC50	=	8.2	Functional	NoneNone	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	CHEMBL629	397	50	None	-151	26	Human	8.2	pIC50	=	8.2	Functional	NoneNone	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	DB00321	397	50	None	-151	26	Human	8.2	pIC50	=	8.2	Functional	NoneNone	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	46780481	107045	18	None	-	1	Human	8.1	pIC50	=	8.1	Functional	NoneNone	Drug Central	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
	9903970	107045	18	None	-	1	Human	8.1	pIC50	=	8.1	Functional	NoneNone	Drug Central	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
	CHEMBL3187365	107045	18	None	-	1	Human	8.1	pIC50	=	8.1	Functional	NoneNone	Drug Central	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
	CHEMBL3544974	107045	18	None	-	1	Human	8.1	pIC50	=	8.1	Functional	NoneNone	Drug Central	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None

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Ligands					Receptor			Assay information							Chemical information
Sel. page	Common name	GPCRdb ID	#Vendors	Reference ligand	Fold selectivity (Affinity)	# tested GPCRs (Affinity)	Species	p-value (-log)	Type	Activity Relation	Activity Value	Assay Type	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	25149708	187852	0	None	-	0	Human	7.0	pEC50	=	7.0	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	319	7	4	4	2.2	CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1cccs1	10.1021/jm800841w
	CHEMBL502339	187852	0	None	-	0	Human	7.0	pEC50	=	7.0	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	319	7	4	4	2.2	CC(CC(=O)NC(=N)NCCCc1c[nH]cn1)c1cccs1	10.1021/jm800841w
	42625304	178522	0	None	-	1	Human	7.0	pEC50	=	7.0	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	237	5	3	2	0.4	CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL471724	178522	0	None	-	1	Human	7.0	pEC50	=	7.0	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	237	5	3	2	0.4	CC(C)C(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
	25149613	178621	0	None	-	1	Human	6.9	pEC50	=	6.9	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	382	8	4	5	2.7	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1	10.1021/jm800841w
	CHEMBL472441	178621	0	None	-	1	Human	6.9	pEC50	=	6.9	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	382	8	4	5	2.7	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1nccs1	10.1021/jm800841w
	1204	1901	114	None	-173	23	Human	5.9	pEC50	=	5.9	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm800841w
	1247	1901	114	None	-173	23	Human	5.9	pEC50	=	5.9	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm800841w
	1375	1901	114	None	-173	23	Human	5.9	pEC50	=	5.9	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm800841w
	774	1901	114	None	-173	23	Human	5.9	pEC50	=	5.9	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm800841w
	CHEMBL90	1901	114	None	-173	23	Human	5.9	pEC50	=	5.9	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm800841w
	DB05381	1901	114	None	-173	23	Human	5.9	pEC50	=	5.9	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm800841w
	1204	1901	114	None	-173	23	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm9000693
	1247	1901	114	None	-173	23	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm9000693
	1375	1901	114	None	-173	23	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm9000693
	774	1901	114	None	-173	23	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm9000693
	CHEMBL90	1901	114	None	-173	23	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm9000693
	DB05381	1901	114	None	-173	23	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm9000693
	1204	1901	114	None	-173	23	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
	1247	1901	114	None	-173	23	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
	1375	1901	114	None	-173	23	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
	774	1901	114	None	-173	23	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
	CHEMBL90	1901	114	None	-173	23	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
	DB05381	1901	114	None	-173	23	Human	5.9	pEC50	=	5.9	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1039/C3MD00245D
	46890166	7235	0	None	-	2	Human	6.9	pEC50	=	6.9	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells	ChEMBL	419	6	2	4	4.5	Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1	10.1016/j.bmcl.2010.04.017
	CHEMBL1086105	7235	0	None	-	2	Human	6.9	pEC50	=	6.9	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells	ChEMBL	419	6	2	4	4.5	Cc1cc(OCCCN2CCc3nc[nH]c3C2)ccc1-c1nc2c(C)c(F)ccc2[nH]1	10.1016/j.bmcl.2010.04.017
	42625386	177778	0	None	-	1	Human	6.9	pEC50	=	6.9	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	237	6	3	2	0.6	CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL465170	177778	0	None	-	1	Human	6.9	pEC50	=	6.9	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	237	6	3	2	0.6	CCCC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
	90667232	108983	0	None	-	1	Human	6.6	pEC50	=	6.6	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1cn[nH]c1)c1ccccc1	10.1039/C3MD00245D
	CHEMBL3220633	108983	0	None	-	1	Human	6.6	pEC50	=	6.6	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1cn[nH]c1)c1ccccc1	10.1039/C3MD00245D
	10103168	25899	5	None	-	2	Human	5.6	pEC50	=	5.6	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	123	1	2	2	0.2	N[C@@H]1C[C@H]1c1c[nH]cn1	10.1021/jm020415q
	CHEMBL13559	25899	5	None	-	2	Human	5.6	pEC50	=	5.6	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	123	1	2	2	0.2	N[C@@H]1C[C@H]1c1c[nH]cn1	10.1021/jm020415q
	182527	110079	7	None	-	0	Human	5.6	pEC50	=	5.6	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	167	4	4	2	-0.2	N=C(N)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL325327	110079	7	None	-	0	Human	5.6	pEC50	=	5.6	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	167	4	4	2	-0.2	N=C(N)NCCCc1c[nH]cn1	10.1021/jm9000693
	42626110	179189	0	None	-	0	Human	6.5	pEC50	=	6.5	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	310	5	4	2	1.6	N/C(=N\C(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL474448	179189	0	None	-	0	Human	6.5	pEC50	=	6.5	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	310	5	4	2	1.6	N/C(=N\C(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1	10.1021/jm9000693
	42625224	180182	0	None	-	1	Human	7.5	pEC50	=	7.5	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	395	9	5	3	1.5	N/C(=N\C(=O)CCCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL475620	180182	0	None	-	1	Human	7.5	pEC50	=	7.5	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	395	9	5	3	1.5	N/C(=N\C(=O)CCCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1	10.1021/jm9000693
	42625223	179345	0	None	-	1	Human	6.5	pEC50	=	6.5	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	395	8	4	3	1.4	CN(CCC(=O)/N=C(\N)NCCCc1c[nH]cn1)C(=O)c1cc2ccccc2[nH]1	10.1021/jm9000693
	CHEMBL474617	179345	0	None	-	1	Human	6.5	pEC50	=	6.5	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	395	8	4	3	1.4	CN(CCC(=O)/N=C(\N)NCCCc1c[nH]cn1)C(=O)c1cc2ccccc2[nH]1	10.1021/jm9000693
	42626109	179188	0	None	-	1	Human	7.4	pEC50	=	7.4	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	324	6	4	2	1.5	N/C(=N\C(=O)Cc1c[nH]c2ccccc12)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL474447	179188	0	None	-	1	Human	7.4	pEC50	=	7.4	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	324	6	4	2	1.5	N/C(=N\C(=O)Cc1c[nH]c2ccccc12)NCCCc1c[nH]cn1	10.1021/jm9000693
	42625303	180184	0	None	-	1	Human	6.4	pEC50	=	6.4	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	223	5	3	2	0.2	CCC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL475621	180184	0	None	-	1	Human	6.4	pEC50	=	6.4	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	223	5	3	2	0.2	CCC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
	90667235	108986	0	None	-	1	Human	6.4	pEC50	=	6.4	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	376	8	3	3	2.4	N/C(=N\C(=O)CC(c1ccccc1)c1ccccc1)NCCCc1ncn[nH]1	10.1039/C3MD00245D
	CHEMBL3220636	108986	0	None	-	1	Human	6.4	pEC50	=	6.4	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	376	8	3	3	2.4	N/C(=N\C(=O)CC(c1ccccc1)c1ccccc1)NCCCc1ncn[nH]1	10.1039/C3MD00245D
	1204	1901	114	None	-173	23	Human	6.3	pEC50	=	6.3	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm020415q
	1247	1901	114	None	-173	23	Human	6.3	pEC50	=	6.3	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm020415q
	1375	1901	114	None	-173	23	Human	6.3	pEC50	=	6.3	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm020415q
	774	1901	114	None	-173	23	Human	6.3	pEC50	=	6.3	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm020415q
	CHEMBL90	1901	114	None	-173	23	Human	6.3	pEC50	=	6.3	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm020415q
	DB05381	1901	114	None	-173	23	Human	6.3	pEC50	=	6.3	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm020415q
	25149335	183643	0	None	-	1	Human	7.2	pEC50	=	7.2	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/jm800841w
	CHEMBL483406	183643	0	None	-	1	Human	7.2	pEC50	=	7.2	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/jm800841w
	25149335	183643	0	None	-	1	Human	7.2	pEC50	=	7.2	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/jm9000693
	CHEMBL483406	183643	0	None	-	1	Human	7.2	pEC50	=	7.2	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/jm9000693
	25149335	183643	0	None	-	1	Human	7.2	pEC50	=	7.2	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1039/C3MD00245D
	CHEMBL483406	183643	0	None	-	1	Human	7.2	pEC50	=	7.2	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	313	7	3	2	2.0	CC(CC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1039/C3MD00245D
	10374457	28682	2	None	-	2	Human	6.2	pEC50	=	6.2	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	123	1	2	2	0.2	N[C@H]1C[C@@H]1c1c[nH]cn1	10.1021/jm020415q
	CHEMBL13795	28682	2	None	-	2	Human	6.2	pEC50	=	6.2	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	123	1	2	2	0.2	N[C@H]1C[C@@H]1c1c[nH]cn1	10.1021/jm020415q
	42625384	169206	0	None	-	1	Human	6.1	pEC50	=	6.1	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	209	4	3	2	-0.2	CC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL443896	169206	0	None	-	1	Human	6.1	pEC50	=	6.1	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	209	4	3	2	-0.2	CC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1021/jm9000693
	90667234	108985	0	None	-	1	Human	6.1	pEC50	=	6.1	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	314	7	3	3	1.4	CC(CC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1039/C3MD00245D
	CHEMBL3220635	108985	0	None	-	1	Human	6.1	pEC50	=	6.1	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	314	7	3	3	1.4	CC(CC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1039/C3MD00245D
	25149521	178474	0	None	-	1	Human	7.1	pEC50	=	7.1	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	375	8	4	3	3.2	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1	10.1021/jm800841w
	CHEMBL471413	178474	0	None	-	1	Human	7.1	pEC50	=	7.1	Binding	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assayActivity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	ChEMBL	375	8	4	3	3.2	N=C(NCCCc1c[nH]cn1)NC(=O)CC(c1ccccc1)c1ccccc1	10.1021/jm800841w
	42625221	188997	0	None	-	1	Human	7.1	pEC50	=	7.1	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	338	7	4	2	1.9	N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL514641	188997	0	None	-	1	Human	7.1	pEC50	=	7.1	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	338	7	4	2	1.9	N/C(=N\C(=O)CCc1c[nH]c2ccccc12)NCCCc1c[nH]cn1	10.1021/jm9000693
	42626111	189102	0	None	-	0	Human	7.1	pEC50	=	7.1	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	381	8	5	3	1.1	N/C(=N\C(=O)CCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL515428	189102	0	None	-	0	Human	7.1	pEC50	=	7.1	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	381	8	5	3	1.1	N/C(=N\C(=O)CCNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1	10.1021/jm9000693
	90667262	108992	0	None	-	0	Human	6.1	pEC50	=	6.1	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	324	7	2	2	2.6	CC(CC(=O)/N=C(\N)NCCCc1ccccn1)c1ccccc1	10.1039/C3MD00245D
	CHEMBL3220665	108992	0	None	-	0	Human	6.1	pEC50	=	6.1	Binding	Agonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay	ChEMBL	324	7	2	2	2.6	CC(CC(=O)/N=C(\N)NCCCc1ccccn1)c1ccccc1	10.1039/C3MD00245D
	11829635	162688	4	None	-	1	Human	7.0	pEC50	=	7.0	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	151	3	2	2	0.9	NCC[C@H]1C[C@H]1c1c[nH]cn1	10.1021/jm020415q
	CHEMBL418470	162688	4	None	-	1	Human	7.0	pEC50	=	7.0	Binding	Inhibition of human Histamine H2 receptor using [3H]tiotidineInhibition of human Histamine H2 receptor using [3H]tiotidine	ChEMBL	151	3	2	2	0.9	NCC[C@H]1C[C@H]1c1c[nH]cn1	10.1021/jm020415q
	42625222	179190	0	None	-	0	Human	6.0	pEC50	=	6.0	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	367	7	5	3	0.7	N/C(=N\C(=O)CNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1	10.1021/jm9000693
	CHEMBL474449	179190	0	None	-	0	Human	6.0	pEC50	=	6.0	Binding	Agonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H2 receptor expressed in insect Sf9 cells co-expressing GsalphaS fusion protein assessed as gamma[32P]GTP binding by liquid scintillation counting	ChEMBL	367	7	5	3	0.7	N/C(=N\C(=O)CNC(=O)c1cc2ccccc2[nH]1)NCCCc1c[nH]cn1	10.1021/jm9000693
	11539632	70217	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibitory concentration against histamine H2 receptorInhibitory concentration against histamine H2 receptor	ChEMBL	447	8	1	5	4.8	Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12	10.1021/jm050103y
	CHEMBL194837	70217	0	None	-	0	Human	9.1	pIC50	=	9.1	Binding	Inhibitory concentration against histamine H2 receptorInhibitory concentration against histamine H2 receptor	ChEMBL	447	8	1	5	4.8	Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12	10.1021/jm050103y
	132609385	157550	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]-aminopotentidine receptor from histamine H2 receptor (unknown origin)Displacement of [125I]-aminopotentidine receptor from histamine H2 receptor (unknown origin)	ChEMBL	324	5	0	3	3.8	COc1ccc(CN2CCCN(Cc3ccccc3)[C@@H](C)C2)cc1	10.1016/j.bmc.2017.07.027
	CHEMBL4086541	157550	0	None	-	0	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]-aminopotentidine receptor from histamine H2 receptor (unknown origin)Displacement of [125I]-aminopotentidine receptor from histamine H2 receptor (unknown origin)	ChEMBL	324	5	0	3	3.8	COc1ccc(CN2CCCN(Cc3ccccc3)[C@@H](C)C2)cc1	10.1016/j.bmc.2017.07.027
	1231	924	112	None	-2	7	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.11.014
	2756	924	112	None	-2	7	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.11.014
	645	924	112	None	-2	7	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.11.014
	CHEMBL30	924	112	None	-2	7	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.11.014
	DB00501	924	112	None	-2	7	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting methodDisplacement of [125I]APT from human recombinant H2 receptor expressed in CHO cells measured after 120 mins by scintillation counting method	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.11.014
	1231	924	112	None	-2	7	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.03.006
	2756	924	112	None	-2	7	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.03.006
	645	924	112	None	-2	7	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.03.006
	CHEMBL30	924	112	None	-2	7	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.03.006
	DB00501	924	112	None	-2	7	Human	6.0	pIC50	=	6	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cellsDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2016.03.006
	17747460	61000	8	None	-	4	Human	5.0	pIC50	=	5	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	ChEMBL	640	14	0	6	7.8	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
	CHEMBL1767164	61000	8	None	-	4	Human	5.0	pIC50	=	5	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	ChEMBL	640	14	0	6	7.8	O=c1c2ccccc2c(Cc2ccc(Cl)cc2)nn1C[C@H]1CCCN1CCCCc1ccc(OCCCN2CCCCCC2)cc1	10.1021/jm1013874
	10205121	66359	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	464	6	1	4	6.5	O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4ccccc34)CC2)c1	10.1021/jm0498203
	CHEMBL185489	66359	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	464	6	1	4	6.5	O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4ccccc34)CC2)c1	10.1021/jm0498203
	10138404	136359	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	444	8	1	5	5.2	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccco3)c3ccccc23)CC1	10.1021/jm0498203
	CHEMBL374218	136359	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	444	8	1	5	5.2	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccco3)c3ccccc23)CC1	10.1021/jm0498203
	9932752	141451	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	8	1	4	5.1	O=C(O)c1ccccc1OCCN1CCC(c2cn(CC3CC3)c3cc(F)ccc23)CC1	10.1021/jm0498203
	CHEMBL387391	141451	0	None	-	0	Human	5.0	pIC50	=	5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	8	1	4	5.1	O=C(O)c1ccccc1OCCN1CCC(c2cn(CC3CC3)c3cc(F)ccc23)CC1	10.1021/jm0498203
	44326821	206174	0	None	-	0	Rat	4.0	pIC50	=	4	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	559	12	5	6	2.2	CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)C	10.1021/jm00381a002
	CHEMBL96738	206174	0	None	-	0	Rat	4.0	pIC50	=	4	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	559	12	5	6	2.2	CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N(C)C	10.1021/jm00381a002
	CHEMBL95063	214140	0	None	-	0	Rat	4.0	pIC50	=	4	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
	135	2496	38	None	-39	57	Human	6.0	pIC50	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
	1796	2496	38	None	-39	57	Human	6.0	pIC50	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
	4184	2496	38	None	-39	57	Human	6.0	pIC50	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
	CHEMBL6437	2496	38	None	-39	57	Human	6.0	pIC50	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
	DB06148	2496	38	None	-39	57	Human	6.0	pIC50	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
	11785584	136441	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	512	8	1	5	6.5	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3cc(F)ccc23)CC1	10.1021/jm0498203
	CHEMBL374459	136441	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	512	8	1	5	6.5	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3cc(F)ccc23)CC1	10.1021/jm0498203
	10885636	110527	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	503	9	0	4	5.7	N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1	10.1021/jm010878g
	CHEMBL326263	110527	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	503	9	0	4	5.7	N#Cc1ccc(CCOC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1	10.1021/jm010878g
	1588	2294	24	None	-323	43	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
	28864	2294	24	None	-323	43	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
	43	2294	24	None	-323	43	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
	CHEMBL157138	2294	24	None	-323	43	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
	DB00589	2294	24	None	-323	43	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
	176	394	63	None	-6	31	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	2157	394	63	None	-6	31	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	2566	394	63	None	-6	31	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	CHEMBL633	394	63	None	-6	31	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	DB01118	394	63	None	-6	31	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	657255	197406	29	None	-3	15	Human	7.0	pIC50	=	7.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	12	2	3	5.6	CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1	nan
	CHEMBL588119	197406	29	None	-3	15	Human	7.0	pIC50	=	7.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	12	2	3	5.6	CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1	nan
	124087	1362	106	None	-29	15	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
	7157	1362	106	None	-29	15	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
	814	1362	106	None	-29	15	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
	CHEMBL1172	1362	106	None	-29	15	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
	DB00967	1362	106	None	-29	15	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
	11057	175575	19	None	-2	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	nan
	3468	175575	19	None	-2	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	nan
	CHEMBL459265	175575	19	None	-2	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	nan
	CHEMBL64894	175575	19	None	-2	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	nan
	2286	3134	48	None	-26	29	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
	4927	3134	48	None	-26	29	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
	7282	3134	48	None	-26	29	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
	CHEMBL643	3134	48	None	-26	29	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
	DB01069	3134	48	None	-26	29	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
	1353	1880	85	None	-131	85	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
	3559	1880	85	None	-131	85	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
	86	1880	85	None	-131	85	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
	CHEMBL54	1880	85	None	-131	85	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
	DB00502	1880	85	None	-131	85	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
	11362693	141080	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	440	9	1	5	4.4	COCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21	10.1021/jm0498203
	CHEMBL385133	141080	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	440	9	1	5	4.4	COCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21	10.1021/jm0498203
	1201549	590	22	None	-74	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
	333	590	22	None	-74	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
	7601	590	22	None	-74	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
	CHEMBL1201203	590	22	None	-74	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
	CHEMBL438151	590	22	None	-74	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
	DB00245	590	22	None	-74	20	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
	1212	1632	45	None	-323	65	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
	204	1632	45	None	-323	65	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
	3372	1632	45	None	-323	65	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
	CHEMBL726	1632	45	None	-323	65	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
	DB00623	1632	45	None	-323	65	Human	5.9	pIC50	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
	9889247	84337	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.6	CCOCCn1cc(C2CCN(CCOc3cccc(C(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
	CHEMBL223024	84337	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.6	CCOCCn1cc(C2CCN(CCOc3cccc(C(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
	11071079	110104	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	496	9	0	3	6.0	O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1021/jm010878g
	CHEMBL325516	110104	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	496	9	0	3	6.0	O=C(OCCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1021/jm010878g
	10202996	84219	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	430	6	1	4	5.8	O=C(O)c1cccc(CN2CCC(c3cn(Cc4cccs4)c4ccccc34)CC2)c1	10.1021/jm0498203
	CHEMBL222372	84219	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	430	6	1	4	5.8	O=C(O)c1cccc(CN2CCC(c3cn(Cc4cccs4)c4ccccc34)CC2)c1	10.1021/jm0498203
	11113605	10407	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	480	9	0	2	5.8	O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1021/jm010878g
	CHEMBL116735	10407	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	480	9	0	2	5.8	O=C(CCc1ccc(F)cc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1021/jm010878g
	11329753	84140	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	514	10	1	5	5.4	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cccc(Br)c21	10.1021/jm0498203
	CHEMBL222083	84140	0	None	-	0	Human	5.9	pIC50	=	5.9	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	514	10	1	5	5.4	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cccc(Br)c21	10.1021/jm0498203
	1231	924	112	None	-2	7	Human	6.9	pIC50	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
	2756	924	112	None	-2	7	Human	6.9	pIC50	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
	645	924	112	None	-2	7	Human	6.9	pIC50	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
	CHEMBL30	924	112	None	-2	7	Human	6.9	pIC50	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
	DB00501	924	112	None	-2	7	Human	6.9	pIC50	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
	104903	56050	14	None	-5	6	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	624	6	0	8	5.5	C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1	nan
	CHEMBL1630578	56050	14	None	-5	6	Human	4.9	pIC50	=	4.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	624	6	0	8	5.5	C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1	nan
	72548703	161019	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor after 120 mins by scintillation counting analysisDisplacement of [125I]APT from human recombinant histamine H2 receptor after 120 mins by scintillation counting analysis	ChEMBL	583	8	3	6	5.8	CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12	10.1016/j.bmcl.2018.03.093
	CHEMBL4128926	161019	0	None	-	0	Human	6.9	pIC50	=	6.9	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor after 120 mins by scintillation counting analysisDisplacement of [125I]APT from human recombinant histamine H2 receptor after 120 mins by scintillation counting analysis	ChEMBL	583	8	3	6	5.8	CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12	10.1016/j.bmcl.2018.03.093
	2389	3279	114	None	-275	67	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
	5073	3279	114	None	-275	67	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
	96	3279	114	None	-275	67	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
	CHEMBL85	3279	114	None	-275	67	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
	DB00734	3279	114	None	-275	67	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
	10139591	84217	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	462	7	1	5	5.5	COc1ccc(CN2CCC(c3cn(Cc4ccoc4)c4cc(F)ccc34)CC2)cc1C(=O)O	10.1021/jm0498203
	CHEMBL222356	84217	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	462	7	1	5	5.5	COc1ccc(CN2CCC(c3cn(Cc4ccoc4)c4cc(F)ccc34)CC2)cc1C(=O)O	10.1021/jm0498203
	11329754	141450	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	514	10	1	5	5.4	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(Br)ccc21	10.1021/jm0498203
	CHEMBL387390	141450	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	514	10	1	5	5.4	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(Br)ccc21	10.1021/jm0498203
	CHEMBL96946	214145	0	None	-	0	Rat	4.8	pIC50	=	4.8	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
	57469	18678	120	None	-1	3	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	240	2	1	4	2.8	CC(C)Cn1cnc2c(N)nc3ccccc3c21	nan
	CHEMBL1282	18678	120	None	-1	3	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	240	2	1	4	2.8	CC(C)Cn1cnc2c(N)nc3ccccc3c21	nan
	3198	203802	73	None	-19	34	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	380	6	0	3	5.8	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1	nan
	CHEMBL1201049	203802	73	None	-19	34	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	380	6	0	3	5.8	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1	nan
	CHEMBL808	203802	73	None	-19	34	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	380	6	0	3	5.8	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1	nan
	3042	1386	31	None	-53	15	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
	355	1386	31	None	-53	15	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
	868	1386	31	None	-53	15	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
	CHEMBL1123	1386	31	None	-53	15	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
	DB00804	1386	31	None	-53	15	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
	2247	502	77	None	-56	41	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
	249	502	77	None	-56	41	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
	2603	502	77	None	-56	41	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
	CHEMBL296419	502	77	None	-56	41	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
	DB00637	502	77	None	-56	41	Human	5.8	pIC50	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
	9822631	122444	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	406	8	1	4	4.8	CCOCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
	CHEMBL360791	122444	0	None	-	0	Human	5.8	pIC50	=	5.8	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	406	8	1	4	4.8	CCOCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
	1231	924	112	None	-2	7	Human	6.8	pIC50	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
	2756	924	112	None	-2	7	Human	6.8	pIC50	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
	645	924	112	None	-2	7	Human	6.8	pIC50	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
	CHEMBL30	924	112	None	-2	7	Human	6.8	pIC50	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
	DB00501	924	112	None	-2	7	Human	6.8	pIC50	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
	10141470	123040	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	494	8	1	5	6.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3ccccc23)CC1	10.1021/jm0498203
	CHEMBL361805	123040	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	494	8	1	5	6.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccc(Cl)s3)c3ccccc23)CC1	10.1021/jm0498203
	3158	55974	21	None	-12589	20	Human	5.7	pIC50	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	279	3	0	2	4.0	CN(C)CCC=C1c2ccccc2COc2ccccc21	nan
	CHEMBL1628227	55974	21	None	-12589	20	Human	5.7	pIC50	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	279	3	0	2	4.0	CN(C)CCC=C1c2ccccc2COc2ccccc21	nan
	11476077	135884	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.5	CCOCCn1cc(C2CCN(Cc3cccc(OCC(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
	CHEMBL373534	135884	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.5	CCOCCn1cc(C2CCN(Cc3cccc(OCC(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
	5291	205704	115	None	-1	2	Human	5.7	pIC50	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	493	7	2	7	4.6	Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1	nan
	CHEMBL941	205704	115	None	-1	2	Human	5.7	pIC50	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	493	7	2	7	4.6	Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1	nan
	277	1274	55	None	-43	45	Human	6.7	pIC50	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
	2913	1274	55	None	-43	45	Human	6.7	pIC50	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
	765	1274	55	None	-43	45	Human	6.7	pIC50	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
	CHEMBL516	1274	55	None	-43	45	Human	6.7	pIC50	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
	DB00434	1274	55	None	-43	45	Human	6.7	pIC50	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
	11730467	10925	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	476	10	0	2	6.0	O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1021/jm010878g
	CHEMBL117537	10925	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	476	10	0	2	6.0	O=C(CCCc1ccccc1)N1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1021/jm010878g
	CHEMBL328512	209551	0	None	-	0	Rat	4.7	pIC50	=	4.7	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
	CHEMBL96681	214141	0	None	-	0	Rat	4.7	pIC50	=	4.7	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CCC(=O)O)C(N)=O	10.1021/jm00381a002
	2801	161325	56	None	-12	28	Human	5.7	pIC50	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21	nan
	CHEMBL1200710	161325	56	None	-12	28	Human	5.7	pIC50	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21	nan
	CHEMBL415	161325	56	None	-12	28	Human	5.7	pIC50	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21	nan
	11430513	84208	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.5	CCOCCn1cc(C2CCN(Cc3ccccc3OCC(=O)O)CC2)c2ccccc21	10.1021/jm0498203
	CHEMBL222217	84208	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.5	CCOCCn1cc(C2CCN(Cc3ccccc3OCC(=O)O)CC2)c2ccccc21	10.1021/jm0498203
	10140544	141107	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	478	9	1	6	4.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(CCC3COCCO3)c3ccccc23)CC1	10.1021/jm0498203
	CHEMBL385311	141107	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	478	9	1	6	4.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(CCC3COCCO3)c3ccccc23)CC1	10.1021/jm0498203
	11189839	83917	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	438	9	1	4	5.5	CCCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21	10.1021/jm0498203
	CHEMBL221664	83917	0	None	-	0	Human	5.7	pIC50	=	5.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	438	9	1	4	5.5	CCCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21	10.1021/jm0498203
	3823	49951	38	None	-66	11	Human	4.7	pIC50	=	4.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	530	7	0	7	4.2	CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1	nan
	76973198	49951	38	None	-66	11	Human	4.7	pIC50	=	4.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	530	7	0	7	4.2	CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1	nan
	CHEMBL157101	49951	38	None	-66	11	Human	4.7	pIC50	=	4.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	530	7	0	7	4.2	CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1	nan
	1235	3763	32	None	-2	4	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs	ChEMBL	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	10.1016/j.bmcl.2013.01.025
	3959	3763	32	None	-2	4	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs	ChEMBL	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	10.1016/j.bmcl.2013.01.025
	50287	3763	32	None	-2	4	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs	ChEMBL	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	10.1016/j.bmcl.2013.01.025
	CHEMBL269646	3763	32	None	-2	4	Human	7.7	pIC50	=	7.7	Binding	Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs	ChEMBL	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	10.1016/j.bmcl.2013.01.025
	11166846	83885	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	450	10	1	5	4.9	CCOCCn1cc(C2CCN(CCOc3ccc(C)cc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
	CHEMBL221462	83885	0	None	-	0	Human	6.7	pIC50	=	6.7	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	450	10	1	5	4.9	CCOCCn1cc(C2CCN(CCOc3ccc(C)cc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
	4543	169982	36	None	-15	29	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2ccccc21	nan
	CHEMBL1201156	169982	36	None	-15	29	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2ccccc21	nan
	CHEMBL445	169982	36	None	-15	29	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2ccccc21	nan
	CHEMBL44345	212174	0	None	-	0	Rat	4.6	pIC50	=	4.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
	2060890	201359	26	None	-	0	Rat	3.6	pIC50	=	3.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	342	5	3	2	3.2	O=C(N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)c1ccc(Cl)cc1	10.1021/jm00381a002
	CHEMBL63544	201359	26	None	-	0	Rat	3.6	pIC50	=	3.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	342	5	3	2	3.2	O=C(N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)c1ccc(Cl)cc1	10.1021/jm00381a002
	2281	3126	76	None	-	0	Rat	2.6	pIC50	=	2.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	10.1021/jm00381a002
	4922	3126	76	None	-	0	Rat	2.6	pIC50	=	2.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	10.1021/jm00381a002
	893	3126	76	None	-	0	Rat	2.6	pIC50	=	2.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	10.1021/jm00381a002
	CHEMBL316561	3126	76	None	-	0	Rat	2.6	pIC50	=	2.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	10.1021/jm00381a002
	DB13431	3126	76	None	-	0	Rat	2.6	pIC50	=	2.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	10.1021/jm00381a002
	2520	202310	65	None	-20	11	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	nan
	CHEMBL1280	202310	65	None	-20	11	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	nan
	CHEMBL6966	202310	65	None	-20	11	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	nan
	11293983	83875	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	454	10	1	5	4.8	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21	10.1021/jm0498203
	CHEMBL221413	83875	0	None	-	0	Human	6.6	pIC50	=	6.6	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	454	10	1	5	4.8	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(F)cc21	10.1021/jm0498203
	2726	906	64	None	-85	72	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
	621	906	64	None	-85	72	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
	83	906	64	None	-85	72	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
	CHEMBL71	906	64	None	-85	72	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
	DB00477	906	64	None	-85	72	Human	5.6	pIC50	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
	118139356	179143	20	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Antagonist activity at human H2 receptorAntagonist activity at human H2 receptor	ChEMBL	435	7	2	7	3.2	Cc1cc(-c2ccnc(Nc3cnn(C)c3)n2)ccc1CNC(=O)N1CC(OC(C)C)C1	10.1021/acs.jmedchem.0c00702
	CHEMBL4744041	179143	20	None	-	0	Human	4.6	pIC50	=	4.6	Binding	Antagonist activity at human H2 receptorAntagonist activity at human H2 receptor	ChEMBL	435	7	2	7	3.2	Cc1cc(-c2ccnc(Nc3cnn(C)c3)n2)ccc1CNC(=O)N1CC(OC(C)C)C1	10.1021/acs.jmedchem.0c00702
	1231	924	112	None	-2	7	Human	6.6	pIC50	=	6.6	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2013.03.016
	2756	924	112	None	-2	7	Human	6.6	pIC50	=	6.6	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2013.03.016
	645	924	112	None	-2	7	Human	6.6	pIC50	=	6.6	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2013.03.016
	CHEMBL30	924	112	None	-2	7	Human	6.6	pIC50	=	6.6	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2013.03.016
	DB00501	924	112	None	-2	7	Human	6.6	pIC50	=	6.6	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmc.2013.03.016
	18609376	202656	61	None	-	1	Human	4.6	pIC50	=	4.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	386	2	0	4	4.7	CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C	nan
	6279	202656	61	None	-	1	Human	4.6	pIC50	=	4.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	386	2	0	4	4.7	CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C	nan
	CHEMBL717	202656	61	None	-	1	Human	4.6	pIC50	=	4.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	386	2	0	4	4.7	CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C	nan
	2284	3133	27	None	-53	28	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
	4926	3133	27	None	-53	28	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
	7281	3133	27	None	-53	28	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
	CHEMBL564	3133	27	None	-53	28	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
	DB00420	3133	27	None	-53	28	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
	11443495	83932	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	504	10	1	5	5.7	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(C(F)(F)F)cc21	10.1021/jm0498203
	CHEMBL221718	83932	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	504	10	1	5	5.7	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccc(C(F)(F)F)cc21	10.1021/jm0498203
	10298838	168229	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	469	9	1	5	5.2	O=C(O)c1ccccc1OCCN1CCC(c2cn(CCc3ccccn3)c3ccccc23)CC1	10.1021/jm0498203
	CHEMBL437519	168229	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	469	9	1	5	5.2	O=C(O)c1ccccc1OCCN1CCC(c2cn(CCc3ccccn3)c3ccccc23)CC1	10.1021/jm0498203
	3191	102385	93	None	-24	25	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	469	9	0	3	7.2	CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1	nan
	CHEMBL305660	102385	93	None	-24	25	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	469	9	0	3	7.2	CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1	nan
	10162727	84195	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	478	7	1	5	6.0	COc1ccc(CN2CCC(c3cn(Cc4cccs4)c4cc(F)ccc34)CC2)cc1C(=O)O	10.1021/jm0498203
	CHEMBL222139	84195	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	478	7	1	5	6.0	COc1ccc(CN2CCC(c3cn(Cc4cccs4)c4cc(F)ccc34)CC2)cc1C(=O)O	10.1021/jm0498203
	CHEMBL2370238	208066	0	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N1CCCC[C@H]1C(=O)O	10.1021/jm00381a002
	CHEMBL262692	208800	0	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
	CHEMBL289310	209126	0	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CSCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
	CHEMBL318221	209466	0	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)O	10.1021/jm00381a002
	CHEMBL91765	214127	0	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
	11211919	84329	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	406	8	1	4	4.8	CCOCCn1cc(C2CCN(Cc3ccccc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
	CHEMBL222984	84329	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	406	8	1	4	4.8	CCOCCn1cc(C2CCN(Cc3ccccc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
	10279311	83933	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	512	7	1	5	6.6	COc1ccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4cc(F)ccc34)CC2)cc1C(=O)O	10.1021/jm0498203
	CHEMBL221730	83933	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	512	7	1	5	6.6	COc1ccc(CN2CCC(c3cn(Cc4ccc(Cl)s4)c4cc(F)ccc34)CC2)cc1C(=O)O	10.1021/jm0498203
	1599	2309	47	None	-154	15	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
	3955	2309	47	None	-154	15	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
	7215	2309	47	None	-154	15	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
	CHEMBL841	2309	47	None	-154	15	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
	DB00836	2309	47	None	-154	15	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
	11247939	136581	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	450	10	1	5	4.9	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cccc(C)c21	10.1021/jm0498203
	CHEMBL374754	136581	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	450	10	1	5	4.9	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cccc(C)c21	10.1021/jm0498203
	10226501	137348	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	460	7	1	5	5.8	COc1ccc(CN2CCC(c3cn(Cc4cccs4)c4ccccc34)CC2)cc1C(=O)O	10.1021/jm0498203
	CHEMBL376202	137348	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	460	7	1	5	5.8	COc1ccc(CN2CCC(c3cn(Cc4cccs4)c4ccccc34)CC2)cc1C(=O)O	10.1021/jm0498203
	11282005	65735	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.6	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
	CHEMBL183706	65735	0	None	-	0	Human	5.5	pIC50	=	5.5	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.6	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
	CHEMBL330142	209580	0	None	-	0	Rat	4.5	pIC50	=	4.5	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
	237	203157	43	None	-3	13	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	nan
	CHEMBL546257	203157	43	None	-3	13	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	nan
	CHEMBL554190	203157	43	None	-3	13	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	nan
	CHEMBL7568	203157	43	None	-3	13	Human	5.5	pIC50	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	nan
	135398737	944	89	None	-64	91	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
	38	944	89	None	-64	91	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
	722	944	89	None	-64	91	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
	CHEMBL42	944	89	None	-64	91	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
	DB00363	944	89	None	-64	91	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
	11005810	10367	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	517	10	1	4	6.2	N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1	10.1021/jm010878g
	CHEMBL116463	10367	0	None	-	0	Human	6.4	pIC50	=	6.4	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	517	10	1	4	6.2	N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1	10.1021/jm010878g
	26987	936	29	None	-177	21	Human	6.4	pIC50	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
	6063	936	29	None	-177	21	Human	6.4	pIC50	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
	671	936	29	None	-177	21	Human	6.4	pIC50	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
	CHEMBL1626	936	29	None	-177	21	Human	6.4	pIC50	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
	DB00283	936	29	None	-177	21	Human	6.4	pIC50	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
	11212029	84196	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	410	7	1	4	4.5	COCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccc(F)cc21	10.1021/jm0498203
