GPCRdb

Ligand source activities (1 row/activity)

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Ligands (move mouse cursor over ligand name to see structure)					Receptor	Activity									Chemical information
Sel. page	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	4418	34231	None	58	Human	Functional	pAC50	=	5.9	5.9	-23	18	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	392	7	1	5	3.4	COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1	10.1038/s41467-023-40064-9
	4418.0	34231	None	58	Human	Functional	pAC50	=	5.9	5.9	-23	18	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	392	7	1	5	3.4	COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1	10.1038/s41467-023-40064-9
	CHEMBL142635	34231	None	58	Human	Functional	pAC50	=	5.9	5.9	-23	18	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	392	7	1	5	3.4	COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1	10.1038/s41467-023-40064-9
	DB12092	34231	None	58	Human	Functional	pAC50	=	5.9	5.9	-23	18	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	392	7	1	5	3.4	COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1	10.1038/s41467-023-40064-9
	2601	3780	None	25	Human	Functional	pAC50	=	4.8	4.8	-4897	17	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	340	3	2	2	2.9	CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC	10.1038/s41467-023-40064-9
	443951	3780	None	25	Human	Functional	pAC50	=	4.8	4.8	-4897	17	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	340	3	2	2	2.9	CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC	10.1038/s41467-023-40064-9
	56	3780	None	25	Human	Functional	pAC50	=	4.8	4.8	-4897	17	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	340	3	2	2	2.9	CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC	10.1038/s41467-023-40064-9
	CHEMBL73151	3780	None	25	Human	Functional	pAC50	=	4.8	4.8	-4897	17	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	340	3	2	2	2.9	CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC	10.1038/s41467-023-40064-9
	DB13399	3780	None	25	Human	Functional	pAC50	=	4.8	4.8	-4897	17	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	340	3	2	2	2.9	CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC	10.1038/s41467-023-40064-9
	12574	2605	None	60	Human	Functional	pAC50	=	4.8	4.8	-257	8	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	241	2	2	6	0.8	CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC	10.1038/s41467-023-40064-9
	4810	2605	None	60	Human	Functional	pAC50	=	4.8	4.8	-257	8	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	241	2	2	6	0.8	CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC	10.1038/s41467-023-40064-9
	4810.0	2605	None	60	Human	Functional	pAC50	=	4.8	4.8	-257	8	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	241	2	2	6	0.8	CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC	10.1038/s41467-023-40064-9
	CHEMBL19236	2605	None	60	Human	Functional	pAC50	=	4.8	4.8	-257	8	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	241	2	2	6	0.8	CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC	10.1038/s41467-023-40064-9
	DB09242	2605	None	60	Human	Functional	pAC50	=	4.8	4.8	-257	8	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	241	2	2	6	0.8	CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC	10.1038/s41467-023-40064-9
	31101	729	None	28	Human	Functional	pAC50	=	5.7	5.7	-676	29	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	653	5	3	6	3.2	CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C	10.1038/s41467-023-40064-9
	31101.0	729	None	28	Human	Functional	pAC50	=	5.7	5.7	-676	29	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	653	5	3	6	3.2	CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C	10.1038/s41467-023-40064-9
	35	729	None	28	Human	Functional	pAC50	=	5.7	5.7	-676	29	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	653	5	3	6	3.2	CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C	10.1038/s41467-023-40064-9
	403	729	None	28	Human	Functional	pAC50	=	5.7	5.7	-676	29	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	653	5	3	6	3.2	CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C	10.1038/s41467-023-40064-9
	CHEMBL493	729	None	28	Human	Functional	pAC50	=	5.7	5.7	-676	29	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	653	5	3	6	3.2	CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C	10.1038/s41467-023-40064-9
	DB01200	729	None	28	Human	Functional	pAC50	=	5.7	5.7	-676	29	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	653	5	3	6	3.2	CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C	10.1038/s41467-023-40064-9
	135564886	14499	None	5	Human	Functional	pAC50	=	4.6	4.6	-7	25	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	752	14	1	6	8.7	CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21	10.1038/s41467-023-40064-9
	135673376	14499	None	5	Human	Functional	pAC50	=	4.6	4.6	-7	25	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	752	14	1	6	8.7	CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21	10.1038/s41467-023-40064-9
	137157436	14499	None	5	Human	Functional	pAC50	=	4.6	4.6	-7	25	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	752	14	1	6	8.7	CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21	10.1038/s41467-023-40064-9
	145948239	14499	None	5	Human	Functional	pAC50	=	4.6	4.6	-7	25	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	752	14	1	6	8.7	CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21	10.1038/s41467-023-40064-9
	71587099	14499	None	5	Human	Functional	pAC50	=	4.6	4.6	-7	25	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	752	14	1	6	8.7	CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21	10.1038/s41467-023-40064-9
	CHEMBL1201304	14499	None	5	Human	Functional	pAC50	=	4.6	4.6	-7	25	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	752	14	1	6	8.7	CC1(C)C(/C=C/C=C/C=C/C=C2\N(CCCCS(=O)(=O)O)c3ccc4ccccc4c3C2(C)C)=[N+](CCCCS(=O)(=O)[O-])c2ccc3ccccc3c21	10.1038/s41467-023-40064-9
	134	2514	None	19	Human	Functional	pAC50	=	5.6	5.6	-1380	18	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	10.1038/s41467-023-40064-9
	1775	2514	None	19	Human	Functional	pAC50	=	5.6	5.6	-1380	18	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	10.1038/s41467-023-40064-9
	9681	2514	None	19	Human	Functional	pAC50	=	5.6	5.6	-1380	18	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	10.1038/s41467-023-40064-9
	9681.0	2514	None	19	Human	Functional	pAC50	=	5.6	5.6	-1380	18	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	10.1038/s41467-023-40064-9
	CHEMBL1065	2514	None	19	Human	Functional	pAC50	=	5.6	5.6	-1380	18	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	10.1038/s41467-023-40064-9
	DB00247	2514	None	19	Human	Functional	pAC50	=	5.6	5.6	-1380	18	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	10.1038/s41467-023-40064-9
	168871	89164	None	10	Human	Functional	pAC50	=	5.5	5.5	-234	13	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	563	4	3	6	2.1	CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12	10.1038/s41467-023-40064-9
	CHEMBL2365712	89164	None	10	Human	Functional	pAC50	=	5.5	5.5	-234	13	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	563	4	3	6	2.1	CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12	10.1038/s41467-023-40064-9
	2803	955	None	40	Human	Functional	pAC50	=	6.4	6.4	-93	14	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	229	1	2	3	2.4	Clc1cccc(c1NC1=NCCN1)Cl	10.1038/s41467-023-40064-9
	2803.0	955	None	40	Human	Functional	pAC50	=	6.4	6.4	-93	14	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	229	1	2	3	2.4	Clc1cccc(c1NC1=NCCN1)Cl	10.1038/s41467-023-40064-9
	516	955	None	40	Human	Functional	pAC50	=	6.4	6.4	-93	14	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	229	1	2	3	2.4	Clc1cccc(c1NC1=NCCN1)Cl	10.1038/s41467-023-40064-9
	704	955	None	40	Human	Functional	pAC50	=	6.4	6.4	-93	14	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	229	1	2	3	2.4	Clc1cccc(c1NC1=NCCN1)Cl	10.1038/s41467-023-40064-9
	CHEMBL134	955	None	40	Human	Functional	pAC50	=	6.4	6.4	-93	14	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	229	1	2	3	2.4	Clc1cccc(c1NC1=NCCN1)Cl	10.1038/s41467-023-40064-9
	DB00575	955	None	40	Human	Functional	pAC50	=	6.4	6.4	-93	14	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	229	1	2	3	2.4	Clc1cccc(c1NC1=NCCN1)Cl	10.1038/s41467-023-40064-9
	37	778	None	41	Human	Functional	pAC50	=	5.4	5.4	-891	12	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	451	8	2	4	3.2	C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C	10.1038/s41467-023-40064-9
	460	778	None	41	Human	Functional	pAC50	=	5.4	5.4	-891	12	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	451	8	2	4	3.2	C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C	10.1038/s41467-023-40064-9
	54746	778	None	41	Human	Functional	pAC50	=	5.4	5.4	-891	12	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	451	8	2	4	3.2	C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C	10.1038/s41467-023-40064-9
	54746.0	778	None	41	Human	Functional	pAC50	=	5.4	5.4	-891	12	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	451	8	2	4	3.2	C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C	10.1038/s41467-023-40064-9
	CHEMBL1201087	778	None	41	Human	Functional	pAC50	=	5.4	5.4	-891	12	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	451	8	2	4	3.2	C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C	10.1038/s41467-023-40064-9
	DB00248	778	None	41	Human	Functional	pAC50	=	5.4	5.4	-891	12	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	451	8	2	4	3.2	C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C	10.1038/s41467-023-40064-9
	150	2509	None	14	Human	Functional	pAC50	=	7.2	7.2	-22	17	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	339	4	3	3	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO	10.1038/s41467-023-40064-9
	1764	2509	None	14	Human	Functional	pAC50	=	7.2	7.2	-22	17	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	339	4	3	3	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO	10.1038/s41467-023-40064-9
	8226	2509	None	14	Human	Functional	pAC50	=	7.2	7.2	-22	17	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	339	4	3	3	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO	10.1038/s41467-023-40064-9
	8226.0	2509	None	14	Human	Functional	pAC50	=	7.2	7.2	-22	17	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	339	4	3	3	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO	10.1038/s41467-023-40064-9
	CHEMBL1201356	2509	None	14	Human	Functional	pAC50	=	7.2	7.2	-22	17	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	339	4	3	3	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO	10.1038/s41467-023-40064-9
	DB00353	2509	None	14	Human	Functional	pAC50	=	7.2	7.2	-22	17	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	339	4	3	3	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO	10.1038/s41467-023-40064-9
	10531	1420	None	13	Human	Functional	pAC50	=	6.2	6.2	-467	29	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	583	4	3	6	2.1	CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O	10.1038/s41467-023-40064-9
	10531.0	1420	None	13	Human	Functional	pAC50	=	6.2	6.2	-467	29	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	583	4	3	6	2.1	CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O	10.1038/s41467-023-40064-9
	121	1420	None	13	Human	Functional	pAC50	=	6.2	6.2	-467	29	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	583	4	3	6	2.1	CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O	10.1038/s41467-023-40064-9
	888	1420	None	13	Human	Functional	pAC50	=	6.2	6.2	-467	29	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	583	4	3	6	2.1	CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O	10.1038/s41467-023-40064-9
	CHEMBL1732	1420	None	13	Human	Functional	pAC50	=	6.2	6.2	-467	29	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	583	4	3	6	2.1	CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O	10.1038/s41467-023-40064-9
	DB00320	1420	None	13	Human	Functional	pAC50	=	6.2	6.2	-467	29	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	583	4	3	6	2.1	CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O	10.1038/s41467-023-40064-9
	119570	3159	None	58	Human	Functional	pAC50	=	6.1	6.1	-602	11	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1038/s41467-023-40064-9
	119570.0	3159	None	58	Human	Functional	pAC50	=	6.1	6.1	-602	11	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1038/s41467-023-40064-9
	2233	3159	None	58	Human	Functional	pAC50	=	6.1	6.1	-602	11	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1038/s41467-023-40064-9
	953	3159	None	58	Human	Functional	pAC50	=	6.1	6.1	-602	11	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1038/s41467-023-40064-9
	CHEMBL301265	3159	None	58	Human	Functional	pAC50	=	6.1	6.1	-602	11	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1038/s41467-023-40064-9
	DB00413	3159	None	58	Human	Functional	pAC50	=	6.1	6.1	-602	11	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1038/s41467-023-40064-9
	7741	14503	None	47	Human	Functional	pAC50	=	6.0	6.0	-	1	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	111	2	2	2	-0.1	NCCc1cc[nH]n1	10.1038/s41467-023-40064-9
	CHEMBL1201323	14503	None	47	Human	Functional	pAC50	=	6.0	6.0	-	1	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	111	2	2	2	-0.1	NCCc1cc[nH]n1	10.1038/s41467-023-40064-9
	2683	3834	None	40	Human	Functional	pAC50	=	6.0	6.0	-22	6	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	253	1	2	6	1.7	Clc1ccc2c(c1NC1=NCCN1)nsn2	10.1038/s41467-023-40064-9
	5487	3834	None	40	Human	Functional	pAC50	=	6.0	6.0	-22	6	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	253	1	2	6	1.7	Clc1ccc2c(c1NC1=NCCN1)nsn2	10.1038/s41467-023-40064-9
	5487.0	3834	None	40	Human	Functional	pAC50	=	6.0	6.0	-22	6	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	253	1	2	6	1.7	Clc1ccc2c(c1NC1=NCCN1)nsn2	10.1038/s41467-023-40064-9
	7308	3834	None	40	Human	Functional	pAC50	=	6.0	6.0	-22	6	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	253	1	2	6	1.7	Clc1ccc2c(c1NC1=NCCN1)nsn2	10.1038/s41467-023-40064-9
	CHEMBL1079	3834	None	40	Human	Functional	pAC50	=	6.0	6.0	-22	6	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	253	1	2	6	1.7	Clc1ccc2c(c1NC1=NCCN1)nsn2	10.1038/s41467-023-40064-9
	DB00697	3834	None	40	Human	Functional	pAC50	=	6.0	6.0	-22	6	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	253	1	2	6	1.7	Clc1ccc2c(c1NC1=NCCN1)nsn2	10.1038/s41467-023-40064-9
	2105	3054	None	28	Human	Functional	pAC50	=	6.0	6.0	-398	25	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	314	4	1	2	4.3	CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3	10.1038/s41467-023-40064-9
	47811	3054	None	28	Human	Functional	pAC50	=	6.0	6.0	-398	25	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	314	4	1	2	4.3	CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3	10.1038/s41467-023-40064-9
	48	3054	None	28	Human	Functional	pAC50	=	6.0	6.0	-398	25	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	314	4	1	2	4.3	CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3	10.1038/s41467-023-40064-9
	CHEMBL531	3054	None	28	Human	Functional	pAC50	=	6.0	6.0	-398	25	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	314	4	1	2	4.3	CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3	10.1038/s41467-023-40064-9
	DB01186	3054	None	28	Human	Functional	pAC50	=	6.0	6.0	-398	25	Agonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human HRH2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method	ChEMBL	314	4	1	2	4.3	CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3	10.1038/s41467-023-40064-9
	168294449	193127	None	0	Human	Functional	pEC50	=	8.0	8.0	50	2	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	193127	None	0	Human	Functional	pEC50	=	8.0	8.0	50	2	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	193127	None	0	Human	Functional	pEC50	=	8.0	8.0	50	2	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	218043	None	0	Human	Functional	pEC50	=	7	7.0	-	1	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	218043	None	0	Human	Functional	pEC50	=	7	7.0	-	1	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	185194	None	0	Human	Functional	pEC50	=	7	7.0	-1	3	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	185194	None	0	Human	Functional	pEC50	=	7	7.0	-1	3	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	174967	None	0	Human	Functional	pEC50	=	7	7.0	13	2	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	174967	None	0	Human	Functional	pEC50	=	7	7.0	13	2	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	193082	None	0	Human	Functional	pEC50	=	6.0	6.0	10	2	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	193082	None	0	Human	Functional	pEC50	=	6.0	6.0	10	2	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	193082	None	0	Human	Functional	pEC50	=	6.0	6.0	10	2	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	218024	None	0	Human	Functional	pEC50	=	6.0	6.0	-	1	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	218024	None	0	Human	Functional	pEC50	=	6.0	6.0	-	1	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	1932	None	74	Human	Functional	pEC50	=	6.9	6.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.9	6.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.9	6.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.9	6.9	-181	11	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
	774.0	1932	None	74	Human	Functional	pEC50	=	6.9	6.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.9	6.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.9	6.9	-181	11	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	218019	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	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	218019	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	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	1932	None	74	Human	Functional	pEC50	=	6.9	6.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.9	6.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.9	6.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.9	6.9	-181	11	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
	774.0	1932	None	74	Human	Functional	pEC50	=	6.9	6.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.9	6.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.9	6.9	-181	11	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	192894	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	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	192894	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	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	192894	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	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	8762	None	1	Human	Functional	pEC50	=	6.9	6.9	-5	4	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	8762	None	1	Human	Functional	pEC50	=	6.9	6.9	-5	4	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	217845	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	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	218019	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	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	218019	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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
	774.0	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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
	774.0	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	5628	None	0	Human	Functional	pEC50	=	4.9	4.9	-	1	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	5628	None	0	Human	Functional	pEC50	=	4.9	4.9	-	1	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	5796	None	0	Human	Functional	pEC50	=	4.9	4.9	-	1	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	5796	None	0	Human	Functional	pEC50	=	4.9	4.9	-	1	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	217773	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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
	774.0	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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
	774.0	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	218024	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	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	218024	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	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	192894	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	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	192894	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	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	192894	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	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	218031	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	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	218031	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	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	175183	None	0	Human	Functional	pEC50	=	5.9	5.9	2	2	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	175183	None	0	Human	Functional	pEC50	=	5.9	5.9	2	2	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	193127	None	0	Human	Functional	pEC50	=	7.9	7.9	50	2	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	193127	None	0	Human	Functional	pEC50	=	7.9	7.9	50	2	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	193127	None	0	Human	Functional	pEC50	=	7.9	7.9	50	2	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	82114	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	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	82114	None	0	Human	Functional	pEC50	=	7.9	7.9	-	1	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	217836	None	0	Human	Functional	pEC50	=	6.9	6.9	-	1	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	185009	None	0	Human	Functional	pEC50	=	6.9	6.9	3	3	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	185009	None	0	Human	Functional	pEC50	=	6.9	6.9	3	3	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	193127	None	0	Human	Functional	pEC50	=	6.9	6.9	50	2	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	193127	None	0	Human	Functional	pEC50	=	6.9	6.9	50	2	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	193127	None	0	Human	Functional	pEC50	=	6.9	6.9	50	2	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	193140	None	0	Human	Functional	pEC50	=	6.9	6.9	31	9	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	193140	None	0	Human	Functional	pEC50	=	6.9	6.9	31	9	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	193140	None	0	Human	Functional	pEC50	=	6.9	6.9	31	9	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	217461	None	0	Human	Functional	pEC50	=	5.9	5.9	-	1	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	175183	None	0	Human	Functional	pEC50	=	5.9	5.9	2	2	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	175183	None	0	Human	Functional	pEC50	=	5.9	5.9	2	2	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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
	774.0	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.9	5.9	-181	11	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	5715	None	0	Human	Functional	pEC50	=	4.9	4.9	-18	2	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	5715	None	0	Human	Functional	pEC50	=	4.9	4.9	-18	2	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	218052	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	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	218052	None	0	Human	Functional	pEC50	=	5.8	5.8	-	1	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	186573	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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	186573	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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	186579	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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	186579	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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	82097	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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	82097	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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	185238	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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	185238	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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	1932	None	74	Human	Functional	pEC50	=	5.8	5.8	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.8	5.8	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.8	5.8	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.8	5.8	-181	11	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
	774.0	1932	None	74	Human	Functional	pEC50	=	5.8	5.8	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.8	5.8	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.8	5.8	-181	11	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	82101	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	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	82101	None	0	Human	Functional	pEC50	=	7.8	7.8	-	1	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	80170	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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	80170	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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	109531	None	0	Human	Functional	pEC50	=	4.8	4.8	-	1	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	109531	None	0	Human	Functional	pEC50	=	4.8	4.8	-	1	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	185722	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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	185722	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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	3159	None	58	Human	Functional	pEC50	=	6.8	6.8	-602	11	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