	CHEMBL222142	84196	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	410	7	1	4	4.5	COCCn1cc(C2CCN(Cc3cccc(C(=O)O)c3)CC2)c2ccc(F)cc21	10.1021/jm0498203
	11259138	84588	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.5	CCOCCn1cc(C2CCN(Cc3ccc(OCC(=O)O)cc3)CC2)c2ccccc21	10.1021/jm0498203
	CHEMBL223882	84588	0	None	-	0	Human	5.4	pIC50	=	5.4	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.5	CCOCCn1cc(C2CCN(Cc3ccc(OCC(=O)O)cc3)CC2)c2ccccc21	10.1021/jm0498203
	4011	81996	43	None	-27	23	Human	6.4	pIC50	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	4	1	1	4.2	CNCCCC12CCC(c3ccccc31)c1ccccc12	nan
	CHEMBL21731	81996	43	None	-27	23	Human	6.4	pIC50	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	4	1	1	4.2	CNCCCC12CCC(c3ccccc31)c1ccccc12	nan
	CHEMBL94917	214138	0	None	-	0	Rat	4.4	pIC50	=	4.4	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OCc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
	1530	2151	44	None	-151	20	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
	3827	2151	44	None	-151	20	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
	7206	2151	44	None	-151	20	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
	CHEMBL534	2151	44	None	-151	20	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
	DB00920	2151	44	None	-151	20	Human	5.4	pIC50	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
	1129	1591	89	None	-	1	Human	7.4	pIC50	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
	3325	1591	89	None	-	1	Human	7.4	pIC50	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
	5353622	1591	89	None	-	1	Human	7.4	pIC50	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
	5702160	1591	89	None	-	1	Human	7.4	pIC50	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
	7074	1591	89	None	-	1	Human	7.4	pIC50	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
	CHEMBL902	1591	89	None	-	1	Human	7.4	pIC50	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
	DB00927	1591	89	None	-	1	Human	7.4	pIC50	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
	10161929	136663	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	464	9	1	6	4.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(CCC3OCCO3)c3ccccc23)CC1	10.1021/jm0498203
	CHEMBL374869	136663	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	464	9	1	6	4.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(CCC3OCCO3)c3ccccc23)CC1	10.1021/jm0498203
	1231	924	112	None	-2	7	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
	2756	924	112	None	-2	7	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
	645	924	112	None	-2	7	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
	CHEMBL30	924	112	None	-2	7	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
	DB00501	924	112	None	-2	7	Human	6.3	pIC50	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
	11238716	83876	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	592	10	1	5	6.2	CCOCCn1cc(C2CCN(CCOc3c(Br)cc(Br)cc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
	CHEMBL221414	83876	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	592	10	1	5	6.2	CCOCCn1cc(C2CCN(CCOc3c(Br)cc(Br)cc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
	10204866	84312	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	460	8	1	5	5.7	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3cccs3)c3ccccc23)CC1	10.1021/jm0498203
	CHEMBL222881	84312	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	460	8	1	5	5.7	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3cccs3)c3ccccc23)CC1	10.1021/jm0498203
	11396873	136461	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	454	10	1	5	4.8	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(F)ccc21	10.1021/jm0498203
	CHEMBL374585	136461	0	None	-	0	Human	6.3	pIC50	=	6.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	454	10	1	5	4.8	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(F)ccc21	10.1021/jm0498203
	44326564	206136	0	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	531	12	6	6	1.6	CC(C)CC(NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
	CHEMBL96530	206136	0	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL	531	12	6	6	1.6	CC(C)CC(NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
	CHEMBL1790763	207162	0	None	-	0	Rat	4.3	pIC50	=	4.3	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC[C@H](C)[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
	2812	4711	96	None	-33	34	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	nan
	CHEMBL104	4711	96	None	-33	34	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	nan
	10478188	122427	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	9	1	5	4.8	CCOCCn1cc(C2CCN(Cc3ccc(OC)c(C(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
	CHEMBL360712	122427	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	9	1	5	4.8	CCOCCn1cc(C2CCN(Cc3ccc(OC)c(C(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
	1231	924	112	None	-2	7	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
	2756	924	112	None	-2	7	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
	645	924	112	None	-2	7	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
	CHEMBL30	924	112	None	-2	7	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
	DB00501	924	112	None	-2	7	Human	5.3	pIC50	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
	11363750	84207	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	484	8	1	4	5.5	CCOCCn1cc(C2CCN(Cc3cc(C(=O)O)ccc3Br)CC2)c2ccccc21	10.1021/jm0498203
	CHEMBL222214	84207	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	484	8	1	4	5.5	CCOCCn1cc(C2CCN(Cc3cc(C(=O)O)ccc3Br)CC2)c2ccccc21	10.1021/jm0498203
	11247290	136180	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	424	8	1	4	4.9	CCOCCn1cc(C2CCN(Cc3ccc(F)c(C(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
	CHEMBL374059	136180	0	None	-	0	Human	5.3	pIC50	=	5.3	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	424	8	1	4	4.9	CCOCCn1cc(C2CCN(Cc3ccc(F)c(C(=O)O)c3)CC2)c2ccccc21	10.1021/jm0498203
	10273238	84330	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	414	6	1	4	5.4	O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccco4)c4ccccc34)CC2)c1	10.1021/jm0498203
	CHEMBL222985	84330	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	414	6	1	4	5.4	O=C(O)c1cccc(CN2CCC(c3cn(Cc4ccco4)c4ccccc34)CC2)c1	10.1021/jm0498203
	11351801	83931	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	466	11	1	6	4.6	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(OC)ccc21	10.1021/jm0498203
	CHEMBL221716	83931	0	None	-	0	Human	5.2	pIC50	=	5.2	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	466	11	1	6	4.6	CCOCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2cc(OC)ccc21	10.1021/jm0498203
	4189	205195	91	None	-36	34	Human	5.2	pIC50	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
	CHEMBL1559	205195	91	None	-36	34	Human	5.2	pIC50	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
	CHEMBL91	205195	91	None	-36	34	Human	5.2	pIC50	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
	9889248	84306	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.6	CCOCCn1cc(C2CCN(CCOc3ccc(C(=O)O)cc3)CC2)c2ccccc21	10.1021/jm0498203
	CHEMBL222853	84306	0	None	-	0	Human	6.2	pIC50	=	6.2	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	436	10	1	5	4.6	CCOCCn1cc(C2CCN(CCOc3ccc(C(=O)O)cc3)CC2)c2ccccc21	10.1021/jm0498203
	4601	205020	29	None	-7	17	Human	5.2	pIC50	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	nan
	CHEMBL1201023	205020	29	None	-7	17	Human	5.2	pIC50	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	nan
	CHEMBL900	205020	29	None	-7	17	Human	5.2	pIC50	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	nan
	CHEMBL91752	214126	0	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(=O)O)C(N)=O	10.1021/jm00381a002
	CHEMBL94448	214133	0	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)O	10.1021/jm00381a002
	CHEMBL94902	214136	1	None	-	0	Rat	4.2	pIC50	=	4.2	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	ChEMBL		None	None	None		CC(C)C[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)O	10.1021/jm00381a002
	180	397	50	None	-1412	38	Human	6.1	pIC50	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
	200	397	50	None	-1412	38	Human	6.1	pIC50	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
	2160	397	50	None	-1412	38	Human	6.1	pIC50	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
	CHEMBL629	397	50	None	-1412	38	Human	6.1	pIC50	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
	DB00321	397	50	None	-1412	38	Human	6.1	pIC50	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
	10907460	9735	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	521	11	1	3	5.8	CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1	10.1021/jm010878g
	CHEMBL113956	9735	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	521	11	1	3	5.8	CCOc1ccc(CCNC(=O)N2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1	10.1021/jm010878g
	11340290	64033	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	466	11	1	6	4.6	CCOCCn1cc(C2CCN(CCOc3cc(OC)ccc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
	CHEMBL181278	64033	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	466	11	1	6	4.6	CCOCCn1cc(C2CCN(CCOc3cc(OC)ccc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
	1231	924	112	None	-2	7	Human	6.1	pIC50	=	6.1	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm701575k
	2756	924	112	None	-2	7	Human	6.1	pIC50	=	6.1	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm701575k
	645	924	112	None	-2	7	Human	6.1	pIC50	=	6.1	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm701575k
	CHEMBL30	924	112	None	-2	7	Human	6.1	pIC50	=	6.1	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm701575k
	DB00501	924	112	None	-2	7	Human	6.1	pIC50	=	6.1	Binding	Inhibition of histamine H2 receptorInhibition of histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm701575k
	1210	905	45	None	-281	20	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	1213	905	45	None	-281	20	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	2725	905	45	None	-281	20	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	33036	905	45	None	-281	20	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	4411	905	45	None	-281	20	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	616	905	45	None	-281	20	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	6976	905	45	None	-281	20	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	716121	905	45	None	-281	20	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	90475904	905	45	None	-281	20	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	CHEMBL1201353	905	45	None	-281	20	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	CHEMBL1554789	905	45	None	-281	20	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	CHEMBL505	905	45	None	-281	20	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	DB01114	905	45	None	-281	20	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	DB13679	905	45	None	-281	20	Human	5.1	pIC50	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	11328514	137333	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	454	10	1	5	4.8	CCOCCn1cc(C2CCN(CCOc3cccc(F)c3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
	CHEMBL376025	137333	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	454	10	1	5	4.8	CCOCCn1cc(C2CCN(CCOc3cccc(F)c3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
	9804849	67117	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibitory concentration against Histamine H2 receptorInhibitory concentration against Histamine H2 receptor	ChEMBL	472	8	1	5	5.1	Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12	10.1021/jm050103y
	CHEMBL189118	67117	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Inhibitory concentration against Histamine H2 receptorInhibitory concentration against Histamine H2 receptor	ChEMBL	472	8	1	5	5.1	Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12	10.1021/jm050103y
	10139592	84580	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	462	8	1	5	5.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccco3)c3cc(F)ccc23)CC1	10.1021/jm0498203
	CHEMBL223837	84580	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	462	8	1	5	5.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccco3)c3cc(F)ccc23)CC1	10.1021/jm0498203
	11385692	136525	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	462	8	1	5	5.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccoc3)c3cc(F)ccc23)CC1	10.1021/jm0498203
	CHEMBL374675	136525	0	None	-	0	Human	6.1	pIC50	=	6.1	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	462	8	1	5	5.4	O=C(O)c1ccccc1OCCN1CCC(c2cn(Cc3ccoc3)c3cc(F)ccc23)CC1	10.1021/jm0498203
	9802248	165690	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	420	9	1	4	5.4	CCCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
	CHEMBL426786	165690	0	None	-	0	Human	5.0	pIC50	=	5.0	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	420	9	1	4	5.4	CCCCn1cc(C2CCN(CCOc3ccccc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
	1016	3690	75	None	-41	35	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
	2561	3690	75	None	-41	35	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
	2733526	3690	75	None	-41	35	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
	5384	3690	75	None	-41	35	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
	CHEMBL83	3690	75	None	-41	35	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
	DB00675	3690	75	None	-41	35	Human	5.0	pIC50	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
	100	3745	52	None	-46	55	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
	2637	3745	52	None	-46	55	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
	5452	3745	52	None	-46	55	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
	CHEMBL479	3745	52	None	-46	55	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
	DB00679	3745	52	None	-46	55	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
	11202401	136583	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	478	11	1	6	4.8	CCOCCn1cc(C2CCN(CCOc3ccc(C(C)=O)cc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
	CHEMBL374755	136583	0	None	-	0	Human	6.0	pIC50	=	6.0	Binding	Displacement of [3H]ketanserin from histamine H2 receptor in human cortex membranesDisplacement of [3H]ketanserin from histamine H2 receptor in human cortex membranes	ChEMBL	478	11	1	6	4.8	CCOCCn1cc(C2CCN(CCOc3ccc(C(C)=O)cc3C(=O)O)CC2)c2ccccc21	10.1021/jm0498203
	133	2460	48	None	-141	42	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	nan
	1723	2460	48	None	-141	42	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	nan
	28693	2460	48	None	-141	42	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	nan
	CHEMBL19215	2460	48	None	-141	42	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	nan
	DB13520	2460	48	None	-141	42	Human	6.0	pIC50	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	nan
	CHEMBL5087637	213779	0	None	-	1	Human	6.0	pKd	=	6	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095891	213779	0	None	-	1	Human	6.0	pKd	=	6	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5093461	213777	0	None	-	1	Human	7.0	pKd	=	7.0	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095884	213777	0	None	-	1	Human	7.0	pKd	=	7.0	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	126688	400	28	None	-2	3	Rat	4.9	pKd	=	4.9	Binding	Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligandAffinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1016/S0960-894X(01)80533-3
	4025	400	28	None	-2	3	Rat	4.9	pKd	=	4.9	Binding	Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligandAffinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1016/S0960-894X(01)80533-3
	CHEMBL293762	400	28	None	-2	3	Rat	4.9	pKd	=	4.9	Binding	Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligandAffinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1016/S0960-894X(01)80533-3
	1204	1901	114	None	-173	23	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	1247	1901	114	None	-173	23	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	1375	1901	114	None	-173	23	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	774	1901	114	None	-173	23	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	CHEMBL90	1901	114	None	-173	23	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	DB05381	1901	114	None	-173	23	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	119570	3110	90	None	-281	40	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	2233	3110	90	None	-281	40	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	953	3110	90	None	-281	40	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	CHEMBL301265	3110	90	None	-281	40	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	DB00413	3110	90	None	-281	40	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	168268716	192160	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	3	4	4	3.5	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5170276	192160	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	3	4	4	3.5	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221176	192160	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	3	4	4	3.5	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
	168268680	192164	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5172675	192164	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221210	192164	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
	168268827	192177	0	None	3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5179906	192177	0	None	3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221314	192177	0	None	3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
	168268853	192183	0	None	-2	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5180504	192183	0	None	-2	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221353	192183	0	None	-2	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	168273471	192199	0	None	12	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	596	17	8	10	0.7	N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5173079	192199	0	None	12	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	596	17	8	10	0.7	N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221433	192199	0	None	12	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	596	17	8	10	0.7	N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	168273549	192201	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5174342	192201	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221438	192201	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
	168273640	192203	0	None	-6	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5176229	192203	0	None	-6	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221444	192203	0	None	-6	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	168273745	192206	0	None	-13	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5178472	192206	0	None	-13	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221451	192206	0	None	-13	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	168274129	192207	0	None	-6	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	370	12	5	6	1.0	NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5176780	192207	0	None	-6	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	370	12	5	6	1.0	NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221468	192207	0	None	-6	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	370	12	5	6	1.0	NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	168275750	192224	0	None	-87	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	3	4	1.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5175558	192224	0	None	-87	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	3	4	1.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221581	192224	0	None	-87	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	3	4	1.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1	10.1021/acs.jmedchem.1c00692
	168276867	192233	0	None	-1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5174278	192233	0	None	-1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221653	192233	0	None	-1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1	10.1021/acs.jmedchem.1c00692
	168277996	192244	0	None	-20	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5173373	192244	0	None	-20	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221736	192244	0	None	-20	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
	168278471	192246	0	None	-18	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5183205	192246	0	None	-18	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221757	192246	0	None	-18	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	168278543	192249	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	358	4	4	4	1.6	N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
	CHEMBL5184846	192249	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	358	4	4	4	1.6	N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221764	192249	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	358	4	4	4	1.6	N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
	168280339	192263	0	None	-52	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	8	3	5	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5188592	192263	0	None	-52	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	8	3	5	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221885	192263	0	None	-52	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	8	3	5	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	168281536	192279	0	None	-9	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	369	12	4	5	1.7	Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5189006	192279	0	None	-9	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	369	12	4	5	1.7	Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221966	192279	0	None	-9	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	369	12	4	5	1.7	Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1	10.1021/acs.jmedchem.1c00692
	168281746	192280	0	None	-676	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5184911	192280	0	None	-676	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221974	192280	0	None	-676	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
	168283097	192291	0	None	-22	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	311	9	4	5	0.8	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1	10.1021/acs.jmedchem.1c00692
	CHEMBL5186770	192291	0	None	-22	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	311	9	4	5	0.8	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222043	192291	0	None	-22	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	311	9	4	5	0.8	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1	10.1021/acs.jmedchem.1c00692
	168283321	192293	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	364	7	4	4	2.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5183015	192293	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	364	7	4	4	2.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222057	192293	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	364	7	4	4	2.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	168283536	192298	0	None	-53	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	3	4	1.6	CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5187758	192298	0	None	-53	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	3	4	1.6	CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222074	192298	0	None	-53	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	3	4	1.6	CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1	10.1021/acs.jmedchem.1c00692
	168284289	192304	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	428	8	4	4	3.1	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
	CHEMBL5194860	192304	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	428	8	4	4	3.1	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222123	192304	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	428	8	4	4	3.1	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
	168284480	192308	0	None	-22	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	330	6	4	4	1.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5197548	192308	0	None	-22	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	330	6	4	4	1.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222137	192308	0	None	-22	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	330	6	4	4	1.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1021/acs.jmedchem.1c00692
	168286141	192322	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5192993	192322	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222231	192322	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
	168286426	192324	0	None	-5	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5198795	192324	0	None	-5	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222241	192324	0	None	-5	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	168290235	192366	0	None	-1737	20	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5201074	192366	0	None	-1737	20	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222491	192366	0	None	-1737	20	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	168290815	192371	0	None	-537	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5200771	192371	0	None	-537	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222529	192371	0	None	-537	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	168291233	192377	0	None	-5	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	373	8	4	5	1.4	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5200106	192377	0	None	-5	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	373	8	4	5	1.4	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222556	192377	0	None	-5	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	373	8	4	5	1.4	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1	10.1021/acs.jmedchem.1c00692
	168292954	192395	0	None	-11	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5202592	192395	0	None	-11	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222660	192395	0	None	-11	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	168294161	192404	0	None	3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5204739	192404	0	None	3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222742	192404	0	None	3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1	10.1021/acs.jmedchem.1c00692
	168294445	192408	0	None	-1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	6	4	4	2.6	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5208113	192408	0	None	-1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	6	4	4	2.6	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222768	192408	0	None	-1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	6	4	4	2.6	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1	10.1021/acs.jmedchem.1c00692
	168294166	192412	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5209081	192412	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222775	192412	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1	10.1021/acs.jmedchem.1c00692
	168294449	192416	0	None	-6	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5204599	192416	0	None	-6	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222793	192416	0	None	-6	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	168294767	192417	0	None	-117	20	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5207281	192417	0	None	-117	20	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222802	192417	0	None	-117	20	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	168294770	192418	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5208327	192418	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222806	192418	0	None	2	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1	10.1021/acs.jmedchem.1c00692
	168294776	192424	0	None	-7	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	366	7	3	4	2.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5209479	192424	0	None	-7	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	366	7	3	4	2.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222831	192424	0	None	-7	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	366	7	3	4	2.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1	10.1021/acs.jmedchem.1c00692
	168295528	192429	0	None	-147	20	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5206565	192429	0	None	-147	20	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222872	192429	0	None	-147	20	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	168294178	192433	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	5	4	4	4.4	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5205197	192433	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	5	4	4	4.4	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222887	192433	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	5	4	4	4.4	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
	168295541	192438	0	None	-851	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5208845	192438	0	None	-851	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222926	192438	0	None	-851	6	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	168295543	192439	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5209021	192439	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222929	192439	0	None	1	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
	168295803	192443	0	None	3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	338	6	4	4	1.6	CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
	CHEMBL5207206	192443	0	None	3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	338	6	4	4	1.6	CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222937	192443	0	None	3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	338	6	4	4	1.6	CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
	168294182	192446	0	None	-3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	314	6	4	2	1.7	C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5208722	192446	0	None	-3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	314	6	4	2	1.7	C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222960	192446	0	None	-3	4	Human	7.9	pKd	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	314	6	4	2	1.7	C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	156021166	177762	0	None	-	1	Human	7.9	pKd	=	7.9	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	908	25	3	8	10.3	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4647775	177762	0	None	-	1	Human	7.9	pKd	=	7.9	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	908	25	3	8	10.3	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4651205	177762	0	None	-	1	Human	7.9	pKd	=	7.9	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	908	25	3	8	10.3	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
	156015793	177684	0	None	-	1	Human	6.9	pKd	=	6.9	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	880	23	3	8	9.5	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4645867	177684	0	None	-	1	Human	6.9	pKd	=	6.9	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	880	23	3	8	9.5	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4650701	177684	0	None	-	1	Human	6.9	pKd	=	6.9	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	880	23	3	8	9.5	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
	156011186	177668	0	None	-	1	Human	7.8	pKd	=	7.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	704	20	2	7	7.5	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4637893	177668	0	None	-	1	Human	7.8	pKd	=	7.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	704	20	2	7	7.5	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4650588	177668	0	None	-	1	Human	7.8	pKd	=	7.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	704	20	2	7	7.5	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	156021166	177762	0	None	-	1	Human	7.8	pKd	=	7.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	908	25	3	8	10.3	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4647775	177762	0	None	-	1	Human	7.8	pKd	=	7.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	908	25	3	8	10.3	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4651205	177762	0	None	-	1	Human	7.8	pKd	=	7.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	908	25	3	8	10.3	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
	156015041	177658	0	None	-	1	Human	7.8	pKd	=	7.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	1029	30	3	11	10.0	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4637356	177658	0	None	-	1	Human	7.8	pKd	=	7.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	1029	30	3	11	10.0	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4650547	177658	0	None	-	1	Human	7.8	pKd	=	7.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	1029	30	3	11	10.0	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	156015643	177720	0	None	-	1	Human	6.8	pKd	=	6.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	1001	28	3	11	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4645213	177720	0	None	-	1	Human	6.8	pKd	=	6.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	1001	28	3	11	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4650968	177720	0	None	-	1	Human	6.8	pKd	=	6.8	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	1001	28	3	11	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	156015722	177698	0	None	-	1	Human	7.7	pKd	=	7.7	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4644467	177698	0	None	-	1	Human	7.7	pKd	=	7.7	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4650837	177698	0	None	-	1	Human	7.7	pKd	=	7.7	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL5088914	213786	0	None	-	1	Human	6.6	pKd	=	6.6	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095949	213786	0	None	-	1	Human	6.6	pKd	=	6.6	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	44403829	71108	0	None	-	1	Human	6.6	pKd	=	6.6	Binding	Negative logarithm of the drug concentration against H2 histamine receptorNegative logarithm of the drug concentration against H2 histamine receptor	ChEMBL	743	15	4	7	5.3	CN1C(=O)[C@H](NC(=O)Nc2ccc(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)cc2)N=C(c2ccccc2)c2ccccc21	10.1021/jm058225d
	CHEMBL196143	71108	0	None	-	1	Human	6.6	pKd	=	6.6	Binding	Negative logarithm of the drug concentration against H2 histamine receptorNegative logarithm of the drug concentration against H2 histamine receptor	ChEMBL	743	15	4	7	5.3	CN1C(=O)[C@H](NC(=O)Nc2ccc(CC(=O)NCCC(=O)NCCCOc3cccc(CN4CCCCC4)c3)cc2)N=C(c2ccccc2)c2ccccc21	10.1021/jm058225d
	5105	176253	49	None	-	1	Human	6.6	pKd	=	6.6	Binding	Negative logarithm of the drug concentration against H2 histamine receptorNegative logarithm of the drug concentration against H2 histamine receptor	ChEMBL	348	9	1	5	2.1	CC(=O)OCC(=O)NCCCOc1cccc(CN2CCCCC2)c1	10.1021/jm058225d
	CHEMBL46102	176253	49	None	-	1	Human	6.6	pKd	=	6.6	Binding	Negative logarithm of the drug concentration against H2 histamine receptorNegative logarithm of the drug concentration against H2 histamine receptor	ChEMBL	348	9	1	5	2.1	CC(=O)OCC(=O)NCCCOc1cccc(CN2CCCCC2)c1	10.1021/jm058225d
	156015152	177731	0	None	-	1	Human	7.6	pKd	=	7.6	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4641916	177731	0	None	-	1	Human	7.6	pKd	=	7.6	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4651017	177731	0	None	-	1	Human	7.6	pKd	=	7.6	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	156015793	177684	0	None	-	1	Human	6.5	pKd	=	6.5	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	880	23	3	8	9.5	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4645867	177684	0	None	-	1	Human	6.5	pKd	=	6.5	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	880	23	3	8	9.5	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4650701	177684	0	None	-	1	Human	6.5	pKd	=	6.5	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	880	23	3	8	9.5	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
	156015633	177680	0	None	-	1	Human	7.5	pKd	=	7.5	Binding	Binding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter methodBinding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter method	ChEMBL	498	17	3	7	3.6	CCC(=O)NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	156020426	177680	0	None	-	1	Human	7.5	pKd	=	7.5	Binding	Binding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter methodBinding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter method	ChEMBL	498	17	3	7	3.6	CCC(=O)NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4648685	177680	0	None	-	1	Human	7.5	pKd	=	7.5	Binding	Binding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter methodBinding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter method	ChEMBL	498	17	3	7	3.6	CCC(=O)NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4650687	177680	0	None	-	1	Human	7.5	pKd	=	7.5	Binding	Binding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter methodBinding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter method	ChEMBL	498	17	3	7	3.6	CCC(=O)NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL5094663	213730	0	None	-	1	Human	7.5	pKd	=	7.5	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](C)c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	156014823	177752	0	None	-	1	Human	6.4	pKd	=	6.4	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	1109	31	4	13	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4641747	177752	0	None	-	1	Human	6.4	pKd	=	6.4	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	1109	31	4	13	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4651132	177752	0	None	-	1	Human	6.4	pKd	=	6.4	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	1109	31	4	13	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	156015041	177658	0	None	-	1	Human	7.3	pKd	=	7.3	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	1029	30	3	11	10.0	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4637356	177658	0	None	-	1	Human	7.3	pKd	=	7.3	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	1029	30	3	11	10.0	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4650547	177658	0	None	-	1	Human	7.3	pKd	=	7.3	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	1029	30	3	11	10.0	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL5075713	213753	0	None	-	1	Human	7.3	pKd	=	7.3	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095559	213753	0	None	-	1	Human	7.3	pKd	=	7.3	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	156015643	177720	0	None	-	1	Human	6.3	pKd	=	6.3	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	1001	28	3	11	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4645213	177720	0	None	-	1	Human	6.3	pKd	=	6.3	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	1001	28	3	11	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4650968	177720	0	None	-	1	Human	6.3	pKd	=	6.3	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometryBinding affinity to human H2R expressed in human HEK293T cells incubated for 90 mins by flowcytometry	ChEMBL	1001	28	3	11	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	5039	62853	13	None	-	1	Human	7.2	pKd	=	7.2	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	314	10	2	7	1.5	CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1	10.1007/s00044-004-0012-z
	CHEMBL1790041	62853	13	None	-	1	Human	7.2	pKd	=	7.2	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	314	10	2	7	1.5	CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1	10.1007/s00044-004-0012-z
	156015722	177698	0	None	-	1	Human	7.2	pKd	=	7.2	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysis	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4644467	177698	0	None	-	1	Human	7.2	pKd	=	7.2	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysis	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4650837	177698	0	None	-	1	Human	7.2	pKd	=	7.2	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysis	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL5083588	213758	0	None	-	1	Human	7.2	pKd	=	7.2	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095633	213758	0	None	-	1	Human	7.2	pKd	=	7.2	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	156015152	177731	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4641916	177731	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4651017	177731	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	3032915	15321	20	None	-25	6	Human	5.1	pKd	=	5.1	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	10.1007/s00044-004-0012-z
	CHEMBL12160	15321	20	None	-25	6	Human	5.1	pKd	=	5.1	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	10.1007/s00044-004-0012-z
	CHEMBL5078202	213760	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1	10.1016/j.bmcl.2021.128388
	CHEMBL5095695	213760	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysisBinding affinity to human H2R expressed in HEK293T-qs5-HA cells by flow cytometry analysis	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1	10.1016/j.bmcl.2021.128388
	156015152	177731	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysis	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4641916	177731	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysis	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4651017	177731	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by imaging flow cytometry analysis	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	156015722	177698	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4644467	177698	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4650837	177698	0	None	-	1	Human	7.1	pKd	=	7.1	Binding	Binding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysisBinding affinity to human H2R expressed in human HEK293T cells incubated for 60 mins by automated cell imaging analysis	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	9990475	56183	0	None	-3	3	Rat	5.0	pKd	=	5.0	Binding	Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligandAffinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand	ChEMBL	205	2	2	3	-0.5	Cc1nc(N)[se]c1CCN	10.1016/S0960-894X(01)80533-3
	CHEMBL1632408	56183	0	None	-3	3	Rat	5.0	pKd	=	5.0	Binding	Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligandAffinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand	ChEMBL	205	2	2	3	-0.5	Cc1nc(N)[se]c1CCN	10.1016/S0960-894X(01)80533-3
	CHEMBL2448450	56183	0	None	-3	3	Rat	5.0	pKd	=	5.0	Binding	Affinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligandAffinity to the Histamine H2 receptor was determined expressed in CHO cell using [125I]iodoaminopotentidine as radioligand	ChEMBL	205	2	2	3	-0.5	Cc1nc(N)[se]c1CCN	10.1016/S0960-894X(01)80533-3
	9805944	55934	31	None	-2	9	Human	8.8	pKi	=	8.8	Binding	Displacement of [3H]tiotidine from human histamine H2 receptorDisplacement of [3H]tiotidine from human histamine H2 receptor	ChEMBL	462	7	2	3	4.7	CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1	10.1021/jm800510m
	CHEMBL1627	55934	31	None	-2	9	Human	8.8	pKi	=	8.8	Binding	Displacement of [3H]tiotidine from human histamine H2 receptorDisplacement of [3H]tiotidine from human histamine H2 receptor	ChEMBL	462	7	2	3	4.7	CNC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1	10.1021/jm800510m
	164622259	185148	0	None	2290	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	336	6	4	5	1.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccco1	10.1016/j.ejmech.2021.113190
	CHEMBL4865965	185148	0	None	2290	4	Human	8.0	pKi	=	8.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	336	6	4	5	1.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccco1	10.1016/j.ejmech.2021.113190
	164610648	184255	0	None	87	4	Human	7.0	pKi	=	7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	374	7	4	4	2.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4852212	184255	0	None	87	4	Human	7.0	pKi	=	7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	374	7	4	4	2.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	44334025	4479	0	None	-269	3	Human	6.0	pKi	=	6	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	462	10	1	5	3.8	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3Cl)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
	CHEMBL102384	4479	0	None	-269	3	Human	6.0	pKi	=	6	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	462	10	1	5	3.8	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3Cl)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
	44334781	5334	0	None	-346	3	Human	6.0	pKi	=	6	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	458	11	1	6	3.1	COc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
	CHEMBL107162	5334	0	None	-346	3	Human	6.0	pKi	=	6	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	458	11	1	6	3.1	COc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
	33630	178379	94	None	-13	27	Human	6.0	pKi	=	6	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	523	7	1	2	7.5	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
	CHEMBL47050	178379	94	None	-13	27	Human	6.0	pKi	=	6	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	523	7	1	2	7.5	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