	119570.0	3159	None	58	Human	Functional	pEC50	=	6.8	6.8	-602	11	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	3159	None	58	Human	Functional	pEC50	=	6.8	6.8	-602	11	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	3159	None	58	Human	Functional	pEC50	=	6.8	6.8	-602	11	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	3159	None	58	Human	Functional	pEC50	=	6.8	6.8	-602	11	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	3159	None	58	Human	Functional	pEC50	=	6.8	6.8	-602	11	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	186427	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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	186427	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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	185304	None	0	Human	Functional	pEC50	=	7.8	7.8	4	3	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	185304	None	0	Human	Functional	pEC50	=	7.8	7.8	4	3	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	185483	None	0	Human	Functional	pEC50	=	6.8	6.8	-11	11	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	185483	None	0	Human	Functional	pEC50	=	6.8	6.8	-11	11	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	186427	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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	186427	None	0	Human	Functional	pEC50	=	6.8	6.8	-	1	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	8764	None	0	Human	Functional	pEC50	=	7.7	7.7	-6	4	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	8764	None	0	Human	Functional	pEC50	=	7.7	7.7	-6	4	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	217996	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	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	192914	None	0	Human	Functional	pEC50	=	7.7	7.7	4	3	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	192914	None	0	Human	Functional	pEC50	=	7.7	7.7	4	3	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	192914	None	0	Human	Functional	pEC50	=	7.7	7.7	4	3	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	193149	None	0	Human	Functional	pEC50	=	7.7	7.7	14	2	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	193149	None	0	Human	Functional	pEC50	=	7.7	7.7	14	2	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	193149	None	0	Human	Functional	pEC50	=	7.7	7.7	14	2	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	217996	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	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	404	None	24	Human	Functional	pEC50	=	6.7	6.7	57	2	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	404	None	24	Human	Functional	pEC50	=	6.7	6.7	57	2	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	404	None	24	Human	Functional	pEC50	=	6.7	6.7	57	2	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	217836	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	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	5738	None	0	Human	Functional	pEC50	=	5.7	5.7	-	1	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	5738	None	0	Human	Functional	pEC50	=	5.7	5.7	-	1	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	8547	None	0	Human	Functional	pEC50	=	7.7	7.7	-	1	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	8547	None	0	Human	Functional	pEC50	=	7.7	7.7	-	1	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	82115	None	0	Human	Functional	pEC50	=	7.7	7.7	-	1	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	82115	None	0	Human	Functional	pEC50	=	7.7	7.7	-	1	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	218015	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	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	218015	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	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	218017	None	0	Human	Functional	pEC50	=	5.7	5.7	-	1	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	218017	None	0	Human	Functional	pEC50	=	5.7	5.7	-	1	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	82105	None	0	Human	Functional	pEC50	=	7.7	7.7	-	1	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	82105	None	0	Human	Functional	pEC50	=	7.7	7.7	-	1	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	184560	None	0	Human	Functional	pEC50	=	7.7	7.7	3	3	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	184560	None	0	Human	Functional	pEC50	=	7.7	7.7	3	3	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	175137	None	0	Human	Functional	pEC50	=	5.7	5.7	2	2	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	175137	None	0	Human	Functional	pEC50	=	5.7	5.7	2	2	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	82109	None	0	Human	Functional	pEC50	=	6.7	6.7	-2	2	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	82109	None	0	Human	Functional	pEC50	=	6.7	6.7	-2	2	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	186671	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	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	186671	None	0	Human	Functional	pEC50	=	6.7	6.7	-	1	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	175137	None	0	Human	Functional	pEC50	=	5.7	5.7	2	2	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	175137	None	0	Human	Functional	pEC50	=	5.7	5.7	2	2	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	184560	None	0	Human	Functional	pEC50	=	6.7	6.7	3	3	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	184560	None	0	Human	Functional	pEC50	=	6.7	6.7	3	3	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	193035	None	0	Human	Functional	pEC50	=	7.6	7.6	5	2	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	193035	None	0	Human	Functional	pEC50	=	7.6	7.6	5	2	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	193035	None	0	Human	Functional	pEC50	=	7.6	7.6	5	2	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	184542	None	0	Human	Functional	pEC50	=	6.6	6.6	-2	3	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	184542	None	0	Human	Functional	pEC50	=	6.6	6.6	-2	3	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	193106	None	0	Human	Functional	pEC50	=	6.6	6.6	7	3	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	193106	None	0	Human	Functional	pEC50	=	6.6	6.6	7	3	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	193106	None	0	Human	Functional	pEC50	=	6.6	6.6	7	3	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	193128	None	0	Human	Functional	pEC50	=	6.6	6.6	40	10	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	193128	None	0	Human	Functional	pEC50	=	6.6	6.6	40	10	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	193128	None	0	Human	Functional	pEC50	=	6.6	6.6	40	10	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	218017	None	0	Human	Functional	pEC50	=	5.6	5.6	-	1	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	218017	None	0	Human	Functional	pEC50	=	5.6	5.6	-	1	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	82112	None	0	Human	Functional	pEC50	=	7.6	7.6	13	2	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	82112	None	0	Human	Functional	pEC50	=	7.6	7.6	13	2	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	170849	None	0	Human	Functional	pEC50	=	6.6	6.6	-3	2	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	170849	None	0	Human	Functional	pEC50	=	6.6	6.6	-3	2	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	82102	None	0	Human	Functional	pEC50	=	7.6	7.6	-	1	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	82102	None	0	Human	Functional	pEC50	=	7.6	7.6	-	1	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	193077	None	0	Human	Functional	pEC50	=	7.6	7.6	9	9	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	193077	None	0	Human	Functional	pEC50	=	7.6	7.6	9	9	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	193077	None	0	Human	Functional	pEC50	=	7.6	7.6	9	9	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	193128	None	0	Human	Functional	pEC50	=	7.6	7.6	40	10	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	193128	None	0	Human	Functional	pEC50	=	7.6	7.6	40	10	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	193128	None	0	Human	Functional	pEC50	=	7.6	7.6	40	10	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	170849	None	0	Human	Functional	pEC50	=	6.6	6.6	-3	2	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	170849	None	0	Human	Functional	pEC50	=	6.6	6.6	-3	2	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	217845	None	0	Human	Functional	pEC50	=	5.6	5.6	-	1	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	184531	None	0	Human	Functional	pEC50	=	5.6	5.6	-6	3	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	184531	None	0	Human	Functional	pEC50	=	5.6	5.6	-6	3	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	218043	None	0	Human	Functional	pEC50	=	6.6	6.6	-	1	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	218043	None	0	Human	Functional	pEC50	=	6.6	6.6	-	1	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	184696	None	0	Human	Functional	pEC50	=	6.6	6.6	-2	3	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	184696	None	0	Human	Functional	pEC50	=	6.6	6.6	-2	3	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	9006	None	0	Human	Functional	pEC50	=	7.6	7.6	-	1	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	9006	None	0	Human	Functional	pEC50	=	7.6	7.6	-	1	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	8513	None	0	Human	Functional	pEC50	=	7.5	7.5	47	3	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	8513	None	0	Human	Functional	pEC50	=	7.5	7.5	47	3	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	184696	None	0	Human	Functional	pEC50	=	7.5	7.5	-2	3	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	184696	None	0	Human	Functional	pEC50	=	7.5	7.5	-2	3	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	185194	None	0	Human	Functional	pEC50	=	7.5	7.5	-1	3	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	185194	None	0	Human	Functional	pEC50	=	7.5	7.5	-1	3	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	186189	None	0	Human	Functional	pEC50	=	6.6	6.6	-	1	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	186189	None	0	Human	Functional	pEC50	=	6.6	6.6	-	1	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	193149	None	0	Human	Functional	pEC50	=	6.6	6.6	14	2	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	193149	None	0	Human	Functional	pEC50	=	6.6	6.6	14	2	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	193149	None	0	Human	Functional	pEC50	=	6.6	6.6	14	2	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	193035	None	0	Human	Functional	pEC50	=	6.5	6.5	5	2	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	193035	None	0	Human	Functional	pEC50	=	6.5	6.5	5	2	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	193035	None	0	Human	Functional	pEC50	=	6.5	6.5	5	2	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	None	34	Human	Functional	pEC50	=	5.5	5.5	-67	6	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	None	34	Human	Functional	pEC50	=	5.5	5.5	-67	6	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	None	34	Human	Functional	pEC50	=	5.5	5.5	-67	6	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	185828	None	0	Human	Functional	pEC50	=	7.5	7.5	8	3	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	185828	None	0	Human	Functional	pEC50	=	7.5	7.5	8	3	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	193140	None	0	Human	Functional	pEC50	=	8.5	8.5	31	9	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	193140	None	0	Human	Functional	pEC50	=	8.5	8.5	31	9	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	193140	None	0	Human	Functional	pEC50	=	8.5	8.5	31	9	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	82104	None	0	Human	Functional	pEC50	=	7.5	7.5	-	1	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	82104	None	0	Human	Functional	pEC50	=	7.5	7.5	-	1	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	185238	None	0	Human	Functional	pEC50	=	7.5	7.5	-	1	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	185238	None	0	Human	Functional	pEC50	=	7.5	7.5	-	1	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	185304	None	0	Human	Functional	pEC50	=	6.5	6.5	4	3	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	185304	None	0	Human	Functional	pEC50	=	6.5	6.5	4	3	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	175720	None	0	Human	Functional	pEC50	=	6.5	6.5	-5	2	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	175720	None	0	Human	Functional	pEC50	=	6.5	6.5	-5	2	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	None	34	Human	Functional	pEC50	=	5.5	5.5	-67	6	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	None	34	Human	Functional	pEC50	=	5.5	5.5	-67	6	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	None	34	Human	Functional	pEC50	=	5.5	5.5	-67	6	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	193077	None	0	Human	Functional	pEC50	=	6.5	6.5	9	9	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	193077	None	0	Human	Functional	pEC50	=	6.5	6.5	9	9	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	193077	None	0	Human	Functional	pEC50	=	6.5	6.5	9	9	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	217957	None	0	Human	Functional	pEC50	=	7.5	7.5	-	1	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	186514	None	0	Human	Functional	pEC50	=	6.5	6.5	-	1	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	186514	None	0	Human	Functional	pEC50	=	6.5	6.5	-	1	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	218019	None	0	Human	Functional	pEC50	=	6.5	6.5	-	1	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	218019	None	0	Human	Functional	pEC50	=	6.5	6.5	-	1	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	218043	None	0	Human	Functional	pEC50	=	6.5	6.5	-	1	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	218043	None	0	Human	Functional	pEC50	=	6.5	6.5	-	1	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	218024	None	0	Human	Functional	pEC50	=	6.5	6.5	-	1	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	218024	None	0	Human	Functional	pEC50	=	6.5	6.5	-	1	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	185366	None	0	Human	Functional	pEC50	=	5.5	5.5	-	1	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	185366	None	0	Human	Functional	pEC50	=	5.5	5.5	-	1	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	192914	None	0	Human	Functional	pEC50	=	7.5	7.5	4	3	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	192914	None	0	Human	Functional	pEC50	=	7.5	7.5	4	3	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	192914	None	0	Human	Functional	pEC50	=	7.5	7.5	4	3	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	186189	None	0	Human	Functional	pEC50	=	7.5	7.5	-	1	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	186189	None	0	Human	Functional	pEC50	=	7.5	7.5	-	1	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	185828	None	0	Human	Functional	pEC50	=	6.5	6.5	8	3	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	185828	None	0	Human	Functional	pEC50	=	6.5	6.5	8	3	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	175956	None	0	Human	Functional	pEC50	=	6.4	6.4	-1	2	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	175956	None	0	Human	Functional	pEC50	=	6.4	6.4	-1	2	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	175956	None	0	Human	Functional	pEC50	=	6.4	6.4	-1	2	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	175956	None	0	Human	Functional	pEC50	=	6.4	6.4	-1	2	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	185056	None	0	Human	Functional	pEC50	=	6.4	6.4	-2	3	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	185056	None	0	Human	Functional	pEC50	=	6.4	6.4	-2	3	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	185049	None	0	Human	Functional	pEC50	=	7.4	7.4	-2	3	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	185049	None	0	Human	Functional	pEC50	=	7.4	7.4	-2	3	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	5795	None	0	Human	Functional	pEC50	=	6.4	6.4	-	1	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	5795	None	0	Human	Functional	pEC50	=	6.4	6.4	-	1	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	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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
	774.0	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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
	774.0	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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
	774.0	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.4	5.4	-181	11	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	186573	None	0	Human	Functional	pEC50	=	6.4	6.4	-	1	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	186573	None	0	Human	Functional	pEC50	=	6.4	6.4	-	1	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	218045	None	0	Human	Functional	pEC50	=	5.4	5.4	-	1	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	218045	None	0	Human	Functional	pEC50	=	5.4	5.4	-	1	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	6109	None	0	Human	Functional	pEC50	=	5.4	5.4	-	1	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	6109	None	0	Human	Functional	pEC50	=	5.4	5.4	-	1	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	94207	None	39	Human	Functional	pEC50	=	4.4	4.4	-	1	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	94207	None	39	Human	Functional	pEC50	=	4.4	4.4	-	1	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	192917	None	0	Human	Functional	pEC50	=	8.3	8.3	4	3	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	192917	None	0	Human	Functional	pEC50	=	8.3	8.3	4	3	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	192917	None	0	Human	Functional	pEC50	=	8.3	8.3	4	3	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	192914	None	0	Human	Functional	pEC50	=	6.4	6.4	4	3	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	192914	None	0	Human	Functional	pEC50	=	6.4	6.4	4	3	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	192914	None	0	Human	Functional	pEC50	=	6.4	6.4	4	3	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	218019	None	0	Human	Functional	pEC50	=	6.4	6.4	-	1	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	218019	None	0	Human	Functional	pEC50	=	6.4	6.4	-	1	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	5739	None	0	Human	Functional	pEC50	=	6.4	6.4	-	1	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	5739	None	0	Human	Functional	pEC50	=	6.4	6.4	-	1	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	186671	None	0	Human	Functional	pEC50	=	5.4	5.4	-	1	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	186671	None	0	Human	Functional	pEC50	=	5.4	5.4	-	1	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	82099	None	0	Human	Functional	pEC50	=	7.4	7.4	-	1	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	82099	None	0	Human	Functional	pEC50	=	7.4	7.4	-	1	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	185722	None	0	Human	Functional	pEC50	=	7.4	7.4	-	1	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	185722	None	0	Human	Functional	pEC50	=	7.4	7.4	-	1	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	185204	None	0	Human	Functional	pEC50	=	7.3	7.3	-2	3	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	185204	None	0	Human	Functional	pEC50	=	7.3	7.3	-2	3	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	82098	None	0	Human	Functional	pEC50	=	7.3	7.3	-	1	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	82098	None	0	Human	Functional	pEC50	=	7.3	7.3	-	1	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	192917	None	0	Human	Functional	pEC50	=	7.3	7.3	4	3	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	192917	None	0	Human	Functional	pEC50	=	7.3	7.3	4	3	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	192917	None	0	Human	Functional	pEC50	=	7.3	7.3	4	3	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	193128	None	0	Human	Functional	pEC50	=	8.2	8.2	40	10	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	193128	None	0	Human	Functional	pEC50	=	8.2	8.2	40	10	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	193128	None	0	Human	Functional	pEC50	=	8.2	8.2	40	10	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	8960	None	0	Human	Functional	pEC50	=	7.3	7.3	-	1	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	8960	None	0	Human	Functional	pEC50	=	7.3	7.3	-	1	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	217996	None	0	Human	Functional	pEC50	=	6.3	6.3	-	1	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	217996	None	0	Human	Functional	pEC50	=	6.3	6.3	-	1	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	173187	None	0	Human	Functional	pEC50	=	5.3	5.3	-1	2	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	173187	None	0	Human	Functional	pEC50	=	5.3	5.3	-1	2	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	192457	None	0	Human	Functional	pEC50	=	6.3	6.3	-	1	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	192457	None	0	Human	Functional	pEC50	=	6.3	6.3	-	1	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	185366	None	0	Human	Functional	pEC50	=	6.3	6.3	-	1	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	185366	None	0	Human	Functional	pEC50	=	6.3	6.3	-	1	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	173187	None	0	Human	Functional	pEC50	=	5.3	5.3	-1	2	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	173187	None	0	Human	Functional	pEC50	=	5.3	5.3	-1	2	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	175047	None	0	Human	Functional	pEC50	=	5.3	5.3	2	2	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	175047	None	0	Human	Functional	pEC50	=	5.3	5.3	2	2	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	9005	None	0	Human	Functional	pEC50	=	7.3	7.3	-	1	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	9005	None	0	Human	Functional	pEC50	=	7.3	7.3	-	1	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	175047	None	0	Human	Functional	pEC50	=	5.3	5.3	2	2	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	175047	None	0	Human	Functional	pEC50	=	5.3	5.3	2	2	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	1932	None	74	Human	Functional	pEC50	=	5.3	5.3	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.3	5.3	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.3	5.3	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.3	5.3	-181	11	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
	774.0	1932	None	74	Human	Functional	pEC50	=	5.3	5.3	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.3	5.3	-181	11	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	1932	None	74	Human	Functional	pEC50	=	5.3	5.3	-181	11	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	82110	None	0	Human	Functional	pEC50	=	7.3	7.3	-13	3	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	82110	None	0	Human	Functional	pEC50	=	7.3	7.3	-13	3	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	192957	None	0	Human	Functional	pEC50	=	7.3	7.3	2	3	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	192957	None	0	Human	Functional	pEC50	=	7.3	7.3	2	3	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	192957	None	0	Human	Functional	pEC50	=	7.3	7.3	2	3	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	218045	None	0	Human	Functional	pEC50	=	6.3	6.3	-	1	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	218045	None	0	Human	Functional	pEC50	=	6.3	6.3	-	1	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	82116	None	0	Human	Functional	pEC50	=	7.2	7.2	-	1	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	82116	None	0	Human	Functional	pEC50	=	7.2	7.2	-	1	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	192957	None	0	Human	Functional	pEC50	=	8.2	8.2	2	3	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	192957	None	0	Human	Functional	pEC50	=	8.2	8.2	2	3	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	192957	None	0	Human	Functional	pEC50	=	8.2	8.2	2	3	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	193082	None	0	Human	Functional	pEC50	=	8.2	8.2	10	2	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	193082	None	0	Human	Functional	pEC50	=	8.2	8.2	10	2	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	193082	None	0	Human	Functional	pEC50	=	8.2	8.2	10	2	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	82111	None	0	Human	Functional	pEC50	=	8.2	8.2	-3	3	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	82111	None	0	Human	Functional	pEC50	=	8.2	8.2	-3	3	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	8765	None	0	Human	Functional	pEC50	=	8.2	8.2	-1	4	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	8765	None	0	Human	Functional	pEC50	=	8.2	8.2	-1	4	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	185009	None	0	Human	Functional	pEC50	=	7.2	7.2	3	3	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	185009	None	0	Human	Functional	pEC50	=	7.2	7.2	3	3	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	192894	None	0	Human	Functional	pEC50	=	7.2	7.2	-	1	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	192894	None	0	Human	Functional	pEC50	=	7.2	7.2	-	1	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	192894	None	0	Human	Functional	pEC50	=	7.2	7.2	-	1	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	218024	None	0	Human	Functional	pEC50	=	6.2	6.2	-	1	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	218024	None	0	Human	Functional	pEC50	=	6.2	6.2	-	1	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	179092	None	0	Human	Functional	pEC50	=	7.2	7.2	-25	3	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	179092	None	0	Human	Functional	pEC50	=	7.2	7.2	-25	3	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	184331	None	0	Human	Functional	pEC50	=	7.2	7.2	-26	3	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	184331	None	0	Human	Functional	pEC50	=	7.2	7.2	-26	3	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	218043	None	0	Human	Functional	pEC50	=	7.2	7.2	-	1	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	218043	None	0	Human	Functional	pEC50	=	7.2	7.2	-	1	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	186484	None	0	Human	Functional	pEC50	=	7.2	7.2	1	3	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	186484	None	0	Human	Functional	pEC50	=	7.2	7.2	1	3	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	5739	None	0	Human	Functional	pEC50	=	6.2	6.2	-	1	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	5739	None	0	Human	Functional	pEC50	=	6.2	6.2	-	1	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	1932	None	74	Human	Functional	pEC50	=	6.2	6.2	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.2	6.2	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.2	6.2	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.2	6.2	-181	11	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
	774.0	1932	None	74	Human	Functional	pEC50	=	6.2	6.2	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.2	6.2	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.2	6.2	-181	11	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	218015	None	0	Human	Functional	pEC50	=	6.2	6.2	-	1	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	218015	None	0	Human	Functional	pEC50	=	6.2	6.2	-	1	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	218052	None	0	Human	Functional	pEC50	=	6.2	6.2	-	1	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	218052	None	0	Human	Functional	pEC50	=	6.2	6.2	-	1	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	217461	None	0	Human	Functional	pEC50	=	7.2	7.2	-	1	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	217836	None	0	Human	Functional	pEC50	=	8.1	8.1	-	1	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	217957	None	0	Human	Functional	pEC50	=	8.1	8.1	-	1	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	82096	None	0	Human	Functional	pEC50	=	8.1	8.1	-2	3	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	82096	None	0	Human	Functional	pEC50	=	8.1	8.1	-2	3	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	82100	None	0	Human	Functional	pEC50	=	8.1	8.1	-	1	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	82100	None	0	Human	Functional	pEC50	=	8.1	8.1	-	1	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	218026	None	0	Human	Functional	pEC50	=	7.1	7.1	-	1	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	218026	None	0	Human	Functional	pEC50	=	7.1	7.1	-	1	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	5765	None	0	Human	Functional	pEC50	=	5.1	5.1	-5	2	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	5765	None	0	Human	Functional	pEC50	=	5.1	5.1	-5	2	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	192991	None	0	Human	Functional	pEC50	=	7.1	7.1	77	2	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	192991	None	0	Human	Functional	pEC50	=	7.1	7.1	77	2	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	192991	None	0	Human	Functional	pEC50	=	7.1	7.1	77	2	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	171157	None	0	Human	Functional	pEC50	=	7.1	7.1	7	2	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	171157	None	0	Human	Functional	pEC50	=	7.1	7.1	7	2	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	218031	None	0	Human	Functional	pEC50	=	6.1	6.1	-	1	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	218031	None	0	Human	Functional	pEC50	=	6.1	6.1	-	1	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	193106	None	0	Human	Functional	pEC50	=	7.1	7.1	7	3	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	193106	None	0	Human	Functional	pEC50	=	7.1	7.1	7	3	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	193106	None	0	Human	Functional	pEC50	=	7.1	7.1	7	3	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	175561	None	0	Human	Functional	pEC50	=	7.1	7.1	11	2	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	175561	None	0	Human	Functional	pEC50	=	7.1	7.1	11	2	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	8763	None	0	Human	Functional	pEC50	=	7.1	7.1	-42	4	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	8763	None	0	Human	Functional	pEC50	=	7.1	7.1	-42	4	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	179158	None	0	Human	Functional	pEC50	=	7.1	7.1	-9	2	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	179158	None	0	Human	Functional	pEC50	=	7.1	7.1	-9	2	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	192991	None	0	Human	Functional	pEC50	=	8.1	8.1	77	2	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	192991	None	0	Human	Functional	pEC50	=	8.1	8.1	77	2	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	192991	None	0	Human	Functional	pEC50	=	8.1	8.1	77	2	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	171157	None	0	Human	Functional	pEC50	=	7.1	7.1	7	2	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	171157	None	0	Human	Functional	pEC50	=	7.1	7.1	7	2	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	175561	None	0	Human	Functional	pEC50	=	7.1	7.1	11	2	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	175561	None	0	Human	Functional	pEC50	=	7.1	7.1	11	2	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	175720	None	0	Human	Functional	pEC50	=	6.1	6.1	-5	2	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	175720	None	0	Human	Functional	pEC50	=	6.1	6.1	-5	2	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	185049	None	0	Human	Functional	pEC50	=	7.1	7.1	-2	3	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	185049	None	0	Human	Functional	pEC50	=	7.1	7.1	-2	3	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	94207	None	39	Human	Functional	pEC50	=	5.1	5.1	-	1	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	94207	None	39	Human	Functional	pEC50	=	5.1	5.1	-	1	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	171888	None	0	Human	Functional	pEC50	=	6.1	6.1	3	2	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	171888	None	0	Human	Functional	pEC50	=	6.1	6.1	3	2	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	217773	None	0	Human	Functional	pEC50	=	7.1	7.1	-	1	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	171888	None	0	Human	Functional	pEC50	=	6.1	6.1	3	2	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	171888	None	0	Human	Functional	pEC50	=	6.1	6.1	3	2	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	5716	None	0	Human	Functional	pEC50	=	5.1	5.1	-	1	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	5716	None	0	Human	Functional	pEC50	=	5.1	5.1	-	1	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	8511	None	0	Human	Functional	pEC50	=	8.0	8.0	478	3	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	8511	None	0	Human	Functional	pEC50	=	8.0	8.0	478	3	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	82106	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	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	82106	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	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	217957	None	0	Human	Functional	pEC50	=	7.0	7.0	-	1	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	174967	None	0	Human	Functional	pEC50	=	7.0	7.0	13	2	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	174967	None	0	Human	Functional	pEC50	=	7.0	7.0	13	2	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	1932	None	74	Human	Functional	pEC50	=	6.0	6.0	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.0	6.0	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.0	6.0	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.0	6.0	-181	11	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
	774.0	1932	None	74	Human	Functional	pEC50	=	6.0	6.0	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.0	6.0	-181	11	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	1932	None	74	Human	Functional	pEC50	=	6.0	6.0	-181	11	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	116795	None	0	Rat	Functional	pKd	=	6	6.0	-	3	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	116795	None	0	Rat	Functional	pKd	=	6	6.0	-	3	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	168198	None	0	Rat	Functional	pKd	=	6	6.0	-	3	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	99231	None	0	Rat	Functional	pKd	=	6	6.0	-	3	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	99231	None	0	Rat	Functional	pKd	=	6	6.0	-	3	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	103032	None	0	Rat	Functional	pKd	=	6	6.0	-	3	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	103032	None	0	Rat	Functional	pKd	=	6	6.0	-	3	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	99797	None	0	Rat	Functional	pKd	=	5.9	5.9	-	3	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	99797	None	0	Rat	Functional	pKd	=	5.9	5.9	-	3	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	100087	None	0	Rat	Functional	pKd	=	5.9	5.9	-	3	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	100087	None	0	Rat	Functional	pKd	=	5.9	5.9	-	3	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	99879	None	0	Rat	Functional	pKd	=	7.8	7.8	-	0	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	99879	None	0	Rat	Functional	pKd	=	7.8	7.8	-	0	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	114858	None	0	Rat	Functional	pKd	=	6.8	6.8	-	3	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	114858	None	0	Rat	Functional	pKd	=	6.8	6.8	-	3	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	100073	None	0	Rat	Functional	pKd	=	5.7	5.7	-	0	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	937	None	69	Rat	Functional	pKd	=	6.6	6.6	-	4	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	937	None	69	Rat	Functional	pKd	=	6.6	6.6	-	4	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
	2756.0	937	None	69	Rat	Functional	pKd	=	6.6	6.6	-	4	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	937	None	69	Rat	Functional	pKd	=	6.6	6.6	-	4	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	937	None	69	Rat	Functional	pKd	=	6.6	6.6	-	4	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	937	None	69	Rat	Functional	pKd	=	6.6	6.6	-	4	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	116708	None	0	Rat	Functional	pKd	=	6.6	6.6	-	3	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	116708	None	0	Rat	Functional	pKd	=	6.6	6.6	-	3	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	937	None	69	Rat	Functional	pKd	=	6.6	6.6	-	4	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	937	None	69	Rat	Functional	pKd	=	6.6	6.6	-	4	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
	2756.0	937	None	69	Rat	Functional	pKd	=	6.6	6.6	-	4	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	937	None	69	Rat	Functional	pKd	=	6.6	6.6	-	4	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	937	None	69	Rat	Functional	pKd	=	6.6	6.6	-	4	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	937	None	69	Rat	Functional	pKd	=	6.6	6.6	-	4	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	96978	None	0	Rat	Functional	pKd	=	6.6	6.6	-	3	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	96978	None	0	Rat	Functional	pKd	=	6.6	6.6	-	3	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	99904	None	0	Rat	Functional	pKd	=	6.5	6.5	-	3	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	99904	None	0	Rat	Functional	pKd	=	6.5	6.5	-	3	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	156653	None	0	Rat	Functional	pKd	=	6.5	6.5	-	3	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	156653	None	0	Rat	Functional	pKd	=	6.5	6.5	-	3	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	99441	None	0	Rat	Functional	pKd	=	6.5	6.5	-	3	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	99441	None	0	Rat	Functional	pKd	=	6.5	6.5	-	3	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	99375	None	0	Rat	Functional	pKd	=	5.5	5.5	-	3	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	100086	None	0	Rat	Functional	pKd	=	5.5	5.5	-	3	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	100086	None	0	Rat	Functional	pKd	=	5.5	5.5	-	3	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	100461	None	0	Rat	Functional	pKd	=	6.4	6.4	-	3	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	100461	None	0	Rat	Functional	pKd	=	6.4	6.4	-	3	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	100878	None	0	Rat	Functional	pKd	=	6.4	6.4	-	3	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	100878	None	0	Rat	Functional	pKd	=	6.4	6.4	-	3	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	103239	None	0	Rat	Functional	pKd	=	6.4	6.4	-	3	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	103239	None	0	Rat	Functional	pKd	=	6.4	6.4	-	3	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	103899	None	0	Rat	Functional	pKd	=	6.4	6.4	-	3	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	103899	None	0	Rat	Functional	pKd	=	6.4	6.4	-	3	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	99195	None	0	Rat	Functional	pKd	=	5.4	5.4	-	3	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	99195	None	0	Rat	Functional	pKd	=	5.4	5.4	-	3	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	99712	None	0	Rat	Functional	pKd	=	7.3	7.3	-	0	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	99712	None	0	Rat	Functional	pKd	=	7.3	7.3	-	0	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	100133	None	0	Rat	Functional	pKd	=	6.3	6.3	-	3	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	100133	None	0	Rat	Functional	pKd	=	6.3	6.3	-	3	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	96494	None	0	Rat	Functional	pKd	=	6.3	6.3	-	3	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	96494	None	0	Rat	Functional	pKd	=	6.3	6.3	-	3	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	99442	None	0	Rat	Functional	pKd	=	6.3	6.3	-	3	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	99442	None	0	Rat	Functional	pKd	=	6.3	6.3	-	3	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	116933	None	0	Rat	Functional	pKd	=	6.3	6.3	-	3	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	116933	None	0	Rat	Functional	pKd	=	6.3	6.3	-	3	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	99184	None	0	Rat	Functional	pKd	=	5.3	5.3	-	3	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	99184	None	0	Rat	Functional	pKd	=	5.3	5.3	-	3	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	101673	None	0	Rat	Functional	pKd	=	5.3	5.3	-	3	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	101673	None	0	Rat	Functional	pKd	=	5.3	5.3	-	3	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	114882	None	0	Rat	Functional	pKd	=	6.2	6.2	-	3	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	114882	None	0	Rat	Functional	pKd	=	6.2	6.2	-	3	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	99021	None	0	Rat	Functional	pKd	=	6.2	6.2	-	3	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	99021	None	0	Rat	Functional	pKd	=	6.2	6.2	-	3	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	103083	None	0	Rat	Functional	pKd	=	6.2	6.2	-	3	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	103083	None	0	Rat	Functional	pKd	=	6.2	6.2	-	3	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	107358	None	0	Rat	Functional	pKd	=	6.2	6.2	-	3	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	107358	None	0	Rat	Functional	pKd	=	6.2	6.2	-	3	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	98831	None	0	Rat	Functional	pKd	=	5.2	5.2	-	3	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	98831	None	0	Rat	Functional	pKd	=	5.2	5.2	-	3	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	99798	None	0	Rat	Functional	pKd	=	6.1	6.1	-	3	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	99798	None	0	Rat	Functional	pKd	=	6.1	6.1	-	3	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	99946	None	0	Rat	Functional	pKd	=	6.1	6.1	-	3	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	99884	None	0	Rat	Functional	pKd	=	6.1	6.1	-	3	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	99884	None	0	Rat	Functional	pKd	=	6.1	6.1	-	3	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	100017	None	0	Rat	Functional	pKd	=	6.1	6.1	-	3	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	100017	None	0	Rat	Functional	pKd	=	6.1	6.1	-	3	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	104840	None	0	Rat	Functional	pKd	=	6.1	6.1	-	3	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	104840	None	0	Rat	Functional	pKd	=	6.1	6.1	-	3	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	68239	None	0	Human	Functional	pKi	=	5.5	5.5	-	0	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	68239	None	0	Human	Functional	pKi	=	5.5	5.5	-	0	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	68238	None	0	Human	Functional	pKi	=	5.1	5.1	-	0	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	68238	None	0	Human	Functional	pKi	=	5.1	5.1	-	0	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
	1204	1932	None	74	Guinea pig	Functional	pEC50	=	8.2	8.2	2	11	Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1247	1932	None	74	Guinea pig	Functional	pEC50	=	8.2	8.2	2	11	Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	1375	1932	None	74	Guinea pig	Functional	pEC50	=	8.2	8.2	2	11	Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	774	1932	None	74	Guinea pig	Functional	pEC50	=	8.2	8.2	2	11	Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	774.0	1932	None	74	Guinea pig	Functional	pEC50	=	8.2	8.2	2	11	Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	CHEMBL90	1932	None	74	Guinea pig	Functional	pEC50	=	8.2	8.2	2	11	Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	DB05381	1932	None	74	Guinea pig	Functional	pEC50	=	8.2	8.2	2	11	Agonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 minsAgonist activity at guinea pig atrium histamine H2 receptor assessed as potentiation of histamine-induced response after 30 mins	Drug Central	111	2	2	2	-0.1	NCCc1cnc[nH]1	None
	126688	404	None	24	Human	Functional	pEC50	=	6.4	6.4	57	2	UnclassifiedUnclassified	Guide to Pharmacology	157	2	2	4	0.5	NCCc1sc(nc1C)N	19072936
	4025	404	None	24	Human	Functional	pEC50	=	6.4	6.4	57	2	UnclassifiedUnclassified	Guide to Pharmacology	157	2	2	4	0.5	NCCc1sc(nc1C)N	19072936
	CHEMBL293762	404	None	24	Human	Functional	pEC50	=	6.4	6.4	57	2	UnclassifiedUnclassified	Guide to Pharmacology	157	2	2	4	0.5	NCCc1sc(nc1C)N	19072936
	1229	743	None	0	Human	Functional	pEC50	None	5.7	5.7	-	1	UnclassifiedUnclassified	Guide to Pharmacology	262	5	3	2	2.0	CNC(=S)NCCCCc1cccc2c1cn[nH]2	9681472
	5311293	743	None	0	Human	Functional	pEC50	None	5.7	5.7	-	1	UnclassifiedUnclassified	Guide to Pharmacology	262	5	3	2	2.0	CNC(=S)NCCCCc1cccc2c1cn[nH]2	9681472
	18381	220193	None	0	Human	Functional	pIC50	=	8.3	8.3	1	4	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	220190	None	0	Human	Functional	pIC50	=	8.3	8.3	-1	14	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	401	None	38	Human	Functional	pIC50	=	8.2	8.2	-100	38	NoneNone	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	200	401	None	38	Human	Functional	pIC50	=	8.2	8.2	-100	38	NoneNone	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	2160	401	None	38	Human	Functional	pIC50	=	8.2	8.2	-100	38	NoneNone	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	2160.0	401	None	38	Human	Functional	pIC50	=	8.2	8.2	-100	38	NoneNone	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	CHEMBL629	401	None	38	Human	Functional	pIC50	=	8.2	8.2	-100	38	NoneNone	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	DB00321	401	None	38	Human	Functional	pIC50	=	8.2	8.2	-100	38	NoneNone	Drug Central	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	None
	3036780	107587	None	16	Human	Functional	pIC50	=	8.1	8.1	-40	15	NoneNone	Drug Central	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
	3036780.0	107587	None	16	Human	Functional	pIC50	=	8.1	8.1	-40	15	NoneNone	Drug Central	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
	46780481	107587	None	16	Human	Functional	pIC50	=	8.1	8.1	-40	15	NoneNone	Drug Central	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
	9903970	107587	None	16	Human	Functional	pIC50	=	8.1	8.1	-40	15	NoneNone	Drug Central	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
	9903970.0	107587	None	16	Human	Functional	pIC50	=	8.1	8.1	-40	15	NoneNone	Drug Central	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
	CHEMBL3187365	107587	None	16	Human	Functional	pIC50	=	8.1	8.1	-40	15	NoneNone	Drug Central	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
	CHEMBL3544974	107587	None	16	Human	Functional	pIC50	=	8.1	8.1	-40	15	NoneNone	Drug Central	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
	CHEMBL504548	107587	None	16	Human	Functional	pIC50	=	8.1	8.1	-40	15	NoneNone	Drug Central	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None
	DB06216	107587	None	16	Human	Functional	pIC50	=	8.1	8.1	-40	15	NoneNone	Drug Central	285	0	0	2	4.3	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	None

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Ligands (move mouse cursor over ligand name to see structure)					Receptor	Activity									Chemical information
Sel. page	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI
	213	3853	None	34	Human	Binding	pAC50	=	5.0	5.0	-7	43	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	10.1038/s41467-023-40064-9
	2717	3853	None	34	Human	Binding	pAC50	=	5.0	5.0	-7	43	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	10.1038/s41467-023-40064-9
	5533	3853	None	34	Human	Binding	pAC50	=	5.0	5.0	-7	43	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	10.1038/s41467-023-40064-9
	5533.0	3853	None	34	Human	Binding	pAC50	=	5.0	5.0	-7	43	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	10.1038/s41467-023-40064-9
	CHEMBL621	3853	None	34	Human	Binding	pAC50	=	5.0	5.0	-7	43	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	10.1038/s41467-023-40064-9
	DB00656	3853	None	34	Human	Binding	pAC50	=	5.0	5.0	-7	43	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	371	5	0	6	2.4	Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2	10.1038/s41467-023-40064-9
	104850	3330	None	58	Human	Binding	pAC50	=	5.0	5.0	-	6	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
	4150	3330	None	58	Human	Binding	pAC50	=	5.0	5.0	-	6	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
	743	3330	None	58	Human	Binding	pAC50	=	5.0	5.0	-	6	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
	CHEMBL111	3330	None	58	Human	Binding	pAC50	=	5.0	5.0	-	6	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
	DB06155	3330	None	58	Human	Binding	pAC50	=	5.0	5.0	-	6	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	462	4	1	4	5.9	Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1	10.1038/s41467-023-40064-9
	2284	3182	None	26	Human	Binding	pAC50	=	7.0	7.0	-53	28	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1038/s41467-023-40064-9
	4926	3182	None	26	Human	Binding	pAC50	=	7.0	7.0	-53	28	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1038/s41467-023-40064-9
	7281	3182	None	26	Human	Binding	pAC50	=	7.0	7.0	-53	28	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1038/s41467-023-40064-9
	CHEMBL564	3182	None	26	Human	Binding	pAC50	=	7.0	7.0	-53	28	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1038/s41467-023-40064-9
	DB00420	3182	None	26	Human	Binding	pAC50	=	7.0	7.0	-53	28	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	284	4	0	3	4.2	CN(CCCN1c2ccccc2Sc2c1cccc2)C	10.1038/s41467-023-40064-9
	1353	1911	None	63	Human	Binding	pAC50	=	6.9	6.9	-131	85	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
	3559	1911	None	63	Human	Binding	pAC50	=	6.9	6.9	-131	85	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
	3559.0	1911	None	63	Human	Binding	pAC50	=	6.9	6.9	-131	85	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
	86	1911	None	63	Human	Binding	pAC50	=	6.9	6.9	-131	85	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
	CHEMBL54	1911	None	63	Human	Binding	pAC50	=	6.9	6.9	-131	85	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
	DB00502	1911	None	63	Human	Binding	pAC50	=	6.9	6.9	-131	85	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	375	6	1	3	4.4	Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl	10.1038/s41467-023-40064-9
	4212	201135	None	57	Human	Binding	pAC50	=	4.9	4.9	-	4	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	444	12	8	10	-0.1	O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21	10.1038/s41467-023-40064-9
	CHEMBL1417019	201135	None	57	Human	Binding	pAC50	=	4.9	4.9	-	4	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	444	12	8	10	-0.1	O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21	10.1038/s41467-023-40064-9
	CHEMBL58	201135	None	57	Human	Binding	pAC50	=	4.9	4.9	-	4	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	444	12	8	10	-0.1	O=C1c2c(O)ccc(O)c2C(=O)c2c(NCCNCCO)ccc(NCCNCCO)c21	10.1038/s41467-023-40064-9
	39186	85969	None	36	Human	Binding	pAC50	=	4.9	4.9	-	2	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	414	6	0	6	3.4	COc1ccc([C@@H]2Sc3ccccc3N(CCN(C)C)C(=O)[C@@H]2OC(C)=O)cc1	10.1038/s41467-023-40064-9
	CHEMBL23	85969	None	36	Human	Binding	pAC50	=	4.9	4.9	-	2	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	414	6	0	6	3.4	COc1ccc([C@@H]2Sc3ccccc3N(CCN(C)C)C(=O)[C@@H]2OC(C)=O)cc1	10.1038/s41467-023-40064-9
	9915743	63562	None	59	Human	Binding	pAC50	=	5.9	5.9	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	556	11	2	8	5.9	CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)/C=C/CN(C)C	10.1038/s41467-023-40064-9