	4023	196	19	None	-3467	4	Human	5.0	pKi	=	5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	349	7	0	4	3.6	N#Cc1ccc(cc1)c1ccc(cc1)OCCCN1CC[C@H](C1)N(C)C	10.1016/s0960-894x(02)00648-0
	9884746	196	19	None	-3467	4	Human	5.0	pKi	=	5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	349	7	0	4	3.6	N#Cc1ccc(cc1)c1ccc(cc1)OCCCN1CC[C@H](C1)N(C)C	10.1016/s0960-894x(02)00648-0
	CHEMBL319000	196	19	None	-3467	4	Human	5.0	pKi	=	5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	349	7	0	4	3.6	N#Cc1ccc(cc1)c1ccc(cc1)OCCCN1CC[C@H](C1)N(C)C	10.1016/s0960-894x(02)00648-0
	44335456	4485	0	None	-316	4	Human	5.0	pKi	=	5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	336	6	1	4	3.5	N#Cc1ccc(-c2ccc(OCCCN3CCC(O)CC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	CHEMBL102416	4485	0	None	-316	4	Human	5.0	pKi	=	5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	336	6	1	4	3.5	N#Cc1ccc(-c2ccc(OCCCN3CCC(O)CC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	10268636	5211	0	None	-1174	4	Human	5.0	pKi	=	5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	335	7	1	4	3.3	CN[C@@H]1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1	10.1016/s0960-894x(02)00648-0
	CHEMBL106545	5211	0	None	-1174	4	Human	5.0	pKi	=	5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	335	7	1	4	3.3	CN[C@@H]1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1	10.1016/s0960-894x(02)00648-0
	44304327	199198	0	None	-2511	3	Human	5.0	pKi	=	5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	535	11	1	6	4.3	CC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL60143	199198	0	None	-2511	3	Human	5.0	pKi	=	5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	535	11	1	6	4.3	CC(C)(C)OC(=O)N[C@H](Cc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	44304295	201181	0	None	-2290	3	Human	5.0	pKi	=	5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	357	8	1	5	1.5	O=C1C[C@@H](N2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)CC2)N1	10.1016/s0960-894x(02)00310-4
	CHEMBL62596	201181	0	None	-2290	3	Human	5.0	pKi	=	5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	357	8	1	5	1.5	O=C1C[C@@H](N2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)CC2)N1	10.1016/s0960-894x(02)00310-4
	44304331	201431	0	None	-2187	3	Human	5.0	pKi	=	5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	449	11	1	5	3.2	N[C@H](CCc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL64059	201431	0	None	-2187	3	Human	5.0	pKi	=	5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	449	11	1	5	3.2	N[C@H](CCc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	44275807	98513	0	None	-9120	10	Human	5.0	pKi	=	5	Binding	Binding affinity towards human histaminergic (H2) receptorBinding affinity towards human histaminergic (H2) receptor	ChEMBL	422	7	0	4	4.5	C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1	10.1016/s0960-894x(03)00118-5
	CHEMBL27979	98513	0	None	-9120	10	Human	5.0	pKi	=	5	Binding	Binding affinity towards human histaminergic (H2) receptorBinding affinity towards human histaminergic (H2) receptor	ChEMBL	422	7	0	4	4.5	C[C@H]1CC[C@H](C)N1CCCOc1ccc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1	10.1016/s0960-894x(03)00118-5
	10422468	202457	0	None	-501	3	Human	5.0	pKi	=	5	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	254	7	3	2	2.4	CC(C)/N=C(\S)NCCCCCc1c[nH]cn1	10.1021/jm00012a025
	CHEMBL70603	202457	0	None	-501	3	Human	5.0	pKi	=	5	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	254	7	3	2	2.4	CC(C)/N=C(\S)NCCCCCc1c[nH]cn1	10.1021/jm00012a025
	10466840	202776	0	None	-1000	4	Human	5.0	pKi	=	5	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	240	7	3	2	2.0	CC/N=C(\S)NCCCCCc1c[nH]cn1	10.1021/jm00012a025
	CHEMBL72424	202776	0	None	-1000	4	Human	5.0	pKi	=	5	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	240	7	3	2	2.0	CC/N=C(\S)NCCCCCc1c[nH]cn1	10.1021/jm00012a025
	9990475	56183	0	None	-3	3	Human	5.0	pKi	=	5	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	205	2	2	3	-0.5	Cc1nc(N)[se]c1CCN	10.1016/j.bmcl.2010.10.041
	CHEMBL1632408	56183	0	None	-3	3	Human	5.0	pKi	=	5	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	205	2	2	3	-0.5	Cc1nc(N)[se]c1CCN	10.1016/j.bmcl.2010.10.041
	CHEMBL2448450	56183	0	None	-3	3	Human	5.0	pKi	=	5	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	205	2	2	3	-0.5	Cc1nc(N)[se]c1CCN	10.1016/j.bmcl.2010.10.041
	10466840	202776	0	None	-1000	4	Human	5.0	pKi	=	5	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	240	7	3	2	2.0	CC/N=C(\S)NCCCCCc1c[nH]cn1	10.1016/j.bmcl.2010.10.041
	CHEMBL72424	202776	0	None	-1000	4	Human	5.0	pKi	=	5	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	240	7	3	2	2.0	CC/N=C(\S)NCCCCCc1c[nH]cn1	10.1016/j.bmcl.2010.10.041
	44334252	4480	0	None	-323	3	Human	4.0	pKi	=	4	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	449	10	3	7	1.7	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](CO)NC(=O)OC(C)(C)C)C2)cc1	10.1016/s0960-894x(02)00685-6
	CHEMBL102390	4480	0	None	-323	3	Human	4.0	pKi	=	4	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	449	10	3	7	1.7	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](CO)NC(=O)OC(C)(C)C)C2)cc1	10.1016/s0960-894x(02)00685-6
	44335350	5011	0	None	-389	3	Human	4.0	pKi	=	4	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	398	8	0	5	3.9	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(OC)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	CHEMBL105483	5011	0	None	-389	3	Human	4.0	pKi	=	4	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	398	8	0	5	3.9	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(OC)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	44304211	101727	0	None	-19054	3	Human	4.0	pKi	=	4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.9	CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL302829	101727	0	None	-19054	3	Human	4.0	pKi	=	4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.9	CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	10451094	200786	0	None	-199526	3	Human	4.0	pKi	=	4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359	9	1	5	1.5	NCCC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL61120	200786	0	None	-199526	3	Human	4.0	pKi	=	4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359	9	1	5	1.5	NCCC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	29298	201758	1	None	-1047	4	Human	5.0	pKi	=	5.0	Binding	Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor	ChEMBL	297	5	1	3	3.9	CN(C)CCCNc1c2c(nc3ccccc13)CCCCC2	10.1016/s0960-894x(03)00356-1
	CHEMBL65849	201758	1	None	-1047	4	Human	5.0	pKi	=	5.0	Binding	Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor	ChEMBL	297	5	1	3	3.9	CN(C)CCCNc1c2c(nc3ccccc13)CCCCC2	10.1016/s0960-894x(03)00356-1
	164614645	184549	0	None	57	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	402	8	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C	10.1016/j.ejmech.2021.113190
	CHEMBL4856572	184549	0	None	57	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	402	8	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)C(C)C	10.1016/j.ejmech.2021.113190
	164622886	185360	0	None	93	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	374	7	4	4	2.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4869389	185360	0	None	93	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	374	7	4	4	2.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC[C@@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	1588	2294	24	None	-323	43	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
	28864	2294	24	None	-323	43	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
	43	2294	24	None	-323	43	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
	CHEMBL157138	2294	24	None	-323	43	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
	DB00589	2294	24	None	-323	43	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	nan
	10069595	201438	0	None	-3235	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	400	11	0	4	4.2	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C3CCC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL64100	201438	0	None	-3235	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	400	11	0	4	4.2	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C3CCC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304318	201570	0	None	-1584	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.8	C[C@@H](CN)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL64608	201570	0	None	-1584	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.8	C[C@@H](CN)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	112936251	136742	1	None	-10	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation counting	ChEMBL	359	5	1	5	3.5	CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1	10.1016/j.bmcl.2015.12.035
	CHEMBL3752085	136742	1	None	-10	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation counting	ChEMBL	359	5	1	5	3.5	CN1CCN(c2cc(-c3ccccc3)nc(NCc3ccccc3)n2)CC1	10.1016/j.bmcl.2015.12.035
	127052293	139708	1	None	-218	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method	ChEMBL	368	7	3	4	3.1	N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1	10.1021/acs.jmedchem.6b00120
	CHEMBL3805361	139708	1	None	-218	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method	ChEMBL	368	7	3	4	3.1	N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@H](c2c[nH]cn2)C1	10.1021/acs.jmedchem.6b00120
	176	394	63	None	-6	31	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	2157	394	63	None	-6	31	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	2566	394	63	None	-6	31	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	CHEMBL633	394	63	None	-6	31	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	DB01118	394	63	None	-6	31	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	nan
	164627189	185739	0	None	275	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	298	6	4	4	1.0	CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	CHEMBL4874758	185739	0	None	275	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	298	6	4	4	1.0	CCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	168294776	192424	0	None	-7	4	Human	6.0	pKi	=	6.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	366	7	3	4	2.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5209479	192424	0	None	-7	4	Human	6.0	pKi	=	6.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	366	7	3	4	2.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222831	192424	0	None	-7	4	Human	6.0	pKi	=	6.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	366	7	3	4	2.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCC(C)C2CCCCC2)s1	10.1021/acs.jmedchem.1c00692
	168294445	192408	0	None	-1	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	6	4	4	2.6	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5208113	192408	0	None	-1	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	6	4	4	2.6	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222768	192408	0	None	-1	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	6	4	4	2.6	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCC2CCc3nc(N)sc3C2)cc1	10.1021/acs.jmedchem.1c00692
	44304320	162723	0	None	-4265	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.9	CC[C@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL418666	162723	0	None	-4265	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.9	CC[C@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	44304319	200947	0	None	-1202	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.8	C[C@H](CN)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL61288	200947	0	None	-1202	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.8	C[C@H](CN)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	44304494	201303	0	None	-8709	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	489	12	1	6	4.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](C)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	CHEMBL63125	201303	0	None	-8709	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	489	12	1	6	4.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](C)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	132060746	162520	0	None	-6	5	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	405	4	0	4	4.4	O=C(OCc1ccccc1)N1Cc2ccc(N3CCN(C4CCCC4)CC3)cc2C1	10.1016/j.ejmech.2018.02.024
	CHEMBL4176474	162520	0	None	-6	5	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	405	4	0	4	4.4	O=C(OCc1ccccc1)N1Cc2ccc(N3CCN(C4CCCC4)CC3)cc2C1	10.1016/j.ejmech.2018.02.024
	124087	1362	106	None	-29	15	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
	7157	1362	106	None	-29	15	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
	814	1362	106	None	-29	15	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
	CHEMBL1172	1362	106	None	-29	15	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
	DB00967	1362	106	None	-29	15	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	nan
	168284289	192304	0	None	1	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	428	8	4	4	3.1	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
	CHEMBL5194860	192304	0	None	1	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	428	8	4	4	3.1	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222123	192304	0	None	1	4	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	428	8	4	4	3.1	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
	44304211	101727	0	None	-19054	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.9	CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL302829	101727	0	None	-19054	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	373	9	1	5	1.9	CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	132060752	162376	0	None	-3	4	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	437	7	0	6	3.4	CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1	10.1016/j.ejmech.2018.02.024
	CHEMBL4174189	162376	0	None	-3	4	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	437	7	0	6	3.4	CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1	10.1016/j.ejmech.2018.02.024
	CHEMBL5085542	213199	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C	10.1016/j.bmcl.2021.128388
	164626370	185891	0	None	1	6	Human	6.0	pKi	=	6.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	338	6	4	4	1.8	CCCCCCNC(=O)/N=C(\N)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	CHEMBL4876799	185891	0	None	1	6	Human	6.0	pKi	=	6.0	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	338	6	4	4	1.8	CCCCCCNC(=O)/N=C(\N)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	44304382	201611	0	None	-1174	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	403	11	1	4	4.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)NC(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL64773	201611	0	None	-1174	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	403	11	1	4	4.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)NC(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
	11057	175575	19	None	-2	20	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	nan
	3468	175575	19	None	-2	20	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	nan
	CHEMBL459265	175575	19	None	-2	20	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	nan
	CHEMBL64894	175575	19	None	-2	20	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	nan
	164616851	184367	0	None	-1	5	Human	6.9	pKi	=	6.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	376	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4853772	184367	0	None	-1	5	Human	6.9	pKi	=	6.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	376	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	2286	3134	48	None	-26	29	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
	4927	3134	48	None	-26	29	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
	7282	3134	48	None	-26	29	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
	CHEMBL643	3134	48	None	-26	29	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
	DB01069	3134	48	None	-26	29	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	nan
	1353	1880	85	None	-131	85	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
	3559	1880	85	None	-131	85	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
	86	1880	85	None	-131	85	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
	CHEMBL54	1880	85	None	-131	85	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
	DB00502	1880	85	None	-131	85	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	nan
	164612760	184135	0	None	38	4	Human	5.9	pKi	=	5.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	390	7	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4850490	184135	0	None	38	4	Human	5.9	pKi	=	5.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	390	7	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	44582678	180992	0	None	-7	10	Human	5.9	pKi	=	5.9	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	401	9	1	4	4.3	COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1	10.1016/j.bmc.2009.03.021
	CHEMBL476839	180992	0	None	-7	10	Human	5.9	pKi	=	5.9	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	401	9	1	4	4.3	COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1	10.1016/j.bmc.2009.03.021
	73353884	91890	0	None	2	8	Human	5.9	pKi	=	5.9	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	295	3	1	3	2.7	c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2	10.1016/j.bmc.2013.07.045
	CHEMBL2429890	91890	0	None	2	8	Human	5.9	pKi	=	5.9	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	295	3	1	3	2.7	c1cc2c(cc1CN[C@H]1C3C4CC5C6C4CC3C6C51)OCO2	10.1016/j.bmc.2013.07.045
	44304245	201637	0	None	-2884	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	425	11	0	5	4.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccn3C)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL64884	201637	0	None	-2884	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	425	11	0	5	4.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccn3C)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44335559	109221	0	None	-6918	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	334	6	0	3	4.7	CC1CCCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1	10.1016/s0960-894x(02)00648-0
	CHEMBL322873	109221	0	None	-6918	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	334	6	0	3	4.7	CC1CCCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1	10.1016/s0960-894x(02)00648-0
	1201549	590	22	None	-74	20	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
	333	590	22	None	-74	20	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
	7601	590	22	None	-74	20	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
	CHEMBL1201203	590	22	None	-74	20	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
	CHEMBL438151	590	22	None	-74	20	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
	DB00245	590	22	None	-74	20	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	nan
	168295541	192438	0	None	-851	6	Human	7.9	pKi	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5208845	192438	0	None	-851	6	Human	7.9	pKi	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222926	192438	0	None	-851	6	Human	7.9	pKi	=	7.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	347	6	4	5	1.4	C[C@@H](NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	44334430	4388	0	None	-398	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	428	10	1	5	3.1	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
	CHEMBL101691	4388	0	None	-398	3	Human	5.9	pKi	=	5.9	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	428	10	1	5	3.1	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
	44304457	201522	0	None	-3981	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	376	10	0	5	3.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL64408	201522	0	None	-3981	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	376	10	0	5	3.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304431	201252	0	None	-512	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	566	14	1	7	4.9	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](Cc3ccncc3)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	CHEMBL62903	201252	0	None	-512	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	566	14	1	7	4.9	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](Cc3ccncc3)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	1212	1632	45	None	-323	65	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
	204	1632	45	None	-323	65	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
	3372	1632	45	None	-323	65	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
	CHEMBL726	1632	45	None	-323	65	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
	DB00623	1632	45	None	-323	65	Human	5.9	pKi	=	5.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	nan
	9872676	77826	0	None	-3090	17	Human	5.9	pKi	=	5.9	Binding	Binding affinity to H2 receptorBinding affinity to H2 receptor	ChEMBL	565	11	2	10	4.8	COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1	10.1021/jm060012g
	CHEMBL210514	77826	0	None	-3090	17	Human	5.9	pKi	=	5.9	Binding	Binding affinity to H2 receptorBinding affinity to H2 receptor	ChEMBL	565	11	2	10	4.8	COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1	10.1021/jm060012g
	44304751	100554	0	None	-338	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	422	11	0	4	4.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccccc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL294519	100554	0	None	-338	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	422	11	0	4	4.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccccc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304990	201373	0	None	-331	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	483	12	0	6	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(S(=O)(=O)c3ccc(C#N)cc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL63632	201373	0	None	-331	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	483	12	0	6	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(S(=O)(=O)c3ccc(C#N)cc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44335225	163603	0	None	-812	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	347	6	1	4	3.1	N#Cc1ccc(-c2ccc(OCCCN3CC4CNCC4C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	CHEMBL421026	163603	0	None	-812	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	347	6	1	4	3.1	N#Cc1ccc(-c2ccc(OCCCN3CC4CNCC4C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	44304303	201638	0	None	-954	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	371	8	1	5	1.6	O=C(c1ccc(OCCCN2CCN(C(=O)[C@@H]3CCN3)CC2)cc1)C1CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL64896	201638	0	None	-954	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	371	8	1	5	1.6	O=C(c1ccc(OCCCN2CCN(C(=O)[C@@H]3CCN3)CC2)cc1)C1CC1	10.1016/s0960-894x(02)00310-4
	164621681	184998	0	None	64	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	444	7	4	5	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(OC(F)(F)F)cc1	10.1016/j.ejmech.2021.113190
	CHEMBL4863523	184998	0	None	64	4	Human	6.9	pKi	=	6.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	444	7	4	5	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(OC(F)(F)F)cc1	10.1016/j.ejmech.2021.113190
	409544	201225	3	None	-8912	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	390	11	0	5	4.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL62803	201225	3	None	-8912	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	390	11	0	5	4.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304035	201618	0	None	-181	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	410	9	0	5	3.7	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)Cc3ccccc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	CHEMBL64799	201618	0	None	-181	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	410	9	0	5	3.7	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)Cc3ccccc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	44304393	105477	0	None	-128	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	517	13	1	6	4.9	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](NC(=O)OC(C)(C)C)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	CHEMBL312958	105477	0	None	-128	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	517	13	1	6	4.9	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](NC(=O)OC(C)(C)C)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	10039772	103882	0	None	-501	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	288	7	3	2	3.1	S=C(NCCCCCc1c[nH]cn1)Nc1ccccc1	10.1021/jm00012a025
	CHEMBL310087	103882	0	None	-501	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	288	7	3	2	3.1	S=C(NCCCCCc1c[nH]cn1)Nc1ccccc1	10.1021/jm00012a025
	44304246	200964	0	None	-1513	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	426	11	0	5	4.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3occc3C)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL61396	200964	0	None	-1513	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	426	11	0	5	4.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3occc3C)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44335463	4389	0	None	-229	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	357	7	1	4	3.2	CCOC(=O)N1CCN(CCCOc2ccc(-c3cc[nH]c3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	CHEMBL101692	4389	0	None	-229	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	357	7	1	4	3.2	CCOC(=O)N1CCN(CCCOc2ccc(-c3cc[nH]c3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	44335483	5221	0	None	-426	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	336	6	1	4	3.5	N#Cc1ccc(-c2ccc(OCCCN3CCCC(O)C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	CHEMBL106596	5221	0	None	-426	4	Human	4.9	pKi	=	4.9	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	336	6	1	4	3.5	N#Cc1ccc(-c2ccc(OCCCN3CCCC(O)C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	156017225	177770	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	442	15	3	7	3.1	NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4642548	177770	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	442	15	3	7	3.1	NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4651234	177770	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	442	15	3	7	3.1	NCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	156015555	177737	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	456	16	3	7	3.5	NCCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4644794	177737	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	456	16	3	7	3.5	NCCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4651059	177737	0	None	-	1	Human	7.9	pKi	=	7.9	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	456	16	3	7	3.5	NCCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	156014823	177752	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1109	31	4	13	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4641747	177752	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1109	31	4	13	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4651132	177752	0	None	-	1	Human	5.9	pKi	=	5.9	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1109	31	4	13	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	44304412	199963	0	None	-912	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	517	13	1	6	4.9	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](NC(=O)OC(C)(C)C)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	CHEMBL60598	199963	0	None	-912	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	517	13	1	6	4.9	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](NC(=O)OC(C)(C)C)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	59868	93720	56	None	-20892	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	211	3	2	4	1.6	CCCN[C@@H]1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	CHEMBL249420	93720	56	None	-20892	3	Human	4.9	pKi	=	4.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	211	3	2	4	1.6	CCCN[C@@H]1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	119570	3110	90	None	-281	40	Human	4.9	pKi	=	4.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	2233	3110	90	None	-281	40	Human	4.9	pKi	=	4.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	953	3110	90	None	-281	40	Human	4.9	pKi	=	4.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	CHEMBL301265	3110	90	None	-281	40	Human	4.9	pKi	=	4.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	DB00413	3110	90	None	-281	40	Human	4.9	pKi	=	4.9	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1021/acs.jmedchem.1c00692
	104903	56050	14	None	-5	6	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	624	6	0	8	5.5	C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1	nan
	CHEMBL1630578	56050	14	None	-5	6	Human	4.9	pKi	=	4.9	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	624	6	0	8	5.5	C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1	nan
	CHEMBL4535474	212235	34	None	-1	6	Human	6.9	pKi	=	6.9	Binding	Selectivity interaction (GPCR panel (PDSP screen)) EUB0000320b HRH2Selectivity interaction (GPCR panel (PDSP screen)) EUB0000320b HRH2	ChEMBL		None	None	None		CNCc1ccccc1-c1csc([C@@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1	nan
	1231	924	112	None	-2	7	Human	6.9	pKi	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
	2756	924	112	None	-2	7	Human	6.9	pKi	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
	645	924	112	None	-2	7	Human	6.9	pKi	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
	CHEMBL30	924	112	None	-2	7	Human	6.9	pKi	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
	DB00501	924	112	None	-2	7	Human	6.9	pKi	=	6.9	Binding	Binding affinity to human histamine H2 receptor by radioligand displacement assayBinding affinity to human histamine H2 receptor by radioligand displacement assay	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.ejmech.2013.01.044
	44568347	191055	0	None	-67	15	Human	5.9	pKi	=	5.9	Binding	Antagonist activity at histamine H2 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	356	6	0	4	5.2	CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21	10.1016/j.bmcl.2013.04.082
	CHEMBL519609	191055	0	None	-67	15	Human	5.9	pKi	=	5.9	Binding	Antagonist activity at histamine H2 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	356	6	0	4	5.2	CCN(CC)CCCOC(=O)N1c2ccccc2Sc2ccccc21	10.1016/j.bmcl.2013.04.082
	44304560	102290	0	None	-10715	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	371	8	1	5	1.6	O=C(c1ccc(OCCCN2CCN(C(=O)[C@H]3CCN3)CC2)cc1)C1CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL305144	102290	0	None	-10715	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	371	8	1	5	1.6	O=C(c1ccc(OCCCN2CCN(C(=O)[C@H]3CCN3)CC2)cc1)C1CC1	10.1016/s0960-894x(02)00310-4
	44304760	201212	0	None	-229	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	431	13	1	5	3.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)CC(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	CHEMBL62741	201212	0	None	-229	3	Human	4.9	pKi	=	4.9	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	431	13	1	5	3.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)CC(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	71525678	89295	0	None	-1479	6	Human	4.9	pKi	=	4.9	Binding	Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells	ChEMBL	258	3	2	6	0.6	CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1	10.1016/j.bmcl.2013.02.091
	CHEMBL2376800	89295	0	None	-1479	6	Human	4.9	pKi	=	4.9	Binding	Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells	ChEMBL	258	3	2	6	0.6	CCc1cnc2c(N3CC(NC)C3)nc(N)nc2c1	10.1016/j.bmcl.2013.02.091
	164610824	184527	0	None	14	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	452	8	4	4	3.6	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NCC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4856200	184527	0	None	14	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	452	8	4	4	3.6	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NCC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
	18539962	101661	0	None	-537	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	318	10	1	4	3.1	CCCCCC(=O)c1ccc(OCCCN2CCNCC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL302445	101661	0	None	-537	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	318	10	1	4	3.1	CCCCCC(=O)c1ccc(OCCCN2CCNCC2)cc1	10.1016/s0960-894x(02)00309-8
	2389	3279	114	None	-275	67	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
	5073	3279	114	None	-275	67	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
	96	3279	114	None	-275	67	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
	CHEMBL85	3279	114	None	-275	67	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
	DB00734	3279	114	None	-275	67	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	nan
	164620704	185501	0	None	17	4	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	416	8	4	4	3.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1	10.1016/j.ejmech.2021.113190
	CHEMBL4871482	185501	0	None	17	4	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	416	8	4	4	3.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)c1ccc(C(C)C)cc1	10.1016/j.ejmech.2021.113190
	44304287	201209	0	None	-912	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	428	11	0	5	4.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccs3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL62726	201209	0	None	-912	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	428	11	0	5	4.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccs3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304310	201583	0	None	-1995	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	415	10	0	4	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)N3CCCC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL64667	201583	0	None	-1995	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	415	10	0	4	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)N3CCCC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304349	201113	0	None	-275	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	566	14	1	7	4.9	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](Cc3ccncc3)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	CHEMBL62266	201113	0	None	-275	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	566	14	1	7	4.9	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](Cc3ccncc3)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	73347825	92108	0	None	-1	3	Human	5.8	pKi	=	5.8	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	311	5	1	3	2.9	COc1ccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC	10.1016/j.bmc.2013.07.045
	CHEMBL2432046	92108	0	None	-1	3	Human	5.8	pKi	=	5.8	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	311	5	1	3	2.9	COc1ccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC	10.1016/j.bmc.2013.07.045
	57469	18678	120	None	-1	3	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	240	2	1	4	2.8	CC(C)Cn1cnc2c(N)nc3ccccc3c21	nan
	CHEMBL1282	18678	120	None	-1	3	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	240	2	1	4	2.8	CC(C)Cn1cnc2c(N)nc3ccccc3c21	nan
	168286426	192324	0	None	-5	6	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5198795	192324	0	None	-5	6	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222241	192324	0	None	-5	6	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	403	10	4	5	2.3	CC(CCCc1ccccc1)CNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	135156	177229	7	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter methodBinding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter method	ChEMBL	343	8	2	6	1.7	Nc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4643501	177229	7	None	-	1	Human	7.8	pKi	=	7.8	Binding	Binding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter methodBinding affinity to human H2R expressing Sf9 cells incubated for 60 mins by microbeta scintillation counter method	ChEMBL	343	8	2	6	1.7	Nc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	69355600	78275	0	None	-3715	4	Human	4.8	pKi	=	4.8	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	336	6	1	4	3.5	C[C@@]1(O)CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1	10.1016/s0960-894x(02)00648-0
	CHEMBL2112461	78275	0	None	-3715	4	Human	4.8	pKi	=	4.8	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	336	6	1	4	3.5	C[C@@]1(O)CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)C1	10.1016/s0960-894x(02)00648-0
	44304293	201273	0	None	-52	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	491	10	1	6	4.0	N[C@H](Cc1cc2ccccc2s1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL63002	201273	0	None	-52	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	491	10	1	6	4.0	N[C@H](Cc1cc2ccccc2s1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	168295803	192443	0	None	3	4	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	338	6	4	4	1.6	CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
	CHEMBL5207206	192443	0	None	3	4	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	338	6	4	4	1.6	CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222937	192443	0	None	3	4	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	338	6	4	4	1.6	CCCCCNC(=O)/N=C(\N)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
	44304283	201483	0	None	-117	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	452	8	0	5	4.8	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(C(C)(C)C)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	CHEMBL64247	201483	0	None	-117	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	452	8	0	5	4.8	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(C(C)(C)C)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	44334396	4847	0	None	-575	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	446	10	1	5	3.2	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3F)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
	CHEMBL104618	4847	0	None	-575	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	446	10	1	5	3.2	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccccc3F)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
	3198	203802	73	None	-19	34	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	380	6	0	3	5.8	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1	nan
	CHEMBL1201049	203802	73	None	-19	34	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	380	6	0	3	5.8	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1	nan
	CHEMBL808	203802	73	None	-19	34	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	380	6	0	3	5.8	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1	nan
	164622190	185034	0	None	93	2	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	360	7	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4864067	185034	0	None	93	2	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	360	7	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCc1ccccc1	10.1016/j.ejmech.2021.113190
	10017820	202494	0	None	-79	3	Human	5.8	pKi	=	5.8	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	302	8	3	2	2.8	S=C(NCCCCCc1c[nH]cn1)NCc1ccccc1	10.1021/jm00012a025
	CHEMBL70811	202494	0	None	-79	3	Human	5.8	pKi	=	5.8	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	302	8	3	2	2.8	S=C(NCCCCCc1c[nH]cn1)NCc1ccccc1	10.1021/jm00012a025
	9974306	202769	0	None	-199	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	336	8	3	2	3.4	S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1	10.1021/jm00012a025
	CHEMBL72372	202769	0	None	-199	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	336	8	3	2	3.4	S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1	10.1021/jm00012a025
	9974306	202769	0	None	-199	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	336	8	3	2	3.4	S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1	10.1016/j.bmcl.2010.10.041
	CHEMBL72372	202769	0	None	-199	4	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	336	8	3	2	3.4	S=C(NCCCCCc1c[nH]cn1)NCc1ccc(Cl)cc1	10.1016/j.bmcl.2010.10.041
	3042	1386	31	None	-53	15	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
	355	1386	31	None	-53	15	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
	868	1386	31	None	-53	15	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
	CHEMBL1123	1386	31	None	-53	15	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
	DB00804	1386	31	None	-53	15	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	nan
	10343536	4893	0	None	-1000	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	446	10	1	5	3.2	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3cccc(F)c3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
	CHEMBL104809	4893	0	None	-1000	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	446	10	1	5	3.2	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3cccc(F)c3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
	71452695	78273	0	None	-398	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	453	10	1	6	3.0	N#Cc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
	CHEMBL2112451	78273	0	None	-398	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	453	10	1	6	3.0	N#Cc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
	2247	502	77	None	-56	41	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
	249	502	77	None	-56	41	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
	2603	502	77	None	-56	41	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
	CHEMBL296419	502	77	None	-56	41	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
	DB00637	502	77	None	-56	41	Human	5.8	pKi	=	5.8	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	nan
	44335185	106907	0	None	-14	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	446	7	0	4	4.7	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(Br)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	CHEMBL317900	106907	0	None	-14	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	446	7	0	4	4.7	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(Br)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	44304743	100143	0	None	-97	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	431	13	1	5	3.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)CC(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	CHEMBL291847	100143	0	None	-97	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	431	13	1	5	3.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)CC(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	164628701	185885	0	None	144	3	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	338	5	4	4	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1	10.1016/j.ejmech.2021.113190
	CHEMBL4876743	185885	0	None	144	3	Human	6.8	pKi	=	6.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	338	5	4	4	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC1CCCCC1	10.1016/j.ejmech.2021.113190
	9880208	4855	0	None	-2041	4	Human	4.8	pKi	=	4.8	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	322	6	1	4	3.1	N#Cc1ccc(-c2ccc(OCCCN3CC[C@@H](O)C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	CHEMBL104669	4855	0	None	-2041	4	Human	4.8	pKi	=	4.8	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	322	6	1	4	3.1	N#Cc1ccc(-c2ccc(OCCCN3CC[C@@H](O)C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	156015722	177698	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4644467	177698	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4650837	177698	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	718	21	2	7	7.9	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	156015152	177731	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4641916	177731	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4651017	177731	0	None	-	1	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	676	18	2	7	6.7	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	164609729	184515	0	None	-2	6	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	360	6	4	4	2.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4856059	184515	0	None	-2	6	Human	7.8	pKi	=	7.8	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	360	6	4	4	2.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	1231	924	112	None	-2	7	Human	6.8	pKi	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
	2756	924	112	None	-2	7	Human	6.8	pKi	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
	645	924	112	None	-2	7	Human	6.8	pKi	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
	CHEMBL30	924	112	None	-2	7	Human	6.8	pKi	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
	DB00501	924	112	None	-2	7	Human	6.8	pKi	=	6.8	Binding	Displacement of radiolabeled cimetidine from human histamine H2 receptorDisplacement of radiolabeled cimetidine from human histamine H2 receptor	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/jm8007618
	9906447	193904	1	None	-2344	13	Human	5.8	pKi	=	5.8	Binding	Binding affinity to human recombinant H2 receptorBinding affinity to human recombinant H2 receptor	ChEMBL	351	5	0	3	4.8	C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1	10.1021/jm201690h
	CHEMBL2031738	193904	1	None	-2344	13	Human	5.8	pKi	=	5.8	Binding	Binding affinity to human recombinant H2 receptorBinding affinity to human recombinant H2 receptor	ChEMBL	351	5	0	3	4.8	C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1	10.1021/jm201690h