	CHEMBL180022	63562	None	59	Human	Binding	pAC50	=	5.9	5.9	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	556	11	2	8	5.9	CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)/C=C/CN(C)C	10.1038/s41467-023-40064-9
	5472	208276	None	49	Human	Binding	pAC50	=	4.9	4.9	-	3	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	263	2	0	2	4.0	Clc1ccccc1CN1CCc2sccc2C1	10.1038/s41467-023-40064-9
	5472.0	208276	None	49	Human	Binding	pAC50	=	4.9	4.9	-	3	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	263	2	0	2	4.0	Clc1ccccc1CN1CCc2sccc2C1	10.1038/s41467-023-40064-9
	CHEMBL1717	208276	None	49	Human	Binding	pAC50	=	4.9	4.9	-	3	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	263	2	0	2	4.0	Clc1ccccc1CN1CCc2sccc2C1	10.1038/s41467-023-40064-9
	CHEMBL833	208276	None	49	Human	Binding	pAC50	=	4.9	4.9	-	3	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	263	2	0	2	4.0	Clc1ccccc1CN1CCc2sccc2C1	10.1038/s41467-023-40064-9
	DB00208	208276	None	49	Human	Binding	pAC50	=	4.9	4.9	-	3	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	263	2	0	2	4.0	Clc1ccccc1CN1CCc2sccc2C1	10.1038/s41467-023-40064-9
	10096344	89628	None	56	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	472	4	1	10	1.1	CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(Cc1nc(C)c3ccccc3n1)c(=O)n2C	10.1038/s41467-023-40064-9
	CHEMBL237500	89628	None	56	Human	Binding	pAC50	=	4.9	4.9	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	472	4	1	10	1.1	CC#CCn1c(N2CCC[C@@H](N)C2)nc2c1c(=O)n(Cc1nc(C)c3ccccc3n1)c(=O)n2C	10.1038/s41467-023-40064-9
	1613	2348	None	42	Human	Binding	pAC50	=	6.9	6.9	-8	44	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	205	2348	None	42	Human	Binding	pAC50	=	6.9	6.9	-8	44	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	3964	2348	None	42	Human	Binding	pAC50	=	6.9	6.9	-8	44	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	3964.0	2348	None	42	Human	Binding	pAC50	=	6.9	6.9	-8	44	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	CHEMBL831	2348	None	42	Human	Binding	pAC50	=	6.9	6.9	-8	44	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	DB00408	2348	None	42	Human	Binding	pAC50	=	6.9	6.9	-8	44	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	327	0	0	4	3.8	CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2	10.1038/s41467-023-40064-9
	1890	2759	None	31	Human	Binding	pAC50	=	5.8	5.8	-	26	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	469	10	0	7	3.6	CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl	10.1038/s41467-023-40064-9
	4449	2759	None	31	Human	Binding	pAC50	=	5.8	5.8	-	26	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	469	10	0	7	3.6	CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl	10.1038/s41467-023-40064-9
	7247	2759	None	31	Human	Binding	pAC50	=	5.8	5.8	-	26	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	469	10	0	7	3.6	CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl	10.1038/s41467-023-40064-9
	CHEMBL623	2759	None	31	Human	Binding	pAC50	=	5.8	5.8	-	26	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	469	10	0	7	3.6	CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl	10.1038/s41467-023-40064-9
	DB01149	2759	None	31	Human	Binding	pAC50	=	5.8	5.8	-	26	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	469	10	0	7	3.6	CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl	10.1038/s41467-023-40064-9
	212	3806	None	35	Human	Binding	pAC50	=	6.8	6.8	-6	25	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	10.1038/s41467-023-40064-9
	2639	3806	None	35	Human	Binding	pAC50	=	6.8	6.8	-6	25	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	10.1038/s41467-023-40064-9
	941651	3806	None	35	Human	Binding	pAC50	=	6.8	6.8	-6	25	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	10.1038/s41467-023-40064-9
	941651.0	3806	None	35	Human	Binding	pAC50	=	6.8	6.8	-6	25	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	10.1038/s41467-023-40064-9
	CHEMBL1201	3806	None	35	Human	Binding	pAC50	=	6.8	6.8	-6	25	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	10.1038/s41467-023-40064-9
	DB01623	3806	None	35	Human	Binding	pAC50	=	6.8	6.8	-6	25	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	443	5	0	5	3.5	CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C	10.1038/s41467-023-40064-9
	4034	55838	None	37	Human	Binding	pAC50	=	5.8	5.8	-	1	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	390	5	0	2	5.6	Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1	10.1038/s41467-023-40064-9
	4034.0	55838	None	37	Human	Binding	pAC50	=	5.8	5.8	-	1	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	390	5	0	2	5.6	Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1	10.1038/s41467-023-40064-9
	CHEMBL1623	55838	None	37	Human	Binding	pAC50	=	5.8	5.8	-	1	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	390	5	0	2	5.6	Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1	10.1038/s41467-023-40064-9
	DB00737	55838	None	37	Human	Binding	pAC50	=	5.8	5.8	-	1	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	390	5	0	2	5.6	Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1	10.1038/s41467-023-40064-9
	1209	1658	None	52	Human	Binding	pAC50	=	5.8	5.8	-	31	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	309	6	1	2	4.4	CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F	10.1038/s41467-023-40064-9
	203	1658	None	52	Human	Binding	pAC50	=	5.8	5.8	-	31	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	309	6	1	2	4.4	CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F	10.1038/s41467-023-40064-9
	3386	1658	None	52	Human	Binding	pAC50	=	5.8	5.8	-	31	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	309	6	1	2	4.4	CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F	10.1038/s41467-023-40064-9
	CHEMBL41	1658	None	52	Human	Binding	pAC50	=	5.8	5.8	-	31	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	309	6	1	2	4.4	CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F	10.1038/s41467-023-40064-9
	DB00472	1658	None	52	Human	Binding	pAC50	=	5.8	5.8	-	31	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	309	6	1	2	4.4	CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F	10.1038/s41467-023-40064-9
	2585	803	None	59	Human	Binding	pAC50	=	5.8	5.8	-	22	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
	2585.0	803	None	59	Human	Binding	pAC50	=	5.8	5.8	-	22	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
	522	803	None	59	Human	Binding	pAC50	=	5.8	5.8	-	22	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
	551	803	None	59	Human	Binding	pAC50	=	5.8	5.8	-	22	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
	CHEMBL723	803	None	59	Human	Binding	pAC50	=	5.8	5.8	-	22	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
	DB01136	803	None	59	Human	Binding	pAC50	=	5.8	5.8	-	22	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	406	10	3	5	3.7	COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O	10.1038/s41467-023-40064-9
	48041	107137	None	37	Human	Binding	pAC50	=	4.8	4.8	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	352	6	1	3	4.4	COc1ccc(C(=O)Nc2ccccc2CCC2CCCCN2C)cc1	10.1038/s41467-023-40064-9
	CHEMBL315838	107137	None	37	Human	Binding	pAC50	=	4.8	4.8	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	352	6	1	3	4.4	COc1ccc(C(=O)Nc2ccccc2CCC2CCCCN2C)cc1	10.1038/s41467-023-40064-9
	31101	729	None	28	Human	Binding	pAC50	=	5.8	5.8	-	35	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	653	5	3	6	3.2	CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C	10.1038/s41467-023-40064-9
	31101.0	729	None	28	Human	Binding	pAC50	=	5.8	5.8	-	35	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	653	5	3	6	3.2	CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C	10.1038/s41467-023-40064-9
	35	729	None	28	Human	Binding	pAC50	=	5.8	5.8	-	35	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	653	5	3	6	3.2	CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C	10.1038/s41467-023-40064-9
	403	729	None	28	Human	Binding	pAC50	=	5.8	5.8	-	35	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	653	5	3	6	3.2	CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C	10.1038/s41467-023-40064-9
	CHEMBL493	729	None	28	Human	Binding	pAC50	=	5.8	5.8	-	35	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	653	5	3	6	3.2	CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C	10.1038/s41467-023-40064-9
	DB01200	729	None	28	Human	Binding	pAC50	=	5.8	5.8	-	35	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	653	5	3	6	3.2	CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C	10.1038/s41467-023-40064-9
	2726	919	None	48	Human	Binding	pAC50	=	6.8	6.8	-85	72	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	2726.0	919	None	48	Human	Binding	pAC50	=	6.8	6.8	-85	72	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	621	919	None	48	Human	Binding	pAC50	=	6.8	6.8	-85	72	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	83	919	None	48	Human	Binding	pAC50	=	6.8	6.8	-85	72	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	CHEMBL71	919	None	48	Human	Binding	pAC50	=	6.8	6.8	-85	72	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	DB00477	919	None	48	Human	Binding	pAC50	=	6.8	6.8	-85	72	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	318	4	0	3	4.9	CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C	10.1038/s41467-023-40064-9
	2600	3779	None	53	Human	Binding	pAC50	=	5.8	5.8	-	13	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
	2608	3779	None	53	Human	Binding	pAC50	=	5.8	5.8	-	13	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
	5405	3779	None	53	Human	Binding	pAC50	=	5.8	5.8	-	13	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
	CHEMBL17157	3779	None	53	Human	Binding	pAC50	=	5.8	5.8	-	13	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
	DB00342	3779	None	53	Human	Binding	pAC50	=	5.8	5.8	-	13	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	471	8	2	3	6.4	OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O	10.1038/s41467-023-40064-9
	2812	4781	None	63	Human	Binding	pAC50	=	4.8	4.8	-33	34	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	10.1038/s41467-023-40064-9
	CHEMBL104	4781	None	63	Human	Binding	pAC50	=	4.8	4.8	-33	34	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	344	4	0	2	5.4	Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1	10.1038/s41467-023-40064-9
	1016	3747	None	45	Human	Binding	pAC50	=	5.8	5.8	-41	35	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	10.1038/s41467-023-40064-9
	2561	3747	None	45	Human	Binding	pAC50	=	5.8	5.8	-41	35	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	10.1038/s41467-023-40064-9
	2733526	3747	None	45	Human	Binding	pAC50	=	5.8	5.8	-41	35	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	10.1038/s41467-023-40064-9
	5384	3747	None	45	Human	Binding	pAC50	=	5.8	5.8	-41	35	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL83	3747	None	45	Human	Binding	pAC50	=	5.8	5.8	-41	35	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	10.1038/s41467-023-40064-9
	DB00675	3747	None	45	Human	Binding	pAC50	=	5.8	5.8	-41	35	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	371	8	0	2	6.0	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1	10.1038/s41467-023-40064-9
	1222	881	None	0	Human	Binding	pAC50	=	5.7	5.7	-	2	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	388	8	1	4	3.1	OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	2678	881	None	0	Human	Binding	pAC50	=	5.7	5.7	-	2	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	388	8	1	4	3.1	OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	2678.0	881	None	0	Human	Binding	pAC50	=	5.7	5.7	-	2	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	388	8	1	4	3.1	OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	581	881	None	0	Human	Binding	pAC50	=	5.7	5.7	-	2	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	388	8	1	4	3.1	OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL1000	881	None	0	Human	Binding	pAC50	=	5.7	5.7	-	2	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	388	8	1	4	3.1	OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	DB00341	881	None	0	Human	Binding	pAC50	=	5.7	5.7	-	2	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	388	8	1	4	3.1	OC(=O)COCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	1400	1957	None	46	Human	Binding	pAC50	=	6.7	6.7	-	3	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	3658	1957	None	46	Human	Binding	pAC50	=	6.7	6.7	-	3	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	3658.0	1957	None	46	Human	Binding	pAC50	=	6.7	6.7	-	3	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	7199	1957	None	46	Human	Binding	pAC50	=	6.7	6.7	-	3	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	91513	1957	None	46	Human	Binding	pAC50	=	6.7	6.7	-	3	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	CHEMBL896	1957	None	46	Human	Binding	pAC50	=	6.7	6.7	-	3	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	DB00557	1957	None	46	Human	Binding	pAC50	=	6.7	6.7	-	3	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	374	8	1	4	3.1	OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1	10.1038/s41467-023-40064-9
	102	4127	None	36	Human	Binding	pAC50	=	4.7	4.7	-	50	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	354	1	2	4	2.6	COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1	10.1038/s41467-023-40064-9
	3659	4127	None	36	Human	Binding	pAC50	=	4.7	4.7	-	50	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	354	1	2	4	2.6	COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1	10.1038/s41467-023-40064-9
	8969	4127	None	36	Human	Binding	pAC50	=	4.7	4.7	-	50	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	354	1	2	4	2.6	COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1	10.1038/s41467-023-40064-9
	8969.0	4127	None	36	Human	Binding	pAC50	=	4.7	4.7	-	50	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	354	1	2	4	2.6	COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1	10.1038/s41467-023-40064-9
	CHEMBL15245	4127	None	36	Human	Binding	pAC50	=	4.7	4.7	-	50	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	354	1	2	4	2.6	COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1	10.1038/s41467-023-40064-9
	DB01392	4127	None	36	Human	Binding	pAC50	=	4.7	4.7	-	50	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	354	1	2	4	2.6	COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1	10.1038/s41467-023-40064-9
	1231	937	None	69	Human	Binding	pAC50	=	6.7	6.7	-4	8	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1038/s41467-023-40064-9
	2756	937	None	69	Human	Binding	pAC50	=	6.7	6.7	-4	8	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1038/s41467-023-40064-9
	2756.0	937	None	69	Human	Binding	pAC50	=	6.7	6.7	-4	8	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1038/s41467-023-40064-9
	645	937	None	69	Human	Binding	pAC50	=	6.7	6.7	-4	8	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1038/s41467-023-40064-9
	CHEMBL30	937	None	69	Human	Binding	pAC50	=	6.7	6.7	-4	8	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1038/s41467-023-40064-9
	DB00501	937	None	69	Human	Binding	pAC50	=	6.7	6.7	-4	8	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	252	5	3	4	0.6	N#CNC(=NC)NCCSCc1nc[nH]c1C	10.1038/s41467-023-40064-9
	180	401	None	38	Human	Binding	pAC50	=	7.7	7.7	-1412	39	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	200	401	None	38	Human	Binding	pAC50	=	7.7	7.7	-1412	39	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	2160	401	None	38	Human	Binding	pAC50	=	7.7	7.7	-1412	39	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	2160.0	401	None	38	Human	Binding	pAC50	=	7.7	7.7	-1412	39	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	CHEMBL629	401	None	38	Human	Binding	pAC50	=	7.7	7.7	-1412	39	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	DB00321	401	None	38	Human	Binding	pAC50	=	7.7	7.7	-1412	39	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	277	3	0	1	4.2	CN(CCC=C1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	5328940	100270	None	65	Human	Binding	pAC50	=	5.7	5.7	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	529	9	1	8	5.2	COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl	10.1038/s41467-023-40064-9
	CHEMBL288441	100270	None	65	Human	Binding	pAC50	=	5.7	5.7	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	529	9	1	8	5.2	COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl	10.1038/s41467-023-40064-9
	242	470	None	70	Human	Binding	pAC50	=	5.7	5.7	-7244	51	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1038/s41467-023-40064-9
	34	470	None	70	Human	Binding	pAC50	=	5.7	5.7	-7244	51	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1038/s41467-023-40064-9
	60795	470	None	70	Human	Binding	pAC50	=	5.7	5.7	-7244	51	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1038/s41467-023-40064-9
	60795.0	470	None	70	Human	Binding	pAC50	=	5.7	5.7	-7244	51	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1038/s41467-023-40064-9
	CHEMBL1112	470	None	70	Human	Binding	pAC50	=	5.7	5.7	-7244	51	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1038/s41467-023-40064-9
	DB01238	470	None	70	Human	Binding	pAC50	=	5.7	5.7	-7244	51	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	447	7	1	4	4.9	O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl	10.1038/s41467-023-40064-9
	5039	63203	None	12	Human	Binding	pAC50	=	6.6	6.6	-	1	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	314	10	2	7	1.5	CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1	10.1038/s41467-023-40064-9
	5039.0	63203	None	12	Human	Binding	pAC50	=	6.6	6.6	-	1	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	314	10	2	7	1.5	CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1	10.1038/s41467-023-40064-9
	CHEMBL1790041	63203	None	12	Human	Binding	pAC50	=	6.6	6.6	-	1	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	314	10	2	7	1.5	CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1	10.1038/s41467-023-40064-9
	DB00863	63203	None	12	Human	Binding	pAC50	=	6.6	6.6	-	1	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	314	10	2	7	1.5	CNC(=C[N+](=O)[O-])NCCSCc1ccc(CN(C)C)o1	10.1038/s41467-023-40064-9
	3157	1470	None	44	Human	Binding	pAC50	=	5.6	5.6	-	11	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	451	4	2	8	1.5	COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2	10.1038/s41467-023-40064-9
	3157.0	1470	None	44	Human	Binding	pAC50	=	5.6	5.6	-	11	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	451	4	2	8	1.5	COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2	10.1038/s41467-023-40064-9
	7170	1470	None	44	Human	Binding	pAC50	=	5.6	5.6	-	11	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	451	4	2	8	1.5	COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2	10.1038/s41467-023-40064-9
	954	1470	None	44	Human	Binding	pAC50	=	5.6	5.6	-	11	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	451	4	2	8	1.5	COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2	10.1038/s41467-023-40064-9
	CHEMBL707	1470	None	44	Human	Binding	pAC50	=	5.6	5.6	-	11	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	451	4	2	8	1.5	COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2	10.1038/s41467-023-40064-9
	DB00590	1470	None	44	Human	Binding	pAC50	=	5.6	5.6	-	11	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	451	4	2	8	1.5	COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2	10.1038/s41467-023-40064-9
	134	2514	None	19	Human	Binding	pAC50	=	5.6	5.6	-8511	67	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	10.1038/s41467-023-40064-9
	1775	2514	None	19	Human	Binding	pAC50	=	5.6	5.6	-8511	67	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	10.1038/s41467-023-40064-9
	9681	2514	None	19	Human	Binding	pAC50	=	5.6	5.6	-8511	67	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	10.1038/s41467-023-40064-9
	9681.0	2514	None	19	Human	Binding	pAC50	=	5.6	5.6	-8511	67	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	10.1038/s41467-023-40064-9
	CHEMBL1065	2514	None	19	Human	Binding	pAC50	=	5.6	5.6	-8511	67	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	10.1038/s41467-023-40064-9
	DB00247	2514	None	19	Human	Binding	pAC50	=	5.6	5.6	-8511	67	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	353	4	2	4	1.9	CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO	10.1038/s41467-023-40064-9
	1224	1432	None	51	Human	Binding	pAC50	=	6.6	6.6	-	13	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	3100	1432	None	51	Human	Binding	pAC50	=	6.6	6.6	-	13	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	3100.0	1432	None	51	Human	Binding	pAC50	=	6.6	6.6	-	13	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	8980	1432	None	51	Human	Binding	pAC50	=	6.6	6.6	-	13	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	916	1432	None	51	Human	Binding	pAC50	=	6.6	6.6	-	13	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	CHEMBL657	1432	None	51	Human	Binding	pAC50	=	6.6	6.6	-	13	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	DB01075	1432	None	51	Human	Binding	pAC50	=	6.6	6.6	-	13	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	255	6	0	2	3.4	CN(CCOC(c1ccccc1)c1ccccc1)C	10.1038/s41467-023-40064-9
	10531	1420	None	13	Human	Binding	pAC50	=	6.6	6.6	-	30	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	583	4	3	6	2.1	CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O	10.1038/s41467-023-40064-9
	10531.0	1420	None	13	Human	Binding	pAC50	=	6.6	6.6	-	30	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	583	4	3	6	2.1	CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O	10.1038/s41467-023-40064-9
	121	1420	None	13	Human	Binding	pAC50	=	6.6	6.6	-	30	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	583	4	3	6	2.1	CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O	10.1038/s41467-023-40064-9
	888	1420	None	13	Human	Binding	pAC50	=	6.6	6.6	-	30	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	583	4	3	6	2.1	CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O	10.1038/s41467-023-40064-9
	CHEMBL1732	1420	None	13	Human	Binding	pAC50	=	6.6	6.6	-	30	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	583	4	3	6	2.1	CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O	10.1038/s41467-023-40064-9
	DB00320	1420	None	13	Human	Binding	pAC50	=	6.6	6.6	-	30	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	583	4	3	6	2.1	CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O	10.1038/s41467-023-40064-9
	1212	1662	None	37	Human	Binding	pAC50	=	6.6	6.6	-323	65	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	204	1662	None	37	Human	Binding	pAC50	=	6.6	6.6	-323	65	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	3372	1662	None	37	Human	Binding	pAC50	=	6.6	6.6	-323	65	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	3372.0	1662	None	37	Human	Binding	pAC50	=	6.6	6.6	-323	65	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	CHEMBL726	1662	None	37	Human	Binding	pAC50	=	6.6	6.6	-323	65	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	DB00623	1662	None	37	Human	Binding	pAC50	=	6.6	6.6	-323	65	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	437	6	1	5	4.3	OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	191	403	None	60	Human	Binding	pAC50	=	6.6	6.6	-	28	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	201	403	None	60	Human	Binding	pAC50	=	6.6	6.6	-	28	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	2170	403	None	60	Human	Binding	pAC50	=	6.6	6.6	-	28	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	2170.0	403	None	60	Human	Binding	pAC50	=	6.6	6.6	-	28	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	CHEMBL1113	403	None	60	Human	Binding	pAC50	=	6.6	6.6	-	28	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	DB00543	403	None	60	Human	Binding	pAC50	=	6.6	6.6	-	28	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	313	0	1	4	3.4	Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1	10.1038/s41467-023-40064-9
	176	398	None	47	Human	Binding	pAC50	=	5.6	5.6	-6	31	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
	2157	398	None	47	Human	Binding	pAC50	=	5.6	5.6	-6	31	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
	2157.0	398	None	47	Human	Binding	pAC50	=	5.6	5.6	-6	31	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
	2566	398	None	47	Human	Binding	pAC50	=	5.6	5.6	-6	31	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
	CHEMBL633	398	None	47	Human	Binding	pAC50	=	5.6	5.6	-6	31	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
	DB01118	398	None	47	Human	Binding	pAC50	=	5.6	5.6	-6	31	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	645	11	0	4	6.9	CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2	10.1038/s41467-023-40064-9
	124087	1389	None	72	Human	Binding	pAC50	=	8.5	8.5	-29	15	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
	124087.0	1389	None	72	Human	Binding	pAC50	=	8.5	8.5	-29	15	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
	7157	1389	None	72	Human	Binding	pAC50	=	8.5	8.5	-29	15	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
	814	1389	None	72	Human	Binding	pAC50	=	8.5	8.5	-29	15	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
	CHEMBL1172	1389	None	72	Human	Binding	pAC50	=	8.5	8.5	-29	15	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
	DB00967	1389	None	72	Human	Binding	pAC50	=	8.5	8.5	-29	15	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	310	0	1	2	4.0	Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1	10.1038/s41467-023-40064-9
	3180	14479	None	25	Human	Binding	pAC50	=	5.5	5.5	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	289	8	0	3	3.9	CCCCOc1ccc(C(=O)CCN2CCCCC2)cc1	10.1038/s41467-023-40064-9
	CHEMBL1201217	14479	None	25	Human	Binding	pAC50	=	5.5	5.5	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	289	8	0	3	3.9	CCCCOc1ccc(C(=O)CCN2CCCCC2)cc1	10.1038/s41467-023-40064-9