	CHEMBL555146	193904	1	None	-2344	13	Human	5.8	pKi	=	5.8	Binding	Binding affinity to human recombinant H2 receptorBinding affinity to human recombinant H2 receptor	ChEMBL	351	5	0	3	4.8	C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc(F)cc3)ccc2o1	10.1021/jm201690h
	10064805	101906	0	None	-95	4	Human	5.8	pKi	=	5.8	Binding	Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor	ChEMBL	323	4	1	3	4.4	CN1CCCC1CCNc1c2c(nc3ccccc13)CCCCC2	10.1016/s0960-894x(03)00356-1
	CHEMBL303824	101906	0	None	-95	4	Human	5.8	pKi	=	5.8	Binding	Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor	ChEMBL	323	4	1	3	4.4	CN1CCCC1CCNc1c2c(nc3ccccc13)CCCCC2	10.1016/s0960-894x(03)00356-1
	73349359	92111	0	None	-2	8	Human	5.8	pKi	=	5.8	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	341	6	1	4	2.9	COc1cc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC	10.1016/j.bmc.2013.07.045
	CHEMBL2432051	92111	0	None	-2	8	Human	5.8	pKi	=	5.8	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	341	6	1	4	2.9	COc1cc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc(OC)c1OC	10.1016/j.bmc.2013.07.045
	44304308	102012	0	None	-691	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	432	8	0	5	3.7	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3cccc(F)c3F)cc2)CC1	10.1016/s0960-894x(02)00309-8
	CHEMBL304027	102012	0	None	-691	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	432	8	0	5	3.7	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3cccc(F)c3F)cc2)CC1	10.1016/s0960-894x(02)00309-8
	44582676	189187	0	None	-13	17	Human	5.8	pKi	=	5.8	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	403	9	0	4	4.3	COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1	10.1016/j.bmc.2009.03.021
	CHEMBL516088	189187	0	None	-13	17	Human	5.8	pKi	=	5.8	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	403	9	0	4	4.3	COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1	10.1016/j.bmc.2009.03.021
	132060776	161852	0	None	-6	16	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	419	4	0	4	4.4	O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1	10.1016/j.ejmech.2018.02.024
	CHEMBL4165863	161852	0	None	-6	16	Human	5.8	pKi	=	5.8	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	419	4	0	4	4.4	O=C(OCc1ccccc1)N1CCc2ccc(N3CCN(C4CCCC4)CC3)cc2C1	10.1016/j.ejmech.2018.02.024
	73346042	91402	3	None	-17782	17	Human	5.8	pKi	=	5.8	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	405	9	0	8	0.9	Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O	10.1016/j.bmc.2013.05.050
	CHEMBL2413153	91402	3	None	-17782	17	Human	5.8	pKi	=	5.8	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	405	9	0	8	0.9	Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O	10.1016/j.bmc.2013.05.050
	44304385	201488	0	None	-3548	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	404	11	0	5	4.4	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OC(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL64259	201488	0	None	-3548	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	404	11	0	5	4.4	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OC(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
	10455457	201712	0	None	-3019	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	431	10	0	5	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)N3CCOCC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL65518	201712	0	None	-3019	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	431	10	0	5	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)N3CCOCC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304066	201077	0	None	-407	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	449	11	1	5	3.0	CN[C@H](Cc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL62050	201077	0	None	-407	3	Human	4.8	pKi	=	4.8	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	449	11	1	5	3.0	CN[C@H](Cc1ccccc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	71452383	83382	0	None	1	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	339	5	1	4	2.0	COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC	10.1016/j.bmcl.2012.08.046
	CHEMBL2205814	83382	0	None	1	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	339	5	1	4	2.0	COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC	10.1016/j.bmcl.2012.08.046
	1235	3763	32	None	-2	4	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs	ChEMBL	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	10.1016/j.bmcl.2013.01.025
	3959	3763	32	None	-2	4	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs	ChEMBL	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	10.1016/j.bmcl.2013.01.025
	50287	3763	32	None	-2	4	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs	ChEMBL	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	10.1016/j.bmcl.2013.01.025
	CHEMBL269646	3763	32	None	-2	4	Human	7.8	pKi	=	7.8	Binding	Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrsDisplacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs	ChEMBL	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	10.1016/j.bmcl.2013.01.025
	4806	3945	85	None	-5	13	Human	6.8	pKi	=	6.8	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	ChEMBL	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	10.1021/jm101459g
	7351	3945	85	None	-5	13	Human	6.8	pKi	=	6.8	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	ChEMBL	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	10.1021/jm101459g
	9966051	3945	85	None	-5	13	Human	6.8	pKi	=	6.8	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	ChEMBL	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	10.1021/jm101459g
	CHEMBL2104993	3945	85	None	-5	13	Human	6.8	pKi	=	6.8	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	ChEMBL	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	10.1021/jm101459g
	DB09068	3945	85	None	-5	13	Human	6.8	pKi	=	6.8	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	ChEMBL	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	10.1021/jm101459g
	10003483	4576	0	None	-660	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	442	10	1	5	3.4	Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1	10.1016/s0960-894x(02)00685-6
	CHEMBL103027	4576	0	None	-660	3	Human	5.8	pKi	=	5.8	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	442	10	1	5	3.4	Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1	10.1016/s0960-894x(02)00685-6
	CHEMBL5076746	213749	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(N)(=O)=O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095519	213749	0	None	-	1	Human	6.7	pKi	=	6.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(N)(=O)=O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	156015638	177697	0	None	-1819	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranes	ChEMBL	415	10	1	2	5.5	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1	10.1021/acs.jmedchem.0c00160
	CHEMBL4642520	177697	0	None	-1819	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranes	ChEMBL	415	10	1	2	5.5	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1	10.1021/acs.jmedchem.0c00160
	CHEMBL4650832	177697	0	None	-1819	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranes	ChEMBL	415	10	1	2	5.5	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCc1c[nH]cn1	10.1021/acs.jmedchem.0c00160
	168281536	192279	0	None	-9	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	369	12	4	5	1.7	Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5189006	192279	0	None	-9	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	369	12	4	5	1.7	Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221966	192279	0	None	-9	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	369	12	4	5	1.7	Cc1nnc(CCCN/C(N)=N/C(=O)NCCCCCCCCN)s1	10.1021/acs.jmedchem.1c00692
	3158	55974	21	None	-12589	20	Human	5.7	pKi	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	279	3	0	2	4.0	CN(C)CCC=C1c2ccccc2COc2ccccc21	nan
	CHEMBL1628227	55974	21	None	-12589	20	Human	5.7	pKi	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	279	3	0	2	4.0	CN(C)CCC=C1c2ccccc2COc2ccccc21	nan
	44304399	201503	0	None	-91	3	Human	5.7	pKi	=	5.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	418	13	0	5	4.8	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCCCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL64317	201503	0	None	-91	3	Human	5.7	pKi	=	5.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	418	13	0	5	4.8	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCCCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304376	201281	0	None	-354	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	423	11	0	5	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccccn3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL63036	201281	0	None	-354	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	423	11	0	5	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccccn3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304244	201486	0	None	-1174	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	372	12	0	4	4.2	CCCCCC(=O)c1ccc(OCCCN2CCN(CC3CC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL64253	201486	0	None	-1174	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	372	12	0	4	4.2	CCCCCC(=O)c1ccc(OCCCN2CCN(CC3CC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44335384	4570	0	None	-2630	4	Human	4.7	pKi	=	4.7	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	334	6	0	3	4.9	CC1CCCCN1CCCOc1ccc(-c2ccc(C#N)cc2)cc1	10.1016/s0960-894x(02)00648-0
	CHEMBL102984	4570	0	None	-2630	4	Human	4.7	pKi	=	4.7	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	334	6	0	3	4.9	CC1CCCCN1CCCOc1ccc(-c2ccc(C#N)cc2)cc1	10.1016/s0960-894x(02)00648-0
	73355418	92114	0	None	-1	3	Human	5.7	pKi	=	5.7	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	325	5	0	3	3.3	COc1ccc(CN(C)[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC	10.1016/j.bmc.2013.07.045
	CHEMBL2432056	92114	0	None	-1	3	Human	5.7	pKi	=	5.7	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	325	5	0	3	3.3	COc1ccc(CN(C)[C@H]2C3C4CC5C6C4CC3C6C52)cc1OC	10.1016/j.bmc.2013.07.045
	156011186	177668	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	704	20	2	7	7.5	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4637893	177668	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	704	20	2	7	7.5	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4650588	177668	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	704	20	2	7	7.5	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	168294449	192416	0	None	-6	6	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5204599	192416	0	None	-6	6	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222793	192416	0	None	-6	6	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	367	7	4	5	1.9	CC(CNC(=O)/N=C(\N)NCCCc1nnc(N)s1)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	168294161	192404	0	None	3	4	Human	6.7	pKi	=	6.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5204739	192404	0	None	3	4	Human	6.7	pKi	=	6.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222742	192404	0	None	3	4	Human	6.7	pKi	=	6.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1cccc(-c2sc(N)nc2C)c1	10.1021/acs.jmedchem.1c00692
	9923186	107056	0	None	-977	4	Human	4.7	pKi	=	4.7	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	322	6	1	4	3.1	N#Cc1ccc(-c2ccc(OCCCN3CC[C@H](O)C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	CHEMBL318801	107056	0	None	-977	4	Human	4.7	pKi	=	4.7	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	322	6	1	4	3.1	N#Cc1ccc(-c2ccc(OCCCN3CC[C@H](O)C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	12192007	167844	35	None	-724	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	191	2	2	2	0.8	N[C@@H](C(=O)O)C1Cc2ccccc2C1	10.1016/s0960-894x(02)00310-4
	CHEMBL434785	167844	35	None	-724	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	191	2	2	2	0.8	N[C@@H](C(=O)O)C1Cc2ccccc2C1	10.1016/s0960-894x(02)00310-4
	44304013	201205	0	None	-363	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	401	8	1	5	2.6	CC(C)(C)[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL62716	201205	0	None	-363	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	401	8	1	5	2.6	CC(C)(C)[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	72901200	119272	21	None	-1318	4	Human	5.7	pKi	=	5.7	Binding	Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HRH2Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HRH2	ChEMBL	322	7	2	4	3.8	Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1	nan
	CHEMBL3480577	119272	21	None	-1318	4	Human	5.7	pKi	=	5.7	Binding	Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HRH2Selectivity interaction (PRESTO-Tango GPCR-ome screening) EUB0000539a HRH2	ChEMBL	322	7	2	4	3.8	Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1	nan
	5291	205704	115	None	-1	2	Human	5.7	pKi	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	493	7	2	7	4.6	Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1	nan
	CHEMBL941	205704	115	None	-1	2	Human	5.7	pKi	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	493	7	2	7	4.6	Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1	nan
	44304259	100148	0	None	-660	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	462	11	0	5	5.4	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3sccc3Cl)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL291882	100148	0	None	-660	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	462	11	0	5	5.4	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3sccc3Cl)CC2)cc1	10.1016/s0960-894x(02)00309-8
	10341609	198586	0	None	-4365	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	412	11	1	5	3.4	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3c[nH]cn3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL59715	198586	0	None	-4365	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	412	11	1	5	3.4	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3c[nH]cn3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	277	1274	55	None	-43	45	Human	6.7	pKi	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
	2913	1274	55	None	-43	45	Human	6.7	pKi	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
	765	1274	55	None	-43	45	Human	6.7	pKi	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
	CHEMBL516	1274	55	None	-43	45	Human	6.7	pKi	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
	DB00434	1274	55	None	-43	45	Human	6.7	pKi	=	6.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	nan
	153287553	170538	0	None	-316	6	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]-Iodoaminopotentidine from human recombinant histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodoaminopotentidine from human recombinant histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	264	1	1	2	3.7	C[C@@]12CN(c3ccccc3)c3ccccc3[C@@H]1CCN2	10.1021/acsmedchemlett.9b00225
	CHEMBL4457754	170538	0	None	-316	6	Human	5.7	pKi	=	5.7	Binding	Displacement of [125I]-Iodoaminopotentidine from human recombinant histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodoaminopotentidine from human recombinant histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	264	1	1	2	3.7	C[C@@]12CN(c3ccccc3)c3ccccc3[C@@H]1CCN2	10.1021/acsmedchemlett.9b00225
	164619039	185566	0	None	17	2	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	366	4	4	4	3.0	N/C(=N\C(=O)NCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
	CHEMBL4872277	185566	0	None	17	2	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	366	4	4	4	3.0	N/C(=N\C(=O)NCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
	10263017	205729	2	None	-31	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	223	10	2	2	3.0	NCCCCCCCCCCc1c[nH]cn1	10.1021/jm00002a008
	CHEMBL94249	205729	2	None	-31	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	223	10	2	2	3.0	NCCCCCCCCCCc1c[nH]cn1	10.1021/jm00002a008
	44304247	201121	0	None	-1905	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	412	11	0	5	4.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccco3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL62312	201121	0	None	-1905	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	412	11	0	5	4.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccco3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	5250783	168821	3	None	-1995	3	Human	4.7	pKi	=	4.7	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	226	6	3	2	1.6	C/N=C(\S)NCCCCCc1c[nH]cn1	10.1021/jm00012a025
	CHEMBL44220	168821	3	None	-1995	3	Human	4.7	pKi	=	4.7	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	226	6	3	2	1.6	C/N=C(\S)NCCCCCc1c[nH]cn1	10.1021/jm00012a025
	164626153	185796	0	None	4	6	Human	8.7	pKi	=	8.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	378	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1	10.1016/j.ejmech.2021.113190
	CHEMBL4875600	185796	0	None	4	6	Human	8.7	pKi	=	8.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	378	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccc(F)c1	10.1016/j.ejmech.2021.113190
	2801	161325	56	None	-12	28	Human	5.7	pKi	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21	nan
	CHEMBL1200710	161325	56	None	-12	28	Human	5.7	pKi	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21	nan
	CHEMBL415	161325	56	None	-12	28	Human	5.7	pKi	=	5.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21	nan
	156015243	177663	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1081	29	4	13	8.5	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4648203	177663	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1081	29	4	13	8.5	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4650564	177663	0	None	-	1	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1081	29	4	13	8.5	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3cc(S(=O)(=O)O)ccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	44304068	101877	0	None	-125	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	441	10	1	5	3.5	N[C@H](CC1CCCCC1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL303737	101877	0	None	-125	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	441	10	1	5	3.5	N[C@H](CC1CCCCC1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	44304030	199277	0	None	-154	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	511	11	1	5	4.4	N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL60189	199277	0	None	-154	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	511	11	1	5	4.4	N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	44304991	201372	0	None	-1659	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	424	12	0	5	3.6	CCCCCC(=O)c1ccc(OCCCN2CCN(S(=O)(=O)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL63631	201372	0	None	-1659	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	424	12	0	5	3.6	CCCCCC(=O)c1ccc(OCCCN2CCN(S(=O)(=O)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304294	201274	0	None	-97	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	485	10	1	5	3.9	N[C@H](Cc1cccc2ccccc12)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL63003	201274	0	None	-97	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	485	10	1	5	3.9	N[C@H](Cc1cccc2ccccc12)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL4520788	212225	6	None	3	25	Human	7.7	pKi	=	7.7	Binding	Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HRH2Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HRH2	ChEMBL		None	None	None		CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1	nan
	156021166	177762	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	908	25	3	8	10.3	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4647775	177762	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	908	25	3	8	10.3	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4651205	177762	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	908	25	3	8	10.3	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL5094663	213730	0	None	-	1	Human	7.7	pKi	=	7.7	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](C)c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	21830793	91403	5	None	-14125	46	Human	5.7	pKi	=	5.7	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	373	7	0	8	0.6	COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1	10.1016/j.bmc.2013.05.050
	CHEMBL2413154	91403	5	None	-14125	46	Human	5.7	pKi	=	5.7	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	373	7	0	8	0.6	COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1	10.1016/j.bmc.2013.05.050
	11948707	165614	0	None	-5248	13	Human	5.7	pKi	=	5.7	Binding	Binding affinity to histamine H2 receptor by radioligand binding assayBinding affinity to histamine H2 receptor by radioligand binding assay	ChEMBL	373	7	0	8	0.6	COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1	10.1016/j.bmcl.2006.01.052
	CHEMBL426317	165614	0	None	-5248	13	Human	5.7	pKi	=	5.7	Binding	Binding affinity to histamine H2 receptor by radioligand binding assayBinding affinity to histamine H2 receptor by radioligand binding assay	ChEMBL	373	7	0	8	0.6	COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1	10.1016/j.bmcl.2006.01.052
	168295543	192439	0	None	1	4	Human	6.7	pKi	=	6.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5209021	192439	0	None	1	4	Human	6.7	pKi	=	6.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222929	192439	0	None	1	4	Human	6.7	pKi	=	6.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
	44304459	172031	0	None	-575	3	Human	5.7	pKi	=	5.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	418	13	0	5	4.8	CCCCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL449040	172031	0	None	-575	3	Human	5.7	pKi	=	5.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	418	13	0	5	4.8	CCCCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	53320569	56559	0	None	3	2	Human	5.7	pKi	=	5.7	Binding	Inhibition of H2 receptorInhibition of H2 receptor	ChEMBL	269	3	1	1	3.1	Fc1cccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)c1	10.1016/j.bmcl.2010.11.075
	CHEMBL1643899	56559	0	None	3	2	Human	5.7	pKi	=	5.7	Binding	Inhibition of H2 receptorInhibition of H2 receptor	ChEMBL	269	3	1	1	3.1	Fc1cccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)c1	10.1016/j.bmcl.2010.11.075
	53320569	56559	0	None	3	2	Human	5.7	pKi	=	5.7	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	269	3	1	1	3.1	Fc1cccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)c1	10.1016/j.bmc.2013.07.045
	CHEMBL1643899	56559	0	None	3	2	Human	5.7	pKi	=	5.7	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	269	3	1	1	3.1	Fc1cccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)c1	10.1016/j.bmc.2013.07.045
	3823	49951	38	None	-66	11	Human	4.7	pKi	=	4.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	530	7	0	7	4.2	CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1	nan
	76973198	49951	38	None	-66	11	Human	4.7	pKi	=	4.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	530	7	0	7	4.2	CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1	nan
	CHEMBL157101	49951	38	None	-66	11	Human	4.7	pKi	=	4.7	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	530	7	0	7	4.2	CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1	nan
	168283536	192298	0	None	-53	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	3	4	1.6	CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5187758	192298	0	None	-53	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	3	4	1.6	CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222074	192298	0	None	-53	4	Human	5.7	pKi	=	5.7	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	3	4	1.6	CCCCCNC(=O)/N=C(/N)NCCCc1nnc(C)s1	10.1021/acs.jmedchem.1c00692
	44304021	102322	0	None	-562	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	374	8	0	5	3.4	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C=C(C)C)cc2)CC1	10.1016/s0960-894x(02)00309-8
	CHEMBL305313	102322	0	None	-562	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	374	8	0	5	3.4	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C=C(C)C)cc2)CC1	10.1016/s0960-894x(02)00309-8
	168278471	192246	0	None	-18	6	Human	7.6	pKi	=	7.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5183205	192246	0	None	-18	6	Human	7.6	pKi	=	7.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221757	192246	0	None	-18	6	Human	7.6	pKi	=	7.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	312	8	4	4	1.5	CCCCCNC(=O)/N=C(\N)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	44334235	4563	0	None	-199	3	Human	5.7	pKi	=	5.7	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	442	10	1	5	3.4	Cc1ccccc1S(=O)(=O)N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1	10.1016/s0960-894x(02)00685-6
	CHEMBL102929	4563	0	None	-199	3	Human	5.7	pKi	=	5.7	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	442	10	1	5	3.4	Cc1ccccc1S(=O)(=O)N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1	10.1016/s0960-894x(02)00685-6
	44334503	4926	0	None	-144	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	349	9	3	6	0.2	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](N)CO)C2)cc1	10.1016/s0960-894x(02)00685-6
	CHEMBL104994	4926	0	None	-144	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	349	9	3	6	0.2	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](N)CO)C2)cc1	10.1016/s0960-894x(02)00685-6
	44304036	96334	0	None	-407	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	360	8	0	5	3.0	C=C(C)C(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL264761	96334	0	None	-407	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	360	8	0	5	3.0	C=C(C)C(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304269	100078	0	None	-3548	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	423	11	0	5	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccncc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL291394	100078	0	None	-3548	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	423	11	0	5	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccncc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304037	102220	0	None	-6165	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	362	9	0	5	3.2	CCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL304714	102220	0	None	-6165	3	Human	4.7	pKi	=	4.7	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	362	9	0	5	3.2	CCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL5094083	213692	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		C=C(/N=C(\C)NCCCc1nnc(N)s1)NCCCCCCCCN	10.1016/j.bmcl.2021.128388
	164611143	184133	0	None	75	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	414	6	4	4	2.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(F)(F)F	10.1016/j.ejmech.2021.113190
	CHEMBL4850448	184133	0	None	75	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	414	6	4	4	2.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(F)(F)F	10.1016/j.ejmech.2021.113190
	44304438	201478	0	None	-2089	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	420	13	0	5	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CSCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL64235	201478	0	None	-2089	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	420	13	0	5	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CSCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304307	201542	0	None	-3548	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	388	12	0	4	4.2	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL64479	201542	0	None	-3548	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	388	12	0	4	4.2	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44335405	5034	0	None	-194	4	Human	4.6	pKi	=	4.6	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	321	6	1	4	2.9	N#Cc1ccc(-c2ccc(OCCCN3CCNCC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	CHEMBL105594	5034	0	None	-194	4	Human	4.6	pKi	=	4.6	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	321	6	1	4	2.9	N#Cc1ccc(-c2ccc(OCCCN3CCNCC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	44304415	200343	0	None	-9549	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	505	13	2	7	3.2	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](CO)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	CHEMBL60837	200343	0	None	-9549	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	505	13	2	7	3.2	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](CO)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	4543	169982	36	None	-15	29	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2ccccc21	nan
	CHEMBL1201156	169982	36	None	-15	29	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2ccccc21	nan
	CHEMBL445	169982	36	None	-15	29	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2ccccc21	nan
	44334214	4547	0	None	-380	3	Human	5.6	pKi	=	5.6	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	427	9	1	6	2.6	CC(=O)c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(C#N)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
	CHEMBL102840	4547	0	None	-380	3	Human	5.6	pKi	=	5.6	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	427	9	1	6	2.6	CC(=O)c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(C#N)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
	168268827	192177	0	None	3	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5179906	192177	0	None	3	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221314	192177	0	None	3	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
	168294770	192418	0	None	2	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5208327	192418	0	None	2	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222806	192418	0	None	2	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)cc1	10.1021/acs.jmedchem.1c00692
	44304325	199993	0	None	-1096	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	389	11	1	4	3.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)NCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL60620	199993	0	None	-1096	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	389	11	1	4	3.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)NCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44335368	4981	0	None	-63	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	393	7	0	5	3.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3cccc(C#N)c3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	CHEMBL105268	4981	0	None	-63	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	393	7	0	5	3.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3cccc(C#N)c3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	44335238	5020	0	None	-11220	4	Human	4.6	pKi	=	4.6	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	348	6	0	3	5.3	CC1CCCC(C)N1CCCOc1ccc(-c2ccc(C#N)cc2)cc1	10.1016/s0960-894x(02)00648-0
	CHEMBL105515	5020	0	None	-11220	4	Human	4.6	pKi	=	4.6	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	348	6	0	3	5.3	CC1CCCC(C)N1CCCOc1ccc(-c2ccc(C#N)cc2)cc1	10.1016/s0960-894x(02)00648-0
	44333987	108062	0	None	-26	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	433	9	2	6	2.8	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C2)cc1	10.1016/s0960-894x(02)00685-6
	CHEMBL320174	108062	0	None	-26	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	433	9	2	6	2.8	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@H](C)NC(=O)OC(C)(C)C)C2)cc1	10.1016/s0960-894x(02)00685-6
	44582675	189109	0	None	-40	15	Human	5.6	pKi	=	5.6	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	405	9	1	4	4.2	COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1	10.1016/j.bmc.2009.03.021
	CHEMBL515472	189109	0	None	-40	15	Human	5.6	pKi	=	5.6	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	405	9	1	4	4.2	COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1	10.1016/j.bmc.2009.03.021
	168283321	192293	0	None	2	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	364	7	4	4	2.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5183015	192293	0	None	2	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	364	7	4	4	2.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222057	192293	0	None	2	4	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	364	7	4	4	2.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1021/acs.jmedchem.1c00692
	44304437	100527	0	None	-426	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	404	11	1	5	3.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C(C)(C)O)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL294349	100527	0	None	-426	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	404	11	1	5	3.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C(C)(C)O)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304049	101668	0	None	-891	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	421	9	1	5	2.9	N[C@@H](C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1)c1ccccc1	10.1016/s0960-894x(02)00310-4
	CHEMBL302468	101668	0	None	-891	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	421	9	1	5	2.9	N[C@@H](C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1)c1ccccc1	10.1016/s0960-894x(02)00310-4
	146025727	171119	0	None	-93	27	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	411	3	0	5	6.4	FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12	10.1021/acs.jmedchem.9b00351
	CHEMBL4466483	171119	0	None	-93	27	Human	5.6	pKi	=	5.6	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	411	3	0	5	6.4	FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12	10.1021/acs.jmedchem.9b00351
	CHEMBL5087637	213779	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095891	213779	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	44304304	169496	0	None	-3981	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	423	9	0	6	3.5	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)/C=C/c3cccnc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	CHEMBL444307	169496	0	None	-3981	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	423	9	0	6	3.5	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)/C=C/c3cccnc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	1248	1396	27	None	-123	6	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	161	4	2	3	0.6	CN(CCCSC(=N)N)C	10.1016/j.bmcl.2010.10.041
	3077	1396	27	None	-123	6	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	161	4	2	3	0.6	CN(CCCSC(=N)N)C	10.1016/j.bmcl.2010.10.041
	90045	1396	27	None	-123	6	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	161	4	2	3	0.6	CN(CCCSC(=N)N)C	10.1016/j.bmcl.2010.10.041
	CHEMBL12344	1396	27	None	-123	6	Human	4.6	pKi	=	4.6	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	161	4	2	3	0.6	CN(CCCSC(=N)N)C	10.1016/j.bmcl.2010.10.041
	145988693	166613	0	None	-10	17	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	524	7	1	3	7.1	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
	CHEMBL4291048	166613	0	None	-10	17	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	524	7	1	3	7.1	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCN(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
	2520	202310	65	None	-20	11	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	nan
	CHEMBL1280	202310	65	None	-20	11	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	nan
	CHEMBL6966	202310	65	None	-20	11	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	nan
	2726	906	64	None	-85	72	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
	621	906	64	None	-85	72	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
	83	906	64	None	-85	72	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
	CHEMBL71	906	64	None	-85	72	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
	DB00477	906	64	None	-85	72	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	nan
	168273745	192206	0	None	-13	6	Human	7.6	pKi	=	7.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5178472	192206	0	None	-13	6	Human	7.6	pKi	=	7.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221451	192206	0	None	-13	6	Human	7.6	pKi	=	7.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	4	4	1.5	N/C(=N\C(=O)NCc1ccccc1)NCCCc1cnc(N)s1	10.1021/acs.jmedchem.1c00692
	155543832	172640	0	None	-234	7	Human	5.6	pKi	=	5.6	Binding	Inhibition of histamine H2 receptor (unknown origin)Inhibition of histamine H2 receptor (unknown origin)	ChEMBL	451	6	3	7	3.4	O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc32)[C@H]2C[C@@]2(CCl)[C@H]1O	10.1021/acs.jmedchem.8b01662
	CHEMBL4522864	172640	0	None	-234	7	Human	5.6	pKi	=	5.6	Binding	Inhibition of histamine H2 receptor (unknown origin)Inhibition of histamine H2 receptor (unknown origin)	ChEMBL	451	6	3	7	3.4	O[C@H]1[C@H](n2cnc3c(NC(C4CCC4)C4CCC4)nc(Cl)nc32)[C@H]2C[C@@]2(CCl)[C@H]1O	10.1021/acs.jmedchem.8b01662
	1204	1901	114	None	-173	23	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1247	1901	114	None	-173	23	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	1375	1901	114	None	-173	23	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	774	1901	114	None	-173	23	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	CHEMBL90	1901	114	None	-173	23	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	DB05381	1901	114	None	-173	23	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2021.128388
	CHEMBL5077939	213765	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095769	213765	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)O)c3ccccc3C2(C)C)c2cc(S(=O)(=O)[O-])ccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5093461	213777	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095884	213777	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2nnc(N)s2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	1204	1901	114	None	-173	23	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	1247	1901	114	None	-173	23	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	1375	1901	114	None	-173	23	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	774	1901	114	None	-173	23	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	CHEMBL90	1901	114	None	-173	23	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	DB05381	1901	114	None	-173	23	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.ejmech.2021.113190
	1204	1901	114	None	-173	23	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	1247	1901	114	None	-173	23	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	1375	1901	114	None	-173	23	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	774	1901	114	None	-173	23	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	CHEMBL90	1901	114	None	-173	23	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	DB05381	1901	114	None	-173	23	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.1c00692
	156015793	177684	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	880	23	3	8	9.5	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4645867	177684	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	880	23	3	8	9.5	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4650701	177684	0	None	-	1	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	880	23	3	8	9.5	C[N+]1=C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)C(C)(C)c2ccccc21	10.1021/acsmedchemlett.0c00033
	44304091	201262	0	None	-338	3	Human	5.6	pKi	=	5.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	432	14	0	5	5.2	CCCCCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL62949	201262	0	None	-338	3	Human	5.6	pKi	=	5.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	432	14	0	5	5.2	CCCCCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304516	164804	0	None	-630	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	357	8	1	5	1.5	O=C1C[C@H](N2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)CC2)N1	10.1016/s0960-894x(02)00310-4
	CHEMBL423666	164804	0	None	-630	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	357	8	1	5	1.5	O=C1C[C@H](N2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)CC2)N1	10.1016/s0960-894x(02)00310-4
	18609376	202656	61	None	-	1	Human	4.6	pKi	=	4.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	386	2	0	4	4.7	CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C	nan
	6279	202656	61	None	-	1	Human	4.6	pKi	=	4.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	386	2	0	4	4.7	CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C	nan
	CHEMBL717	202656	61	None	-	1	Human	4.6	pKi	=	4.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	386	2	0	4	4.7	CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C	nan
	44304256	167456	0	None	-1000	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	360	12	0	4	4.2	CCCCCC(=O)c1ccc(OCCCN2CCN(CCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL432144	167456	0	None	-1000	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	360	12	0	4	4.2	CCCCCC(=O)c1ccc(OCCCN2CCN(CCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304032	199802	0	None	-616	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	413	11	0	6	3.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cnco3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL60509	199802	0	None	-616	3	Human	4.6	pKi	=	4.6	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	413	11	0	6	3.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cnco3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	53324045	56776	0	None	-7	16	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	487	7	1	2	7.3	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1	10.1016/j.bmcl.2018.10.036
	CHEMBL1644980	56776	0	None	-7	16	Human	6.6	pKi	=	6.6	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	487	7	1	2	7.3	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccccc2)c2ccccc2)CC1	10.1016/j.bmcl.2018.10.036
	164614549	184360	0	None	-2	6	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	340	9	4	4	2.2	CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	CHEMBL4853668	184360	0	None	-2	6	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	340	9	4	4	2.2	CCCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	164619208	185080	0	None	446	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	378	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccccc1F	10.1016/j.ejmech.2021.113190
	CHEMBL4864852	185080	0	None	446	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	378	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccccc1F	10.1016/j.ejmech.2021.113190
	2284	3133	27	None	-53	28	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
	4926	3133	27	None	-53	28	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
	7281	3133	27	None	-53	28	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
	CHEMBL564	3133	27	None	-53	28	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
	DB00420	3133	27	None	-53	28	Human	5.6	pKi	=	5.6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	nan
	71525681	89298	0	None	-346	6	Human	5.6	pKi	=	5.6	Binding	Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells	ChEMBL	298	3	2	6	1.7	CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1	10.1016/j.bmcl.2013.02.091
	CHEMBL2376803	89298	0	None	-346	6	Human	5.6	pKi	=	5.6	Binding	Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells	ChEMBL	298	3	2	6	1.7	CNC1CN(c2nc(N)nc3cc(C4CCCC4)cnc23)C1	10.1016/j.bmcl.2013.02.091
	132060743	161686	0	None	-1	13	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	351	3	0	4	3.1	CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1	10.1016/j.ejmech.2018.02.024
	CHEMBL4163428	161686	0	None	-1	13	Human	6.5	pKi	=	6.5	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	351	3	0	4	3.1	CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1	10.1016/j.ejmech.2018.02.024
	3191	102385	93	None	-24	25	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	469	9	0	3	7.2	CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1	nan
	CHEMBL305660	102385	93	None	-24	25	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	469	9	0	3	7.2	CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1	nan
	44335387	108063	0	None	-1023	4	Human	4.5	pKi	=	4.5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	393	7	0	5	3.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	CHEMBL320178	108063	0	None	-1023	4	Human	4.5	pKi	=	4.5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	393	7	0	5	3.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	44334406	4794	0	None	-75	3	Human	6.5	pKi	=	6.5	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	462	10	1	5	3.8	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(Cl)cc3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
	CHEMBL104344	4794	0	None	-75	3	Human	6.5	pKi	=	6.5	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	462	10	1	5	3.8	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(Cl)cc3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
	44334368	108730	0	None	-57	3	Human	6.5	pKi	=	6.5	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	506	10	1	5	3.9	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(Br)cc3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
	CHEMBL321709	108730	0	None	-57	3	Human	6.5	pKi	=	6.5	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	506	10	1	5	3.9	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(Br)cc3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
	1204	1901	114	None	-173	23	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
	1247	1901	114	None	-173	23	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
	1375	1901	114	None	-173	23	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
	774	1901	114	None	-173	23	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
	CHEMBL90	1901	114	None	-173	23	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
	DB05381	1901	114	None	-173	23	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acsmedchemlett.0c00033
	44304291	201164	0	None	-6606	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	388	11	0	4	4.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL62527	201164	0	None	-6606	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	388	11	0	4	4.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
	168294767	192417	0	None	-117	20	Human	8.5	pKi	=	8.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5207281	192417	0	None	-117	20	Human	8.5	pKi	=	8.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222802	192417	0	None	-117	20	Human	8.5	pKi	=	8.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	313	8	4	5	0.9	CCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5078202	213760	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1	10.1016/j.bmcl.2021.128388
	CHEMBL5095695	213760	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCNC(=O)COc1ccc(/C=C/C2=[N+]3C(=Cc4ccc(-c5cccs5)n4[B-]3(F)F)C=C2)cc1	10.1016/j.bmcl.2021.128388
	164627241	185847	0	None	95	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	438	6	4	4	3.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Br)cc1	10.1016/j.ejmech.2021.113190
	CHEMBL4876267	185847	0	None	95	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	438	6	4	4	3.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Br)cc1	10.1016/j.ejmech.2021.113190
	164618508	185350	0	None	165	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	374	6	4	4	2.7	Cc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
	CHEMBL4869194	185350	0	None	165	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	374	6	4	4	2.7	Cc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
	10324985	76428	7	None	-223	17	Human	6.5	pKi	=	6.5	Binding	Binding affinity to histamine H2 receptorBinding affinity to histamine H2 receptor	ChEMBL	423	7	0	8	1.7	COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1	10.1021/jm050725j
	CHEMBL199824	76428	7	None	-223	17	Human	6.5	pKi	=	6.5	Binding	Binding affinity to histamine H2 receptorBinding affinity to histamine H2 receptor	ChEMBL	423	7	0	8	1.7	COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1	10.1021/jm050725j
	CHEMBL2068762	76428	7	None	-223	17	Human	6.5	pKi	=	6.5	Binding	Binding affinity to histamine H2 receptorBinding affinity to histamine H2 receptor	ChEMBL	423	7	0	8	1.7	COc1ccc2cccc(N3CCN(CCCCn4ncc(=O)n(C)c4=O)CC3)c2c1	10.1021/jm050725j
	156010170	177759	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	414	13	3	7	2.3	NCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4632998	177759	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	414	13	3	7	2.3	NCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	CHEMBL4651192	177759	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	414	13	3	7	2.3	NCCCCNc1c(NCCCOc2cccc(CN3CCCCC3)c2)c(=O)c1=O	10.1021/acsmedchemlett.0c00033
	168277996	192244	0	None	-20	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5173373	192244	0	None	-20	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221736	192244	0	None	-20	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	380	4	4	4	3.3	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCc2ccccc2)c1	10.1021/acs.jmedchem.1c00692
	168278543	192249	0	None	2	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	358	4	4	4	1.6	N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
	CHEMBL5184846	192249	0	None	2	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	358	4	4	4	1.6	N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221764	192249	0	None	2	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	358	4	4	4	1.6	N/C(=N\C(=O)NCc1ccccc1)NCC1CCc2nc(N)sc2C1	10.1021/acs.jmedchem.1c00692
	1599	2309	47	None	-154	15	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
	3955	2309	47	None	-154	15	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
	7215	2309	47	None	-154	15	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
	CHEMBL841	2309	47	None	-154	15	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
	DB00836	2309	47	None	-154	15	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	nan
	73349361	92116	0	None	-3	7	Human	5.5	pKi	=	5.5	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	279	4	0	1	3.3	CN(CCc1ccccc1)[C@H]1C2C3CC4C5C3CC2C5C41	10.1016/j.bmc.2013.07.045
	CHEMBL2432058	92116	0	None	-3	7	Human	5.5	pKi	=	5.5	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	279	4	0	1	3.3	CN(CCc1ccccc1)[C@H]1C2C3CC4C5C3CC2C5C41	10.1016/j.bmc.2013.07.045
	168294178	192433	0	None	1	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	5	4	4	4.4	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5205197	192433	0	None	1	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	5	4	4	4.4	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222887	192433	0	None	1	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	414	5	4	4	4.4	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)C2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
	164609493	183854	0	None	-1	6	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	350	6	4	5	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1	10.1016/j.ejmech.2021.113190
	CHEMBL4846380	183854	0	None	-1	6	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	350	6	4	5	1.9	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccco1	10.1016/j.ejmech.2021.113190
	164614907	184001	0	None	323	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	378	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(F)cc1	10.1016/j.ejmech.2021.113190
	CHEMBL4848697	184001	0	None	323	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	378	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(F)cc1	10.1016/j.ejmech.2021.113190
	44334521	107350	0	None	-36	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards human Histamine H2 receptor (For compound 11)Binding affinity towards human Histamine H2 receptor (For compound 11)	ChEMBL	262	6	1	4	1.7	CC(=O)c1ccc(OCCCN2CC[C@H](N)C2)cc1	10.1016/s0960-894x(02)00685-6
	CHEMBL319231	107350	0	None	-36	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards human Histamine H2 receptor (For compound 11)Binding affinity towards human Histamine H2 receptor (For compound 11)	ChEMBL	262	6	1	4	1.7	CC(=O)c1ccc(OCCCN2CC[C@H](N)C2)cc1	10.1016/s0960-894x(02)00685-6
	168286141	192322	0	None	2	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5192993	192322	0	None	2	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222231	192322	0	None	2	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	450	8	4	4	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCC(C)CCCc2ccccc2)cc1	10.1021/acs.jmedchem.1c00692
	50898777	56146	0	None	-29512	8	Human	5.5	pKi	=	5.5	Binding	Binding affinity to Histamine receptor H2Binding affinity to Histamine receptor H2	ChEMBL	441	9	1	6	3.6	COC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1	10.1016/j.bmc.2010.10.011
	CHEMBL1632158	56146	0	None	-29512	8	Human	5.5	pKi	=	5.5	Binding	Binding affinity to Histamine receptor H2Binding affinity to Histamine receptor H2	ChEMBL	441	9	1	6	3.6	COC(=O)CCCCCN1CCC(CNC(=O)c2c3n(c4ccccc24)CCCO3)CC1	10.1016/j.bmc.2010.10.011
	11723317	102421	0	None	-100	3	Human	5.5	pKi	=	5.5	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	316	9	3	2	2.8	S=C(NCCCCCc1c[nH]cn1)NCCc1ccccc1	10.1021/jm00012a025
	CHEMBL305929	102421	0	None	-100	3	Human	5.5	pKi	=	5.5	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	316	9	3	2	2.8	S=C(NCCCCCc1c[nH]cn1)NCCc1ccccc1	10.1021/jm00012a025
	164610421	184678	0	None	7	2	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	332	5	4	4	2.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4858567	184678	0	None	7	2	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	332	5	4	4	2.1	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)Nc1ccccc1	10.1016/j.ejmech.2021.113190
	71525679	89296	0	None	-223	6	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells	ChEMBL	272	3	2	6	1.0	CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1	10.1016/j.bmcl.2013.02.091
	CHEMBL2376801	89296	0	None	-223	6	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]histamine from human histamine H2 receptor expressed in HEK cellsDisplacement of [3H]histamine from human histamine H2 receptor expressed in HEK cells	ChEMBL	272	3	2	6	1.0	CCc1cnc2c(N3CC[C@@H](NC)C3)nc(N)nc2c1	10.1016/j.bmcl.2013.02.091
	10420190	205033	0	None	-31	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	195	8	2	2	2.3	NCCCCCCCCc1c[nH]cn1	10.1021/jm00002a008
	CHEMBL90063	205033	0	None	-31	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	195	8	2	2	2.3	NCCCCCCCCc1c[nH]cn1	10.1021/jm00002a008
	44304558	100550	0	None	-10000	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	374	11	0	4	3.8	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL294502	100550	0	None	-10000	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	374	11	0	4	3.8	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)CC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304288	101737	0	None	-14791	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	386	11	0	4	3.8	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C3CC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL302886	101737	0	None	-14791	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	386	11	0	4	3.8	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)C3CC3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304451	101820	0	None	-1862	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	417	12	1	5	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	CHEMBL303369	101820	0	None	-1862	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	417	12	1	5	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	25128822	186898	0	None	-5888	5	Human	4.5	pKi	=	4.5	Binding	Displacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation counting	ChEMBL	295	1	1	5	1.6	CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1	10.1016/j.bmcl.2015.12.035
	CHEMBL494093	186898	0	None	-5888	5	Human	4.5	pKi	=	4.5	Binding	Displacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation counting	ChEMBL	295	1	1	5	1.6	CN1CCN(c2nc(N)nc3c2CCc2ccccc2-3)CC1	10.1016/j.bmcl.2015.12.035
	44455426	154610	0	None	-44	12	Human	5.5	pKi	=	5.5	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	405	9	1	4	4.2	COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1	10.1016/j.bmc.2009.03.021
	CHEMBL402143	154610	0	None	-44	12	Human	5.5	pKi	=	5.5	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	405	9	1	4	4.2	COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1	10.1016/j.bmc.2009.03.021
	71456046	83661	0	None	-2089	7	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	389	6	0	4	4.2	COc1ccccc1N1CCN(Cc2cc(CN(C)C)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
	CHEMBL2207637	83661	0	None	-2089	7	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	389	6	0	4	4.2	COc1ccccc1N1CCN(Cc2cc(CN(C)C)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
	44307779	201865	0	None	-275	4	Human	5.5	pKi	=	5.5	Binding	Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor	ChEMBL	332	2	0	2	4.7	C(#Cc1c2c(nc3ccccc13)CCCCC2)CCN1CCCCC1	10.1016/s0960-894x(03)00356-1
	CHEMBL66660	201865	0	None	-275	4	Human	5.5	pKi	=	5.5	Binding	Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor	ChEMBL	332	2	0	2	4.7	C(#Cc1c2c(nc3ccccc13)CCCCC2)CCN1CCCCC1	10.1016/s0960-894x(03)00356-1
	156015643	177720	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1001	28	3	11	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4645213	177720	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1001	28	3	11	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4650968	177720	0	None	-	1	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1001	28	3	11	9.2	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL5092102	213572	0	None	-	1	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		NCCCCCCCCNC(=O)/N=C(\N)NCCCc1c[nH]cn1	10.1016/j.bmcl.2021.128388
	168274129	192207	0	None	-6	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	370	12	5	6	1.0	NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5176780	192207	0	None	-6	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	370	12	5	6	1.0	NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221468	192207	0	None	-6	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	370	12	5	6	1.0	NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	44334212	4561	0	None	-72	3	Human	6.5	pKi	=	6.5	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	456	11	1	5	3.7	CCc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
	CHEMBL102925	4561	0	None	-72	3	Human	6.5	pKi	=	6.5	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	456	11	1	5	3.7	CCc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
	168273549	192201	0	None	1	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5174342	192201	0	None	1	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221438	192201	0	None	1	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	436	6	4	4	4.3	Cc1ccc(CC(C)CNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
	44335430	5225	0	None	-144	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	374	7	0	5	4.0	CCOC(=O)N1CCN(CCCOc2ccc(-c3cccs3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	CHEMBL106602	5225	0	None	-144	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	374	7	0	5	4.0	CCOC(=O)N1CCN(CCCOc2ccc(-c3cccs3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	44304064	102337	0	None	-1096	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	451	10	2	6	2.5	N[C@H](Cc1ccc(O)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL305371	102337	0	None	-1096	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	451	10	2	6	2.5	N[C@H](Cc1ccc(O)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	164611807	184401	0	None	162	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	376	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4854278	184401	0	None	162	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	376	6	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)N[C@@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	122442272	137820	0	None	-120	15	Human	5.5	pKi	=	5.5	Binding	Binding affinity to histamine H2 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H2 receptor (unknown origin) by radioligand binding assay	ChEMBL	239	5	1	2	2.6	C=CCOc1cc(F)c(F)cc1C1CC1CN	10.1021/acs.jmedchem.5b01153
	CHEMBL3769968	137820	0	None	-120	15	Human	5.5	pKi	=	5.5	Binding	Binding affinity to histamine H2 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H2 receptor (unknown origin) by radioligand binding assay	ChEMBL	239	5	1	2	2.6	C=CCOc1cc(F)c(F)cc1C1CC1CN	10.1021/acs.jmedchem.5b01153
	CHEMBL3771384	137820	0	None	-120	15	Human	5.5	pKi	=	5.5	Binding	Binding affinity to histamine H2 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H2 receptor (unknown origin) by radioligand binding assay	ChEMBL	239	5	1	2	2.6	C=CCOc1cc(F)c(F)cc1C1CC1CN	10.1021/acs.jmedchem.5b01153
	122442272	137820	0	None	-120	15	Human	5.5	pKi	=	5.5	Binding	Binding affinity to histamine H2 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H2 receptor (unknown origin) by radioligand binding assay	ChEMBL	239	5	1	2	2.6	C=CCOc1cc(F)c(F)cc1C1CC1CN	10.1021/acs.jmedchem.5b01153
	CHEMBL3769968	137820	0	None	-120	15	Human	5.5	pKi	=	5.5	Binding	Binding affinity to histamine H2 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H2 receptor (unknown origin) by radioligand binding assay	ChEMBL	239	5	1	2	2.6	C=CCOc1cc(F)c(F)cc1C1CC1CN	10.1021/acs.jmedchem.5b01153
	CHEMBL3771384	137820	0	None	-120	15	Human	5.5	pKi	=	5.5	Binding	Binding affinity to histamine H2 receptor (unknown origin) by radioligand binding assayBinding affinity to histamine H2 receptor (unknown origin) by radioligand binding assay	ChEMBL	239	5	1	2	2.6	C=CCOc1cc(F)c(F)cc1C1CC1CN	10.1021/acs.jmedchem.5b01153
	44335336	4490	0	None	-263	4	Human	4.5	pKi	=	4.5	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	335	6	1	4	3.4	N#Cc1ccc(-c2ccc(OCCCN3CCC(N)CC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	CHEMBL102452	4490	0	None	-263	4	Human	4.5	pKi	=	4.5	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	335	6	1	4	3.4	N#Cc1ccc(-c2ccc(OCCCN3CCC(N)CC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	168268680	192164	0	None	1	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5172675	192164	0	None	1	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221210	192164	0	None	1	4	Human	6.5	pKi	=	6.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2ccc(-c3sc(N)nc3C)cc2)cc1	10.1021/acs.jmedchem.1c00692
	44304445	201299	0	None	-30	3	Human	5.5	pKi	=	5.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	531	14	1	6	5.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](CC(C)C)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	CHEMBL63112	201299	0	None	-30	3	Human	5.5	pKi	=	5.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	531	14	1	6	5.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](CC(C)C)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	44304462	201193	0	None	-4897	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	405	12	2	6	1.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)CO)CC2)cc1	10.1016/s0960-894x(02)00310-4
	CHEMBL62660	201193	0	None	-4897	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	405	12	2	6	1.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)CO)CC2)cc1	10.1016/s0960-894x(02)00310-4
	44304741	201228	0	None	-3388	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	466	13	1	6	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)Cc3ccncc3)CC2)cc1	10.1016/s0960-894x(02)00310-4
	CHEMBL62808	201228	0	None	-3388	3	Human	4.5	pKi	=	4.5	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	466	13	1	6	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)Cc3ccncc3)CC2)cc1	10.1016/s0960-894x(02)00310-4
	73355417	92107	0	None	1	3	Human	5.5	pKi	=	5.5	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	251	3	1	1	2.9	c1ccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc1	10.1016/j.bmc.2013.07.045
	CHEMBL2432045	92107	0	None	1	3	Human	5.5	pKi	=	5.5	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	251	3	1	1	2.9	c1ccc(CN[C@H]2C3C4CC5C6C4CC3C6C52)cc1	10.1016/j.bmc.2013.07.045
	237	203157	43	None	-3	13	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	nan
	CHEMBL546257	203157	43	None	-3	13	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	nan
	CHEMBL554190	203157	43	None	-3	13	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	nan
	CHEMBL7568	203157	43	None	-3	13	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	nan
	164614841	184692	0	None	223	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	388	7	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(C)C	10.1016/j.ejmech.2021.113190
	CHEMBL4858849	184692	0	None	223	4	Human	7.5	pKi	=	7.5	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	388	7	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)C(C)C	10.1016/j.ejmech.2021.113190
	44333988	4467	0	None	-93	3	Human	5.5	pKi	=	5.5	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	367	8	1	5	2.6	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3cccnc3)C2)cc1	10.1016/s0960-894x(02)00685-6
	CHEMBL102331	4467	0	None	-93	3	Human	5.5	pKi	=	5.5	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	367	8	1	5	2.6	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3cccnc3)C2)cc1	10.1016/s0960-894x(02)00685-6
	156013896	177665	0	None	-1548	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranes	ChEMBL	401	9	1	2	5.1	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1	10.1021/acs.jmedchem.0c00160
	CHEMBL4635634	177665	0	None	-1548	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranes	ChEMBL	401	9	1	2	5.1	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1	10.1021/acs.jmedchem.0c00160
	CHEMBL4650570	177665	0	None	-1548	4	Human	5.5	pKi	=	5.5	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranesDisplacement of [3H]UR-DE257 from Gsalphas-coupled human recombinant H2R expressed in baculovirus infected Sf9 insect cell membranes	ChEMBL	401	9	1	2	5.1	Cc1cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc(C)[n+]1CCCCc1c[nH]cn1	10.1021/acs.jmedchem.0c00160
	135398737	944	89	None	-64	91	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
	38	944	89	None	-64	91	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
	722	944	89	None	-64	91	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
	CHEMBL42	944	89	None	-64	91	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
	DB00363	944	89	None	-64	91	Human	5.5	pKi	=	5.5	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	nan
	71455894	83388	0	None	-3	12	Human	5.5	pKi	=	5.5	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	325	4	1	4	2.0	COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC	10.1016/j.bmcl.2012.08.046
	CHEMBL2205827	83388	0	None	-3	12	Human	5.5	pKi	=	5.5	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	325	4	1	4	2.0	COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC	10.1016/j.bmcl.2012.08.046
	71455894	83388	0	None	-3	12	Human	5.5	pKi	=	5.5	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	325	4	1	4	2.0	COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC	10.1016/j.bmc.2013.07.045
	CHEMBL2205827	83388	0	None	-3	12	Human	5.5	pKi	=	5.5	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	325	4	1	4	2.0	COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1OC	10.1016/j.bmc.2013.07.045
	44335407	171278	0	None	-15	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	452	8	0	5	4.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(OC(F)(F)F)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	CHEMBL446885	171278	0	None	-15	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	452	8	0	5	4.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(OC(F)(F)F)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	26987	936	29	None	-177	21	Human	6.4	pKi	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
	6063	936	29	None	-177	21	Human	6.4	pKi	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
	671	936	29	None	-177	21	Human	6.4	pKi	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
	CHEMBL1626	936	29	None	-177	21	Human	6.4	pKi	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
	DB00283	936	29	None	-177	21	Human	6.4	pKi	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	nan
	155513890	169254	0	None	-177	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting methodDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting method	ChEMBL	369	2	2	5	4.1	Clc1ccc(C#Cc2nc(N[C@H]3C[C@H]4CC[C@@H]3C4)c3nc[nH]c3n2)s1	10.1039/C8MD00317C
	CHEMBL4439593	169254	0	None	-177	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting methodDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting method	ChEMBL	369	2	2	5	4.1	Clc1ccc(C#Cc2nc(N[C@H]3C[C@H]4CC[C@@H]3C4)c3nc[nH]c3n2)s1	10.1039/C8MD00317C
	126720252	164123	0	None	-12	12	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method	ChEMBL	697	15	2	6	9.2	NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1	10.1021/acs.jmedchem.8b00168
	CHEMBL4216870	164123	0	None	-12	12	Human	6.4	pKi	=	6.4	Binding	Displacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method	ChEMBL	697	15	2	6	9.2	NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1	10.1021/acs.jmedchem.8b00168
	164618283	183961	0	None	158	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	390	7	4	5	2.4	COc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
	CHEMBL4848026	183961	0	None	158	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	390	7	4	5	2.4	COc1ccc(C(C)NC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
	44304282	201423	0	None	-12	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	410	8	0	5	3.8	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3cccc(C)c3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	CHEMBL64021	201423	0	None	-12	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	410	8	0	5	3.8	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3cccc(C)c3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	44304383	201612	0	None	-371	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	418	12	0	5	4.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL64775	201612	0	None	-371	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	418	12	0	5	4.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)OCC(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304753	201505	0	None	-4073	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	466	13	1	6	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)Cc3ccncc3)CC2)cc1	10.1016/s0960-894x(02)00310-4
	CHEMBL64321	201505	0	None	-4073	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	466	13	1	6	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@H](N)Cc3ccncc3)CC2)cc1	10.1016/s0960-894x(02)00310-4
	9818650	201831	0	None	-1513	4	Human	5.4	pKi	=	5.4	Binding	Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor	ChEMBL	323	5	1	3	4.4	c1ccc2c(NCCCN3CCCC3)c3c(nc2c1)CCCCC3	10.1016/s0960-894x(03)00356-1
	CHEMBL66388	201831	0	None	-1513	4	Human	5.4	pKi	=	5.4	Binding	Compound was tested for its binding affinity towards human H2 receptorCompound was tested for its binding affinity towards human H2 receptor	ChEMBL	323	5	1	3	4.4	c1ccc2c(NCCCN3CCCC3)c3c(nc2c1)CCCCC3	10.1016/s0960-894x(03)00356-1
	CHEMBL4777443	212286	0	None	-181	14	Human	5.4	pKi	=	5.4	Binding	Selectivity interaction (GPCR panel (PDSP screen)) EUB0000741a HRH2Selectivity interaction (GPCR panel (PDSP screen)) EUB0000741a HRH2	ChEMBL		None	None	None		CC(C)(C)OC(=O)N1CCCC1CN[C@H]1CC[C@@](c2cc(F)ccc2F)(S(=O)(=O)c2ccc(Cl)cc2)CC1	nan
	44334782	5353	0	None	-91	3	Human	6.4	pKi	=	6.4	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	442	10	1	5	3.4	Cc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
	CHEMBL107293	5353	0	None	-91	3	Human	6.4	pKi	=	6.4	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	442	10	1	5	3.4	Cc1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
	168276867	192233	0	None	-1	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5174278	192233	0	None	-1	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221653	192233	0	None	-1	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	662	11	8	8	4.8	Cc1nc(N)sc1-c1cccc(N/C(N)=N/C(=O)NCCCCCCNC(=O)/N=C(\N)Nc2cccc(-c3sc(N)nc3C)c2)c1	10.1021/acs.jmedchem.1c00692
	44335571	5200	0	None	-1513	4	Human	4.4	pKi	=	4.4	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	322	6	0	4	3.3	N#Cc1ccc(-c2ccc(OCCCN3CCOCC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	CHEMBL106483	5200	0	None	-1513	4	Human	4.4	pKi	=	4.4	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	322	6	0	4	3.3	N#Cc1ccc(-c2ccc(OCCCN3CCOCC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	44304450	201179	0	None	-478	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	417	12	1	5	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	CHEMBL62592	201179	0	None	-478	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	417	12	1	5	3.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](N)C(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	168283097	192291	0	None	-22	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	311	9	4	5	0.8	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1	10.1021/acs.jmedchem.1c00692
	CHEMBL5186770	192291	0	None	-22	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	311	9	4	5	0.8	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222043	192291	0	None	-22	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	311	9	4	5	0.8	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)o1	10.1021/acs.jmedchem.1c00692
	168284480	192308	0	None	-22	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	330	6	4	4	1.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5197548	192308	0	None	-22	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	330	6	4	4	1.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222137	192308	0	None	-22	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	330	6	4	4	1.3	Cc1nc(N)oc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1021/acs.jmedchem.1c00692
	73346334	92109	0	None	-4	7	Human	5.4	pKi	=	5.4	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	265	4	1	1	3.0	c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)cc1	10.1016/j.bmc.2013.07.045
	CHEMBL2432048	92109	0	None	-4	7	Human	5.4	pKi	=	5.4	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	265	4	1	1	3.0	c1ccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)cc1	10.1016/j.bmc.2013.07.045
	164608815	183872	0	None	1	6	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	380	7	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1016/j.ejmech.2021.113190
	CHEMBL4846638	183872	0	None	1	6	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	380	7	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)C1CCCCC1	10.1016/j.ejmech.2021.113190
	4011	81996	43	None	-27	23	Human	6.4	pKi	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	4	1	1	4.2	CNCCCC12CCC(c3ccccc31)c1ccccc12	nan
	CHEMBL21731	81996	43	None	-27	23	Human	6.4	pKi	=	6.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	4	1	1	4.2	CNCCCC12CCC(c3ccccc31)c1ccccc12	nan
	44335237	5052	0	None	-144	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	407	7	0	5	4.1	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(C#N)cc3C)cc2)CC1	10.1016/s0960-894x(02)00648-0
	CHEMBL105669	5052	0	None	-144	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	407	7	0	5	4.1	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(C#N)cc3C)cc2)CC1	10.1016/s0960-894x(02)00648-0
	3032915	15321	20	None	-25	6	Human	5.4	pKi	=	5.4	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	10.1021/jm00012a025
	CHEMBL12160	15321	20	None	-25	6	Human	5.4	pKi	=	5.4	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	10.1021/jm00012a025
	10085839	202797	0	None	-125	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	294	7	3	2	2.9	S=C(NCCCCCc1c[nH]cn1)NC1CCCCC1	10.1021/jm00012a025
	CHEMBL72571	202797	0	None	-125	3	Human	5.4	pKi	=	5.4	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	294	7	3	2	2.9	S=C(NCCCCCc1c[nH]cn1)NC1CCCCC1	10.1021/jm00012a025
	3032915	15321	20	None	-25	6	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	10.1016/j.bmcl.2010.10.041
	CHEMBL12160	15321	20	None	-25	6	Human	5.4	pKi	=	5.4	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	10.1016/j.bmcl.2010.10.041
	164619427	185487	0	None	7	2	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	380	5	4	4	3.1	N/C(=N\C(=O)NCCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
	CHEMBL4871221	185487	0	None	7	2	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	380	5	4	4	3.1	N/C(=N\C(=O)NCCc1ccccc1)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
	1204	1901	114	None	-173	23	Human	4.4	pKi	=	4.4	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm00002a008
	1247	1901	114	None	-173	23	Human	4.4	pKi	=	4.4	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm00002a008
	1375	1901	114	None	-173	23	Human	4.4	pKi	=	4.4	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm00002a008
	774	1901	114	None	-173	23	Human	4.4	pKi	=	4.4	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm00002a008
	CHEMBL90	1901	114	None	-173	23	Human	4.4	pKi	=	4.4	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm00002a008
	DB05381	1901	114	None	-173	23	Human	4.4	pKi	=	4.4	Binding	Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.Binding affinity against human H2 receptor by the displacement of [125I]iodoaminopotentidine, bound to membranes of CHO cells.	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/jm00002a008
	44304387	201239	0	None	-7943	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	334	7	0	5	2.4	CCOC(=O)N1CCN(CCCOc2ccc(C(C)=O)cc2)CC1	10.1016/s0960-894x(02)00309-8
	CHEMBL62840	201239	0	None	-7943	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	334	7	0	5	2.4	CCOC(=O)N1CCN(CCCOc2ccc(C(C)=O)cc2)CC1	10.1016/s0960-894x(02)00309-8
	44304312	162237	0	None	-1348	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	453	10	1	5	2.9	N[C@H](Cc1ccc(F)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL417215	162237	0	None	-1348	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	453	10	1	5	2.9	N[C@H](Cc1ccc(F)cc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	164612037	184795	0	None	-85	20	Human	8.4	pKi	=	8.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	326	8	4	4	1.8	CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	CHEMBL4860528	184795	0	None	-85	20	Human	8.4	pKi	=	8.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	326	8	4	4	1.8	CCCCCNC(=O)/N=C(\N)NCCCc1sc(N)nc1C	10.1016/j.ejmech.2021.113190
	46884734	7890	0	None	-6	2	Human	8.4	pKi	=	8.4	Binding	Inhibition of H2 receptorInhibition of H2 receptor	ChEMBL	341	6	0	4	3.7	COc1nccnc1[C@H](C)C1=C(CCN(C)C)Cc2cc(F)ccc21	10.1016/j.bmcl.2010.07.117
	CHEMBL1090526	7890	0	None	-6	2	Human	8.4	pKi	=	8.4	Binding	Inhibition of H2 receptorInhibition of H2 receptor	ChEMBL	341	6	0	4	3.7	COc1nccnc1[C@H](C)C1=C(CCN(C)C)Cc2cc(F)ccc21	10.1016/j.bmcl.2010.07.117
	168273471	192199	0	None	12	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	596	17	8	10	0.7	N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5173079	192199	0	None	12	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	596	17	8	10	0.7	N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221433	192199	0	None	12	4	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	596	17	8	10	0.7	N/C(=N\C(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	71452382	83380	0	None	-12	10	Human	6.4	pKi	=	6.4	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	309	4	1	3	2.0	COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1	10.1016/j.bmcl.2012.08.046
	CHEMBL2205812	83380	0	None	-12	10	Human	6.4	pKi	=	6.4	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	309	4	1	3	2.0	COc1ccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1	10.1016/j.bmcl.2012.08.046
	44334035	109556	0	None	-79	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	476	10	1	7	4.1	O=C(N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1)c1csc(-c2cccnc2)n1	10.1016/s0960-894x(02)00685-6
	CHEMBL323517	109556	0	None	-79	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	476	10	1	7	4.1	O=C(N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1)c1csc(-c2cccnc2)n1	10.1016/s0960-894x(02)00685-6
	44334281	4691	0	None	-128	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	433	9	2	6	2.8	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](C)NC(=O)OC(C)(C)C)C2)cc1	10.1016/s0960-894x(02)00685-6
	CHEMBL103828	4691	0	None	-128	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	433	9	2	6	2.8	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@@H](C)NC(=O)OC(C)(C)C)C2)cc1	10.1016/s0960-894x(02)00685-6
	145980875	166154	0	None	-3	11	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	443	7	1	2	6.2	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCCc2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
	CHEMBL4282702	166154	0	None	-3	11	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	443	7	1	2	6.2	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCCc2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
	1530	2151	44	None	-151	20	Human	5.4	pKi	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
	3827	2151	44	None	-151	20	Human	5.4	pKi	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
	7206	2151	44	None	-151	20	Human	5.4	pKi	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
	CHEMBL534	2151	44	None	-151	20	Human	5.4	pKi	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
	DB00920	2151	44	None	-151	20	Human	5.4	pKi	=	5.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	nan
	CHEMBL5090859	213509	0	None	-	1	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C	10.1016/j.bmcl.2021.128388
	44478385	5699	2	None	-70	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in Sf9 cellsDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in Sf9 cells	ChEMBL	342	9	3	4	2.5	N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1	10.1021/jm900526h
	CHEMBL1078642	5699	2	None	-70	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in Sf9 cellsDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in Sf9 cells	ChEMBL	342	9	3	4	2.5	N#C/N=C(/NCCCCc1c[nH]cn1)NCCSc1ccccc1	10.1021/jm900526h
	44304012	201144	0	None	-21379	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	389	11	1	5	2.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](C)N)CC2)cc1	10.1016/s0960-894x(02)00310-4
	CHEMBL62421	201144	0	None	-21379	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	389	11	1	5	2.7	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](C)N)CC2)cc1	10.1016/s0960-894x(02)00310-4
	1129	1591	89	None	-	1	Human	7.4	pKi	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
	3325	1591	89	None	-	1	Human	7.4	pKi	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
	5353622	1591	89	None	-	1	Human	7.4	pKi	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
	5702160	1591	89	None	-	1	Human	7.4	pKi	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
	7074	1591	89	None	-	1	Human	7.4	pKi	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
	CHEMBL902	1591	89	None	-	1	Human	7.4	pKi	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
	DB00927	1591	89	None	-	1	Human	7.4	pKi	=	7.4	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	nan
	12016525	201226	0	None	-2041	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359	8	1	5	1.5	C[C@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL62804	201226	0	None	-2041	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359	8	1	5	1.5	C[C@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	71457844	83662	0	None	-2187	7	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	429	6	0	4	5.1	COc1ccccc1N1CCN(Cc2cc(CN3CCCCC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
	CHEMBL2207638	83662	0	None	-2187	7	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	429	6	0	4	5.1	COc1ccccc1N1CCN(Cc2cc(CN3CCCCC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
	50878551	90314	60	None	-109	18	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis	ChEMBL	270	8	1	2	3.4	C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12	10.1016/j.bmcl.2013.03.066
	CHEMBL2391541	90314	60	None	-109	18	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis	ChEMBL	270	8	1	2	3.4	C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12	10.1016/j.bmcl.2013.03.066
	164608941	183801	0	None	75	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	390	7	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4845733	183801	0	None	75	4	Human	6.4	pKi	=	6.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	390	7	4	4	2.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC[C@@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	50878551	90314	60	None	-109	18	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis	ChEMBL	270	8	1	2	3.4	C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12	10.1016/j.bmcl.2013.03.066
	CHEMBL2391541	90314	60	None	-109	18	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]Tiotidine from human recombinant histamine H2 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis	ChEMBL	270	8	1	2	3.4	C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12	10.1016/j.bmcl.2013.03.066
	44304309	168650	0	None	-630	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	414	8	0	5	3.6	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(F)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	CHEMBL440864	168650	0	None	-630	3	Human	4.4	pKi	=	4.4	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	414	8	0	5	3.6	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(F)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	164627020	185826	0	None	144	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	422	7	4	4	3.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4876025	185826	0	None	144	4	Human	7.4	pKi	=	7.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	422	7	4	4	3.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
	53324553	56560	0	None	-6	10	Human	5.4	pKi	=	5.4	Binding	Inhibition of H2 receptorInhibition of H2 receptor	ChEMBL	283	4	1	1	3.1	Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1	10.1016/j.bmcl.2010.11.075
	CHEMBL1643900	56560	0	None	-6	10	Human	5.4	pKi	=	5.4	Binding	Inhibition of H2 receptorInhibition of H2 receptor	ChEMBL	283	4	1	1	3.1	Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1	10.1016/j.bmcl.2010.11.075
	53324553	56560	0	None	-6	10	Human	5.4	pKi	=	5.4	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	283	4	1	1	3.1	Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1	10.1016/j.bmc.2013.07.045
	CHEMBL1643900	56560	0	None	-6	10	Human	5.4	pKi	=	5.4	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	283	4	1	1	3.1	Fc1cccc(CCN[C@H]2C3C4CC5C6C4CC3C6C52)c1	10.1016/j.bmc.2013.07.045
	53325861	56561	0	None	-2	3	Human	5.4	pKi	=	5.4	Binding	Inhibition of H2 receptorInhibition of H2 receptor	ChEMBL	297	4	0	1	3.4	CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41	10.1016/j.bmcl.2010.11.075
	CHEMBL1643902	56561	0	None	-2	3	Human	5.4	pKi	=	5.4	Binding	Inhibition of H2 receptorInhibition of H2 receptor	ChEMBL	297	4	0	1	3.4	CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41	10.1016/j.bmcl.2010.11.075
	53325861	56561	0	None	-2	3	Human	5.4	pKi	=	5.4	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	297	4	0	1	3.4	CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41	10.1016/j.bmc.2013.07.045
	CHEMBL1643902	56561	0	None	-2	3	Human	5.4	pKi	=	5.4	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	297	4	0	1	3.4	CN(CCc1cccc(F)c1)[C@H]1C2C3CC4C5C3CC2C5C41	10.1016/j.bmc.2013.07.045
	44304449	198815	0	None	-309	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	531	14	1	6	5.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](CC(C)C)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	CHEMBL59870	198815	0	None	-309	3	Human	5.4	pKi	=	5.4	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	531	14	1	6	5.3	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)[C@@H](CC(C)C)NC(=O)OC(C)(C)C)CC2)cc1	10.1016/s0960-894x(02)00310-4
	164626509	185753	0	None	3	2	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	358	3	4	4	3.2	N/C(=N\C(=O)NC1CCCCC1)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
	CHEMBL4874969	185753	0	None	3	2	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	358	3	4	4	3.2	N/C(=N\C(=O)NC1CCCCC1)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
	168280339	192263	0	None	-52	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	8	3	5	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5188592	192263	0	None	-52	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	8	3	5	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221885	192263	0	None	-52	4	Human	5.4	pKi	=	5.4	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	8	3	5	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCn1cc(CN(C)C)nn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	168294166	192412	0	None	1	4	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5209081	192412	0	None	1	4	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222775	192412	0	None	1	4	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	360	6	4	4	3.3	CCCCCNC(=O)/N=C(\N)Nc1ccc(-c2sc(N)nc2C)cc1	10.1021/acs.jmedchem.1c00692
	44304014	100318	0	None	-5370	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	431	10	1	6	2.3	CC(C)(C)OC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL293033	100318	0	None	-5370	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	431	10	1	6	2.3	CC(C)(C)OC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	164622153	184986	0	None	95	4	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	394	6	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Cl)cc1	10.1016/j.ejmech.2021.113190
	CHEMBL4863347	184986	0	None	95	4	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	394	6	4	4	3.0	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1ccc(Cl)cc1	10.1016/j.ejmech.2021.113190
	71459761	83666	0	None	-75	7	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	540	7	0	5	6.1	COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
	CHEMBL2207642	83666	0	None	-75	7	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	540	7	0	5	6.1	COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccc(Cl)cc4)CC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
	44334556	106783	0	None	-77	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	449	10	3	7	1.7	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@H](CO)NC(=O)OC(C)(C)C)C2)cc1	10.1016/s0960-894x(02)00685-6
	CHEMBL316968	106783	0	None	-77	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	449	10	3	7	1.7	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)[C@H](CO)NC(=O)OC(C)(C)C)C2)cc1	10.1016/s0960-894x(02)00685-6