	2705	3842	None	44	Human	Binding	pAC50	=	5.5	5.5	-	11	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	325	7	1	2	5.3	Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O	10.1038/s41467-023-40064-9
	360	3842	None	44	Human	Binding	pAC50	=	5.5	5.5	-	11	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	325	7	1	2	5.3	Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O	10.1038/s41467-023-40064-9
	443879	3842	None	44	Human	Binding	pAC50	=	5.5	5.5	-	11	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	325	7	1	2	5.3	Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O	10.1038/s41467-023-40064-9
	443879.0	3842	None	44	Human	Binding	pAC50	=	5.5	5.5	-	11	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	325	7	1	2	5.3	Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O	10.1038/s41467-023-40064-9
	CHEMBL1382	3842	None	44	Human	Binding	pAC50	=	5.5	5.5	-	11	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	325	7	1	2	5.3	Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O	10.1038/s41467-023-40064-9
	DB01036	3842	None	44	Human	Binding	pAC50	=	5.5	5.5	-	11	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	325	7	1	2	5.3	Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O	10.1038/s41467-023-40064-9
	2520	206466	None	47	Human	Binding	pAC50	=	5.5	5.5	-20	11	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	10.1038/s41467-023-40064-9
	CHEMBL1280	206466	None	47	Human	Binding	pAC50	=	5.5	5.5	-20	11	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	10.1038/s41467-023-40064-9
	CHEMBL6966	206466	None	47	Human	Binding	pAC50	=	5.5	5.5	-20	11	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	454	13	0	6	5.1	COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC	10.1038/s41467-023-40064-9
	2771	197264	None	50	Human	Binding	pAC50	=	6.5	6.5	-	26	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	324	5	0	3	3.8	CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21	10.1038/s41467-023-40064-9
	CHEMBL1200781	197264	None	50	Human	Binding	pAC50	=	6.5	6.5	-	26	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	324	5	0	3	3.8	CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21	10.1038/s41467-023-40064-9
	CHEMBL549	197264	None	50	Human	Binding	pAC50	=	6.5	6.5	-	26	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	324	5	0	3	3.8	CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21	10.1038/s41467-023-40064-9
	2105	3054	None	28	Human	Binding	pAC50	=	5.4	5.4	-	33	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	314	4	1	2	4.3	CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3	10.1038/s41467-023-40064-9
	47811	3054	None	28	Human	Binding	pAC50	=	5.4	5.4	-	33	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	314	4	1	2	4.3	CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3	10.1038/s41467-023-40064-9
	48	3054	None	28	Human	Binding	pAC50	=	5.4	5.4	-	33	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	314	4	1	2	4.3	CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3	10.1038/s41467-023-40064-9
	CHEMBL531	3054	None	28	Human	Binding	pAC50	=	5.4	5.4	-	33	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	314	4	1	2	4.3	CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3	10.1038/s41467-023-40064-9
	DB01186	3054	None	28	Human	Binding	pAC50	=	5.4	5.4	-	33	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	314	4	1	2	4.3	CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3	10.1038/s41467-023-40064-9
	119570	3159	None	58	Human	Binding	pAC50	=	5.4	5.4	-281	40	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1038/s41467-023-40064-9
	119570.0	3159	None	58	Human	Binding	pAC50	=	5.4	5.4	-281	40	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1038/s41467-023-40064-9
	2233	3159	None	58	Human	Binding	pAC50	=	5.4	5.4	-281	40	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1038/s41467-023-40064-9
	953	3159	None	58	Human	Binding	pAC50	=	5.4	5.4	-281	40	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1038/s41467-023-40064-9
	CHEMBL301265	3159	None	58	Human	Binding	pAC50	=	5.4	5.4	-281	40	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1038/s41467-023-40064-9
	DB00413	3159	None	58	Human	Binding	pAC50	=	5.4	5.4	-281	40	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	211	3	2	4	1.6	CCCN[C@H]1CCc2c(C1)sc(n2)N	10.1038/s41467-023-40064-9
	5411	206491	None	57	Human	Binding	pAC50	=	5.4	5.4	-	2	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	264	8	1	4	2.6	CCCCNc1ccc(C(=O)OCCN(C)C)cc1	10.1038/s41467-023-40064-9
	CHEMBL698	206491	None	57	Human	Binding	pAC50	=	5.4	5.4	-	2	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	264	8	1	4	2.6	CCCCNc1ccc(C(=O)OCCN(C)C)cc1	10.1038/s41467-023-40064-9
	2337	3256	None	51	Human	Binding	pAC50	=	6.4	6.4	-1122	62	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	10.1038/s41467-023-40064-9
	50	3256	None	51	Human	Binding	pAC50	=	6.4	6.4	-1122	62	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	10.1038/s41467-023-40064-9
	5002	3256	None	51	Human	Binding	pAC50	=	6.4	6.4	-1122	62	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	10.1038/s41467-023-40064-9
	5002.0	3256	None	51	Human	Binding	pAC50	=	6.4	6.4	-1122	62	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	10.1038/s41467-023-40064-9
	CHEMBL716	3256	None	51	Human	Binding	pAC50	=	6.4	6.4	-1122	62	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	10.1038/s41467-023-40064-9
	DB01224	3256	None	51	Human	Binding	pAC50	=	6.4	6.4	-1122	62	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	383	5	1	6	2.9	OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2	10.1038/s41467-023-40064-9
	2247	505	None	55	Human	Binding	pAC50	=	6.4	6.4	-56	41	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	249	505	None	55	Human	Binding	pAC50	=	6.4	6.4	-56	41	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	2603	505	None	55	Human	Binding	pAC50	=	6.4	6.4	-56	41	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	CHEMBL296419	505	None	55	Human	Binding	pAC50	=	6.4	6.4	-56	41	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	DB00637	505	None	55	Human	Binding	pAC50	=	6.4	6.4	-56	41	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	458	8	1	5	5.4	COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2	10.1038/s41467-023-40064-9
	43815	187026	None	38	Human	Binding	pAC50	=	5.4	5.4	-	24	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	329	4	1	4	3.3	Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1	10.1038/s41467-023-40064-9
	CHEMBL1708	187026	None	38	Human	Binding	pAC50	=	5.4	5.4	-	24	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	329	4	1	4	3.3	Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1	10.1038/s41467-023-40064-9
	CHEMBL490	187026	None	38	Human	Binding	pAC50	=	5.4	5.4	-	24	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	329	4	1	4	3.3	Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1	10.1038/s41467-023-40064-9
	1210	918	None	42	Human	Binding	pAC50	=	6.4	6.4	-446	20	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	1213	918	None	42	Human	Binding	pAC50	=	6.4	6.4	-446	20	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	2725	918	None	42	Human	Binding	pAC50	=	6.4	6.4	-446	20	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	33036	918	None	42	Human	Binding	pAC50	=	6.4	6.4	-446	20	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	33036.0	918	None	42	Human	Binding	pAC50	=	6.4	6.4	-446	20	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	4411	918	None	42	Human	Binding	pAC50	=	6.4	6.4	-446	20	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	616	918	None	42	Human	Binding	pAC50	=	6.4	6.4	-446	20	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	6976	918	None	42	Human	Binding	pAC50	=	6.4	6.4	-446	20	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	716121	918	None	42	Human	Binding	pAC50	=	6.4	6.4	-446	20	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	CHEMBL1201353	918	None	42	Human	Binding	pAC50	=	6.4	6.4	-446	20	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	CHEMBL1554789	918	None	42	Human	Binding	pAC50	=	6.4	6.4	-446	20	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	CHEMBL505	918	None	42	Human	Binding	pAC50	=	6.4	6.4	-446	20	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	DB01114	918	None	42	Human	Binding	pAC50	=	6.4	6.4	-446	20	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	DB13679	918	None	42	Human	Binding	pAC50	=	6.4	6.4	-446	20	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	10.1038/s41467-023-40064-9
	11626560	203394	None	56	Human	Binding	pAC50	=	5.4	5.4	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	449	5	2	6	5.0	C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl	10.1038/s41467-023-40064-9
	CHEMBL601719	203394	None	56	Human	Binding	pAC50	=	5.4	5.4	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	449	5	2	6	5.0	C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl	10.1038/s41467-023-40064-9
	135398745	2914	None	65	Human	Binding	pAC50	=	6.4	6.4	-9	65	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	10.1038/s41467-023-40064-9
	135398745.0	2914	None	65	Human	Binding	pAC50	=	6.4	6.4	-9	65	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	10.1038/s41467-023-40064-9
	47	2914	None	65	Human	Binding	pAC50	=	6.4	6.4	-9	65	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	10.1038/s41467-023-40064-9
	CHEMBL715	2914	None	65	Human	Binding	pAC50	=	6.4	6.4	-9	65	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	10.1038/s41467-023-40064-9
	DB00334	2914	None	65	Human	Binding	pAC50	=	6.4	6.4	-9	65	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	312	1	1	5	1.7	CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C	10.1038/s41467-023-40064-9
	2389	3331	None	72	Human	Binding	pAC50	=	7.3	7.3	-281	67	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1038/s41467-023-40064-9
	5073	3331	None	72	Human	Binding	pAC50	=	7.3	7.3	-281	67	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1038/s41467-023-40064-9
	5073.0	3331	None	72	Human	Binding	pAC50	=	7.3	7.3	-281	67	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1038/s41467-023-40064-9
	96	3331	None	72	Human	Binding	pAC50	=	7.3	7.3	-281	67	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1038/s41467-023-40064-9
	CHEMBL85	3331	None	72	Human	Binding	pAC50	=	7.3	7.3	-281	67	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1038/s41467-023-40064-9
	DB00734	3331	None	72	Human	Binding	pAC50	=	7.3	7.3	-281	67	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	410	4	0	6	3.6	Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2	10.1038/s41467-023-40064-9
	214	3860	None	43	Human	Binding	pAC50	=	6.3	6.3	-	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	2740	3860	None	43	Human	Binding	pAC50	=	6.3	6.3	-	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	5566	3860	None	43	Human	Binding	pAC50	=	6.3	6.3	-	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	5566.0	3860	None	43	Human	Binding	pAC50	=	6.3	6.3	-	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	66064	3860	None	43	Human	Binding	pAC50	=	6.3	6.3	-	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	CHEMBL422	3860	None	43	Human	Binding	pAC50	=	6.3	6.3	-	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	DB00831	3860	None	43	Human	Binding	pAC50	=	6.3	6.3	-	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	407	4	0	4	4.9	CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F	10.1038/s41467-023-40064-9
	2018	3007	None	26	Human	Binding	pAC50	=	5.3	5.3	-	4	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL		None	None	None		None	10.1038/s41467-023-40064-9
	9941444	3007	None	26	Human	Binding	pAC50	=	5.3	5.3	-	4	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL		None	None	None		None	10.1038/s41467-023-40064-9
	CHEMBL3349607	3007	None	26	Human	Binding	pAC50	=	5.3	5.3	-	4	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL		None	None	None		None	10.1038/s41467-023-40064-9
	DB06663	3007	None	26	Human	Binding	pAC50	=	5.3	5.3	-	4	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL		None	None	None		None	10.1038/s41467-023-40064-9
	135398737	958	None	57	Human	Binding	pAC50	=	7.3	7.3	-64	91	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	10.1038/s41467-023-40064-9
	135398737.0	958	None	57	Human	Binding	pAC50	=	7.3	7.3	-64	91	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	10.1038/s41467-023-40064-9
	38	958	None	57	Human	Binding	pAC50	=	7.3	7.3	-64	91	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	10.1038/s41467-023-40064-9
	722	958	None	57	Human	Binding	pAC50	=	7.3	7.3	-64	91	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	10.1038/s41467-023-40064-9
	CHEMBL42	958	None	57	Human	Binding	pAC50	=	7.3	7.3	-64	91	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	10.1038/s41467-023-40064-9
	DB00363	958	None	57	Human	Binding	pAC50	=	7.3	7.3	-64	91	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	326	0	1	4	3.7	CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2	10.1038/s41467-023-40064-9
	10100	15300	None	4	Human	Binding	pAC50	=	5.3	5.3	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	339	8	0	3	4.3	CCC(=O)O[C@](Cc1ccccc1)(c1ccccc1)[C@H](C)CN(C)C	10.1038/s41467-023-40064-9
	CHEMBL1213351	15300	None	4	Human	Binding	pAC50	=	5.3	5.3	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	339	8	0	3	4.3	CCC(=O)O[C@](Cc1ccccc1)(c1ccccc1)[C@H](C)CN(C)C	10.1038/s41467-023-40064-9
	3158	56283	None	21	Human	Binding	pAC50	=	7.3	7.3	-12589	20	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	279	3	0	2	4.0	CN(C)CCC=C1c2ccccc2COc2ccccc21	10.1038/s41467-023-40064-9
	3158.0	56283	None	21	Human	Binding	pAC50	=	7.3	7.3	-12589	20	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	279	3	0	2	4.0	CN(C)CCC=C1c2ccccc2COc2ccccc21	10.1038/s41467-023-40064-9
	CHEMBL1628227	56283	None	21	Human	Binding	pAC50	=	7.3	7.3	-12589	20	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	279	3	0	2	4.0	CN(C)CCC=C1c2ccccc2COc2ccccc21	10.1038/s41467-023-40064-9
	DB01142	56283	None	21	Human	Binding	pAC50	=	7.3	7.3	-12589	20	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	279	3	0	2	4.0	CN(C)CCC=C1c2ccccc2COc2ccccc21	10.1038/s41467-023-40064-9
	2286	3183	None	36	Human	Binding	pAC50	=	7.3	7.3	-36	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
	4927	3183	None	36	Human	Binding	pAC50	=	7.3	7.3	-36	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
	4927.0	3183	None	36	Human	Binding	pAC50	=	7.3	7.3	-36	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
	7282	3183	None	36	Human	Binding	pAC50	=	7.3	7.3	-36	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
	CHEMBL643	3183	None	36	Human	Binding	pAC50	=	7.3	7.3	-36	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
	DB01069	3183	None	36	Human	Binding	pAC50	=	7.3	7.3	-36	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	284	3	0	3	4.2	CN(C(CN1c2ccccc2Sc2c1cccc2)C)C	10.1038/s41467-023-40064-9
	135	2532	None	33	Human	Binding	pAC50	=	7.3	7.3	-39	57	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	10.1038/s41467-023-40064-9
	1796	2532	None	33	Human	Binding	pAC50	=	7.3	7.3	-39	57	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	10.1038/s41467-023-40064-9
	4184	2532	None	33	Human	Binding	pAC50	=	7.3	7.3	-39	57	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	10.1038/s41467-023-40064-9
	4184.0	2532	None	33	Human	Binding	pAC50	=	7.3	7.3	-39	57	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	10.1038/s41467-023-40064-9
	CHEMBL6437	2532	None	33	Human	Binding	pAC50	=	7.3	7.3	-39	57	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	10.1038/s41467-023-40064-9
	DB06148	2532	None	33	Human	Binding	pAC50	=	7.3	7.3	-39	57	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	264	0	0	2	3.1	CN1CCN2C(C1)c1ccccc1Cc1c2cccc1	10.1038/s41467-023-40064-9
	2865	4143	None	47	Human	Binding	pAC50	=	6.2	6.2	-281	53	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	10.1038/s41467-023-40064-9
	59	4143	None	47	Human	Binding	pAC50	=	6.2	6.2	-281	53	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	10.1038/s41467-023-40064-9
	60854	4143	None	47	Human	Binding	pAC50	=	6.2	6.2	-281	53	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	10.1038/s41467-023-40064-9
	60854.0	4143	None	47	Human	Binding	pAC50	=	6.2	6.2	-281	53	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	10.1038/s41467-023-40064-9
	CHEMBL708	4143	None	47	Human	Binding	pAC50	=	6.2	6.2	-281	53	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	10.1038/s41467-023-40064-9
	DB00246	4143	None	47	Human	Binding	pAC50	=	6.2	6.2	-281	53	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	412	4	1	5	3.8	O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2	10.1038/s41467-023-40064-9
	1129	1621	None	68	Human	Binding	pAC50	=	8.2	8.2	-1	2	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	10.1038/s41467-023-40064-9
	3325	1621	None	68	Human	Binding	pAC50	=	8.2	8.2	-1	2	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	10.1038/s41467-023-40064-9
	5353622	1621	None	68	Human	Binding	pAC50	=	8.2	8.2	-1	2	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	10.1038/s41467-023-40064-9
	5702160	1621	None	68	Human	Binding	pAC50	=	8.2	8.2	-1	2	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	10.1038/s41467-023-40064-9
	7074	1621	None	68	Human	Binding	pAC50	=	8.2	8.2	-1	2	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	10.1038/s41467-023-40064-9
	CHEMBL902	1621	None	68	Human	Binding	pAC50	=	8.2	8.2	-1	2	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	10.1038/s41467-023-40064-9
	DB00927	1621	None	68	Human	Binding	pAC50	=	8.2	8.2	-1	2	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	337	7	4	6	-0.8	NC(=Nc1scc(n1)CSCC/C(=N/S(=O)(=O)N)/N)N	10.1038/s41467-023-40064-9
	319	1324	None	32	Human	Binding	pAC50	=	6.2	6.2	-	9	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	426	7	1	3	4.0	NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2	10.1038/s41467-023-40064-9
	321	1324	None	32	Human	Binding	pAC50	=	6.2	6.2	-	9	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	426	7	1	3	4.0	NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2	10.1038/s41467-023-40064-9
	444031	1324	None	32	Human	Binding	pAC50	=	6.2	6.2	-	9	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	426	7	1	3	4.0	NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2	10.1038/s41467-023-40064-9
	444031.0	1324	None	32	Human	Binding	pAC50	=	6.2	6.2	-	9	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	426	7	1	3	4.0	NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2	10.1038/s41467-023-40064-9
	784	1324	None	32	Human	Binding	pAC50	=	6.2	6.2	-	9	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	426	7	1	3	4.0	NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2	10.1038/s41467-023-40064-9
	CHEMBL1346	1324	None	32	Human	Binding	pAC50	=	6.2	6.2	-	9	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	426	7	1	3	4.0	NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2	10.1038/s41467-023-40064-9
	DB00496	1324	None	32	Human	Binding	pAC50	=	6.2	6.2	-	9	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	426	7	1	3	4.0	NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2	10.1038/s41467-023-40064-9
	2132	46238	None	57	Human	Binding	pAC50	=	5.2	5.2	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	376	3	3	3	3.2	Nc1c(Br)cc(Br)cc1CN[C@H]1CC[C@H](O)CC1	10.1038/s41467-023-40064-9
	CHEMBL1514634	46238	None	57	Human	Binding	pAC50	=	5.2	5.2	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	376	3	3	3	3.2	Nc1c(Br)cc(Br)cc1CN[C@H]1CC[C@H](O)CC1	10.1038/s41467-023-40064-9
	CHEMBL153479	46238	None	57	Human	Binding	pAC50	=	5.2	5.2	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	376	3	3	3	3.2	Nc1c(Br)cc(Br)cc1CN[C@H]1CC[C@H](O)CC1	10.1038/s41467-023-40064-9
	16362	3125	None	49	Human	Binding	pAC50	=	6.2	6.2	-	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	16362.0	3125	None	49	Human	Binding	pAC50	=	6.2	6.2	-	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	2172	3125	None	49	Human	Binding	pAC50	=	6.2	6.2	-	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	90	3125	None	49	Human	Binding	pAC50	=	6.2	6.2	-	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	CHEMBL1423	3125	None	49	Human	Binding	pAC50	=	6.2	6.2	-	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	DB01100	3125	None	49	Human	Binding	pAC50	=	6.2	6.2	-	29	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	461	7	1	3	5.9	Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2	10.1038/s41467-023-40064-9
	1427	2013	None	42	Human	Binding	pAC50	=	7.2	7.2	-	26	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	357	2013	None	42	Human	Binding	pAC50	=	7.2	7.2	-	26	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	3696	2013	None	42	Human	Binding	pAC50	=	7.2	7.2	-	26	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	CHEMBL11	2013	None	42	Human	Binding	pAC50	=	7.2	7.2	-	26	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	DB00458	2013	None	42	Human	Binding	pAC50	=	7.2	7.2	-	26	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	280	4	0	2	3.9	CN(CCCN1c2ccccc2CCc2c1cccc2)C	10.1038/s41467-023-40064-9
	1605	2342	None	72	Human	Binding	pAC50	=	6.2	6.2	-	4	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	382	1	0	3	4.9	CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	10.1038/s41467-023-40064-9
	3957	2342	None	72	Human	Binding	pAC50	=	6.2	6.2	-	4	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	382	1	0	3	4.9	CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	10.1038/s41467-023-40064-9
	3957.0	2342	None	72	Human	Binding	pAC50	=	6.2	6.2	-	4	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	382	1	0	3	4.9	CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	10.1038/s41467-023-40064-9
	7216	2342	None	72	Human	Binding	pAC50	=	6.2	6.2	-	4	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	382	1	0	3	4.9	CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	10.1038/s41467-023-40064-9
	CHEMBL998	2342	None	72	Human	Binding	pAC50	=	6.2	6.2	-	4	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	382	1	0	3	4.9	CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	10.1038/s41467-023-40064-9
	DB00455	2342	None	72	Human	Binding	pAC50	=	6.2	6.2	-	4	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	382	1	0	3	4.9	CCOC(=O)N1CCC(=C2c3ccc(cc3CCc3c2nccc3)Cl)CC1	10.1038/s41467-023-40064-9
	21722	17999	None	26	Human	Binding	pAC50	=	6.2	6.2	-	5	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	284	4	0	2	4.3	CN(C)CCCn1c2c(c3ccccc31)CCCCCC2	10.1038/s41467-023-40064-9
	CHEMBL126224	17999	None	26	Human	Binding	pAC50	=	6.2	6.2	-	5	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	284	4	0	2	4.3	CN(C)CCCn1c2c(c3ccccc31)CCCCCC2	10.1038/s41467-023-40064-9
	16129706	211490	None	36	Human	Binding	pAC50	=	5.1	5.1	-	5	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL		None	None	None		C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O	10.1038/s41467-023-40064-9
	CHEMBL1823872	211490	None	36	Human	Binding	pAC50	=	5.1	5.1	-	5	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL		None	None	None		C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O	10.1038/s41467-023-40064-9
	3883	183641	None	69	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	369	5	1	4	3.5	Cc1c(OCC(F)(F)F)ccnc1C[S+]([O-])c1nc2ccccc2[nH]1	10.1038/s41467-023-40064-9
	CHEMBL480	183641	None	69	Human	Binding	pAC50	=	5.1	5.1	-	0	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	369	5	1	4	3.5	Cc1c(OCC(F)(F)F)ccnc1C[S+]([O-])c1nc2ccccc2[nH]1	10.1038/s41467-023-40064-9
	2351	3286	None	44	Human	Binding	pAC50	=	5.1	5.1	-	21	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	473	7	2	6	6.1	Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O	10.1038/s41467-023-40064-9
	2820	3286	None	44	Human	Binding	pAC50	=	5.1	5.1	-	21	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	473	7	2	6	6.1	Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O	10.1038/s41467-023-40064-9
	5035	3286	None	44	Human	Binding	pAC50	=	5.1	5.1	-	21	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	473	7	2	6	6.1	Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O	10.1038/s41467-023-40064-9
	CHEMBL81	3286	None	44	Human	Binding	pAC50	=	5.1	5.1	-	21	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	473	7	2	6	6.1	Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O	10.1038/s41467-023-40064-9
	DB00481	3286	None	44	Human	Binding	pAC50	=	5.1	5.1	-	21	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	473	7	2	6	6.1	Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O	10.1038/s41467-023-40064-9
	2162	41527	None	58	Human	Binding	pAC50	=	5.0	5.0	-	6	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	408	8	2	7	2.3	CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl	10.1038/s41467-023-40064-9
	CHEMBL1491	41527	None	58	Human	Binding	pAC50	=	5.0	5.0	-	6	Binding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtrationBinding affinity towards human HRH2 in an in vitro assay with cellular components measured by membrane filtration	ChEMBL	408	8	2	7	2.3	CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl	10.1038/s41467-023-40064-9
	25149708	188543	None	0	Human	Binding	pEC50	=	7.0	7.0	-	0	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	188543	None	0	Human	Binding	pEC50	=	7.0	7.0	-	0	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	179206	None	0	Human	Binding	pEC50	=	7.0	7.0	-	1	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	179206	None	0	Human	Binding	pEC50	=	7.0	7.0	-	1	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	179306	None	0	Human	Binding	pEC50	=	6.9	6.9	-	1	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	179306	None	0	Human	Binding	pEC50	=	6.9	6.9	-	1	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	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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