	44304377	201089	0	None	-2570	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	424	11	0	6	3.5	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cnccn3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL62115	201089	0	None	-2570	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	424	11	0	6	3.5	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cnccn3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304313	199900	0	None	-2041	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	441	10	1	6	2.8	N[C@H](Cc1ccsc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL60559	199900	0	None	-2041	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	441	10	1	6	2.8	N[C@H](Cc1ccsc1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	44304277	100480	0	None	-645	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	401	10	1	5	2.4	CN[C@@H](C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1)C(C)C	10.1016/s0960-894x(02)00310-4
	CHEMBL294087	100480	0	None	-645	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	401	10	1	5	2.4	CN[C@@H](C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1)C(C)C	10.1016/s0960-894x(02)00310-4
	1231	924	112	None	-2	7	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
	2756	924	112	None	-2	7	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
	645	924	112	None	-2	7	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
	CHEMBL30	924	112	None	-2	7	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
	DB00501	924	112	None	-2	7	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation countingDisplacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1021/acs.jmedchem.6b01422
	44467360	124015	0	None	3	2	Human	5.3	pKi	=	5.3	Binding	Inhibition of human histamine H2 receptorInhibition of human histamine H2 receptor	ChEMBL	420	3	2	6	1.5	COc1nc(N2C[C@H]3C(=O)N(C)C(=N)N[C@@]3(c3ccc(F)cc3F)C2)nc(C)c1F	10.1021/acs.jmedchem.5b01995
	CHEMBL3640290	124015	0	None	3	2	Human	5.3	pKi	=	5.3	Binding	Inhibition of human histamine H2 receptorInhibition of human histamine H2 receptor	ChEMBL	420	3	2	6	1.5	COc1nc(N2C[C@H]3C(=O)N(C)C(=N)N[C@@]3(c3ccc(F)cc3F)C2)nc(C)c1F	10.1021/acs.jmedchem.5b01995
	168295528	192429	0	None	-147	20	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5206565	192429	0	None	-147	20	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222872	192429	0	None	-147	20	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	333	6	4	5	0.9	N/C(=N\C(=O)NCc1ccccc1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	168290815	192371	0	None	-537	6	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5200771	192371	0	None	-537	6	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222529	192371	0	None	-537	6	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	327	9	4	5	1.2	CCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	168273640	192203	0	None	-6	6	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5176229	192203	0	None	-6	6	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221444	192203	0	None	-6	6	Human	8.3	pKi	=	8.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	568	15	8	10	-0.1	N/C(=N\C(=O)NCCCCCCNC(=O)/N=C(\N)NCCCc1nnc(N)s1)NCCCc1nnc(N)s1	10.1021/acs.jmedchem.1c00692
	46780481	107045	18	None	-21	53	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1016/j.bmcl.2013.12.024
	9903970	107045	18	None	-21	53	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1016/j.bmcl.2013.12.024
	CHEMBL3187365	107045	18	None	-21	53	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1016/j.bmcl.2013.12.024
	CHEMBL3544974	107045	18	None	-21	53	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1016/j.bmcl.2013.12.024
	46780481	107045	18	None	-21	53	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1016/j.bmcl.2013.12.024
	9903970	107045	18	None	-21	53	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1016/j.bmcl.2013.12.024
	CHEMBL3187365	107045	18	None	-21	53	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1016/j.bmcl.2013.12.024
	CHEMBL3544974	107045	18	None	-21	53	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	10.1016/j.bmcl.2013.12.024
	44334395	4892	0	None	-144	3	Human	6.3	pKi	=	6.3	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	446	10	1	5	3.2	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(F)cc3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
	CHEMBL104808	4892	0	None	-144	3	Human	6.3	pKi	=	6.3	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	446	10	1	5	3.2	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3ccc(F)cc3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
	1204	1901	114	None	-173	23	Human	5.3	pKi	=	5.3	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.5b00516
	1247	1901	114	None	-173	23	Human	5.3	pKi	=	5.3	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.5b00516
	1375	1901	114	None	-173	23	Human	5.3	pKi	=	5.3	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.5b00516
	774	1901	114	None	-173	23	Human	5.3	pKi	=	5.3	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.5b00516
	CHEMBL90	1901	114	None	-173	23	Human	5.3	pKi	=	5.3	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.5b00516
	DB05381	1901	114	None	-173	23	Human	5.3	pKi	=	5.3	Binding	Binding affinity to histamine H2 receptor (unknown origin)Binding affinity to histamine H2 receptor (unknown origin)	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1021/acs.jmedchem.5b00516
	44334265	109195	0	None	-25	3	Human	5.3	pKi	=	5.3	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	368	8	1	6	2.0	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3cnccn3)C2)cc1	10.1016/s0960-894x(02)00685-6
	CHEMBL322695	109195	0	None	-25	3	Human	5.3	pKi	=	5.3	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	368	8	1	6	2.0	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3cnccn3)C2)cc1	10.1016/s0960-894x(02)00685-6
	44334521	107350	0	None	-36	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	262	6	1	4	1.7	CC(=O)c1ccc(OCCCN2CC[C@H](N)C2)cc1	10.1016/s0960-894x(02)00685-6
	CHEMBL319231	107350	0	None	-36	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	262	6	1	4	1.7	CC(=O)c1ccc(OCCCN2CC[C@H](N)C2)cc1	10.1016/s0960-894x(02)00685-6
	1226	1988	16	None	-7	6	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2010.10.041
	41376	1988	16	None	-7	6	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2010.10.041
	CHEMBL12608	1988	16	None	-7	6	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2010.10.041
	10015196	103145	0	None	-251	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	254	8	3	2	2.4	CCC/N=C(\S)NCCCCCc1c[nH]cn1	10.1021/jm00012a025
	CHEMBL308717	103145	0	None	-251	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptorsDisplacement of [125 I]iodoaminopotentidine bound to membranes of CHO cells expressing human H2 receptors	ChEMBL	254	8	3	2	2.4	CCC/N=C(\S)NCCCCCc1c[nH]cn1	10.1021/jm00012a025
	44304056	102251	0	None	-5754	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	401	10	1	5	2.6	CC(C)N[C@H](C)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL304888	102251	0	None	-5754	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	401	10	1	5	2.6	CC(C)N[C@H](C)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	44304316	201443	0	None	-416	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	485	8	0	6	3.6	CC(C)(C)OC(=O)N1CCC[C@@H]1C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL64120	201443	0	None	-416	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	485	8	0	6	3.6	CC(C)(C)OC(=O)N1CCC[C@@H]1C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	1204	1901	114	None	-173	23	Human	4.3	pKi	=	4.3	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
	1247	1901	114	None	-173	23	Human	4.3	pKi	=	4.3	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
	1375	1901	114	None	-173	23	Human	4.3	pKi	=	4.3	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
	774	1901	114	None	-173	23	Human	4.3	pKi	=	4.3	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
	CHEMBL90	1901	114	None	-173	23	Human	4.3	pKi	=	4.3	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
	DB05381	1901	114	None	-173	23	Human	4.3	pKi	=	4.3	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	111	2	2	2	-0.1	NCCc1cnc[nH]1	10.1016/j.bmcl.2010.10.041
	132060770	162089	0	None	-8	10	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	451	7	0	6	3.5	CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1	10.1016/j.ejmech.2018.02.024
	CHEMBL4169689	162089	0	None	-8	10	Human	6.3	pKi	=	6.3	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	451	7	0	6	3.5	CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1	10.1016/j.ejmech.2018.02.024
	2812	4711	96	None	-33	34	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	nan
	CHEMBL104	4711	96	None	-33	34	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	nan
	164622330	185280	0	None	-2	6	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	360	6	4	4	2.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4867962	185280	0	None	-2	6	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	360	6	4	4	2.3	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)N[C@@H](C)c1ccccc1	10.1016/j.ejmech.2021.113190
	164627774	185983	0	None	1	6	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	344	3	4	4	1.4	N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	CHEMBL4878215	185983	0	None	1	6	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	344	3	4	4	1.4	N/C(=N\C(=O)NCc1ccccc1)NC1CCc2nc(N)sc2C1	10.1016/j.ejmech.2021.113190
	71452172	83105	0	None	-1	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]tiotidine from human recombinant histamine H2 receptor after 1.5 hrs by microbeta scintillation counting analysisDisplacement of [3H]tiotidine from human recombinant histamine H2 receptor after 1.5 hrs by microbeta scintillation counting analysis	ChEMBL	274	6	1	5	2.4	c1ccc(OCc2cc(OC[C@@H]3CCCN3)no2)cc1	10.1021/ml3002715
	CHEMBL2203551	83105	0	None	-1	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]tiotidine from human recombinant histamine H2 receptor after 1.5 hrs by microbeta scintillation counting analysisDisplacement of [3H]tiotidine from human recombinant histamine H2 receptor after 1.5 hrs by microbeta scintillation counting analysis	ChEMBL	274	6	1	5	2.4	c1ccc(OCc2cc(OC[C@@H]3CCCN3)no2)cc1	10.1021/ml3002715
	155552683	173594	0	None	-40	4	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting methodDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting method	ChEMBL	379	4	2	5	4.1	Clc1ccc(C#Cc2nc(NCCc3ccccc3)c3nc[nH]c3n2)s1	10.1039/C8MD00317C
	CHEMBL4546937	173594	0	None	-40	4	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting methodDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting method	ChEMBL	379	4	2	5	4.1	Clc1ccc(C#Cc2nc(NCCc3ccccc3)c3nc[nH]c3n2)s1	10.1039/C8MD00317C
	164622256	185134	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	318	4	4	4	2.2	CCCNC(=O)/N=C(\N)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
	CHEMBL4865670	185134	0	None	-	1	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	318	4	4	4	2.2	CCCNC(=O)/N=C(\N)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
	145992489	166424	0	None	-1	12	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	535	7	1	2	7.8	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC=C(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
	CHEMBL4287623	166424	0	None	-1	12	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	535	7	1	2	7.8	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC=C(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
	168290235	192366	0	None	-1737	20	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5201074	192366	0	None	-1737	20	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222491	192366	0	None	-1737	20	Human	7.3	pKi	=	7.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	315	6	4	3	1.1	C[C@@H](NC(=O)/N=C(\N)NCCCc1ncn[nH]1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	71454295	83665	0	None	-660	7	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	536	8	0	6	5.5	COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccccc4OC)CC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
	CHEMBL2207641	83665	0	None	-660	7	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	536	8	0	6	5.5	COc1ccccc1N1CCN(Cc2cc(CN3CCN(c4ccccc4OC)CC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
	44304329	201536	0	None	-1778	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	385	8	1	5	1.9	O=C(c1ccc(OCCCN2CCN(C(=O)[C@H]3CCCN3)CC2)cc1)C1CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL64461	201536	0	None	-1778	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	385	8	1	5	1.9	O=C(c1ccc(OCCCN2CCN(C(=O)[C@H]3CCCN3)CC2)cc1)C1CC1	10.1016/s0960-894x(02)00310-4
	24841480	183317	0	None	-269	20	Human	6.3	pKi	=	6.3	Binding	Antagonist activity at histamine H2 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	340	3	0	4	4.5	O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21	10.1016/j.bmcl.2013.04.082
	CHEMBL481153	183317	0	None	-269	20	Human	6.3	pKi	=	6.3	Binding	Antagonist activity at histamine H2 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	340	3	0	4	4.5	O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21	10.1016/j.bmcl.2013.04.082
	1231	924	112	None	-2	7	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
	2756	924	112	None	-2	7	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
	645	924	112	None	-2	7	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
	CHEMBL30	924	112	None	-2	7	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
	DB00501	924	112	None	-2	7	Human	5.3	pKi	=	5.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	nan
	155558968	174246	0	None	1	3	Human	6.3	pKi	=	6.3	Binding	Binding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assayBinding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	432	3	2	5	3.2	Cc1cccc(C)c1N1C(=O)[C@H](CC2CNc3ccccc32)NC2(CCN(C)CC2)C1=O	10.1016/j.ejmech.2018.12.048
	CHEMBL4562437	174246	0	None	1	3	Human	6.3	pKi	=	6.3	Binding	Binding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assayBinding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	432	3	2	5	3.2	Cc1cccc(C)c1N1C(=O)[C@H](CC2CNc3ccccc32)NC2(CCN(C)CC2)C1=O	10.1016/j.ejmech.2018.12.048
	53325242	56775	0	None	-2	17	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	537	8	1	2	7.9	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
	CHEMBL1644978	56775	0	None	-2	17	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	537	8	1	2	7.9	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	10.1016/j.bmcl.2018.10.036
	162644910	178831	0	None	-50	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	407	7	0	4	5.0	Clc1cccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)c1	10.1016/j.ejmech.2020.113041
	CHEMBL4740135	178831	0	None	-50	3	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	407	7	0	4	5.0	Clc1cccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)c1	10.1016/j.ejmech.2020.113041
	168268716	192160	0	None	1	4	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	3	4	4	3.5	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5170276	192160	0	None	1	4	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	3	4	4	3.5	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221176	192160	0	None	1	4	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	372	3	4	4	3.5	Cc1nc(N)sc1-c1ccc(N/C(N)=N/C(=O)NC2CCCCC2)cc1	10.1021/acs.jmedchem.1c00692
	71450707	83664	0	None	-1445	7	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	444	6	0	5	3.9	COc1ccccc1N1CCN(Cc2cc(CN3CCN(C)CC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
	CHEMBL2207640	83664	0	None	-1445	7	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	444	6	0	5	3.9	COc1ccccc1N1CCN(Cc2cc(CN3CCN(C)CC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
	155531772	176092	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assayDisplacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assay	ChEMBL	334	8	3	6	3.3	Cc1[nH]cnc1CSCCNc1ccnc(NCC(C)(C)C)n1	10.1021/acs.jmedchem.9b01342
	CHEMBL4466349	176092	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assayDisplacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assay	ChEMBL	334	8	3	6	3.3	Cc1[nH]cnc1CSCCNc1ccnc(NCC(C)(C)C)n1	10.1021/acs.jmedchem.9b01342
	CHEMBL4598197	176092	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assayDisplacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assay	ChEMBL	334	8	3	6	3.3	Cc1[nH]cnc1CSCCNc1ccnc(NCC(C)(C)C)n1	10.1021/acs.jmedchem.9b01342
	CHEMBL5083588	213758	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095633	213758	0	None	-	1	Human	6.3	pKi	=	6.3	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	44335351	4998	0	None	-29	3	Human	5.3	pKi	=	5.3	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	402	7	0	4	4.6	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(Cl)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	CHEMBL105385	4998	0	None	-29	3	Human	5.3	pKi	=	5.3	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	402	7	0	4	4.6	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc(Cl)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	168275750	192224	0	None	-87	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	3	4	1.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5175558	192224	0	None	-87	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	3	4	1.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221581	192224	0	None	-87	4	Human	5.3	pKi	=	5.3	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	332	6	3	4	1.6	Cc1nnc(CCCN/C(N)=N/C(=O)NCc2ccccc2)s1	10.1021/acs.jmedchem.1c00692
	44304475	201079	0	None	-10471	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	348	8	0	5	2.8	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)CC)cc2)CC1	10.1016/s0960-894x(02)00309-8
	CHEMBL62066	201079	0	None	-10471	3	Human	4.3	pKi	=	4.3	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	348	8	0	5	2.8	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)CC)cc2)CC1	10.1016/s0960-894x(02)00309-8
	44335222	162904	0	None	-20	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	369	7	0	5	3.3	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccncc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	CHEMBL419912	162904	0	None	-20	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	369	7	0	5	3.3	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccncc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	44304357	198926	0	None	-4786	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	415	9	1	5	3.0	CC(C)(C)C[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL59931	198926	0	None	-4786	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	415	9	1	5	3.0	CC(C)(C)C[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	137645406	157360	0	None	-75	13	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	491	8	0	7	5.4	COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)CC1	10.1021/acs.jmedchem.9b00412
	CHEMBL4084262	157360	0	None	-75	13	Human	6.2	pKi	=	6.2	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	491	8	0	7	5.4	COc1ccccc1N1CCC2(CCN(CCCSc3nnc(-c4ccccc4)n3C)CC2)CC1	10.1021/acs.jmedchem.9b00412
	168294182	192446	0	None	-3	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	314	6	4	2	1.7	C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5208722	192446	0	None	-3	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	314	6	4	2	1.7	C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222960	192446	0	None	-3	4	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	314	6	4	2	1.7	C[C@@H](NC(=O)/N=C(\N)NCCCc1c[nH]cn1)c1ccccc1	10.1021/acs.jmedchem.1c00692
	168268853	192183	0	None	-2	6	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5180504	192183	0	None	-2	6	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221353	192183	0	None	-2	6	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	389	8	4	5	1.9	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	164609017	183843	0	None	-1	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	416	10	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4846201	183843	0	None	-1	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	416	10	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCCc1ccccc1	10.1016/j.ejmech.2021.113190
	164610289	184550	0	None	38	4	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	438	7	4	4	3.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4856602	184550	0	None	38	4	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	438	7	4	4	3.5	Cc1nc(N)sc1CCCN/C(N)=N/C(=S)NC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
	44304378	162721	0	None	-2951	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	423	11	0	5	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccnc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL418658	162721	0	None	-2951	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	423	11	0	5	4.1	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3cccnc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304348	100136	0	None	-15135	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	387	10	1	5	2.3	CCC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL291821	100136	0	None	-15135	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	387	10	1	5	2.3	CCC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	44334036	167229	0	None	-154	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	391	8	1	5	3.0	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3ccc(C#N)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
	CHEMBL430502	167229	0	None	-154	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	391	8	1	5	3.0	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3ccc(C#N)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
	71454294	83663	0	None	-1348	7	Human	5.2	pKi	=	5.2	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	431	6	0	5	4.0	COc1ccccc1N1CCN(Cc2cc(CN3CCOCC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
	CHEMBL2207639	83663	0	None	-1348	7	Human	5.2	pKi	=	5.2	Binding	Displacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysisDisplacement of [3H]URDE257 from human histamine H2 receptor expressed in insect Sf9 cell membrane preparation after 60 mins by scintillation counting analysis	ChEMBL	431	6	0	5	4.0	COc1ccccc1N1CCN(Cc2cc(CN3CCOCC3)c3cccccc2-3)CC1	10.1016/j.bmcl.2012.09.064
	71449142	79108	0	None	-104	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	442	9	0	6	4.2	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(SC)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	CHEMBL2113738	79108	0	None	-104	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	442	9	0	6	4.2	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(SC)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	44334037	4380	0	None	-112	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	450	9	1	7	3.7	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3csc(-c4cccnc4)n3)C2)cc1	10.1016/s0960-894x(02)00685-6
	CHEMBL101634	4380	0	None	-112	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	450	9	1	7	3.7	CC(=O)c1ccc(OCCCN2CC[C@H](NC(=O)c3csc(-c4cccnc4)n3)C2)cc1	10.1016/s0960-894x(02)00685-6
	73355415	92101	0	None	-32	13	Human	5.2	pKi	=	5.2	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	277	3	1	1	2.1	C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42	10.1016/j.bmc.2013.07.045
	CHEMBL2432039	92101	0	None	-32	13	Human	5.2	pKi	=	5.2	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	277	3	1	1	2.1	C1C2C3CC4C2C2C1C3[C@H](NCC13C5C6C7C5C1C7C63)C42	10.1016/j.bmc.2013.07.045
	CHEMBL5092267	213581	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C	10.1016/j.bmcl.2021.128388
	164611474	184870	0	None	407	4	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	366	6	4	5	2.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccs1	10.1016/j.ejmech.2021.113190
	CHEMBL4861704	184870	0	None	407	4	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	366	6	4	5	2.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NC(C)c1cccs1	10.1016/j.ejmech.2021.113190
	164624107	185140	0	None	-1	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	402	9	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4865765	185140	0	None	-1	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	402	9	4	4	2.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CCc1ccccc1	10.1016/j.ejmech.2021.113190
	164620678	185437	0	None	177	4	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	374	7	4	4	2.7	CCC(NC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4870510	185437	0	None	177	4	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	374	7	4	4	2.7	CCC(NC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1	10.1016/j.ejmech.2021.113190
	126688	400	28	None	-1	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1016/j.bmcl.2010.10.041
	4025	400	28	None	-1	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1016/j.bmcl.2010.10.041
	CHEMBL293762	400	28	None	-1	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	157	2	2	4	0.5	NCCc1sc(nc1C)N	10.1016/j.bmcl.2010.10.041
	155551348	173385	0	None	1	2	Human	5.2	pKi	=	5.2	Binding	Inhibition of histamine H2 receptor (unknown origin)Inhibition of histamine H2 receptor (unknown origin)	ChEMBL	487	7	1	9	3.7	CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@@H]1OC(C)(C)O[C@@H]12	10.1021/acs.jmedchem.8b01662
	CHEMBL4541409	173385	0	None	1	2	Human	5.2	pKi	=	5.2	Binding	Inhibition of histamine H2 receptor (unknown origin)Inhibition of histamine H2 receptor (unknown origin)	ChEMBL	487	7	1	9	3.7	CCOC(=O)[C@@]12C[C@@H]1[C@@H](n1cnc3c(NC(C4CC4)C4CC4)nc(Cl)nc31)[C@@H]1OC(C)(C)O[C@@H]12	10.1021/acs.jmedchem.8b01662
	168292954	192395	0	None	-11	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5202592	192395	0	None	-11	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222660	192395	0	None	-11	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	388	8	4	4	2.5	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2cnc(N)s2)cc1	10.1021/acs.jmedchem.1c00692
	162676676	183007	0	None	-323	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	389	8	0	5	4.5	c1ccc(Oc2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1	10.1016/j.ejmech.2020.113041
	CHEMBL4800672	183007	0	None	-323	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	389	8	0	5	4.5	c1ccc(Oc2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1	10.1016/j.ejmech.2020.113041
	CHEMBL5075713	213753	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	CHEMBL5095559	213753	0	None	-	1	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		CC1(C)C(/C=C/C=C/C=C2\c3ccccc3C(C)(C)N2CCCCCC(=O)NCCCCCCCCNC(=O)/N=C(\N)NCCCc2c[nH]cn2)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1016/j.bmcl.2021.128388
	4189	205195	91	None	-36	34	Human	5.2	pKi	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
	CHEMBL1559	205195	91	None	-36	34	Human	5.2	pKi	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
	CHEMBL91	205195	91	None	-36	34	Human	5.2	pKi	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	nan
	130442572	171342	0	None	-144	24	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	395	3	0	5	6.0	FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12	10.1021/acs.jmedchem.9b00351
	CHEMBL4469848	171342	0	None	-144	24	Human	5.2	pKi	=	5.2	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	395	3	0	5	6.0	FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12	10.1021/acs.jmedchem.9b00351
	181743	177997	3	None	-338	22	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]Tiotidine from human histamine H2 receptorDisplacement of [3H]Tiotidine from human histamine H2 receptor	ChEMBL	339	2	0	5	3.2	COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4	10.1016/j.bmcl.2009.11.053
	CHEMBL467094	177997	3	None	-338	22	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]Tiotidine from human histamine H2 receptorDisplacement of [3H]Tiotidine from human histamine H2 receptor	ChEMBL	339	2	0	5	3.2	COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4	10.1016/j.bmcl.2009.11.053
	168291233	192377	0	None	-5	4	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	373	8	4	5	1.4	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5200106	192377	0	None	-5	4	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	373	8	4	5	1.4	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1	10.1021/acs.jmedchem.1c00692
	CHEMBL5222556	192377	0	None	-5	4	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	373	8	4	5	1.4	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2nnc(N)o2)cc1	10.1021/acs.jmedchem.1c00692
	44304031	100205	0	None	-933	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	452	10	0	6	4.1	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)/C=C/c3ccc(OC)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	CHEMBL292275	100205	0	None	-933	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	452	10	0	6	4.1	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)/C=C/c3ccc(OC)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	18672441	94951	0	None	-9332	4	Human	4.2	pKi	=	4.2	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	306	6	0	3	4.1	N#Cc1ccc(-c2ccc(OCCCN3CCCC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	CHEMBL25688	94951	0	None	-9332	4	Human	4.2	pKi	=	4.2	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	306	6	0	3	4.1	N#Cc1ccc(-c2ccc(OCCCN3CCCC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	4601	205020	29	None	-7	17	Human	5.2	pKi	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	nan
	CHEMBL1201023	205020	29	None	-7	17	Human	5.2	pKi	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	nan
	CHEMBL900	205020	29	None	-7	17	Human	5.2	pKi	=	5.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	nan
	162664702	181628	0	None	-50	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	407	7	0	4	5.0	Clc1ccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1	10.1016/j.ejmech.2020.113041
	CHEMBL4783066	181628	0	None	-50	3	Human	5.2	pKi	=	5.2	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	407	7	0	4	5.0	Clc1ccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1	10.1016/j.ejmech.2020.113041
	164611342	184505	0	None	-1	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	346	6	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4856005	184505	0	None	-1	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	346	6	4	4	1.8	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCc1ccccc1	10.1016/j.ejmech.2021.113190
	164618690	185574	0	None	1	5	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	360	7	4	4	3.4	CCCCCCNC(=O)/N=C(\N)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
	CHEMBL4872375	185574	0	None	1	5	Human	6.2	pKi	=	6.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	360	7	4	4	3.4	CCCCCCNC(=O)/N=C(\N)Nc1cccc(-c2csc(N)n2)c1	10.1016/j.ejmech.2021.113190
	127035835	136761	0	None	-4	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation counting	ChEMBL	385	4	1	5	3.6	CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1	10.1016/j.bmcl.2015.12.035
	CHEMBL3752270	136761	0	None	-4	4	Human	5.2	pKi	=	5.2	Binding	Displacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation countingDisplacement of [3H]UR-DE257 from human histamine 2 receptor expressed in Sf9 cell membranes by liquid scintillation counting	ChEMBL	385	4	1	5	3.6	CN1CCN(c2nc(NCc3ccccc3)nc3c2CCc2ccccc2-3)CC1	10.1016/j.bmcl.2015.12.035
	44304079	200939	0	None	-9549	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	376	9	0	5	3.5	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)CC(C)C)cc2)CC1	10.1016/s0960-894x(02)00309-8
	CHEMBL61231	200939	0	None	-9549	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	376	9	0	5	3.5	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)CC(C)C)cc2)CC1	10.1016/s0960-894x(02)00309-8
	44335428	4915	0	None	-79	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	358	7	1	5	2.6	CCOC(=O)N1CCN(CCCOc2ccc(-c3c[nH]cn3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	CHEMBL104947	4915	0	None	-79	3	Human	4.2	pKi	=	4.2	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	358	7	1	5	2.6	CCOC(=O)N1CCN(CCCOc2ccc(-c3c[nH]cn3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	1231	924	112	None	-2	7	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
	2756	924	112	None	-2	7	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
	645	924	112	None	-2	7	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
	CHEMBL30	924	112	None	-2	7	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
	DB00501	924	112	None	-2	7	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
	1231	924	112	None	-2	7	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
	2756	924	112	None	-2	7	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
	645	924	112	None	-2	7	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
	CHEMBL30	924	112	None	-2	7	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
	DB00501	924	112	None	-2	7	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1016/j.bmcl.2013.12.024
	164610892	184615	0	None	1	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	394	8	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1	10.1016/j.ejmech.2021.113190
	CHEMBL4857560	184615	0	None	1	6	Human	7.2	pKi	=	7.2	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	394	8	4	4	3.2	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(C)CC1CCCCC1	10.1016/j.ejmech.2021.113190
	44334407	108598	0	None	-229	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	462	10	1	5	3.8	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3cccc(Cl)c3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
	CHEMBL321320	108598	0	None	-229	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	462	10	1	5	3.8	O=C(c1ccc(OCCCN2CC[C@H](NS(=O)(=O)c3cccc(Cl)c3)C2)cc1)C1CC1	10.1016/s0960-894x(02)00685-6
	44304402	199527	0	None	-426	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	415	12	0	6	4.5	CCCCCC(=O)c1ccc(OCCCN2CCN(Cc3nccs3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL60360	199527	0	None	-426	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	415	12	0	6	4.5	CCCCCC(=O)c1ccc(OCCCN2CCN(Cc3nccs3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	1258	194	8	None	-35481	5	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359	8	1	5	1.5	C[C@H](C(=O)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1)N	10.1016/s0960-894x(02)00310-4
	9906860	194	8	None	-35481	5	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359	8	1	5	1.5	C[C@H](C(=O)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1)N	10.1016/s0960-894x(02)00310-4
	CHEMBL302196	194	8	None	-35481	5	Human	4.2	pKi	=	4.2	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359	8	1	5	1.5	C[C@H](C(=O)N1CCN(CC1)CCCOc1ccc(cc1)C(=O)C1CC1)N	10.1016/s0960-894x(02)00310-4
	44334042	162937	0	None	-64	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	453	10	1	6	3.0	N#Cc1ccccc1S(=O)(=O)N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1	10.1016/s0960-894x(02)00685-6
	CHEMBL420108	162937	0	None	-64	3	Human	6.2	pKi	=	6.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	453	10	1	6	3.0	N#Cc1ccccc1S(=O)(=O)N[C@H]1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)C1	10.1016/s0960-894x(02)00685-6
	44334234	109191	0	None	-707	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	432	10	1	7	1.8	Cn1cnc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1	10.1016/s0960-894x(02)00685-6
	CHEMBL322678	109191	0	None	-707	3	Human	5.2	pKi	=	5.2	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	432	10	1	7	1.8	Cn1cnc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1	10.1016/s0960-894x(02)00685-6
	180	397	50	None	-1412	38	Human	6.1	pKi	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
	200	397	50	None	-1412	38	Human	6.1	pKi	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
	2160	397	50	None	-1412	38	Human	6.1	pKi	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
	CHEMBL629	397	50	None	-1412	38	Human	6.1	pKi	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
	DB00321	397	50	None	-1412	38	Human	6.1	pKi	=	6.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	nan
	164611757	184320	0	None	1	6	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	402	8	4	4	2.8	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
	CHEMBL4853107	184320	0	None	1	6	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	402	8	4	4	2.8	Cc1ccc(CC(C)CNC(=O)/N=C(\N)NCCCc2sc(N)nc2C)cc1	10.1016/j.ejmech.2021.113190
	44304003	201444	0	None	-2511	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	384	9	1	6	1.4	N#CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL64124	201444	0	None	-2511	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	384	9	1	6	1.4	N#CC[C@@H](N)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	127052294	139772	0	None	-33	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method	ChEMBL	368	7	3	4	3.1	N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1	10.1021/acs.jmedchem.6b00120
	CHEMBL3806079	139772	0	None	-33	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method	ChEMBL	368	7	3	4	3.1	N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@H](c2c[nH]cn2)C1	10.1021/acs.jmedchem.6b00120
	71463063	83387	0	None	-11	8	Human	5.1	pKi	=	5.1	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	295	3	1	3	2.0	COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1	10.1016/j.bmcl.2012.08.046
	CHEMBL2205825	83387	0	None	-11	8	Human	5.1	pKi	=	5.1	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	295	3	1	3	2.0	COc1ccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)cc1	10.1016/j.bmcl.2012.08.046
	44334369	4945	0	None	-138	3	Human	6.1	pKi	=	6.1	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	484	10	1	5	4.4	CC(C)(C)c1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
	CHEMBL105071	4945	0	None	-138	3	Human	6.1	pKi	=	6.1	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	484	10	1	5	4.4	CC(C)(C)c1ccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)cc1	10.1016/s0960-894x(02)00685-6
	127049856	139715	0	None	-25	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method	ChEMBL	368	7	3	4	3.1	N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1	10.1021/acs.jmedchem.6b00120
	CHEMBL3805431	139715	0	None	-25	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method	ChEMBL	368	7	3	4	3.1	N#C/N=C(/NCCSc1ccccc1)NC[C@H]1CC[C@@H](c2c[nH]cn2)C1	10.1021/acs.jmedchem.6b00120
	9923147	4980	0	None	-1202	4	Human	5.1	pKi	=	5.1	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	321	6	1	4	3.0	N#Cc1ccc(-c2ccc(OCCCN3CC[C@@H](N)C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	CHEMBL105267	4980	0	None	-1202	4	Human	5.1	pKi	=	5.1	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	321	6	1	4	3.0	N#Cc1ccc(-c2ccc(OCCCN3CC[C@@H](N)C3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	71463061	83381	0	None	1	9	Human	6.1	pKi	=	6.1	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	339	5	1	4	2.0	COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1OC	10.1016/j.bmcl.2012.08.046
	CHEMBL2205813	83381	0	None	1	9	Human	6.1	pKi	=	6.1	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	339	5	1	4	2.0	COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1OC	10.1016/j.bmcl.2012.08.046
	162662563	181464	0	None	-123	3	Human	5.1	pKi	=	5.1	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	391	7	0	4	4.5	Fc1ccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1	10.1016/j.ejmech.2020.113041
	CHEMBL4781093	181464	0	None	-123	3	Human	5.1	pKi	=	5.1	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	391	7	0	4	4.5	Fc1ccc(-c2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1	10.1016/j.ejmech.2020.113041
	44435200	149143	0	None	-4	4	Human	5.1	pKi	=	5.1	Binding	Antagonist activity at histamine H2 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	345	4	0	2	5.8	O=C(CCCc1ccccc1)N1c2ccccc2Sc2ccccc21	10.1016/j.bmcl.2013.04.082
	CHEMBL394755	149143	0	None	-4	4	Human	5.1	pKi	=	5.1	Binding	Antagonist activity at histamine H2 receptor (unknown origin) by PDSP assayAntagonist activity at histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	345	4	0	2	5.8	O=C(CCCc1ccccc1)N1c2ccccc2Sc2ccccc21	10.1016/j.bmcl.2013.04.082
	44335389	5097	0	None	-46	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	413	8	0	6	3.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccccc3[N+](=O)[O-])cc2)CC1	10.1016/s0960-894x(02)00648-0
	CHEMBL105952	5097	0	None	-46	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	413	8	0	6	3.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccccc3[N+](=O)[O-])cc2)CC1	10.1016/s0960-894x(02)00648-0
	44304243	201509	0	None	-562	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	374	13	0	4	4.6	CCCCCC(=O)c1ccc(OCCCN2CCN(CCCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL64334	201509	0	None	-562	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	374	13	0	4	4.6	CCCCCC(=O)c1ccc(OCCCN2CCN(CCCC)CC2)cc1	10.1016/s0960-894x(02)00309-8
	156015041	177658	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1029	30	3	11	10.0	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4637356	177658	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1029	30	3	11	10.0	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	CHEMBL4650547	177658	0	None	-	1	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in baculovirus infected Sf9 cells incubated for 60 mins by scintillation counting method	ChEMBL	1029	30	3	11	10.0	CC1(C)C(/C=C/C=C/C=C2\N(CCCCCC(=O)NCCCCCCNc3c(NCCCOc4cccc(CN5CCCCC5)c4)c(=O)c3=O)c3ccccc3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccccc21	10.1021/acsmedchemlett.0c00033
	164617783	184007	0	None	-1	6	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	388	8	4	4	2.8	CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4848815	184007	0	None	-1	6	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	388	8	4	4	2.8	CCC(CNC(=O)/N=C(\N)NCCCc1sc(N)nc1C)c1ccccc1	10.1016/j.ejmech.2021.113190
	11393516	5102	0	None	-933	4	Human	5.1	pKi	=	5.1	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	335	6	1	4	3.3	N#Cc1ccc(-c2ccc(OCCCN3CCCNCC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	CHEMBL105967	5102	0	None	-933	4	Human	5.1	pKi	=	5.1	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	335	6	1	4	3.3	N#Cc1ccc(-c2ccc(OCCCN3CCCNCC3)cc2)cc1	10.1016/s0960-894x(02)00648-0
	75306277	108767	0	None	-39	23	Human	7.1	pKi	=	7.1	Binding	Binding affinity to H2 histamine receptor (unknown origin) by PDSP assayBinding affinity to H2 histamine receptor (unknown origin) by PDSP assay	ChEMBL	308	0	0	3	4.2	CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3	10.1039/C2MD00311B
	CHEMBL3217984	108767	0	None	-39	23	Human	7.1	pKi	=	7.1	Binding	Binding affinity to H2 histamine receptor (unknown origin) by PDSP assayBinding affinity to H2 histamine receptor (unknown origin) by PDSP assay	ChEMBL	308	0	0	3	4.2	CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3	10.1039/C2MD00311B
	44304088	200700	0	None	-316	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	402	8	0	5	4.0	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C3CCCCC3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	CHEMBL61070	200700	0	None	-316	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	402	8	0	5	4.0	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C3CCCCC3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	1269	121	33	None	-269	3	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1016/j.bmcl.2010.10.041
	37463	121	33	None	-269	3	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1016/j.bmcl.2010.10.041
	CHEMBL275443	121	33	None	-269	3	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	ChEMBL	125	2	2	2	0.2	Cc1c(CCN)nc[nH]1	10.1016/j.bmcl.2010.10.041
	44304090	201261	0	None	-16982	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	360	8	0	5	2.8	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	CHEMBL62948	201261	0	None	-16982	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	360	8	0	5	2.8	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	44304067	199598	0	None	-34673	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359	9	1	5	1.4	CNCC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL60401	199598	0	None	-34673	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	359	9	1	5	1.4	CNCC(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	168281746	192280	0	None	-676	6	Human	8.1	pKi	=	8.1	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5184911	192280	0	None	-676	6	Human	8.1	pKi	=	8.1	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
	CHEMBL5221974	192280	0	None	-676	6	Human	8.1	pKi	=	8.1	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis	ChEMBL	365	6	4	5	1.6	CC(NC(=O)/N=C(\N)NCCCc1nnc(N)s1)c1cccc(F)c1	10.1021/acs.jmedchem.1c00692
	75201901	165872	14	None	-588	24	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	356	3	0	6	4.9	Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12	10.1021/acs.jmedchem.9b00351
	CHEMBL4277264	165872	14	None	-588	24	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	356	3	0	6	4.9	Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12	10.1021/acs.jmedchem.9b00351
	CHEMBL4448899	212188	40	None	-	1	Human	5.1	pKi	=	5.1	Binding	Selectivity interaction (GPCR panel (PDSP screen)) EUB0000307b HRH2Selectivity interaction (GPCR panel (PDSP screen)) EUB0000307b HRH2	ChEMBL		None	None	None		Cc1c(NC(=O)c2cc(C(N)=O)nc3cc(F)ccc23)c(C(F)(F)F)nn1Cc1ccc(C#N)cc1	nan