	774.0	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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
	774.0	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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
	774.0	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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	1932	None	74	Human	Binding	pEC50	=	5.9	5.9	-173	24	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	7318	None	0	Human	Binding	pEC50	=	6.9	6.9	-	2	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	7318	None	0	Human	Binding	pEC50	=	6.9	6.9	-	2	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	178458	None	0	Human	Binding	pEC50	=	6.9	6.9	-	1	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	178458	None	0	Human	Binding	pEC50	=	6.9	6.9	-	1	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	109527	None	0	Human	Binding	pEC50	=	6.6	6.6	-	1	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	109527	None	0	Human	Binding	pEC50	=	6.6	6.6	-	1	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	26112	None	4	Human	Binding	pEC50	=	5.6	5.6	-	2	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	26112	None	4	Human	Binding	pEC50	=	5.6	5.6	-	2	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	110631	None	3	Human	Binding	pEC50	=	5.6	5.6	-	0	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	110631	None	3	Human	Binding	pEC50	=	5.6	5.6	-	0	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	179875	None	0	Human	Binding	pEC50	=	6.5	6.5	-	0	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	179875	None	0	Human	Binding	pEC50	=	6.5	6.5	-	0	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	180870	None	0	Human	Binding	pEC50	=	7.5	7.5	-	1	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	180870	None	0	Human	Binding	pEC50	=	7.5	7.5	-	1	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	180031	None	0	Human	Binding	pEC50	=	6.5	6.5	-	1	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	180031	None	0	Human	Binding	pEC50	=	6.5	6.5	-	1	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	179874	None	0	Human	Binding	pEC50	=	7.4	7.4	-	1	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	179874	None	0	Human	Binding	pEC50	=	7.4	7.4	-	1	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	180872	None	0	Human	Binding	pEC50	=	6.4	6.4	-	1	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	180872	None	0	Human	Binding	pEC50	=	6.4	6.4	-	1	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	109530	None	0	Human	Binding	pEC50	=	6.4	6.4	-	1	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	109530	None	0	Human	Binding	pEC50	=	6.4	6.4	-	1	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	1932	None	74	Human	Binding	pEC50	=	6.3	6.3	-173	24	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	1932	None	74	Human	Binding	pEC50	=	6.3	6.3	-173	24	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	1932	None	74	Human	Binding	pEC50	=	6.3	6.3	-173	24	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	1932	None	74	Human	Binding	pEC50	=	6.3	6.3	-173	24	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
	774.0	1932	None	74	Human	Binding	pEC50	=	6.3	6.3	-173	24	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	1932	None	74	Human	Binding	pEC50	=	6.3	6.3	-173	24	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	1932	None	74	Human	Binding	pEC50	=	6.3	6.3	-173	24	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	184331	None	0	Human	Binding	pEC50	=	7.2	7.2	-	1	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	184331	None	0	Human	Binding	pEC50	=	7.2	7.2	-	1	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	184331	None	0	Human	Binding	pEC50	=	7.2	7.2	-	1	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	184331	None	0	Human	Binding	pEC50	=	7.2	7.2	-	1	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	184331	None	0	Human	Binding	pEC50	=	7.2	7.2	-	1	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	184331	None	0	Human	Binding	pEC50	=	7.2	7.2	-	1	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	28903	None	2	Human	Binding	pEC50	=	6.2	6.2	-	2	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	28903	None	2	Human	Binding	pEC50	=	6.2	6.2	-	2	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	169876	None	0	Human	Binding	pEC50	=	6.1	6.1	-	1	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	169876	None	0	Human	Binding	pEC50	=	6.1	6.1	-	1	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	109529	None	0	Human	Binding	pEC50	=	6.1	6.1	-	1	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	109529	None	0	Human	Binding	pEC50	=	6.1	6.1	-	1	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	179158	None	0	Human	Binding	pEC50	=	7.1	7.1	-	1	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	179158	None	0	Human	Binding	pEC50	=	7.1	7.1	-	1	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	189697	None	0	Human	Binding	pEC50	=	7.1	7.1	-	1	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	189697	None	0	Human	Binding	pEC50	=	7.1	7.1	-	1	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	189803	None	0	Human	Binding	pEC50	=	7.1	7.1	-	0	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	189803	None	0	Human	Binding	pEC50	=	7.1	7.1	-	0	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	109536	None	0	Human	Binding	pEC50	=	6.1	6.1	-	0	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	109536	None	0	Human	Binding	pEC50	=	6.1	6.1	-	0	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	163334	None	2	Human	Binding	pEC50	=	7.0	7.0	-	1	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	163334	None	2	Human	Binding	pEC50	=	7.0	7.0	-	1	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	179876	None	0	Human	Binding	pEC50	=	6.0	6.0	-	0	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	179876	None	0	Human	Binding	pEC50	=	6.0	6.0	-	0	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	70585	None	0	Human	Binding	pIC50	=	9.1	9.1	-	0	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	70585	None	0	Human	Binding	pIC50	=	9.1	9.1	-	0	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	158187	None	0	Human	Binding	pIC50	=	6	6.0	-	0	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	158187	None	0	Human	Binding	pIC50	=	6	6.0	-	0	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	937	None	69	Human	Binding	pIC50	=	6	6.0	-4	8	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	937	None	69	Human	Binding	pIC50	=	6	6.0	-4	8	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
	2756.0	937	None	69	Human	Binding	pIC50	=	6	6.0	-4	8	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	937	None	69	Human	Binding	pIC50	=	6	6.0	-4	8	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	937	None	69	Human	Binding	pIC50	=	6	6.0	-4	8	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	937	None	69	Human	Binding	pIC50	=	6	6.0	-4	8	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	937	None	69	Human	Binding	pIC50	=	6	6.0	-4	8	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	937	None	69	Human	Binding	pIC50	=	6	6.0	-4	8	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
	2756.0	937	None	69	Human	Binding	pIC50	=	6	6.0	-4	8	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	937	None	69	Human	Binding	pIC50	=	6	6.0	-4	8	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	937	None	69	Human	Binding	pIC50	=	6	6.0	-4	8	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	937	None	69	Human	Binding	pIC50	=	6	6.0	-4	8	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	61349	None	13	Human	Binding	pIC50	=	5	5.0	-	4	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	61349	None	13	Human	Binding	pIC50	=	5	5.0	-	4	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	66713	None	0	Human	Binding	pIC50	=	5	5.0	-	0	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	66713	None	0	Human	Binding	pIC50	=	5	5.0	-	0	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	136969	None	0	Human	Binding	pIC50	=	5	5.0	-	0	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	136969	None	0	Human	Binding	pIC50	=	5	5.0	-	0	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	142070	None	0	Human	Binding	pIC50	=	5	5.0	-	0	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	142070	None	0	Human	Binding	pIC50	=	5	5.0	-	0	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	210370	None	0	Rat	Binding	pIC50	=	4	4.0	-	0	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	210370	None	0	Rat	Binding	pIC50	=	4	4.0	-	0	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	218407	None	0	Rat	Binding	pIC50	=	4	4.0	-	0	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	2532	None	33	Human	Binding	pIC50	=	6	6.0	-39	57	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	2532	None	33	Human	Binding	pIC50	=	6	6.0	-39	57	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	2532	None	33	Human	Binding	pIC50	=	6	6.0	-39	57	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
	4184.0	2532	None	33	Human	Binding	pIC50	=	6	6.0	-39	57	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	2532	None	33	Human	Binding	pIC50	=	6	6.0	-39	57	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	2532	None	33	Human	Binding	pIC50	=	6	6.0	-39	57	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	137051	None	0	Human	Binding	pIC50	=	6.0	6.0	-	0	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	137051	None	0	Human	Binding	pIC50	=	6.0	6.0	-	0	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	111079	None	0	Human	Binding	pIC50	=	6.0	6.0	-	0	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	111079	None	0	Human	Binding	pIC50	=	6.0	6.0	-	0	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	2325	None	21	Human	Binding	pIC50	=	6.0	6.0	-223	43	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	2325	None	21	Human	Binding	pIC50	=	6.0	6.0	-223	43	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
	28864.0	2325	None	21	Human	Binding	pIC50	=	6.0	6.0	-223	43	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	2325	None	21	Human	Binding	pIC50	=	6.0	6.0	-223	43	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	2325	None	21	Human	Binding	pIC50	=	6.0	6.0	-223	43	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	2325	None	21	Human	Binding	pIC50	=	6.0	6.0	-223	43	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	398	None	47	Human	Binding	pIC50	=	5.0	5.0	-6	31	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	398	None	47	Human	Binding	pIC50	=	5.0	5.0	-6	31	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
	2157.0	398	None	47	Human	Binding	pIC50	=	5.0	5.0	-6	31	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	398	None	47	Human	Binding	pIC50	=	5.0	5.0	-6	31	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	398	None	47	Human	Binding	pIC50	=	5.0	5.0	-6	31	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	398	None	47	Human	Binding	pIC50	=	5.0	5.0	-6	31	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
	5354	155746	None	16	Human	Binding	pIC50	=	7.0	7.0	3	14	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	12	2	3	5.6	CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1	nan
	CHEMBL404849	155746	None	16	Human	Binding	pIC50	=	7.0	7.0	3	14	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	337	12	2	3	5.6	CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1	nan
	124087	1389	None	72	Human	Binding	pIC50	=	6.0	6.0	-29	15	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
	124087.0	1389	None	72	Human	Binding	pIC50	=	6.0	6.0	-29	15	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	1389	None	72	Human	Binding	pIC50	=	6.0	6.0	-29	15	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	1389	None	72	Human	Binding	pIC50	=	6.0	6.0	-29	15	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	1389	None	72	Human	Binding	pIC50	=	6.0	6.0	-29	15	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	1389	None	72	Human	Binding	pIC50	=	6.0	6.0	-29	15	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	176253	None	16	Human	Binding	pIC50	=	5.9	5.9	-2	20	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	176253	None	16	Human	Binding	pIC50	=	5.9	5.9	-2	20	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	176253	None	16	Human	Binding	pIC50	=	5.9	5.9	-2	20	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	176253	None	16	Human	Binding	pIC50	=	5.9	5.9	-2	20	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	3183	None	36	Human	Binding	pIC50	=	5.9	5.9	-36	29	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	3183	None	36	Human	Binding	pIC50	=	5.9	5.9	-36	29	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
	4927.0	3183	None	36	Human	Binding	pIC50	=	5.9	5.9	-36	29	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	3183	None	36	Human	Binding	pIC50	=	5.9	5.9	-36	29	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	3183	None	36	Human	Binding	pIC50	=	5.9	5.9	-36	29	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	3183	None	36	Human	Binding	pIC50	=	5.9	5.9	-36	29	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	1911	None	63	Human	Binding	pIC50	=	5.9	5.9	-131	85	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	1911	None	63	Human	Binding	pIC50	=	5.9	5.9	-131	85	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
	3559.0	1911	None	63	Human	Binding	pIC50	=	5.9	5.9	-131	85	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	1911	None	63	Human	Binding	pIC50	=	5.9	5.9	-131	85	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	1911	None	63	Human	Binding	pIC50	=	5.9	5.9	-131	85	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	1911	None	63	Human	Binding	pIC50	=	5.9	5.9	-131	85	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	141699	None	0	Human	Binding	pIC50	=	5.9	5.9	-	0	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	141699	None	0	Human	Binding	pIC50	=	5.9	5.9	-	0	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	597	None	17	Human	Binding	pIC50	=	5.9	5.9	-74	20	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
	1201549.0	597	None	17	Human	Binding	pIC50	=	5.9	5.9	-74	20	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	597	None	17	Human	Binding	pIC50	=	5.9	5.9	-74	20	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	597	None	17	Human	Binding	pIC50	=	5.9	5.9	-74	20	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	597	None	17	Human	Binding	pIC50	=	5.9	5.9	-74	20	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	597	None	17	Human	Binding	pIC50	=	5.9	5.9	-74	20	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	597	None	17	Human	Binding	pIC50	=	5.9	5.9	-74	20	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	1662	None	37	Human	Binding	pIC50	=	5.9	5.9	-323	65	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	1662	None	37	Human	Binding	pIC50	=	5.9	5.9	-323	65	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	1662	None	37	Human	Binding	pIC50	=	5.9	5.9	-323	65	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
	3372.0	1662	None	37	Human	Binding	pIC50	=	5.9	5.9	-323	65	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	1662	None	37	Human	Binding	pIC50	=	5.9	5.9	-323	65	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	1662	None	37	Human	Binding	pIC50	=	5.9	5.9	-323	65	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	84795	None	0	Human	Binding	pIC50	=	6.9	6.9	-	0	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	84795	None	0	Human	Binding	pIC50	=	6.9	6.9	-	0	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	110656	None	0	Human	Binding	pIC50	=	5.9	5.9	-	0	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	110656	None	0	Human	Binding	pIC50	=	5.9	5.9	-	0	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	84676	None	0	Human	Binding	pIC50	=	5.9	5.9	-	0	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	84676	None	0	Human	Binding	pIC50	=	5.9	5.9	-	0	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	10510	None	0	Human	Binding	pIC50	=	5.9	5.9	-	0	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	10510	None	0	Human	Binding	pIC50	=	5.9	5.9	-	0	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	84597	None	0	Human	Binding	pIC50	=	5.9	5.9	-	0	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	84597	None	0	Human	Binding	pIC50	=	5.9	5.9	-	0	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	937	None	69	Human	Binding	pIC50	=	6.9	6.9	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.9	6.9	-4	8	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
	2756.0	937	None	69	Human	Binding	pIC50	=	6.9	6.9	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.9	6.9	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.9	6.9	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.9	6.9	-4	8	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	56360	None	12	Human	Binding	pIC50	=	4.9	4.9	-5	6	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	56360	None	12	Human	Binding	pIC50	=	4.9	4.9	-5	6	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	161661	None	0	Human	Binding	pIC50	=	6.9	6.9	-	0	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	161661	None	0	Human	Binding	pIC50	=	6.9	6.9	-	0	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	3331	None	72	Human	Binding	pIC50	=	5.8	5.8	-281	67	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	3331	None	72	Human	Binding	pIC50	=	5.8	5.8	-281	67	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
	5073.0	3331	None	72	Human	Binding	pIC50	=	5.8	5.8	-281	67	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	3331	None	72	Human	Binding	pIC50	=	5.8	5.8	-281	67	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	3331	None	72	Human	Binding	pIC50	=	5.8	5.8	-281	67	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	3331	None	72	Human	Binding	pIC50	=	5.8	5.8	-281	67	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	84674	None	0	Human	Binding	pIC50	=	5.8	5.8	-	0	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	84674	None	0	Human	Binding	pIC50	=	5.8	5.8	-	0	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	142069	None	0	Human	Binding	pIC50	=	5.8	5.8	-	0	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	142069	None	0	Human	Binding	pIC50	=	5.8	5.8	-	0	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	218412	None	0	Rat	Binding	pIC50	=	4.8	4.8	-	0	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	18873	None	78	Human	Binding	pIC50	=	5.8	5.8	-1	3	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	18873	None	78	Human	Binding	pIC50	=	5.8	5.8	-1	3	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	207971	None	50	Human	Binding	pIC50	=	5.8	5.8	-19	34	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	207971	None	50	Human	Binding	pIC50	=	5.8	5.8	-19	34	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	207971	None	50	Human	Binding	pIC50	=	5.8	5.8	-19	34	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	1414	None	26	Human	Binding	pIC50	=	5.8	5.8	-53	15	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
	3042.0	1414	None	26	Human	Binding	pIC50	=	5.8	5.8	-53	15	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	1414	None	26	Human	Binding	pIC50	=	5.8	5.8	-53	15	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	1414	None	26	Human	Binding	pIC50	=	5.8	5.8	-53	15	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	1414	None	26	Human	Binding	pIC50	=	5.8	5.8	-53	15	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	1414	None	26	Human	Binding	pIC50	=	5.8	5.8	-53	15	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	505	None	55	Human	Binding	pIC50	=	5.8	5.8	-56	41	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	505	None	55	Human	Binding	pIC50	=	5.8	5.8	-56	41	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	505	None	55	Human	Binding	pIC50	=	5.8	5.8	-56	41	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	505	None	55	Human	Binding	pIC50	=	5.8	5.8	-56	41	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	505	None	55	Human	Binding	pIC50	=	5.8	5.8	-56	41	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	123025	None	0	Human	Binding	pIC50	=	5.8	5.8	-	0	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	123025	None	0	Human	Binding	pIC50	=	5.8	5.8	-	0	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	937	None	69	Human	Binding	pIC50	=	6.8	6.8	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.8	6.8	-4	8	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
	2756.0	937	None	69	Human	Binding	pIC50	=	6.8	6.8	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.8	6.8	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.8	6.8	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.8	6.8	-4	8	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	123624	None	0	Human	Binding	pIC50	=	5.7	5.7	-	0	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	123624	None	0	Human	Binding	pIC50	=	5.7	5.7	-	0	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	56283	None	21	Human	Binding	pIC50	=	5.7	5.7	-12589	20	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
	3158.0	56283	None	21	Human	Binding	pIC50	=	5.7	5.7	-12589	20	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	56283	None	21	Human	Binding	pIC50	=	5.7	5.7	-12589	20	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
	DB01142	56283	None	21	Human	Binding	pIC50	=	5.7	5.7	-12589	20	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	136494	None	0	Human	Binding	pIC50	=	5.7	5.7	-	0	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	136494	None	0	Human	Binding	pIC50	=	5.7	5.7	-	0	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	209896	None	64	Human	Binding	pIC50	=	5.7	5.7	-1	2	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	209896	None	64	Human	Binding	pIC50	=	5.7	5.7	-1	2	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	1301	None	39	Human	Binding	pIC50	=	6.7	6.7	-43	49	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	1301	None	39	Human	Binding	pIC50	=	6.7	6.7	-43	49	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
	2913.0	1301	None	39	Human	Binding	pIC50	=	6.7	6.7	-43	49	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	1301	None	39	Human	Binding	pIC50	=	6.7	6.7	-43	49	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	1301	None	39	Human	Binding	pIC50	=	6.7	6.7	-43	49	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	1301	None	39	Human	Binding	pIC50	=	6.7	6.7	-43	49	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	11032	None	0	Human	Binding	pIC50	=	5.7	5.7	-	0	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	11032	None	0	Human	Binding	pIC50	=	5.7	5.7	-	0	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	213756	None	0	Rat	Binding	pIC50	=	4.7	4.7	-	0	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	218408	None	0	Rat	Binding	pIC50	=	4.7	4.7	-	0	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
	2398	954	None	43	Human	Binding	pIC50	=	5.7	5.7	-13	28	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
	2801	954	None	43	Human	Binding	pIC50	=	5.7	5.7	-13	28	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
	2801.0	954	None	43	Human	Binding	pIC50	=	5.7	5.7	-13	28	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
	701	954	None	43	Human	Binding	pIC50	=	5.7	5.7	-13	28	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
	CHEMBL415	954	None	43	Human	Binding	pIC50	=	5.7	5.7	-13	28	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
	DB01242	954	None	43	Human	Binding	pIC50	=	5.7	5.7	-13	28	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
	11430513	84665	None	0	Human	Binding	pIC50	=	5.7	5.7	-	0	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	84665	None	0	Human	Binding	pIC50	=	5.7	5.7	-	0	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	141726	None	0	Human	Binding	pIC50	=	5.7	5.7	-	0	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	141726	None	0	Human	Binding	pIC50	=	5.7	5.7	-	0	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	84368	None	0	Human	Binding	pIC50	=	5.7	5.7	-	0	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	84368	None	0	Human	Binding	pIC50	=	5.7	5.7	-	0	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	50235	None	31	Human	Binding	pIC50	=	4.7	4.7	-66	11	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	50235	None	31	Human	Binding	pIC50	=	4.7	4.7	-66	11	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	50235	None	31	Human	Binding	pIC50	=	4.7	4.7	-66	11	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	3823	None	29	Human	Binding	pIC50	=	7.7	7.7	-2	5	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	3823	None	29	Human	Binding	pIC50	=	7.7	7.7	-2	5	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	3823	None	29	Human	Binding	pIC50	=	7.7	7.7	-2	5	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	3823	None	29	Human	Binding	pIC50	=	7.7	7.7	-2	5	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	84335	None	0	Human	Binding	pIC50	=	6.7	6.7	-	0	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	84335	None	0	Human	Binding	pIC50	=	6.7	6.7	-	0	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
	1971	2866	None	32	Human	Binding	pIC50	=	5.6	5.6	-16	29	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
	2404	2866	None	32	Human	Binding	pIC50	=	5.6	5.6	-16	29	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
	4543	2866	None	32	Human	Binding	pIC50	=	5.6	5.6	-16	29	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
	4543.0	2866	None	32	Human	Binding	pIC50	=	5.6	5.6	-16	29	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
	CHEMBL445	2866	None	32	Human	Binding	pIC50	=	5.6	5.6	-16	29	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
	DB00540	2866	None	32	Human	Binding	pIC50	=	5.6	5.6	-16	29	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