	21509921	103979	0	None	-7	24	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	288	0	0	2	3.7	CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1	10.1016/j.bmcl.2013.12.024
	CHEMBL3104091	103979	0	None	-7	24	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	288	0	0	2	3.7	CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1	10.1016/j.bmcl.2013.12.024
	21509921	103979	0	None	-7	24	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	288	0	0	2	3.7	CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1	10.1016/j.bmcl.2013.12.024
	CHEMBL3104091	103979	0	None	-7	24	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	288	0	0	2	3.7	CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1	10.1016/j.bmcl.2013.12.024
	44304270	199563	0	None	-512	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	442	11	0	5	5.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccc(C)s3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL60383	199563	0	None	-512	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	442	11	0	5	5.0	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)c3ccc(C)s3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	130442480	174698	0	None	-100	24	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	410	3	0	6	5.7	Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F	10.1021/acs.jmedchem.9b00351
	CHEMBL4572614	174698	0	None	-100	24	Human	5.1	pKi	=	5.1	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	410	3	0	6	5.7	Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F	10.1021/acs.jmedchem.9b00351
	1210	905	45	None	-281	20	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	1213	905	45	None	-281	20	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	2725	905	45	None	-281	20	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	33036	905	45	None	-281	20	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	4411	905	45	None	-281	20	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	616	905	45	None	-281	20	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	6976	905	45	None	-281	20	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	716121	905	45	None	-281	20	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	90475904	905	45	None	-281	20	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	CHEMBL1201353	905	45	None	-281	20	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	CHEMBL1554789	905	45	None	-281	20	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	CHEMBL505	905	45	None	-281	20	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	DB01114	905	45	None	-281	20	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	DB13679	905	45	None	-281	20	Human	5.1	pKi	=	5.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	nan
	155539605	172276	0	None	-3	6	Human	6.1	pKi	=	6.1	Binding	Binding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assayBinding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	313	1	0	4	2.1	CC1=NC2(CCN(C)CC2)C(=O)N(c2c(C)cccc2C)C1=O	10.1016/j.ejmech.2018.12.048
	CHEMBL4514672	172276	0	None	-3	6	Human	6.1	pKi	=	6.1	Binding	Binding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assayBinding affinity to human histamine 2 receptor expressed in HEK cells by radioligand binding assay	ChEMBL	313	1	0	4	2.1	CC1=NC2(CCN(C)CC2)C(=O)N(c2c(C)cccc2C)C1=O	10.1016/j.ejmech.2018.12.048
	44582705	186413	0	None	-5	13	Human	6.1	pKi	=	6.1	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	399	9	0	4	4.5	COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1	10.1016/j.bmc.2009.03.021
	CHEMBL490632	186413	0	None	-5	13	Human	6.1	pKi	=	6.1	Binding	Inhibition of human cloned histamine H2 receptor by competitive binding experimentInhibition of human cloned histamine H2 receptor by competitive binding experiment	ChEMBL	399	9	0	4	4.5	COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1	10.1016/j.bmc.2009.03.021
	145973771	164167	0	None	2	7	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method	ChEMBL	797	16	2	7	10.8	CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1	10.1021/acs.jmedchem.8b00168
	CHEMBL4217398	164167	0	None	2	7	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting methodDisplacement of [125I]-Iodoaminopotentidine from human histamine H2 receptor expressed in HEK293T cell membranes after 90 mins by scintillation counting method	ChEMBL	797	16	2	7	10.8	CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1	10.1021/acs.jmedchem.8b00168
	44335412	106973	0	None	-102	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	413	8	0	6	3.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc([N+](=O)[O-])cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	CHEMBL318320	106973	0	None	-102	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity at human cortical Histamine 2 receptorBinding affinity at human cortical Histamine 2 receptor	ChEMBL	413	8	0	6	3.8	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccc([N+](=O)[O-])cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	44304284	162728	0	None	-208	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	426	9	0	6	3.5	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(OC)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	CHEMBL418691	162728	0	None	-208	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	426	9	0	6	3.5	CCOC(=O)N1CCN(CCCOc2ccc(C(=O)c3ccc(OC)cc3)cc2)CC1	10.1016/s0960-894x(02)00309-8
	44304978	167326	0	None	-3890	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	396	11	0	5	2.8	CCCCCC(=O)c1ccc(OCCCN2CCN(S(C)(=O)=O)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL431172	167326	0	None	-3890	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	396	11	0	5	2.8	CCCCCC(=O)c1ccc(OCCCN2CCN(S(C)(=O)=O)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304752	201521	0	None	-39810	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	459	9	1	6	3.1	C[C@@H](NC(=O)OC(C)(C)C)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL64406	201521	0	None	-39810	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	459	9	1	6	3.1	C[C@@H](NC(=O)OC(C)(C)C)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	11496610	4012	11	None	-2	2	Human	6.1	pKi	=	6.1	Binding	Inhibition of human histamine H2 receptorInhibition of human histamine H2 receptor	ChEMBL	476	4	1	5	5.8	CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C	10.1021/jm801572m
	5582	4012	11	None	-2	2	Human	6.1	pKi	=	6.1	Binding	Inhibition of human histamine H2 receptorInhibition of human histamine H2 receptor	ChEMBL	476	4	1	5	5.8	CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C	10.1021/jm801572m
	CHEMBL474991	4012	11	None	-2	2	Human	6.1	pKi	=	6.1	Binding	Inhibition of human histamine H2 receptorInhibition of human histamine H2 receptor	ChEMBL	476	4	1	5	5.8	CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C	10.1021/jm801572m
	73355421	92120	0	None	-	1	Human	5.1	pKi	=	5.1	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	309	3	0	3	3.0	CN(Cc1ccc2c(c1)OCO2)[C@H]1C2C3CC4C5C3CC2C5C41	10.1016/j.bmc.2013.07.045
	CHEMBL2432062	92120	0	None	-	1	Human	5.1	pKi	=	5.1	Binding	Inhibition of histamine H2 receptor (unknown origin) by PDSP assayInhibition of histamine H2 receptor (unknown origin) by PDSP assay	ChEMBL	309	3	0	3	3.0	CN(Cc1ccc2c(c1)OCO2)[C@H]1C2C3CC4C5C3CC2C5C41	10.1016/j.bmc.2013.07.045
	164620139	185206	0	None	56	4	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	436	8	4	4	3.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
	CHEMBL4866734	185206	0	None	56	4	Human	7.1	pKi	=	7.1	Binding	Displacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting methodDisplacement of [3H]UR-DE257 from human histamine H2 receptor expressed in sf9 insect cell membranes co-expressing GSalphaS incubated for 60 mins by microbeta scintillation counting method	ChEMBL	436	8	4	4	3.4	Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCC(c1ccccc1)c1ccccc1	10.1016/j.ejmech.2021.113190
	11846300	79856	3	None	-1071	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [3H]APT from human histamine H2 receptor transfected in COS7 cellsDisplacement of [3H]APT from human histamine H2 receptor transfected in COS7 cells	ChEMBL	327	0	0	4	3.8	CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1	10.1021/jm051008s
	CHEMBL213912	79856	3	None	-1071	4	Human	5.1	pKi	=	5.1	Binding	Displacement of [3H]APT from human histamine H2 receptor transfected in COS7 cellsDisplacement of [3H]APT from human histamine H2 receptor transfected in COS7 cells	ChEMBL	327	0	0	4	3.8	CN1CCN(C2=Nc3ccc(Cl)cc3Oc3ccccc32)CC1	10.1021/jm051008s
	137646281	157264	0	None	-1995	17	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	423	8	0	7	3.8	COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1	10.1021/acs.jmedchem.9b00412
	CHEMBL4083252	157264	0	None	-1995	17	Human	6.1	pKi	=	6.1	Binding	Displacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-Iodo-aminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	423	8	0	7	3.8	COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1	10.1021/acs.jmedchem.9b00412
	657255	197406	29	None	-3	15	Human	7.1	pKi	=	7.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	12	2	3	5.6	CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1	nan
	CHEMBL588119	197406	29	None	-3	15	Human	7.1	pKi	=	7.1	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	12	2	3	5.6	CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1	nan
	44304439	102325	0	None	-891	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	436	12	0	4	4.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)Cc3ccccc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL305338	102325	0	None	-891	3	Human	5.1	pKi	=	5.1	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	436	12	0	4	4.6	CCCCCC(=O)c1ccc(OCCCN2CCN(C(=O)Cc3ccccc3)CC2)cc1	10.1016/s0960-894x(02)00309-8
	44304332	199659	0	None	-19054	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	399	9	1	5	2.3	O=C(c1ccc(OCCCN2CCN(C(=O)C[C@H]3CCCN3)CC2)cc1)C1CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL60435	199659	0	None	-19054	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	399	9	1	5	2.3	O=C(c1ccc(OCCCN2CCN(C(=O)C[C@H]3CCCN3)CC2)cc1)C1CC1	10.1016/s0960-894x(02)00310-4
	44304719	201034	0	None	-19498	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	425	10	2	6	1.5	N[C@H](Cc1c[nH]cn1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL61792	201034	0	None	-19498	3	Human	4.1	pKi	=	4.1	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	425	10	2	6	1.5	N[C@H](Cc1c[nH]cn1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	44334038	4396	0	None	-316	3	Human	6.1	pKi	=	6.1	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	453	10	1	6	3.0	N#Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1	10.1016/s0960-894x(02)00685-6
	CHEMBL101748	4396	0	None	-316	3	Human	6.1	pKi	=	6.1	Binding	Binding affinity to the human Histamine H2 receptorBinding affinity to the human Histamine H2 receptor	ChEMBL	453	10	1	6	3.0	N#Cc1cccc(S(=O)(=O)N[C@H]2CCN(CCCOc3ccc(C(=O)C4CC4)cc3)C2)c1	10.1016/s0960-894x(02)00685-6
	10472082	5072	0	None	-13489	4	Human	5.0	pKi	=	5.0	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	334	6	0	3	4.9	C[C@@H]1CC[C@@H](C)N1CCCOc1ccc(-c2ccc(C#N)cc2)cc1	10.1016/s0960-894x(02)00648-0
	CHEMBL105762	5072	0	None	-13489	4	Human	5.0	pKi	=	5.0	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	334	6	0	3	4.9	C[C@@H]1CC[C@@H](C)N1CCCOc1ccc(-c2ccc(C#N)cc2)cc1	10.1016/s0960-894x(02)00648-0
	44335558	109581	0	None	-933	4	Human	5.0	pKi	=	5.0	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	334	6	0	3	4.7	CC1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	CHEMBL323562	109581	0	None	-933	4	Human	5.0	pKi	=	5.0	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	334	6	0	3	4.7	CC1CCN(CCCOc2ccc(-c3ccc(C#N)cc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	56963799	74546	0	None	-2290	10	Human	6.0	pKi	=	6.0	Binding	Binding affinity to human recombinant H2 receptorBinding affinity to human recombinant H2 receptor	ChEMBL	378	6	0	5	4.6	C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc([N+](=O)[O-])cc3)ccc2o1	10.1021/jm201690h
	CHEMBL2031737	74546	0	None	-2290	10	Human	6.0	pKi	=	6.0	Binding	Binding affinity to human recombinant H2 receptorBinding affinity to human recombinant H2 receptor	ChEMBL	378	6	0	5	4.6	C[C@@H]1CCCN1CCc1cc2cc(C(=O)c3ccc([N+](=O)[O-])cc3)ccc2o1	10.1021/jm201690h
	1016	3690	75	None	-41	35	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
	2561	3690	75	None	-41	35	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
	2733526	3690	75	None	-41	35	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
	5384	3690	75	None	-41	35	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
	CHEMBL83	3690	75	None	-41	35	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
	DB00675	3690	75	None	-41	35	Human	5.0	pKi	=	5.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	nan
	73213196	103981	1	None	-8	13	Human	6.0	pKi	=	6.0	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	288	0	0	2	3.9	CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1	10.1016/j.bmcl.2013.12.024
	CHEMBL3104093	103981	1	None	-8	13	Human	6.0	pKi	=	6.0	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	288	0	0	2	3.9	CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1	10.1016/j.bmcl.2013.12.024
	100	3745	52	None	-46	55	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
	2637	3745	52	None	-46	55	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
	5452	3745	52	None	-46	55	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
	CHEMBL479	3745	52	None	-46	55	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
	DB00679	3745	52	None	-46	55	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	nan
	73213196	103981	1	None	-8	13	Human	6.0	pKi	=	6.0	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	288	0	0	2	3.9	CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1	10.1016/j.bmcl.2013.12.024
	CHEMBL3104093	103981	1	None	-8	13	Human	6.0	pKi	=	6.0	Binding	Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)	ChEMBL	288	0	0	2	3.9	CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1	10.1016/j.bmcl.2013.12.024
	162657344	180350	0	None	-1096	3	Human	5.0	pKi	=	5.0	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	388	8	1	5	4.4	c1ccc(Nc2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1	10.1016/j.ejmech.2020.113041
	CHEMBL4758080	180350	0	None	-1096	3	Human	5.0	pKi	=	5.0	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes measured after 60 mins by scintillation counting analysis	ChEMBL	388	8	1	5	4.4	c1ccc(Nc2ccc(OCCCN3CCN(c4ccncc4)CC3)cc2)cc1	10.1016/j.ejmech.2020.113041
	71459604	83379	0	None	-1	14	Human	6.0	pKi	=	6.0	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	309	4	1	3	2.0	COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1	10.1016/j.bmcl.2012.08.046
	CHEMBL2205811	83379	0	None	-1	14	Human	6.0	pKi	=	6.0	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	309	4	1	3	2.0	COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1	10.1016/j.bmcl.2012.08.046
	CHEMBL5088914	213786	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	CHEMBL5095949	213786	0	None	-	1	Human	7.0	pKi	=	7.0	Binding	Displacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assayDisplacement of [3H]UR-DE257 from Gsalphas-coupled human H2R expressed in Sf9 cell membranes by competitive binding assay	ChEMBL		None	None	None		Cc1nc(N)sc1CCCN/C(N)=N/C(=O)NCCCCCCCCCCNC(=O)CCCCCN1/C(=C/C=C/C=C/C2=[N+](CCCCS(=O)(=O)[O-])c3ccccc3C2(C)C)c2ccccc2C1(C)C	10.1016/j.bmcl.2021.128388
	44304223	198705	0	None	-1023	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	374	12	0	4	4.5	CCCCCC(=O)c1ccc(OCCCN2CCN(CC(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
	CHEMBL59798	198705	0	None	-1023	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity for the human Histamine H2 receptorBinding affinity for the human Histamine H2 receptor	ChEMBL	374	12	0	4	4.5	CCCCCC(=O)c1ccc(OCCCN2CCN(CC(C)C)CC2)cc1	10.1016/s0960-894x(02)00309-8
	133	2460	48	None	-141	42	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	nan
	1723	2460	48	None	-141	42	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	nan
	28693	2460	48	None	-141	42	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	nan
	CHEMBL19215	2460	48	None	-141	42	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	nan
	DB13520	2460	48	None	-141	42	Human	6.0	pKi	=	6.0	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	nan
	44335172	5028	0	None	-467	3	Human	4.0	pKi	=	4.0	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	374	7	0	5	4.0	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccsc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	CHEMBL105567	5028	0	None	-467	3	Human	4.0	pKi	=	4.0	Binding	Binding affinity to the human cortical histamine H2 receptorBinding affinity to the human cortical histamine H2 receptor	ChEMBL	374	7	0	5	4.0	CCOC(=O)N1CCN(CCCOc2ccc(-c3ccsc3)cc2)CC1	10.1016/s0960-894x(02)00648-0
	44304311	198609	0	None	-16982	3	Human	4.0	pKi	=	4.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	442	10	1	7	2.2	N[C@H](Cc1nccs1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	CHEMBL59733	198609	0	None	-16982	3	Human	4.0	pKi	=	4.0	Binding	Binding affinity towards Histamine H2 receptor from human membranesBinding affinity towards Histamine H2 receptor from human membranes	ChEMBL	442	10	1	7	2.2	N[C@H](Cc1nccs1)C(=O)N1CCN(CCCOc2ccc(C(=O)C3CC3)cc2)CC1	10.1016/s0960-894x(02)00310-4
	71450548	83386	0	None	-7	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	295	3	1	3	2.0	COc1cccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)c1	10.1016/j.bmcl.2012.08.046
	CHEMBL2205824	83386	0	None	-7	3	Human	5.0	pKi	=	5.0	Binding	Binding affinity to Histamine H2 receptorBinding affinity to Histamine H2 receptor	ChEMBL	295	3	1	3	2.0	COc1cccc(CN2C3C4C5CC6C7C5C3C7C2(O)C64)c1	10.1016/j.bmcl.2012.08.046
	127049855	139698	0	None	-16	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method	ChEMBL	368	7	3	4	3.1	N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1	10.1021/acs.jmedchem.6b00120
	CHEMBL3805220	139698	0	None	-16	4	Human	5.0	pKi	=	5.0	Binding	Displacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]tiotidine from human histamine H2 receptor expressed in sf9 cell membrane co-expressing Gsalphas incubated for 60 mins by liquid scintillation counting method	ChEMBL	368	7	3	4	3.1	N#C/N=C(/NCCSc1ccccc1)NC[C@@H]1CC[C@@H](c2c[nH]cn2)C1	10.1021/acs.jmedchem.6b00120
	132060763	162311	0	None	-3	8	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	405	5	0	4	4.1	C=C(C)CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1	10.1016/j.ejmech.2018.02.024
	CHEMBL4173095	162311	0	None	-3	8	Human	6.0	pKi	=	6.0	Binding	Displacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [125I]-iodoaminopotentidine from human histamine H2 receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method	ChEMBL	405	5	0	4	4.1	C=C(C)CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1	10.1016/j.ejmech.2018.02.024
	135	2496	38	None	-39	57	Human	6.0	pKi	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
	1796	2496	38	None	-39	57	Human	6.0	pKi	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
	4184	2496	38	None	-39	57	Human	6.0	pKi	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
	CHEMBL6437	2496	38	None	-39	57	Human	6.0	pKi	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
	DB06148	2496	38	None	-39	57	Human	6.0	pKi	=	6	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	nan
	2281	3126	76	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	Drug Central	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	None
	4922	3126	76	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	Drug Central	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	None
	893	3126	76	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	Drug Central	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	None
	CHEMBL316561	3126	76	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	Drug Central	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	None
	DB13431	3126	76	None	-	0	Rat	8.6	pIC50	=	8.6	Binding	Inhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitroInhibitory activity against binding of [125I](Nle11)-HG-13 to Histamine H2 receptor in vitro	Drug Central	334	10	2	3	2.3	CCCN(C(=O)C(NC(=O)c1ccccc1)CCC(=O)O)CCC	None
	1231	924	112	None	-2	7	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	2756	924	112	None	-2	7	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	645	924	112	None	-2	7	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	CHEMBL30	924	112	None	-2	7	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	DB00501	924	112	None	-2	7	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	1234	3239	0	None	-2	6	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
	3001055	3239	0	None	-2	6	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
	CHEMBL512	3239	0	None	-2	6	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
	DB00863	3239	0	None	-2	6	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
	3033637	215992	0	None	-	1	Human	8.2	pKd	=	8.2	Binding	NoneNone	Drug Central	331	10	2	8	1.3	CNC(NCCSCC1=CSC(CN(C)C)=N1)=C[N+]([O-])=O	None
	5105	176253	49	None	-	1	Human	8.1	pKd	=	8.1	Binding	NoneNone	Drug Central	348	9	1	5	2.1	CC(=O)OCC(=O)NCCCOc1cccc(CN2CCCCC2)c1	None
	CHEMBL46102	176253	49	None	-	1	Human	8.1	pKd	=	8.1	Binding	NoneNone	Drug Central	348	9	1	5	2.1	CC(=O)OCC(=O)NCCCOc1cccc(CN2CCCCC2)c1	None
	1129	1591	89	None	-	1	Human	8.1	pKd	=	8.1	Binding	NoneNone	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
	3325	1591	89	None	-	1	Human	8.1	pKd	=	8.1	Binding	NoneNone	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
	5353622	1591	89	None	-	1	Human	8.1	pKd	=	8.1	Binding	NoneNone	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
	5702160	1591	89	None	-	1	Human	8.1	pKd	=	8.1	Binding	NoneNone	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
	7074	1591	89	None	-	1	Human	8.1	pKd	=	8.1	Binding	NoneNone	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
	CHEMBL902	1591	89	None	-	1	Human	8.1	pKd	=	8.1	Binding	NoneNone	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
	DB00927	1591	89	None	-	1	Human	8.1	pKd	=	8.1	Binding	NoneNone	Drug Central	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	None
	1235	3763	32	None	-2	4	Human	8.2	pKd	=	8.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	12869657
	3959	3763	32	None	-2	4	Human	8.2	pKd	=	8.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	12869657
	50287	3763	32	None	-2	4	Human	8.2	pKd	=	8.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	12869657
	CHEMBL269646	3763	32	None	-2	4	Human	8.2	pKd	=	8.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	12869657
	46222048	8896	0	UNDEFINED	-4365	13	Human	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	260	4	1	2	4.0	CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1	None
	CHEMBL1098230	8896	0	UNDEFINED	-4365	13	Human	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	260	4	1	2	4.0	CC(C)(C)c1ccc(SCCc2c[nH]cn2)cc1	None
	179	396	107	3H-TIOTIDINE	-4365	50	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	369	7	2	6	1.3	CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC	None
	2159	396	107	3H-TIOTIDINE	-4365	50	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	369	7	2	6	1.3	CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC	None
	963	396	107	3H-TIOTIDINE	-4365	50	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	369	7	2	6	1.3	CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC	None
	CHEMBL243712	396	107	3H-TIOTIDINE	-4365	50	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	369	7	2	6	1.3	CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC	None
	DB06288	396	107	3H-TIOTIDINE	-4365	50	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	369	7	2	6	1.3	CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC	None
	242	467	117	3H-TIOTIDINE	-7244	51	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	None
	34	467	117	3H-TIOTIDINE	-7244	51	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	None
	60795	467	117	3H-TIOTIDINE	-7244	51	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	None
	CHEMBL1112	467	117	3H-TIOTIDINE	-7244	51	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	None
	DB01238	467	117	3H-TIOTIDINE	-7244	51	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	None
	1231	924	112	3H-Histamine	-2	7	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	2756	924	112	3H-Histamine	-2	7	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	645	924	112	3H-Histamine	-2	7	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	CHEMBL30	924	112	3H-Histamine	-2	7	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	DB00501	924	112	3H-Histamine	-2	7	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	1204	1901	114	3H-TIOTIDINE	-173	23	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1247	1901	114	3H-TIOTIDINE	-173	23	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1375	1901	114	3H-TIOTIDINE	-173	23	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	774	1901	114	3H-TIOTIDINE	-173	23	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	CHEMBL90	1901	114	3H-TIOTIDINE	-173	23	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	DB05381	1901	114	3H-TIOTIDINE	-173	23	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	134	2478	19	3H-TIOTIDINE	-8511	67	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	None
	1775	2478	19	3H-TIOTIDINE	-8511	67	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	None
	9681	2478	19	3H-TIOTIDINE	-8511	67	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	None
	CHEMBL1065	2478	19	3H-TIOTIDINE	-8511	67	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	None
	DB00247	2478	19	3H-TIOTIDINE	-8511	67	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	None
	15897	2817	0	3H-TIOTIDINE	-354	36	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	203	2	1	1	2.6	CC(Cc1cccc(c1)C(F)(F)F)N	None
	215	2817	0	3H-TIOTIDINE	-354	36	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	203	2	1	1	2.6	CC(Cc1cccc(c1)C(F)(F)F)N	None
	CHEMBL1979333	2817	0	3H-TIOTIDINE	-354	36	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	203	2	1	1	2.6	CC(Cc1cccc(c1)C(F)(F)F)N	None
	2337	3205	72	3H-TIOTIDINE	-1122	62	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	None
	50	3205	72	3H-TIOTIDINE	-1122	62	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	None
	5002	3205	72	3H-TIOTIDINE	-1122	62	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	None
	CHEMBL716	3205	72	3H-TIOTIDINE	-1122	62	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	None
	DB01224	3205	72	3H-TIOTIDINE	-1122	62	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	None
	1234	3239	0	3H-Histamine	-2	6	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
	3001055	3239	0	3H-Histamine	-2	6	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
	CHEMBL512	3239	0	3H-Histamine	-2	6	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
	DB00863	3239	0	3H-Histamine	-2	6	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
	6917970	3635	54	3H-TIOTIDINE	-2290	34	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	327	2	2	5	2.8	COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O	None
	8370	3635	54	3H-TIOTIDINE	-2290	34	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	327	2	2	5	2.8	COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O	None
	CHEMBL487387	3635	54	3H-TIOTIDINE	-2290	34	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	327	2	2	5	2.8	COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O	None
	1267	3744	43	3H-TIOTIDINE	-4168	25	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	292	2	2	2	2.8	S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1	None
	3035905	3744	43	3H-TIOTIDINE	-4168	25	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	292	2	2	2	2.8	S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1	None
	CHEMBL260374	3744	43	3H-TIOTIDINE	-4168	25	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	292	2	2	2	2.8	S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1	None
	1235	3763	32	3H-Histamine	-2	4	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
	3959	3763	32	3H-Histamine	-2	4	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
	50287	3763	32	3H-Histamine	-2	4	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
	CHEMBL269646	3763	32	3H-Histamine	-2	4	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
	2662	11279	124	3H-TIOTIDINE	-41	31	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	381	3	1	4	3.5	Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1	None
	CHEMBL118	11279	124	3H-TIOTIDINE	-41	31	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	381	3	1	4	3.5	Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1	None
	10297	26905	29	3H-TIOTIDINE	-38	43	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	151	2	2	2	1.1	C[C@H](N)[C@H](O)c1ccccc1	None
	CHEMBL136560	26905	29	3H-TIOTIDINE	-38	43	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	151	2	2	2	1.1	C[C@H](N)[C@H](O)c1ccccc1	None
	156391	46537	95	3H-TIOTIDINE	-1	30	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	230	3	1	2	3.0	COc1ccc2cc([C@H](C)C(=O)O)ccc2c1	None
	CHEMBL1200806	46537	95	3H-TIOTIDINE	-1	30	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	230	3	1	2	3.0	COc1ccc2cc([C@H](C)C(=O)O)ccc2c1	None
	CHEMBL154	46537	95	3H-TIOTIDINE	-1	30	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	230	3	1	2	3.0	COc1ccc2cc([C@H](C)C(=O)O)ccc2c1	None
	10624	69957	17	3H-TIOTIDINE	-102	32	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	284	5	3	3	1.7	CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12	None
	138543650	69957	17	3H-TIOTIDINE	-102	32	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	284	5	3	3	1.7	CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12	None
	CHEMBL194378	69957	17	3H-TIOTIDINE	-102	32	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	284	5	3	3	1.7	CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12	None
	2244	93798	96	3H-TIOTIDINE	-1	28	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	180	2	1	3	1.3	CC(=O)Oc1ccccc1C(=O)O	None
	CHEMBL25	93798	96	3H-TIOTIDINE	-1	28	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	180	2	1	3	1.3	CC(=O)Oc1ccccc1C(=O)O	None
	446220	132998	13	3H-TIOTIDINE	-1778	45	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	303	3	0	5	1.9	COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C	None
	CHEMBL370805	132998	13	3H-TIOTIDINE	-1778	45	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	303	3	0	5	1.9	COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C	None
	44208932	140176	6	UNDEFINED	-120226	37	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	475	5	1	3	6.8	Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1	None
	CHEMBL381689	140176	6	UNDEFINED	-120226	37	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	475	5	1	3	6.8	Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1	None
	1615	167228	22	3H-PYRILAMINE	-26	44	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	193	3	1	3	1.6	CNC(C)Cc1ccc2c(c1)OCO2	None
	1615	167228	22	3H-TIOTIDINE	-26	44	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	193	3	1	3	1.6	CNC(C)Cc1ccc2c(c1)OCO2	None
	CHEMBL43048	167228	22	3H-PYRILAMINE	-26	44	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	193	3	1	3	1.6	CNC(C)Cc1ccc2c(c1)OCO2	None
	CHEMBL43048	167228	22	3H-TIOTIDINE	-26	44	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	193	3	1	3	1.6	CNC(C)Cc1ccc2c(c1)OCO2	None
	54676228	192874	108	3H-TIOTIDINE	-1	28	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	331	2	2	5	1.6	CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O	None
	CHEMBL527	192874	108	3H-TIOTIDINE	-1	28	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	331	2	2	5	1.6	CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O	None
	4495	194860	87	3H-TIOTIDINE	-1	30	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	308	5	1	5	2.8	CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1	None
	CHEMBL56367	194860	87	3H-TIOTIDINE	-1	30	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	308	5	1	5	2.8	CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1	None
	54677470	198867	110	3H-TIOTIDINE	-1	30	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	351	2	2	6	2.0	Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1	None
	CHEMBL1256873	198867	110	3H-TIOTIDINE	-1	30	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	351	2	2	6	2.0	Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1	None
	CHEMBL599	198867	110	3H-TIOTIDINE	-1	30	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	351	2	2	6	2.0	Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1	None
	162265	200587	19	3H-TIOTIDINE	-239	44	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	151	2	2	2	1.1	CC(N)C(O)c1ccccc1	None
	4786	200587	19	3H-TIOTIDINE	-239	44	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	151	2	2	2	1.1	CC(N)C(O)c1ccccc1	None
	CHEMBL61006	200587	19	3H-TIOTIDINE	-239	44	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	151	2	2	2	1.1	CC(N)C(O)c1ccccc1	None
	1973	201790	12	3H-APT	-3	35	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	462	3	1	7	3.9	Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12	None
	CHEMBL1394464	201790	12	3H-APT	-3	35	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	462	3	1	7	3.9	Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12	None
	CHEMBL66089	201790	12	3H-APT	-3	35	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	462	3	1	7	3.9	Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12	None
	4054	203790	64	3H-TIOTIDINE	-1	37	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	179	0	1	1	2.7	CC12CC3CC(C)(C1)CC(N)(C3)C2	None
	CHEMBL1699	203790	64	3H-TIOTIDINE	-1	37	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	179	0	1	1	2.7	CC12CC3CC(C)(C1)CC(N)(C3)C2	None
	CHEMBL807	203790	64	3H-TIOTIDINE	-1	37	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	179	0	1	1	2.7	CC12CC3CC(C)(C1)CC(N)(C3)C2	None
	11954224	214174	0	3H-TIOTIDINE	-141253	59	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	581	4	3	6	2.0	CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C	None
	None	214217	0	I125- Tiotodine	-1	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	329	2	0	4	3.6	CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl	None
	104911	214249	0	3H-TIOTIDINE	-41686	36	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	530	7	0	5	5.1	COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl	None
	25137849	214425	0	3H-TIOTIDINE	-4	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	165	3	2	2	1.3	CC(C(C1=CC=CC=C1)O)NC	None
	71290	214425	0	3H-TIOTIDINE	-4	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	165	3	2	2	1.3	CC(C(C1=CC=CC=C1)O)NC	None
	3337	214441	0	3H-TIOTIDINE	-1513	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)CC1=CC(=CC=C1)C(F)(F)F	None
	65801	214441	0	3H-TIOTIDINE	-1513	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)CC1=CC(=CC=C1)C(F)(F)F	None
	66264	214441	0	3H-TIOTIDINE	-1513	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)CC1=CC(=CC=C1)C(F)(F)F	None
	91452	214441	0	3H-TIOTIDINE	-1513	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	231	4	1	1	3.2	CCNC(C)CC1=CC(=CC=C1)C(F)(F)F	None
	3821	214549	0	3H-TIOTIDINE	-1	18	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	237	2	1	2	2.9	CNC1(CCCCC1=O)C2=CC=CC=C2Cl	None
	None	214560	0	3H-TIOTIDINE	-1	33	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	240	7	4	6	-0.8	C(C(C(=O)O)N)SSCC(C(=O)O)N	None
	None	214561	0	3H-TIOTIDINE	-1	33	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	149	4	2	3	0.2	CSCCC(C(=O)O)N	None
	None	214562	0	3H-TIOTIDINE	-1	33	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	135	3	3	3	-0.3	C(CS)C(C(=O)O)N	None
	None	214563	0	3H-TIOTIDINE	-1	33	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	121	2	3	3	-0.7	C(C(C(=O)O)N)S	None
	None	214564	0	3H-TIOTIDINE	-1	28	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	117	0	1	3	-0.0	C1CSC(=O)C1N	None
	None	214565	0	3H-TIOTIDINE	-1	39	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	153	3	3	3	-1.4	C(C(C(=O)O)N)S(=O)O	None
	None	214566	0	3H-TIOTIDINE	-1	38	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	169	3	3	4	-1.7	C(C(C(=O)O)N)S(=O)(=O)O	None
	None	214574	0	3H-TIOTIDINE	-13	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	149	2	1	2	1.2	CC(C(=O)C1=CC=CC=C1)N	None
	1576	214575	0	3H-TIOTIDINE	-16	40	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	163	3	1	2	1.5	CC(C(=O)C1=CC=CC=C1)NC	None
	135269	214639	0	3H-TIOTIDINE	-1	30	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	222	5	1	3	2.5	CCCCC(=O)OC1=CC=CC=C1C(=O)O	None
	23681059	214640	0	3H-TIOTIDINE	-1	29	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	230	3	1	2	3.0	CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)O	None
	5018304	214641	0	3H-TIOTIDINE	-1	29	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	317	4	1	3	0.0	C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+]	None
	3672	214642	0	3H-TIOTIDINE	-1	28	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	206	4	1	1	3.1	CC(C)CC1=CC=C(C=C1)C(C)C(=O)O	None
	84003	214643	0	3H-TIOTIDINE	-1	28	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	376	6	5	7	-0.0	C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O	None
	123619	214644	0	3H-TIOTIDINE	-1412	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	358	3	0	4	4.2	CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl	None
	119828	214645	0	3H-TIOTIDINE	-1	30	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	370	5	1	5	3.5	CCC(=O)NS(=O)(=O)C1=CC=C(C=C1)C2=C(ON=C2C3=CC=CC=C3)C	None
	5090	214646	0	3H-TIOTIDINE	-1348	31	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	314	3	0	4	2.6	CS(=O)(=O)C1=CC=C(C=C1)C2=C(C(=O)OC2)C3=CC=CC=C3	None
	119607	214647	0	3H-TIOTIDINE	-97	28	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	314	3	1	4	3.0	CC1=C(C(=NO1)C2=CC=CC=C2)C3=CC=C(C=C3)S(=O)(=O)N	None
	None	214648	0	3H-TIOTIDINE	-7	29	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	517	8	2	5	5.2	CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)NCCC4=CC=C(C=C4)NC(=O)C	None
	None	214703	0	Functional	-660	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	322	5	2	3	4.1	CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl	None
	None	214703	0	UNDEFINED	-660	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	322	5	2	3	4.1	CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl	None
	None	214747	0	3H-TIOTIDINE	-4570	27	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	347	6	0	3	5.0	CC(=O)N(CC1=CC=CC=C1OC)C2=CC=CC=C2OC3=CC=CC=C3	None
	None	214752	0	125I-aminopotentidine	-10471285	17	Rat	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	372	2	1	3	4.4	CC(C)(C)C1=CC=C(C=C1)NC(=O)N2CCN(CC2)C3=C(C=CC=N3)Cl	None
	None	215341	0	UNDEFINED	-3467	5	Human	5.0	pKi	=	5	Binding	NoneNone	PDSP KiDatabase	463	4	1	4	3.7	C1C(C(=NN1C(=NS(=O)(=O)C2=CC=C(C=C2)C#N)N)C3=CC=C(C=C3)Cl)C4=CC=CC=C4	None
	1353	1880	85	3H-TIOTIDINE	-131	85	Human	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
	3559	1880	85	3H-TIOTIDINE	-131	85	Human	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
	86	1880	85	3H-TIOTIDINE	-131	85	Human	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
	CHEMBL54	1880	85	3H-TIOTIDINE	-131	85	Human	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
	DB00502	1880	85	3H-TIOTIDINE	-131	85	Human	6.0	pKi	=	6	Binding	NoneNone	PDSP KiDatabase	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
	2389	3279	114	3H-TIOTIDINE	-275	67	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
	5073	3279	114	3H-TIOTIDINE	-275	67	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
	96	3279	114	3H-TIOTIDINE	-275	67	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
	CHEMBL85	3279	114	3H-TIOTIDINE	-275	67	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
	DB00734	3279	114	3H-TIOTIDINE	-275	67	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
	115237	55296	113	3H-TIOTIDINE	-22	54	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	426	4	1	7	3.1	Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O	None
	CHEMBL1621	55296	113	3H-TIOTIDINE	-22	54	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	426	4	1	7	3.1	Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O	None
	100	3745	52	3H-TIOTIDINE	-46	55	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
	2637	3745	52	3H-TIOTIDINE	-46	55	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
	5452	3745	52	3H-TIOTIDINE	-46	55	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
	CHEMBL479	3745	52	3H-TIOTIDINE	-46	55	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
	DB00679	3745	52	3H-TIOTIDINE	-46	55	Human	6.9	pKi	=	6.9	Binding	NoneNone	PDSP KiDatabase	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
	1204	1901	114	3H-Histamine	-173	23	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1247	1901	114	3H-Histamine	-173	23	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1375	1901	114	3H-Histamine	-173	23	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	774	1901	114	3H-Histamine	-173	23	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	CHEMBL90	1901	114	3H-Histamine	-173	23	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	DB05381	1901	114	3H-Histamine	-173	23	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1235	3763	32	125I-iodoaminopotentidine	-2	4	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
	3959	3763	32	125I-iodoaminopotentidine	-2	4	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
	50287	3763	32	125I-iodoaminopotentidine	-2	4	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
	CHEMBL269646	3763	32	125I-iodoaminopotentidine	-2	4	Human	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	None
	135398737	944	89	3H-TIOTIDINE	-64	91	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
	38	944	89	3H-TIOTIDINE	-64	91	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
	722	944	89	3H-TIOTIDINE	-64	91	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
	CHEMBL42	944	89	3H-TIOTIDINE	-64	91	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
	DB00363	944	89	3H-TIOTIDINE	-64	91	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
	1204	1901	114	3H-TIOTIDINE	-316	23	Rat	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1247	1901	114	3H-TIOTIDINE	-316	23	Rat	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1375	1901	114	3H-TIOTIDINE	-316	23	Rat	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	774	1901	114	3H-TIOTIDINE	-316	23	Rat	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	CHEMBL90	1901	114	3H-TIOTIDINE	-316	23	Rat	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	DB05381	1901	114	3H-TIOTIDINE	-316	23	Rat	7.8	pKi	=	7.8	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	2726	906	64	3H-TIOTIDINE	-85	72	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
	621	906	64	3H-TIOTIDINE	-85	72	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
	83	906	64	3H-TIOTIDINE	-85	72	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
	CHEMBL71	906	64	3H-TIOTIDINE	-85	72	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
	DB00477	906	64	3H-TIOTIDINE	-85	72	Human	6.8	pKi	=	6.8	Binding	NoneNone	PDSP KiDatabase	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
	46780481	107045	18	3H-TIOTIDINE	-21	53	Human	8.6	pKi	=	8.6	Binding	NoneNone	PDSP KiDatabase	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
	9903970	107045	18	3H-TIOTIDINE	-21	53	Human	8.6	pKi	=	8.6	Binding	NoneNone	PDSP KiDatabase	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
	CHEMBL3187365	107045	18	3H-TIOTIDINE	-21	53	Human	8.6	pKi	=	8.6	Binding	NoneNone	PDSP KiDatabase	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
	CHEMBL3544974	107045	18	3H-TIOTIDINE	-21	53	Human	8.6	pKi	=	8.6	Binding	NoneNone	PDSP KiDatabase	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
	1613	2316	44	3H-TIOTIDINE	-8	44	Human	6.7	pKi	=	6.7	Binding	NoneNone	PDSP KiDatabase	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
	205	2316	44	3H-TIOTIDINE	-8	44	Human	6.7	pKi	=	6.7	Binding	NoneNone	PDSP KiDatabase	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
	3964	2316	44	3H-TIOTIDINE	-8	44	Human	6.7	pKi	=	6.7	Binding	NoneNone	PDSP KiDatabase	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
	CHEMBL831	2316	44	3H-TIOTIDINE	-8	44	Human	6.7	pKi	=	6.7	Binding	NoneNone	PDSP KiDatabase	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
	DB00408	2316	44	3H-TIOTIDINE	-8	44	Human	6.7	pKi	=	6.7	Binding	NoneNone	PDSP KiDatabase	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
	21830793	91403	5	3H-8-OH-DPAT	-14125	46	Bovine	5.7	pKi	=	5.7	Binding	NoneNone	PDSP KiDatabase	373	7	0	8	0.6	COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1	None
	CHEMBL2413154	91403	5	3H-8-OH-DPAT	-14125	46	Bovine	5.7	pKi	=	5.7	Binding	NoneNone	PDSP KiDatabase	373	7	0	8	0.6	COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1	None
	1226	1988	16	3H-Histamine	-7	6	Human	7.6	pKi	=	7.6	Binding	NoneNone	PDSP KiDatabase	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	None