	CHEMBL44345	216383	None	0	Rat	Binding	pIC50	=	4.6	4.6	-	0	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
	2281	3175	None	47	Rat	Binding	pIC50	=	2.6	2.6	-	0	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	3175	None	47	Rat	Binding	pIC50	=	2.6	2.6	-	0	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	3175	None	47	Rat	Binding	pIC50	=	2.6	2.6	-	0	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	3175	None	47	Rat	Binding	pIC50	=	2.6	2.6	-	0	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	3175	None	47	Rat	Binding	pIC50	=	2.6	2.6	-	0	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	206466	None	47	Human	Binding	pIC50	=	5.6	5.6	-20	11	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	206466	None	47	Human	Binding	pIC50	=	5.6	5.6	-20	11	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	206466	None	47	Human	Binding	pIC50	=	5.6	5.6	-20	11	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	84325	None	0	Human	Binding	pIC50	=	6.6	6.6	-	0	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	84325	None	0	Human	Binding	pIC50	=	6.6	6.6	-	0	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	919	None	48	Human	Binding	pIC50	=	5.6	5.6	-85	72	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
	2726.0	919	None	48	Human	Binding	pIC50	=	5.6	5.6	-85	72	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	919	None	48	Human	Binding	pIC50	=	5.6	5.6	-85	72	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	919	None	48	Human	Binding	pIC50	=	5.6	5.6	-85	72	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	919	None	48	Human	Binding	pIC50	=	5.6	5.6	-85	72	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	919	None	48	Human	Binding	pIC50	=	5.6	5.6	-85	72	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	179829	None	29	Human	Binding	pIC50	=	4.6	4.6	-	0	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	179829	None	29	Human	Binding	pIC50	=	4.6	4.6	-	0	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	937	None	69	Human	Binding	pIC50	=	6.6	6.6	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.6	6.6	-4	8	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
	2756.0	937	None	69	Human	Binding	pIC50	=	6.6	6.6	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.6	6.6	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.6	6.6	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.6	6.6	-4	8	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	206817	None	38	Human	Binding	pIC50	=	4.6	4.6	-	1	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	206817	None	38	Human	Binding	pIC50	=	4.6	4.6	-	1	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	206817	None	38	Human	Binding	pIC50	=	4.6	4.6	-	1	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	3182	None	26	Human	Binding	pIC50	=	5.5	5.5	-53	28	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	3182	None	26	Human	Binding	pIC50	=	5.5	5.5	-53	28	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	3182	None	26	Human	Binding	pIC50	=	5.5	5.5	-53	28	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	3182	None	26	Human	Binding	pIC50	=	5.5	5.5	-53	28	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	3182	None	26	Human	Binding	pIC50	=	5.5	5.5	-53	28	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	84384	None	0	Human	Binding	pIC50	=	5.5	5.5	-	0	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	84384	None	0	Human	Binding	pIC50	=	5.5	5.5	-	0	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	168897	None	0	Human	Binding	pIC50	=	5.5	5.5	-	0	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	168897	None	0	Human	Binding	pIC50	=	5.5	5.5	-	0	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	102913	None	65	Human	Binding	pIC50	=	5.5	5.5	-24	25	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
	3191.0	102913	None	65	Human	Binding	pIC50	=	5.5	5.5	-24	25	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	102913	None	65	Human	Binding	pIC50	=	5.5	5.5	-24	25	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
	DB11742	102913	None	65	Human	Binding	pIC50	=	5.5	5.5	-24	25	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	84652	None	0	Human	Binding	pIC50	=	5.5	5.5	-	0	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	84652	None	0	Human	Binding	pIC50	=	5.5	5.5	-	0	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	212270	None	0	Rat	Binding	pIC50	=	4.5	4.5	-	0	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	213004	None	0	Rat	Binding	pIC50	=	4.5	4.5	-	0	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	213330	None	0	Rat	Binding	pIC50	=	4.5	4.5	-	0	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	213671	None	0	Rat	Binding	pIC50	=	4.5	4.5	-	0	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	218394	None	0	Rat	Binding	pIC50	=	4.5	4.5	-	0	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	84787	None	0	Human	Binding	pIC50	=	5.5	5.5	-	0	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	84787	None	0	Human	Binding	pIC50	=	5.5	5.5	-	0	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	84385	None	0	Human	Binding	pIC50	=	5.5	5.5	-	0	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	84385	None	0	Human	Binding	pIC50	=	5.5	5.5	-	0	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	2341	None	28	Human	Binding	pIC50	=	5.5	5.5	-128	18	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	2341	None	28	Human	Binding	pIC50	=	5.5	5.5	-128	18	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
	3955.0	2341	None	28	Human	Binding	pIC50	=	5.5	5.5	-128	18	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	2341	None	28	Human	Binding	pIC50	=	5.5	5.5	-128	18	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	2341	None	28	Human	Binding	pIC50	=	5.5	5.5	-128	18	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	2341	None	28	Human	Binding	pIC50	=	5.5	5.5	-128	18	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	137192	None	0	Human	Binding	pIC50	=	5.5	5.5	-	0	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	137192	None	0	Human	Binding	pIC50	=	5.5	5.5	-	0	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	137961	None	0	Human	Binding	pIC50	=	5.5	5.5	-	0	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	137961	None	0	Human	Binding	pIC50	=	5.5	5.5	-	0	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	66087	None	0	Human	Binding	pIC50	=	5.5	5.5	-	0	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	66087	None	0	Human	Binding	pIC50	=	5.5	5.5	-	0	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	213785	None	0	Rat	Binding	pIC50	=	4.5	4.5	-	0	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	207323	None	37	Human	Binding	pIC50	=	5.5	5.5	-3	13	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	207323	None	37	Human	Binding	pIC50	=	5.5	5.5	-3	13	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	207323	None	37	Human	Binding	pIC50	=	5.5	5.5	-3	13	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	207323	None	37	Human	Binding	pIC50	=	5.5	5.5	-3	13	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	958	None	57	Human	Binding	pIC50	=	5.4	5.4	-64	91	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
	135398737.0	958	None	57	Human	Binding	pIC50	=	5.4	5.4	-64	91	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	958	None	57	Human	Binding	pIC50	=	5.4	5.4	-64	91	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	958	None	57	Human	Binding	pIC50	=	5.4	5.4	-64	91	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	958	None	57	Human	Binding	pIC50	=	5.4	5.4	-64	91	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	958	None	57	Human	Binding	pIC50	=	5.4	5.4	-64	91	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	10469	None	0	Human	Binding	pIC50	=	6.4	6.4	-	0	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	10469	None	0	Human	Binding	pIC50	=	6.4	6.4	-	0	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	949	None	27	Human	Binding	pIC50	=	6.4	6.4	-177	21	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
	26987.0	949	None	27	Human	Binding	pIC50	=	6.4	6.4	-177	21	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	949	None	27	Human	Binding	pIC50	=	6.4	6.4	-177	21	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	949	None	27	Human	Binding	pIC50	=	6.4	6.4	-177	21	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	949	None	27	Human	Binding	pIC50	=	6.4	6.4	-177	21	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	949	None	27	Human	Binding	pIC50	=	6.4	6.4	-177	21	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	84653	None	0	Human	Binding	pIC50	=	5.4	5.4	-	0	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	84653	None	0	Human	Binding	pIC50	=	5.4	5.4	-	0	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	85046	None	0	Human	Binding	pIC50	=	5.4	5.4	-	0	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	85046	None	0	Human	Binding	pIC50	=	5.4	5.4	-	0	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	82440	None	34	Human	Binding	pIC50	=	6.4	6.4	-27	23	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	82440	None	34	Human	Binding	pIC50	=	6.4	6.4	-27	23	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	218405	None	0	Rat	Binding	pIC50	=	4.4	4.4	-	0	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	2182	None	36	Human	Binding	pIC50	=	5.4	5.4	-151	24	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	2182	None	36	Human	Binding	pIC50	=	5.4	5.4	-151	24	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
	3827.0	2182	None	36	Human	Binding	pIC50	=	5.4	5.4	-151	24	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	2182	None	36	Human	Binding	pIC50	=	5.4	5.4	-151	24	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	2182	None	36	Human	Binding	pIC50	=	5.4	5.4	-151	24	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	2182	None	36	Human	Binding	pIC50	=	5.4	5.4	-151	24	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	1621	None	68	Human	Binding	pIC50	=	7.4	7.4	-1	2	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	1621	None	68	Human	Binding	pIC50	=	7.4	7.4	-1	2	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	1621	None	68	Human	Binding	pIC50	=	7.4	7.4	-1	2	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	1621	None	68	Human	Binding	pIC50	=	7.4	7.4	-1	2	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	1621	None	68	Human	Binding	pIC50	=	7.4	7.4	-1	2	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	1621	None	68	Human	Binding	pIC50	=	7.4	7.4	-1	2	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	1621	None	68	Human	Binding	pIC50	=	7.4	7.4	-1	2	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	137274	None	0	Human	Binding	pIC50	=	5.3	5.3	-	0	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	137274	None	0	Human	Binding	pIC50	=	5.3	5.3	-	0	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	937	None	69	Human	Binding	pIC50	=	6.3	6.3	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.3	6.3	-4	8	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
	2756.0	937	None	69	Human	Binding	pIC50	=	6.3	6.3	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.3	6.3	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.3	6.3	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.3	6.3	-4	8	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	84326	None	0	Human	Binding	pIC50	=	6.3	6.3	-	0	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	84326	None	0	Human	Binding	pIC50	=	6.3	6.3	-	0	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	84770	None	0	Human	Binding	pIC50	=	6.3	6.3	-	0	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	84770	None	0	Human	Binding	pIC50	=	6.3	6.3	-	0	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	137072	None	0	Human	Binding	pIC50	=	6.3	6.3	-	0	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	137072	None	0	Human	Binding	pIC50	=	6.3	6.3	-	0	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	210331	None	0	Rat	Binding	pIC50	=	4.3	4.3	-	0	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	210331	None	0	Rat	Binding	pIC50	=	4.3	4.3	-	0	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	211364	None	0	Rat	Binding	pIC50	=	4.3	4.3	-	0	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	4781	None	63	Human	Binding	pIC50	=	5.3	5.3	-33	34	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	4781	None	63	Human	Binding	pIC50	=	5.3	5.3	-33	34	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	123008	None	0	Human	Binding	pIC50	=	5.3	5.3	-	0	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	123008	None	0	Human	Binding	pIC50	=	5.3	5.3	-	0	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	937	None	69	Human	Binding	pIC50	=	5.3	5.3	-4	8	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	937	None	69	Human	Binding	pIC50	=	5.3	5.3	-4	8	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
	2756.0	937	None	69	Human	Binding	pIC50	=	5.3	5.3	-4	8	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	937	None	69	Human	Binding	pIC50	=	5.3	5.3	-4	8	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	937	None	69	Human	Binding	pIC50	=	5.3	5.3	-4	8	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	937	None	69	Human	Binding	pIC50	=	5.3	5.3	-4	8	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	84664	None	0	Human	Binding	pIC50	=	5.3	5.3	-	0	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	84664	None	0	Human	Binding	pIC50	=	5.3	5.3	-	0	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	136790	None	0	Human	Binding	pIC50	=	5.3	5.3	-	0	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	136790	None	0	Human	Binding	pIC50	=	5.3	5.3	-	0	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	84788	None	0	Human	Binding	pIC50	=	6.2	6.2	-	0	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	84788	None	0	Human	Binding	pIC50	=	6.2	6.2	-	0	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	84383	None	0	Human	Binding	pIC50	=	5.2	5.2	-	0	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	84383	None	0	Human	Binding	pIC50	=	5.2	5.2	-	0	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	209380	None	58	Human	Binding	pIC50	=	5.2	5.2	-36	34	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	209380	None	58	Human	Binding	pIC50	=	5.2	5.2	-36	34	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	209380	None	58	Human	Binding	pIC50	=	5.2	5.2	-36	34	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	84764	None	0	Human	Binding	pIC50	=	6.2	6.2	-	0	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	84764	None	0	Human	Binding	pIC50	=	6.2	6.2	-	0	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	209205	None	27	Human	Binding	pIC50	=	5.2	5.2	-7	17	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
	4601.0	209205	None	27	Human	Binding	pIC50	=	5.2	5.2	-7	17	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	209205	None	27	Human	Binding	pIC50	=	5.2	5.2	-7	17	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	209205	None	27	Human	Binding	pIC50	=	5.2	5.2	-7	17	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
	DB01173	209205	None	27	Human	Binding	pIC50	=	5.2	5.2	-7	17	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	218393	None	0	Rat	Binding	pIC50	=	4.2	4.2	-	0	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	218400	None	0	Rat	Binding	pIC50	=	4.2	4.2	-	0	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	218403	None	0	Rat	Binding	pIC50	=	4.2	4.2	-	0	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	401	None	38	Human	Binding	pIC50	=	6.1	6.1	-1412	39	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	401	None	38	Human	Binding	pIC50	=	6.1	6.1	-1412	39	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	401	None	38	Human	Binding	pIC50	=	6.1	6.1	-1412	39	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
	2160.0	401	None	38	Human	Binding	pIC50	=	6.1	6.1	-1412	39	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	401	None	38	Human	Binding	pIC50	=	6.1	6.1	-1412	39	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	401	None	38	Human	Binding	pIC50	=	6.1	6.1	-1412	39	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	9830	None	0	Human	Binding	pIC50	=	6.1	6.1	-	0	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	9830	None	0	Human	Binding	pIC50	=	6.1	6.1	-	0	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	64385	None	0	Human	Binding	pIC50	=	6.1	6.1	-	0	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	64385	None	0	Human	Binding	pIC50	=	6.1	6.1	-	0	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	937	None	69	Human	Binding	pIC50	=	6.1	6.1	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.1	6.1	-4	8	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
	2756.0	937	None	69	Human	Binding	pIC50	=	6.1	6.1	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.1	6.1	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.1	6.1	-4	8	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	937	None	69	Human	Binding	pIC50	=	6.1	6.1	-4	8	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	918	None	42	Human	Binding	pIC50	=	5.1	5.1	-446	20	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
	1213	918	None	42	Human	Binding	pIC50	=	5.1	5.1	-446	20	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
	2725	918	None	42	Human	Binding	pIC50	=	5.1	5.1	-446	20	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
	33036	918	None	42	Human	Binding	pIC50	=	5.1	5.1	-446	20	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
	33036.0	918	None	42	Human	Binding	pIC50	=	5.1	5.1	-446	20	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
	4411	918	None	42	Human	Binding	pIC50	=	5.1	5.1	-446	20	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
	616	918	None	42	Human	Binding	pIC50	=	5.1	5.1	-446	20	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
	6976	918	None	42	Human	Binding	pIC50	=	5.1	5.1	-446	20	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
	716121	918	None	42	Human	Binding	pIC50	=	5.1	5.1	-446	20	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
	CHEMBL1201353	918	None	42	Human	Binding	pIC50	=	5.1	5.1	-446	20	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
	CHEMBL1554789	918	None	42	Human	Binding	pIC50	=	5.1	5.1	-446	20	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
	CHEMBL505	918	None	42	Human	Binding	pIC50	=	5.1	5.1	-446	20	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
	DB01114	918	None	42	Human	Binding	pIC50	=	5.1	5.1	-446	20	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
	DB13679	918	None	42	Human	Binding	pIC50	=	5.1	5.1	-446	20	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	274	5	0	2	3.8	CN(CC[C@H](c1ccccn1)c1ccc(cc1)Cl)C	nan
	11328514	137945	None	0	Human	Binding	pIC50	=	6.1	6.1	-	0	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	137945	None	0	Human	Binding	pIC50	=	6.1	6.1	-	0	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	67477	None	0	Human	Binding	pIC50	=	6.1	6.1	-	0	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	67477	None	0	Human	Binding	pIC50	=	6.1	6.1	-	0	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	85038	None	0	Human	Binding	pIC50	=	6.1	6.1	-	0	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	85038	None	0	Human	Binding	pIC50	=	6.1	6.1	-	0	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	137136	None	0	Human	Binding	pIC50	=	6.1	6.1	-	0	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	137136	None	0	Human	Binding	pIC50	=	6.1	6.1	-	0	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	166338	None	0	Human	Binding	pIC50	=	5.0	5.0	-	0	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	166338	None	0	Human	Binding	pIC50	=	5.0	5.0	-	0	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	3747	None	45	Human	Binding	pIC50	=	5.0	5.0	-41	35	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	3747	None	45	Human	Binding	pIC50	=	5.0	5.0	-41	35	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	3747	None	45	Human	Binding	pIC50	=	5.0	5.0	-41	35	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	3747	None	45	Human	Binding	pIC50	=	5.0	5.0	-41	35	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	3747	None	45	Human	Binding	pIC50	=	5.0	5.0	-41	35	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	3747	None	45	Human	Binding	pIC50	=	5.0	5.0	-41	35	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	3805	None	44	Human	Binding	pIC50	=	6.0	6.0	-46	55	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	3805	None	44	Human	Binding	pIC50	=	6.0	6.0	-46	55	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	3805	None	44	Human	Binding	pIC50	=	6.0	6.0	-46	55	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	3805	None	44	Human	Binding	pIC50	=	6.0	6.0	-46	55	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	3805	None	44	Human	Binding	pIC50	=	6.0	6.0	-46	55	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	137194	None	0	Human	Binding	pIC50	=	6.0	6.0	-	0	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	137194	None	0	Human	Binding	pIC50	=	6.0	6.0	-	0	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	2496	None	39	Human	Binding	pIC50	=	6.0	6.0	-141	42	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	2496	None	39	Human	Binding	pIC50	=	6.0	6.0	-141	42	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	2496	None	39	Human	Binding	pIC50	=	6.0	6.0	-141	42	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	2496	None	39	Human	Binding	pIC50	=	6.0	6.0	-141	42	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	2496	None	39	Human	Binding	pIC50	=	6.0	6.0	-141	42	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	218045	None	0	Human	Binding	pKd	=	6	6.0	-	1	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	218045	None	0	Human	Binding	pKd	=	6	6.0	-	1	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	218043	None	0	Human	Binding	pKd	=	7.0	7.0	-	1	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	218043	None	0	Human	Binding	pKd	=	7.0	7.0	-	1	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	404	None	24	Rat	Binding	pKd	=	4.9	4.9	-2	3	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	404	None	24	Rat	Binding	pKd	=	4.9	4.9	-2	3	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	404	None	24	Rat	Binding	pKd	=	4.9	4.9	-2	3	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	1932	None	74	Human	Binding	pKd	=	7.9	7.9	-173	24	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	1932	None	74	Human	Binding	pKd	=	7.9	7.9	-173	24	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	1932	None	74	Human	Binding	pKd	=	7.9	7.9	-173	24	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	1932	None	74	Human	Binding	pKd	=	7.9	7.9	-173	24	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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
	774.0	1932	None	74	Human	Binding	pKd	=	7.9	7.9	-173	24	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	1932	None	74	Human	Binding	pKd	=	7.9	7.9	-173	24	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	1932	None	74	Human	Binding	pKd	=	7.9	7.9	-173	24	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	3159	None	58	Human	Binding	pKd	=	7.9	7.9	-281	40	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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