	41376	1988	16	3H-Histamine	-7	6	Human	7.6	pKi	=	7.6	Binding	NoneNone	PDSP KiDatabase	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	None
	CHEMBL12608	1988	16	3H-Histamine	-7	6	Human	7.6	pKi	=	7.6	Binding	NoneNone	PDSP KiDatabase	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	None
	1248	1396	27	125I-iodoaminopotentidine	-123	6	Human	4.6	pKi	=	4.6	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
	3077	1396	27	125I-iodoaminopotentidine	-123	6	Human	4.6	pKi	=	4.6	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
	90045	1396	27	125I-iodoaminopotentidine	-123	6	Human	4.6	pKi	=	4.6	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
	CHEMBL12344	1396	27	125I-iodoaminopotentidine	-123	6	Human	4.6	pKi	=	4.6	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
	119570	3110	90	3H-TIOTIDINE	-281	40	Human	5.6	pKi	=	5.6	Binding	NoneNone	PDSP KiDatabase	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
	2233	3110	90	3H-TIOTIDINE	-281	40	Human	5.6	pKi	=	5.6	Binding	NoneNone	PDSP KiDatabase	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
	953	3110	90	3H-TIOTIDINE	-281	40	Human	5.6	pKi	=	5.6	Binding	NoneNone	PDSP KiDatabase	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
	CHEMBL301265	3110	90	3H-TIOTIDINE	-281	40	Human	5.6	pKi	=	5.6	Binding	NoneNone	PDSP KiDatabase	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
	DB00413	3110	90	3H-TIOTIDINE	-281	40	Human	5.6	pKi	=	5.6	Binding	NoneNone	PDSP KiDatabase	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
	1248	1396	27	3H-Histamine	-123	6	Human	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
	3077	1396	27	3H-Histamine	-123	6	Human	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
	90045	1396	27	3H-Histamine	-123	6	Human	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
	CHEMBL12344	1396	27	3H-Histamine	-123	6	Human	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	161	4	2	3	0.6	CN(CCCSC(=N)N)C	None
	213	3792	50	3H-TIOTIDINE	-7	43	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
	2717	3792	50	3H-TIOTIDINE	-7	43	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
	5533	3792	50	3H-TIOTIDINE	-7	43	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
	CHEMBL621	3792	50	3H-TIOTIDINE	-7	43	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
	DB00656	3792	50	3H-TIOTIDINE	-7	43	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
	135409468	2004	63	3H-TIOTIDINE	-123	40	Human	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	312	1	2	4	1.7	Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1	None
	333	2004	63	3H-TIOTIDINE	-123	40	Human	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	312	1	2	4	1.7	Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1	None
	CHEMBL845	2004	63	3H-TIOTIDINE	-123	40	Human	6.5	pKi	=	6.5	Binding	NoneNone	PDSP KiDatabase	312	1	2	4	1.7	Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1	None
	2865	4079	67	3H-TIOTIDINE	-281	53	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
	59	4079	67	3H-TIOTIDINE	-281	53	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
	60854	4079	67	3H-TIOTIDINE	-281	53	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
	CHEMBL708	4079	67	3H-TIOTIDINE	-281	53	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
	DB00246	4079	67	3H-TIOTIDINE	-281	53	Human	5.5	pKi	=	5.5	Binding	NoneNone	PDSP KiDatabase	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
	3032915	15321	20	3H-Histamine	-25	6	Human	7.4	pKi	=	7.4	Binding	NoneNone	PDSP KiDatabase	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	None
	CHEMBL12160	15321	20	3H-Histamine	-25	6	Human	7.4	pKi	=	7.4	Binding	NoneNone	PDSP KiDatabase	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	None
	3032915	15321	20	125I-iodoaminopotentidine	-25	6	Human	5.4	pKi	=	5.4	Binding	NoneNone	PDSP KiDatabase	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	None
	CHEMBL12160	15321	20	125I-iodoaminopotentidine	-25	6	Human	5.4	pKi	=	5.4	Binding	NoneNone	PDSP KiDatabase	212	5	3	2	1.2	C/N=C(\S)NCCCCc1c[nH]cn1	None
	1204	1901	114	None	-173	23	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1247	1901	114	None	-173	23	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1375	1901	114	None	-173	23	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	774	1901	114	None	-173	23	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	CHEMBL90	1901	114	None	-173	23	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	DB05381	1901	114	None	-173	23	Human	8.4	pKi	=	8.4	Binding	Displacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cellsDisplacement of [125I]iodoaminopotentidine from human histamine H2 receptor expressed in CHO cells	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	18609376	202656	61	None	-	1	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	386	2	0	4	4.7	CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C	None
	6279	202656	61	None	-	1	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	386	2	0	4	4.7	CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C	None
	CHEMBL717	202656	61	None	-	1	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	386	2	0	4	4.7	CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C[C@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C	None
	3823	49951	38	None	-66	11	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	530	7	0	7	4.2	CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1	None
	76973198	49951	38	None	-66	11	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	530	7	0	7	4.2	CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1	None
	CHEMBL157101	49951	38	None	-66	11	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	530	7	0	7	4.2	CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1	None
	104903	56050	14	None	-5	6	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	624	6	0	8	5.5	C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1	None
	CHEMBL1630578	56050	14	None	-5	6	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	624	6	0	8	5.5	C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)C3=CC[C@]2(C)[C@H]1C(=O)CN1CCN(c2cc(N3CCCC3)nc(N3CCCC3)n2)CC1	None
	5048	3084	57	None	-114	7	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	None
	8924	3084	57	None	-114	7	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	None
	9948102	3084	57	None	-114	7	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	None
	CHEMBL462605	3084	57	None	-114	7	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	None
	DB11642	3084	57	None	-114	7	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	None
	176	394	63	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
	2157	394	63	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
	2566	394	63	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
	CHEMBL633	394	63	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
	DB01118	394	63	None	-6	31	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	None
	11954259	214201	0	3H-TIOTIDINE	-1348	43	Human	6.4	pKi	=	6.4	Binding	NoneNone	PDSP KiDatabase	443	5	0	5	3.5	CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C	None
	135398745	2869	108	3H-TIOTIDINE	-9	65	Human	7.4	pKi	=	7.4	Binding	NoneNone	PDSP KiDatabase	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	None
	47	2869	108	3H-TIOTIDINE	-9	65	Human	7.4	pKi	=	7.4	Binding	NoneNone	PDSP KiDatabase	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	None
	CHEMBL715	2869	108	3H-TIOTIDINE	-9	65	Human	7.4	pKi	=	7.4	Binding	NoneNone	PDSP KiDatabase	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	None
	DB00334	2869	108	3H-TIOTIDINE	-9	65	Human	7.4	pKi	=	7.4	Binding	NoneNone	PDSP KiDatabase	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	None
	1016	3690	75	None	-41	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
	2561	3690	75	None	-41	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
	2733526	3690	75	None	-41	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
	5384	3690	75	None	-41	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
	CHEMBL83	3690	75	None	-41	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
	DB00675	3690	75	None	-41	35	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	None
	1210	905	45	None	-281	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	None
	1213	905	45	None	-281	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	None
	2725	905	45	None	-281	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	None
	33036	905	45	None	-281	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	None
	4411	905	45	None	-281	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	None
	616	905	45	None	-281	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	None
	6976	905	45	None	-281	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	None
	716121	905	45	None	-281	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	None
	90475904	905	45	None	-281	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	None
	CHEMBL1201353	905	45	None	-281	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	None
	CHEMBL1554789	905	45	None	-281	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	None
	CHEMBL505	905	45	None	-281	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	None
	DB01114	905	45	None	-281	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	None
	DB13679	905	45	None	-281	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	274	5	0	2	3.8	CN(CCC(c1ccccn1)c1ccc(cc1)Cl)C	None
	4601	205020	29	None	-7	17	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	None
	CHEMBL1201023	205020	29	None	-7	17	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	None
	CHEMBL900	205020	29	None	-7	17	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	269	6	0	2	3.7	Cc1ccccc1C(OCCN(C)C)c1ccccc1	None
	4189	205195	91	None	-36	34	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	None
	CHEMBL1559	205195	91	None	-36	34	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	None
	CHEMBL91	205195	91	None	-36	34	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	414	6	0	3	6.5	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1	None
	2812	4711	96	None	-33	34	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	None
	CHEMBL104	4711	96	None	-33	34	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	None
	1530	2151	44	None	-151	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	None
	3827	2151	44	None	-151	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	None
	7206	2151	44	None	-151	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	None
	CHEMBL534	2151	44	None	-151	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	None
	DB00920	2151	44	None	-151	20	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	0	0	3	4.0	CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1	None
	237	203157	43	None	-3	13	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	None
	CHEMBL546257	203157	43	None	-3	13	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	None
	CHEMBL554190	203157	43	None	-3	13	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	None
	CHEMBL7568	203157	43	None	-3	13	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	399	9	1	4	6.0	CCN(CC)CCCC(C)Nc1c2ccc(Cl)cc2nc2ccc(OC)cc12	None
	2865	4079	67	None	-281	53	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
	59	4079	67	None	-281	53	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
	60854	4079	67	None	-281	53	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
	CHEMBL708	4079	67	None	-281	53	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
	DB00246	4079	67	None	-281	53	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	None
	213	3792	50	None	-7	43	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
	2717	3792	50	None	-7	43	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
	5533	3792	50	None	-7	43	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
	CHEMBL621	3792	50	None	-7	43	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
	DB00656	3792	50	None	-7	43	Human	8.3	pKi	=	8.3	Binding	NoneNone	Drug Central	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	None
	1599	2309	47	None	-154	15	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	None
	3955	2309	47	None	-154	15	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	None
	7215	2309	47	None	-154	15	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	None
	CHEMBL841	2309	47	None	-154	15	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	None
	DB00836	2309	47	None	-154	15	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	476	7	1	3	5.1	Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1	None
	3191	102385	93	None	-24	25	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	469	9	0	3	7.2	CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1	None
	CHEMBL305660	102385	93	None	-24	25	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	469	9	0	3	7.2	CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1	None
	2284	3133	27	None	-53	28	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	None
	4926	3133	27	None	-53	28	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	None
	7281	3133	27	None	-53	28	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	None
	CHEMBL564	3133	27	None	-53	28	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	None
	DB00420	3133	27	None	-53	28	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	None
	2520	202310	65	None	-20	11	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	None
	CHEMBL1280	202310	65	None	-20	11	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	None
	CHEMBL6966	202310	65	None	-20	11	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	None
	4543	169982	36	None	-15	29	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2ccccc21	None
	CHEMBL1201156	169982	36	None	-15	29	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2ccccc21	None
	CHEMBL445	169982	36	None	-15	29	Human	8.3	pKi	=	8.3	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2ccccc21	None
	2801	161325	56	None	-12	28	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	314	4	0	2	4.5	CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21	None
	CHEMBL1200710	161325	56	None	-12	28	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	314	4	0	2	4.5	CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21	None
	CHEMBL415	161325	56	None	-12	28	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	314	4	0	2	4.5	CN(C)CCCN1c2ccccc2CCc2ccc(Cl)cc21	None
	5291	205704	115	None	-1	2	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	493	7	2	7	4.6	Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1	None
	CHEMBL941	205704	115	None	-1	2	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	493	7	2	7	4.6	Cc1ccc(NC(=O)c2ccc(CN3CCN(C)CC3)cc2)cc1Nc1nccc(-c2cccnc2)n1	None
	1225	1443	24	None	-20	21	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	279	3	0	2	4.0	CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C	None
	3958	1443	24	None	-20	21	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	279	3	0	2	4.0	CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C	None
	667477	1443	24	None	-20	21	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	279	3	0	2	4.0	CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C	None
	CHEMBL860	1443	24	None	-20	21	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	279	3	0	2	4.0	CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C	None
	DB01142	1443	24	None	-20	21	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	279	3	0	2	4.0	CN(CC/C=C\1/c2ccccc2OCc2c1cccc2)C	None
	2247	502	77	None	-56	41	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
	249	502	77	None	-56	41	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
	2603	502	77	None	-56	41	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
	CHEMBL296419	502	77	None	-56	41	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
	DB00637	502	77	None	-56	41	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	None
	3042	1386	31	None	-53	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	None
	355	1386	31	None	-53	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	None
	868	1386	31	None	-53	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	None
	CHEMBL1123	1386	31	None	-53	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	None
	DB00804	1386	31	None	-53	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	309	7	0	3	4.4	CCN(CCOC(=O)C1(CCCCC1)C1CCCCC1)CC	None
	3198	203802	73	None	-19	34	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	380	6	0	3	5.8	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1	None
	CHEMBL1201049	203802	73	None	-19	34	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	380	6	0	3	5.8	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1	None
	CHEMBL808	203802	73	None	-19	34	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	380	6	0	3	5.8	Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1	None
	57469	18678	120	None	-1	3	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	240	2	1	4	2.8	CC(C)Cn1cnc2c(N)nc3ccccc3c21	None
	CHEMBL1282	18678	120	None	-1	3	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	240	2	1	4	2.8	CC(C)Cn1cnc2c(N)nc3ccccc3c21	None
	1231	924	112	None	1	7	Rat	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	2756	924	112	None	1	7	Rat	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	645	924	112	None	1	7	Rat	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	CHEMBL30	924	112	None	1	7	Rat	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	DB00501	924	112	None	1	7	Rat	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	1201549	590	22	None	-74	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	None
	333	590	22	None	-74	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	None
	7601	590	22	None	-74	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	None
	CHEMBL1201203	590	22	None	-74	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	None
	CHEMBL438151	590	22	None	-74	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	None
	DB00245	590	22	None	-74	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	307	4	0	2	4.4	CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1	None
	2286	3134	48	None	-26	29	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	None
	4927	3134	48	None	-26	29	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	None
	7282	3134	48	None	-26	29	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	None
	CHEMBL643	3134	48	None	-26	29	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	None
	DB01069	3134	48	None	-26	29	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	None
	11057	175575	19	None	-2	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	None
	3468	175575	19	None	-2	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	None
	CHEMBL459265	175575	19	None	-2	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	None
	CHEMBL64894	175575	19	None	-2	20	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	372	4	0	2	4.5	CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1	None
	124087	1362	106	None	-29	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	None
	7157	1362	106	None	-29	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	None
	814	1362	106	None	-29	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	None
	CHEMBL1172	1362	106	None	-29	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	None
	DB00967	1362	106	None	-29	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	None
	1588	2294	24	None	-323	43	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	None
	28864	2294	24	None	-323	43	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	None
	43	2294	24	None	-323	43	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	None
	CHEMBL157138	2294	24	None	-323	43	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	None
	DB00589	2294	24	None	-323	43	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	338	3	2	2	2.8	CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC	None
	103	4089	56	3H-TIOTIDINE	-46	53	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
	2875	4089	56	3H-TIOTIDINE	-46	53	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
	5736	4089	56	3H-TIOTIDINE	-46	53	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
	CHEMBL285802	4089	56	3H-TIOTIDINE	-46	53	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
	DB09225	4089	56	3H-TIOTIDINE	-46	53	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
	1226	1988	16	125I-iodoaminopotentidine	-7	6	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	None
	41376	1988	16	125I-iodoaminopotentidine	-7	6	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	None
	CHEMBL12608	1988	16	125I-iodoaminopotentidine	-7	6	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	None
	1204	1901	114	125I-iodoaminopotentidine	-173	23	Human	4.3	pKi	=	4.3	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1247	1901	114	125I-iodoaminopotentidine	-173	23	Human	4.3	pKi	=	4.3	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1375	1901	114	125I-iodoaminopotentidine	-173	23	Human	4.3	pKi	=	4.3	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	774	1901	114	125I-iodoaminopotentidine	-173	23	Human	4.3	pKi	=	4.3	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	CHEMBL90	1901	114	125I-iodoaminopotentidine	-173	23	Human	4.3	pKi	=	4.3	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	DB05381	1901	114	125I-iodoaminopotentidine	-173	23	Human	4.3	pKi	=	4.3	Binding	NoneNone	PDSP KiDatabase	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1212	1632	45	3H-TIOTIDINE	-323	65	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
	204	1632	45	3H-TIOTIDINE	-323	65	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
	3372	1632	45	3H-TIOTIDINE	-323	65	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
	CHEMBL726	1632	45	3H-TIOTIDINE	-323	65	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
	DB00623	1632	45	3H-TIOTIDINE	-323	65	Human	6.3	pKi	=	6.3	Binding	NoneNone	PDSP KiDatabase	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
	1223	940	32	3H-TIOTIDINE	-32359	11	Human	5.2	pKi	=	5.2	Binding	NoneNone	PDSP KiDatabase	308	6	2	3	3.2	Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N	None
	2790	940	32	3H-TIOTIDINE	-32359	11	Human	5.2	pKi	=	5.2	Binding	NoneNone	PDSP KiDatabase	308	6	2	3	3.2	Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N	None
	CHEMBL14690	940	32	3H-TIOTIDINE	-32359	11	Human	5.2	pKi	=	5.2	Binding	NoneNone	PDSP KiDatabase	308	6	2	3	3.2	Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N	None
	135	2496	38	None	-39	57	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	None
	1796	2496	38	None	-39	57	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	None
	4184	2496	38	None	-39	57	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	None
	CHEMBL6437	2496	38	None	-39	57	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	None
	DB06148	2496	38	None	-39	57	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	None
	33630	178379	94	None	-13	27	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	Drug Central	523	7	1	2	7.5	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	None
	CHEMBL47050	178379	94	None	-13	27	Human	8.2	pKi	=	8.2	Binding	Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assayDisplacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells by radioligand binding assay	Drug Central	523	7	1	2	7.5	OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1	None
	1353	1880	85	None	-131	85	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
	3559	1880	85	None	-131	85	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
	86	1880	85	None	-131	85	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
	CHEMBL54	1880	85	None	-131	85	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
	DB00502	1880	85	None	-131	85	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	None
	133	2460	48	None	-141	42	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	None
	1723	2460	48	None	-141	42	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	None
	28693	2460	48	None	-141	42	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	None
	CHEMBL19215	2460	48	None	-141	42	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	None
	DB13520	2460	48	None	-141	42	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	403	4	1	4	4.1	O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C	None
	1234	3239	0	None	2	6	Rat	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
	3001055	3239	0	None	2	6	Rat	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
	CHEMBL512	3239	0	None	2	6	Rat	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
	DB00863	3239	0	None	2	6	Rat	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
	1212	1632	45	None	-323	65	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
	204	1632	45	None	-323	65	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
	3372	1632	45	None	-323	65	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
	CHEMBL726	1632	45	None	-323	65	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
	DB00623	1632	45	None	-323	65	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	None
	3389	215982	0	None	-1	26	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	549	12	0	6	6.8	CCCCCCC(=O)OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1	None
	103	4089	56	None	-46	53	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
	2875	4089	56	None	-46	53	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
	5736	4089	56	None	-46	53	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
	CHEMBL285802	4089	56	None	-46	53	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
	DB09225	4089	56	None	-46	53	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	331	4	0	3	4.9	CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C	None
	212	3746	43	None	-6	25	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	None
	2639	3746	43	None	-6	25	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	None
	941651	3746	43	None	-6	25	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	None
	CHEMBL1201	3746	43	None	-6	25	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	None
	DB01623	3746	43	None	-6	25	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	None
	4011	81996	43	None	-27	23	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	277	4	1	1	4.2	CNCCCC12CCC(c3ccccc31)c1ccccc12	None
	CHEMBL21731	81996	43	None	-27	23	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	277	4	1	1	4.2	CNCCCC12CCC(c3ccccc31)c1ccccc12	None
	26987	936	29	None	-177	21	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	None
	6063	936	29	None	-177	21	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	None
	671	936	29	None	-177	21	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	None
	CHEMBL1626	936	29	None	-177	21	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	None
	DB00283	936	29	None	-177	21	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	343	6	0	2	5.1	Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C	None
	1613	2316	44	None	-8	44	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
	205	2316	44	None	-8	44	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
	3964	2316	44	None	-8	44	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
	CHEMBL831	2316	44	None	-8	44	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
	DB00408	2316	44	None	-8	44	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	None
	277	1274	55	None	-43	45	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	None
	2913	1274	55	None	-43	45	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	None
	765	1274	55	None	-43	45	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	None
	CHEMBL516	1274	55	None	-43	45	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	None
	DB00434	1274	55	None	-43	45	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	287	0	0	1	4.7	CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1	None
	4806	3945	85	None	-5	13	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	Drug Central	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	None
	7351	3945	85	None	-5	13	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	Drug Central	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	None
	9966051	3945	85	None	-5	13	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	Drug Central	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	None
	CHEMBL2104993	3945	85	None	-5	13	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	Drug Central	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	None
	DB09068	3945	85	None	-5	13	Human	8.2	pKi	=	8.2	Binding	Binding affinity to human histamine H2 receptorBinding affinity to human histamine H2 receptor	Drug Central	298	3	1	3	3.9	Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1	None
	2726	906	64	None	-85	72	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
	621	906	64	None	-85	72	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
	83	906	64	None	-85	72	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
	CHEMBL71	906	64	None	-85	72	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
	DB00477	906	64	None	-85	72	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	None
	135398737	944	89	None	-64	91	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
	38	944	89	None	-64	91	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
	722	944	89	None	-64	91	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
	CHEMBL42	944	89	None	-64	91	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
	DB00363	944	89	None	-64	91	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	None
	100	3745	52	None	-46	55	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
	2637	3745	52	None	-46	55	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
	5452	3745	52	None	-46	55	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
	CHEMBL479	3745	52	None	-46	55	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
	DB00679	3745	52	None	-46	55	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	370	4	0	4	5.9	CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1	None
	2389	3279	114	None	-275	67	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
	5073	3279	114	None	-275	67	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
	96	3279	114	None	-275	67	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
	CHEMBL85	3279	114	None	-275	67	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
	DB00734	3279	114	None	-275	67	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	None
	115237	55296	113	None	-22	54	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	426	4	1	7	3.1	Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O	None
	CHEMBL1621	55296	113	None	-22	54	Human	8.2	pKi	=	8.2	Binding	NoneNone	Drug Central	426	4	1	7	3.1	Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O	None
	1231	924	112	125I-iodoaminopotentidine	-2	7	Human	6.2	pKi	=	6.2	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	2756	924	112	125I-iodoaminopotentidine	-2	7	Human	6.2	pKi	=	6.2	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	645	924	112	125I-iodoaminopotentidine	-2	7	Human	6.2	pKi	=	6.2	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	CHEMBL30	924	112	125I-iodoaminopotentidine	-2	7	Human	6.2	pKi	=	6.2	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	DB00501	924	112	125I-iodoaminopotentidine	-2	7	Human	6.2	pKi	=	6.2	Binding	NoneNone	PDSP KiDatabase	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	None
	657255	197406	29	None	-3	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	337	12	2	3	5.6	CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1	None
	CHEMBL588119	197406	29	None	-3	15	Human	8.2	pKi	=	8.2	Binding	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	Drug Central	337	12	2	3	5.6	CCCCCCCCN[C@H](C)[C@@H](O)c1ccc(SC(C)C)cc1	None
	135398745	2869	108	None	-9	65	Human	8.1	pKi	=	8.1	Binding	NoneNone	Drug Central	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	None
	47	2869	108	None	-9	65	Human	8.1	pKi	=	8.1	Binding	NoneNone	Drug Central	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	None
	CHEMBL715	2869	108	None	-9	65	Human	8.1	pKi	=	8.1	Binding	NoneNone	Drug Central	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	None
	DB00334	2869	108	None	-9	65	Human	8.1	pKi	=	8.1	Binding	NoneNone	Drug Central	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	None
	1234	3239	0	125I-iodoaminopotentidine	-2	6	Human	7.1	pKi	=	7.1	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
	3001055	3239	0	125I-iodoaminopotentidine	-2	6	Human	7.1	pKi	=	7.1	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
	CHEMBL512	3239	0	125I-iodoaminopotentidine	-2	6	Human	7.1	pKi	=	7.1	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
	DB00863	3239	0	125I-iodoaminopotentidine	-2	6	Human	7.1	pKi	=	7.1	Binding	NoneNone	PDSP KiDatabase	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	None
	5048	3084	57	None	-114	7	Human	5.0	pKi	=	5.0	Binding	UnclassifiedUnclassified	Guide to Pharmacology	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	26084539
	8924	3084	57	None	-114	7	Human	5.0	pKi	=	5.0	Binding	UnclassifiedUnclassified	Guide to Pharmacology	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	26084539
	9948102	3084	57	None	-114	7	Human	5.0	pKi	=	5.0	Binding	UnclassifiedUnclassified	Guide to Pharmacology	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	26084539
	CHEMBL462605	3084	57	None	-114	7	Human	5.0	pKi	=	5.0	Binding	UnclassifiedUnclassified	Guide to Pharmacology	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	26084539
	DB11642	3084	57	None	-114	7	Human	5.0	pKi	=	5.0	Binding	UnclassifiedUnclassified	Guide to Pharmacology	295	8	0	2	4.2	Clc1ccc(cc1)CCCOCCCN1CCCCC1	26084539
	1231	924	112	None	1	7	Rat	5.9	pKi	=	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	9384502
	2756	924	112	None	1	7	Rat	5.9	pKi	=	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	9384502
	645	924	112	None	1	7	Rat	5.9	pKi	=	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	9384502
	CHEMBL30	924	112	None	1	7	Rat	5.9	pKi	=	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	9384502
	DB00501	924	112	None	1	7	Rat	5.9	pKi	=	5.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	9384502
	1234	3239	0	None	2	6	Rat	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	9384502
	3001055	3239	0	None	2	6	Rat	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	9384502
	CHEMBL512	3239	0	None	2	6	Rat	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	9384502
	DB00863	3239	0	None	2	6	Rat	6.2	pKi	=	6.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	9384502
	1231	924	112	None	-2	7	Human	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	23466604
	2756	924	112	None	-2	7	Human	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	23466604
	645	924	112	None	-2	7	Human	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	23466604
	CHEMBL30	924	112	None	-2	7	Human	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	23466604
	DB00501	924	112	None	-2	7	Human	6.9	pKi	=	6.9	Binding	UnclassifiedUnclassified	Guide to Pharmacology	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	23466604
	1234	3239	0	None	-2	6	Human	7.1	pKi	=	7.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	7921611
	3001055	3239	0	None	-2	6	Human	7.1	pKi	=	7.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	7921611
	CHEMBL512	3239	0	None	-2	6	Human	7.1	pKi	=	7.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	7921611
	DB00863	3239	0	None	-2	6	Human	7.1	pKi	=	7.1	Binding	UnclassifiedUnclassified	Guide to Pharmacology	314	10	2	7	1.5	CN/C(=C\[N+](=O)[O-])/NCCSCc1ccc(o1)CN(C)C	7921611
	1235	3763	32	None	2	4	Rat	7.5	pKi	=	7.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	9384502
	3959	3763	32	None	2	4	Rat	7.5	pKi	=	7.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	9384502
	50287	3763	32	None	2	4	Rat	7.5	pKi	=	7.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	9384502
	CHEMBL269646	3763	32	None	2	4	Rat	7.5	pKi	=	7.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	312	6	4	6	-0.1	N#CNC(=NC)NCCSCc1csc(n1)N=C(N)N	9384502
	1265	929	54	None	-17782	8	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	270	7	1	3	3.0	O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1	26084539
	6422124	929	54	None	-17782	8	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	270	7	1	3	3.0	O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1	26084539
	CHEMBL14638	929	54	None	-17782	8	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	270	7	1	3	3.0	O=C(c1ccc(cc1)OCCCc1[nH]cnc1)C1CC1	26084539
	441082	1140	40	None	-2137	8	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	356	1	0	2	4.8	CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C	26084539
	8981	1140	40	None	-2137	8	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	356	1	0	2	4.8	CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C	26084539
	CHEMBL191703	1140	40	None	-2137	8	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	356	1	0	2	4.8	CN([C@H]1CC[C@]2(C(=CC[C@@H]3[C@@H]2CC[C@]24[C@H]3CC[C@@H]4[C@@H](N(C2)C)C)C1)C)C	26084539
	11697697	2510	19	None	-6309	6	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	431	6	0	5	4.6	Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F	26084539
	7346	2510	19	None	-6309	6	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	431	6	0	5	4.6	Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F	26084539
	CHEMBL476323	2510	19	None	-6309	6	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	431	6	0	5	4.6	Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F	26084539
	DB11910	2510	19	None	-6309	6	Human	5.0	pKi	>	5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	431	6	0	5	4.6	Cc1nc2cccc(c2c(=O)n1c1ccc(cc1)OCCCN1CCCC1)C(F)(F)F	26084539
	117072554	1992	0	None	-1000	4	Human	5.3	pKi	>	5.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology	450	5	2	6	2.3	CN1CCN(CC1)C1=CC(=NC(N1)N)c1ccc2c(c1)CN(CC2)C(=O)CCC1CCCC1	26084539
	8982	1992	0	None	-1000	4	Human	5.3	pKi	>	5.3	Binding	UnclassifiedUnclassified	Guide to Pharmacology	450	5	2	6	2.3	CN1CCN(CC1)C1=CC(=NC(N1)N)c1ccc2c(c1)CN(CC2)C(=O)CCC1CCCC1	26084539
	24994634	2111	26	None	-194	7	Human	6.0	pKi	>	6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	221	2	2	5	0.7	N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C	26084539
	8984	2111	26	None	-194	7	Human	6.0	pKi	>	6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	221	2	2	5	0.7	N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C	26084539
	CHEMBL3236549	2111	26	None	-194	7	Human	6.0	pKi	>	6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	221	2	2	5	0.7	N[C@@H]1CCN(C1)c1cc(nc(n1)N)C(C)C	26084539
	45257132	3626	3	None	-83	4	Human	6.0	pKi	>	6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	366	4	2	6	2.7	CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N	26084539
	8983	3626	3	None	-83	4	Human	6.0	pKi	>	6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	366	4	2	6	2.7	CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N	26084539
	CHEMBL595180	3626	3	None	-83	4	Human	6.0	pKi	>	6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	366	4	2	6	2.7	CN1CCN(CC1)c1cc(NCc2c(Cl)cccc2Cl)nc(n1)N	26084539
	119570	3110	90	None	-281	40	Human	8.3	pKi	None	8.3	Binding	NoneNone	Drug Central	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
	2233	3110	90	None	-281	40	Human	8.3	pKi	None	8.3	Binding	NoneNone	Drug Central	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
	953	3110	90	None	-281	40	Human	8.3	pKi	None	8.3	Binding	NoneNone	Drug Central	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
	CHEMBL301265	3110	90	None	-281	40	Human	8.3	pKi	None	8.3	Binding	NoneNone	Drug Central	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
	DB00413	3110	90	None	-281	40	Human	8.3	pKi	None	8.3	Binding	NoneNone	Drug Central	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	None
	1204	1901	114	None	-316	23	Rat	3.8	pKi	None	3.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	111	2	2	2	-0.1	NCCc1cnc[nH]1	9384502
	1247	1901	114	None	-316	23	Rat	3.8	pKi	None	3.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	111	2	2	2	-0.1	NCCc1cnc[nH]1	9384502
	1375	1901	114	None	-316	23	Rat	3.8	pKi	None	3.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	111	2	2	2	-0.1	NCCc1cnc[nH]1	9384502
	774	1901	114	None	-316	23	Rat	3.8	pKi	None	3.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	111	2	2	2	-0.1	NCCc1cnc[nH]1	9384502
	CHEMBL90	1901	114	None	-316	23	Rat	3.8	pKi	None	3.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	111	2	2	2	-0.1	NCCc1cnc[nH]1	9384502
	DB05381	1901	114	None	-316	23	Rat	3.8	pKi	None	3.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	111	2	2	2	-0.1	NCCc1cnc[nH]1	9384502
	1218	227	47	None	-3548	4	Human	5.2	pKi	None	5.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	330	4	0	3	5.0	N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C	15608078
	9818903	227	47	None	-3548	4	Human	5.2	pKi	None	5.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	330	4	0	3	5.0	N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C	15608078
	CHEMBL351231	227	47	None	-3548	4	Human	5.2	pKi	None	5.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	330	4	0	3	5.0	N#Cc1ccc(cc1)c1ccc2c(c1)cc(o2)CCN1CCC[C@H]1C	15608078
	1223	940	32	None	-32359	11	Human	5.2	pKi	None	5.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	308	6	2	3	3.2	Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N	12606603
	2790	940	32	None	-32359	11	Human	5.2	pKi	None	5.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	308	6	2	3	3.2	Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N	12606603
	CHEMBL14690	940	32	None	-32359	11	Human	5.2	pKi	None	5.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	308	6	2	3	3.2	Clc1ccc(cc1)CN=C(SCCCc1cnc[nH]1)N	12606603
	1229	732	0	None	-63	6	Rat	5.5	pKi	None	5.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	262	5	3	2	2.0	CNC(=S)NCCCCc1cccc2c1cn[nH]2	8692899
	5311293	732	0	None	-63	6	Rat	5.5	pKi	None	5.5	Binding	UnclassifiedUnclassified	Guide to Pharmacology	262	5	3	2	2.0	CNC(=S)NCCCCc1cccc2c1cn[nH]2	8692899
	1233	2479	0	None	6	3	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	244	5	3	3	1.0	CNC(=S)NCCSCc1nc[nH]c1C	9384502
	1548992	2479	0	None	6	3	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	244	5	3	3	1.0	CNC(=S)NCCSCc1nc[nH]c1C	9384502
	CHEMBL275446	2479	0	None	6	3	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	244	5	3	3	1.0	CNC(=S)NCCSCc1nc[nH]c1C	9384502
	DB08805	2479	0	None	6	3	Rat	5.8	pKi	None	5.8	Binding	UnclassifiedUnclassified	Guide to Pharmacology	244	5	3	3	1.0	CNC(=S)NCCSCc1nc[nH]c1C	9384502
	1200	3900	1	None	4	3	Human	6.0	pKi	None	6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	335	8	4	5	0.7	O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C	16394198
	25149519	3900	1	None	4	3	Human	6.0	pKi	None	6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	335	8	4	5	0.7	O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C	16394198
	CHEMBL513056	3900	1	None	4	3	Human	6.0	pKi	None	6	Binding	UnclassifiedUnclassified	Guide to Pharmacology	335	8	4	5	0.7	O=C(NC(=NCCCc1cnc[nH]1)N)CSCc1nc[nH]c1C	16394198
	1199	2928	0	None	37	3	Human	7.0	pKi	None	7	Binding	UnclassifiedUnclassified	Guide to Pharmacology	394	8	3	4	2.5	NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F	16394198
	25149244	2928	0	None	37	3	Human	7.0	pKi	None	7	Binding	UnclassifiedUnclassified	Guide to Pharmacology	394	8	3	4	2.5	NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F	16394198
	CHEMBL472273	2928	0	None	37	3	Human	7.0	pKi	None	7	Binding	UnclassifiedUnclassified	Guide to Pharmacology	394	8	3	4	2.5	NC(=NCCCc1[nH]cnc1)NC(=O)CC(c1ccccn1)c1ccc(cc1)F	16394198
	1221	472	9	None	-2	3	Human	7.2	pKi	None	7.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	380	9	3	3	3.0	NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F	16394198
	65895	472	9	None	-2	3	Human	7.2	pKi	None	7.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	380	9	3	3	3.0	NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F	16394198
	CHEMBL293802	472	9	None	-2	3	Human	7.2	pKi	None	7.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	380	9	3	3	3.0	NC(=NCCCc1[nH]cnc1)NCCC(c1ccccn1)c1ccc(cc1)F	16394198
	1226	1988	16	None	-7	6	Human	7.2	pKi	None	7.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	16394198
	41376	1988	16	None	-7	6	Human	7.2	pKi	None	7.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	16394198
	CHEMBL12608	1988	16	None	-7	6	Human	7.2	pKi	None	7.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	321	9	4	4	1.2	NC(=NCCCc1cnc[nH]1)NCCSCc1nc[nH]c1C	16394198
	1232	2025	6	None	-	1	Rat	9.2	pKi	None	9.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	603	11	4	6	3.1	N#CNC(=NCCCOc1cccc(c1)CN1CCCCC1)NCCNC(=O)c1ccc(c(c1)I)N	9384502
	181461	2025	6	None	-	1	Rat	9.2	pKi	None	9.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	603	11	4	6	3.1	N#CNC(=NCCCOc1cccc(c1)CN1CCCCC1)NCCNC(=O)c1ccc(c(c1)I)N	9384502
	CHEMBL72193	2025	6	None	-	1	Rat	9.2	pKi	None	9.2	Binding	UnclassifiedUnclassified	Guide to Pharmacology	603	11	4	6	3.1	N#CNC(=NCCCOc1cccc(c1)CN1CCCCC1)NCCNC(=O)c1ccc(c(c1)I)N	9384502

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Ligand source activities (1 row/activity)