	119570.0	3159	None	58	Human	Binding	pKd	=	7.9	7.9	-281	40	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	3159	None	58	Human	Binding	pKd	=	7.9	7.9	-281	40	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	3159	None	58	Human	Binding	pKd	=	7.9	7.9	-281	40	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	3159	None	58	Human	Binding	pKd	=	7.9	7.9	-281	40	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	3159	None	58	Human	Binding	pKd	=	7.9	7.9	-281	40	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192871	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192871	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192871	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192875	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192875	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192875	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192888	None	0	Human	Binding	pKd	=	7.9	7.9	3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192888	None	0	Human	Binding	pKd	=	7.9	7.9	3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192888	None	0	Human	Binding	pKd	=	7.9	7.9	3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192894	None	0	Human	Binding	pKd	=	7.9	7.9	-2	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192894	None	0	Human	Binding	pKd	=	7.9	7.9	-2	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192894	None	0	Human	Binding	pKd	=	7.9	7.9	-2	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192910	None	0	Human	Binding	pKd	=	7.9	7.9	12	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192910	None	0	Human	Binding	pKd	=	7.9	7.9	12	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192910	None	0	Human	Binding	pKd	=	7.9	7.9	12	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192912	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192912	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192912	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192914	None	0	Human	Binding	pKd	=	7.9	7.9	-6	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192914	None	0	Human	Binding	pKd	=	7.9	7.9	-6	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192914	None	0	Human	Binding	pKd	=	7.9	7.9	-6	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192917	None	0	Human	Binding	pKd	=	7.9	7.9	-13	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192917	None	0	Human	Binding	pKd	=	7.9	7.9	-13	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192917	None	0	Human	Binding	pKd	=	7.9	7.9	-13	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192918	None	0	Human	Binding	pKd	=	7.9	7.9	-6	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192918	None	0	Human	Binding	pKd	=	7.9	7.9	-6	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192918	None	0	Human	Binding	pKd	=	7.9	7.9	-6	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192935	None	0	Human	Binding	pKd	=	7.9	7.9	-87	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192935	None	0	Human	Binding	pKd	=	7.9	7.9	-87	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192935	None	0	Human	Binding	pKd	=	7.9	7.9	-87	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192944	None	0	Human	Binding	pKd	=	7.9	7.9	-1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192944	None	0	Human	Binding	pKd	=	7.9	7.9	-1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192944	None	0	Human	Binding	pKd	=	7.9	7.9	-1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192955	None	0	Human	Binding	pKd	=	7.9	7.9	-20	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192955	None	0	Human	Binding	pKd	=	7.9	7.9	-20	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192955	None	0	Human	Binding	pKd	=	7.9	7.9	-20	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192957	None	0	Human	Binding	pKd	=	7.9	7.9	-18	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192957	None	0	Human	Binding	pKd	=	7.9	7.9	-18	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192957	None	0	Human	Binding	pKd	=	7.9	7.9	-18	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192960	None	0	Human	Binding	pKd	=	7.9	7.9	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192960	None	0	Human	Binding	pKd	=	7.9	7.9	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192960	None	0	Human	Binding	pKd	=	7.9	7.9	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192974	None	0	Human	Binding	pKd	=	7.9	7.9	-52	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192974	None	0	Human	Binding	pKd	=	7.9	7.9	-52	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192974	None	0	Human	Binding	pKd	=	7.9	7.9	-52	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192990	None	0	Human	Binding	pKd	=	7.9	7.9	-9	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192990	None	0	Human	Binding	pKd	=	7.9	7.9	-9	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192990	None	0	Human	Binding	pKd	=	7.9	7.9	-9	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192991	None	0	Human	Binding	pKd	=	7.9	7.9	-676	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192991	None	0	Human	Binding	pKd	=	7.9	7.9	-676	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192991	None	0	Human	Binding	pKd	=	7.9	7.9	-676	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193002	None	0	Human	Binding	pKd	=	7.9	7.9	-22	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193002	None	0	Human	Binding	pKd	=	7.9	7.9	-22	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193002	None	0	Human	Binding	pKd	=	7.9	7.9	-22	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193004	None	0	Human	Binding	pKd	=	7.9	7.9	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193004	None	0	Human	Binding	pKd	=	7.9	7.9	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193004	None	0	Human	Binding	pKd	=	7.9	7.9	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193009	None	0	Human	Binding	pKd	=	7.9	7.9	-53	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193009	None	0	Human	Binding	pKd	=	7.9	7.9	-53	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193009	None	0	Human	Binding	pKd	=	7.9	7.9	-53	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193015	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193015	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193015	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193019	None	0	Human	Binding	pKd	=	7.9	7.9	-22	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193019	None	0	Human	Binding	pKd	=	7.9	7.9	-22	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193019	None	0	Human	Binding	pKd	=	7.9	7.9	-22	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193033	None	0	Human	Binding	pKd	=	7.9	7.9	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193033	None	0	Human	Binding	pKd	=	7.9	7.9	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193033	None	0	Human	Binding	pKd	=	7.9	7.9	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193035	None	0	Human	Binding	pKd	=	7.9	7.9	-5	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193035	None	0	Human	Binding	pKd	=	7.9	7.9	-5	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193035	None	0	Human	Binding	pKd	=	7.9	7.9	-5	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193077	None	0	Human	Binding	pKd	=	7.9	7.9	-1737	20	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193077	None	0	Human	Binding	pKd	=	7.9	7.9	-1737	20	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193077	None	0	Human	Binding	pKd	=	7.9	7.9	-1737	20	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193082	None	0	Human	Binding	pKd	=	7.9	7.9	-537	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193082	None	0	Human	Binding	pKd	=	7.9	7.9	-537	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193082	None	0	Human	Binding	pKd	=	7.9	7.9	-537	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193088	None	0	Human	Binding	pKd	=	7.9	7.9	-5	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193088	None	0	Human	Binding	pKd	=	7.9	7.9	-5	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193088	None	0	Human	Binding	pKd	=	7.9	7.9	-5	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193106	None	0	Human	Binding	pKd	=	7.9	7.9	-11	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193106	None	0	Human	Binding	pKd	=	7.9	7.9	-11	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193106	None	0	Human	Binding	pKd	=	7.9	7.9	-11	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193115	None	0	Human	Binding	pKd	=	7.9	7.9	3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193115	None	0	Human	Binding	pKd	=	7.9	7.9	3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193115	None	0	Human	Binding	pKd	=	7.9	7.9	3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193119	None	0	Human	Binding	pKd	=	7.9	7.9	-1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193119	None	0	Human	Binding	pKd	=	7.9	7.9	-1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193119	None	0	Human	Binding	pKd	=	7.9	7.9	-1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193123	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193123	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193123	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193127	None	0	Human	Binding	pKd	=	7.9	7.9	-6	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193127	None	0	Human	Binding	pKd	=	7.9	7.9	-6	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193127	None	0	Human	Binding	pKd	=	7.9	7.9	-6	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193128	None	0	Human	Binding	pKd	=	7.9	7.9	-117	20	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193128	None	0	Human	Binding	pKd	=	7.9	7.9	-117	20	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193128	None	0	Human	Binding	pKd	=	7.9	7.9	-117	20	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193129	None	0	Human	Binding	pKd	=	7.9	7.9	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193129	None	0	Human	Binding	pKd	=	7.9	7.9	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193129	None	0	Human	Binding	pKd	=	7.9	7.9	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193135	None	0	Human	Binding	pKd	=	7.9	7.9	-7	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193135	None	0	Human	Binding	pKd	=	7.9	7.9	-7	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193135	None	0	Human	Binding	pKd	=	7.9	7.9	-7	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193140	None	0	Human	Binding	pKd	=	7.9	7.9	-147	20	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193140	None	0	Human	Binding	pKd	=	7.9	7.9	-147	20	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193140	None	0	Human	Binding	pKd	=	7.9	7.9	-147	20	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193144	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193144	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193144	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193149	None	0	Human	Binding	pKd	=	7.9	7.9	-851	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193149	None	0	Human	Binding	pKd	=	7.9	7.9	-851	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193149	None	0	Human	Binding	pKd	=	7.9	7.9	-851	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193150	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193150	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193150	None	0	Human	Binding	pKd	=	7.9	7.9	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193154	None	0	Human	Binding	pKd	=	7.9	7.9	3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193154	None	0	Human	Binding	pKd	=	7.9	7.9	3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193154	None	0	Human	Binding	pKd	=	7.9	7.9	3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193157	None	0	Human	Binding	pKd	=	7.9	7.9	-3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193157	None	0	Human	Binding	pKd	=	7.9	7.9	-3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193157	None	0	Human	Binding	pKd	=	7.9	7.9	-3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	178442	None	0	Human	Binding	pKd	=	7.9	7.9	-	1	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	178442	None	0	Human	Binding	pKd	=	7.9	7.9	-	1	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	178442	None	0	Human	Binding	pKd	=	7.9	7.9	-	1	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	178364	None	0	Human	Binding	pKd	=	6.9	6.9	-	1	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	178364	None	0	Human	Binding	pKd	=	6.9	6.9	-	1	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	178364	None	0	Human	Binding	pKd	=	6.9	6.9	-	1	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	178348	None	0	Human	Binding	pKd	=	7.8	7.8	-	1	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	178348	None	0	Human	Binding	pKd	=	7.8	7.8	-	1	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	178348	None	0	Human	Binding	pKd	=	7.8	7.8	-	1	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	178442	None	0	Human	Binding	pKd	=	7.8	7.8	-	1	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	178442	None	0	Human	Binding	pKd	=	7.8	7.8	-	1	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	178442	None	0	Human	Binding	pKd	=	7.8	7.8	-	1	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	178338	None	0	Human	Binding	pKd	=	7.8	7.8	-	1	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	178338	None	0	Human	Binding	pKd	=	7.8	7.8	-	1	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	178338	None	0	Human	Binding	pKd	=	7.8	7.8	-	1	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	178400	None	0	Human	Binding	pKd	=	6.8	6.8	-	1	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	178400	None	0	Human	Binding	pKd	=	6.8	6.8	-	1	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	178400	None	0	Human	Binding	pKd	=	6.8	6.8	-	1	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	178378	None	0	Human	Binding	pKd	=	7.7	7.7	-	1	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	178378	None	0	Human	Binding	pKd	=	7.7	7.7	-	1	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	178378	None	0	Human	Binding	pKd	=	7.7	7.7	-	1	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	218052	None	0	Human	Binding	pKd	=	6.6	6.6	-	1	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	218052	None	0	Human	Binding	pKd	=	6.6	6.6	-	1	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	71476	None	0	Human	Binding	pKd	=	6.6	6.6	-	1	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	71476	None	0	Human	Binding	pKd	=	6.6	6.6	-	1	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	176932	None	32	Human	Binding	pKd	=	6.6	6.6	-	1	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	176932	None	32	Human	Binding	pKd	=	6.6	6.6	-	1	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	178411	None	0	Human	Binding	pKd	=	7.6	7.6	-	1	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	178411	None	0	Human	Binding	pKd	=	7.6	7.6	-	1	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	178411	None	0	Human	Binding	pKd	=	7.6	7.6	-	1	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	178364	None	0	Human	Binding	pKd	=	6.5	6.5	-	1	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	178364	None	0	Human	Binding	pKd	=	6.5	6.5	-	1	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	178364	None	0	Human	Binding	pKd	=	6.5	6.5	-	1	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	178360	None	0	Human	Binding	pKd	=	7.5	7.5	-	1	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	178360	None	0	Human	Binding	pKd	=	7.5	7.5	-	1	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	178360	None	0	Human	Binding	pKd	=	7.5	7.5	-	1	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	178360	None	0	Human	Binding	pKd	=	7.5	7.5	-	1	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	217996	None	0	Human	Binding	pKd	=	7.5	7.5	-	1	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	178432	None	0	Human	Binding	pKd	=	6.4	6.4	-	1	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	178432	None	0	Human	Binding	pKd	=	6.4	6.4	-	1	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	178432	None	0	Human	Binding	pKd	=	6.4	6.4	-	1	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	178338	None	0	Human	Binding	pKd	=	7.3	7.3	-	1	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	178338	None	0	Human	Binding	pKd	=	7.3	7.3	-	1	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	178338	None	0	Human	Binding	pKd	=	7.3	7.3	-	1	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	218019	None	0	Human	Binding	pKd	=	7.3	7.3	-	1	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	218019	None	0	Human	Binding	pKd	=	7.3	7.3	-	1	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	178400	None	0	Human	Binding	pKd	=	6.3	6.3	-	1	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	178400	None	0	Human	Binding	pKd	=	6.3	6.3	-	1	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	178400	None	0	Human	Binding	pKd	=	6.3	6.3	-	1	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	63203	None	12	Human	Binding	pKd	=	7.2	7.2	-	1	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
	5039.0	63203	None	12	Human	Binding	pKd	=	7.2	7.2	-	1	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	63203	None	12	Human	Binding	pKd	=	7.2	7.2	-	1	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
	DB00863	63203	None	12	Human	Binding	pKd	=	7.2	7.2	-	1	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	178378	None	0	Human	Binding	pKd	=	7.2	7.2	-	1	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	178378	None	0	Human	Binding	pKd	=	7.2	7.2	-	1	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	178378	None	0	Human	Binding	pKd	=	7.2	7.2	-	1	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	218024	None	0	Human	Binding	pKd	=	7.2	7.2	-	1	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	218024	None	0	Human	Binding	pKd	=	7.2	7.2	-	1	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	178411	None	0	Human	Binding	pKd	=	7.1	7.1	-	1	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	178411	None	0	Human	Binding	pKd	=	7.1	7.1	-	1	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	178411	None	0	Human	Binding	pKd	=	7.1	7.1	-	1	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	15502	None	19	Human	Binding	pKd	=	5.1	5.1	-25	7	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	15502	None	19	Human	Binding	pKd	=	5.1	5.1	-25	7	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
	24824726	161203	None	1	Human	Binding	pKd	=	5.1	5.1	-10232	6	Antagonist potency at recombinant human histamine H2 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced cAMP accumulationAntagonist potency at recombinant human histamine H2 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced cAMP accumulation	ChEMBL	496	11	1	6	3.6	COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1021/acsmedchemlett.7b00112
	CHEMBL4060529	161203	None	1	Human	Binding	pKd	=	5.1	5.1	-10232	6	Antagonist potency at recombinant human histamine H2 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced cAMP accumulationAntagonist potency at recombinant human histamine H2 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced cAMP accumulation	ChEMBL	496	11	1	6	3.6	COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1021/acsmedchemlett.7b00112
	CHEMBL4117079	161203	None	1	Human	Binding	pKd	=	5.1	5.1	-10232	6	Antagonist potency at recombinant human histamine H2 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced cAMP accumulationAntagonist potency at recombinant human histamine H2 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced cAMP accumulation	ChEMBL	496	11	1	6	3.6	COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1021/acsmedchemlett.7b00112
	CHEMBL5282336	161203	None	1	Human	Binding	pKd	=	5.1	5.1	-10232	6	Antagonist potency at recombinant human histamine H2 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced cAMP accumulationAntagonist potency at recombinant human histamine H2 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced cAMP accumulation	ChEMBL	496	11	1	6	3.6	COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1021/acsmedchemlett.7b00112
	CHEMBL5286389	161203	None	1	Human	Binding	pKd	=	5.1	5.1	-10232	6	Antagonist potency at recombinant human histamine H2 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced cAMP accumulationAntagonist potency at recombinant human histamine H2 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced cAMP accumulation	ChEMBL	496	11	1	6	3.6	COCCCC(=O)NCCN1CCC[C@@H]1Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O	10.1021/acsmedchemlett.7b00112
	CHEMBL5078202	218026	None	0	Human	Binding	pKd	=	7.1	7.1	-	1	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	218026	None	0	Human	Binding	pKd	=	7.1	7.1	-	1	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	178411	None	0	Human	Binding	pKd	=	7.1	7.1	-	1	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	178411	None	0	Human	Binding	pKd	=	7.1	7.1	-	1	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	178411	None	0	Human	Binding	pKd	=	7.1	7.1	-	1	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	178378	None	0	Human	Binding	pKd	=	7.1	7.1	-	1	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	178378	None	0	Human	Binding	pKd	=	7.1	7.1	-	1	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	178378	None	0	Human	Binding	pKd	=	7.1	7.1	-	1	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	56493	None	0	Rat	Binding	pKd	=	5.0	5.0	-3	3	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	56493	None	0	Rat	Binding	pKd	=	5.0	5.0	-3	3	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	56493	None	0	Rat	Binding	pKd	=	5.0	5.0	-3	3	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	56243	None	30	Human	Binding	pKi	=	8.8	8.8	-2	9	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	56243	None	30	Human	Binding	pKi	=	8.8	8.8	-2	9	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	185836	None	0	Human	Binding	pKi	=	8.0	8.0	2290	4	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	185836	None	0	Human	Binding	pKi	=	8.0	8.0	2290	4	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	184944	None	0	Human	Binding	pKi	=	7	7.0	87	4	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	184944	None	0	Human	Binding	pKi	=	7	7.0	87	4	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	4549	None	0	Human	Binding	pKi	=	6	6.0	-269	3	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	4549	None	0	Human	Binding	pKi	=	6	6.0	-269	3	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	5408	None	0	Human	Binding	pKi	=	6	6.0	-346	3	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	5408	None	0	Human	Binding	pKi	=	6	6.0	-346	3	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	179063	None	62	Human	Binding	pKi	=	6	6.0	-13	27	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	179063	None	62	Human	Binding	pKi	=	6	6.0	-13	27	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	198	None	23	Human	Binding	pKi	=	5	5.0	-3467	4	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	198	None	23	Human	Binding	pKi	=	5	5.0	-3467	4	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	198	None	23	Human	Binding	pKi	=	5	5.0	-3467	4	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	4555	None	0	Human	Binding	pKi	=	5	5.0	-316	4	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	4555	None	0	Human	Binding	pKi	=	5	5.0	-316	4	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	5285	None	0	Human	Binding	pKi	=	5	5.0	-1174	4	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	5285	None	0	Human	Binding	pKi	=	5	5.0	-1174	4	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	203339	None	0	Human	Binding	pKi	=	5	5.0	-2511	3	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	203339	None	0	Human	Binding	pKi	=	5	5.0	-2511	3	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	205327	None	0	Human	Binding	pKi	=	5	5.0	-2290	3	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	205327	None	0	Human	Binding	pKi	=	5	5.0	-2290	3	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	205579	None	0	Human	Binding	pKi	=	5	5.0	-2187	3	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	205579	None	0	Human	Binding	pKi	=	5	5.0	-2187	3	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	99024	None	0	Human	Binding	pKi	=	5	5.0	-9120	10	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	99024	None	0	Human	Binding	pKi	=	5	5.0	-9120	10	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	206616	None	0	Human	Binding	pKi	=	5	5.0	-501	3	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	206616	None	0	Human	Binding	pKi	=	5	5.0	-501	3	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	206939	None	0	Human	Binding	pKi	=	5	5.0	-1000	4	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	206939	None	0	Human	Binding	pKi	=	5	5.0	-1000	4	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	56493	None	0	Human	Binding	pKi	=	5	5.0	-3	3	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	56493	None	0	Human	Binding	pKi	=	5	5.0	-3	3	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	56493	None	0	Human	Binding	pKi	=	5	5.0	-3	3	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	206939	None	0	Human	Binding	pKi	=	5	5.0	-1000	4	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	206939	None	0	Human	Binding	pKi	=	5	5.0	-1000	4	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
	172447536	195938	None	0	Human	Binding	pKi	=	5	5.0	-1905	2	Displacement of [3H]UR-DE257 from human FLAG-tagged histamine H2 receptor stably expressed in HEK293T cells assessed as inhibition constant by competitive binding based radioligand depletion assayDisplacement of [3H]UR-DE257 from human FLAG-tagged histamine H2 receptor stably expressed in HEK293T cells assessed as inhibition constant by competitive binding based radioligand depletion assay	ChEMBL	310	7	1	3	4.7	c1ccc(Nc2ccc(OCCCN3CCCCC3)cc2)cc1	10.1021/acs.jmedchem.3c00430
	CHEMBL5413694	195938	None	0	Human	Binding	pKi	=	5	5.0	-1905	2	Displacement of [3H]UR-DE257 from human FLAG-tagged histamine H2 receptor stably expressed in HEK293T cells assessed as inhibition constant by competitive binding based radioligand depletion assayDisplacement of [3H]UR-DE257 from human FLAG-tagged histamine H2 receptor stably expressed in HEK293T cells assessed as inhibition constant by competitive binding based radioligand depletion assay	ChEMBL	310	7	1	3	4.7	c1ccc(Nc2ccc(OCCCN3CCCCC3)cc2)cc1	10.1021/acs.jmedchem.3c00430
	168475864	196877	None	2	Human	Binding	pKi	=	5	5.0	-1288	3	Displacement of [3H]UR-DE257 from human FLAG-tagged histamine H2 receptor stably expressed in HEK293T cells assessed as inhibition constant by competitive binding based radioligand depletion assayDisplacement of [3H]UR-DE257 from human FLAG-tagged histamine H2 receptor stably expressed in HEK293T cells assessed as inhibition constant by competitive binding based radioligand depletion assay	ChEMBL	397	7	0	4	5.3	N#Cc1ccc(-c2ccc(OCCCN3CCC(c4ccncc4)CC3)cc2)cc1	10.1021/acs.jmedchem.3c00430
	CHEMBL5433976	196877	None	2	Human	Binding	pKi	=	5	5.0	-1288	3	Displacement of [3H]UR-DE257 from human FLAG-tagged histamine H2 receptor stably expressed in HEK293T cells assessed as inhibition constant by competitive binding based radioligand depletion assayDisplacement of [3H]UR-DE257 from human FLAG-tagged histamine H2 receptor stably expressed in HEK293T cells assessed as inhibition constant by competitive binding based radioligand depletion assay	ChEMBL	397	7	0	4	5.3	N#Cc1ccc(-c2ccc(OCCCN3CCC(c4ccncc4)CC3)cc2)cc1	10.1021/acs.jmedchem.3c00430
	44334252	4550	None	0	Human	Binding	pKi	=	4	4.0	-323	3	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	4550	None	0	Human	Binding	pKi	=	4	4.0	-323	3	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	5082	None	0	Human	Binding	pKi	=	4	4.0	-389	3	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	5082	None	0	Human	Binding	pKi	=	4	4.0	-389	3	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	102252	None	0	Human	Binding	pKi	=	4	4.0	-19054	3	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	102252	None	0	Human	Binding	pKi	=	4	4.0	-19054	3	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	204930	None	0	Human	Binding	pKi	=	4	4.0	-199526	3	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	204930	None	0	Human	Binding	pKi	=	4	4.0	-199526	3	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	205908	None	0	Human	Binding	pKi	=	5.0	5.0	-1047	4	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	205908	None	0	Human	Binding	pKi	=	5.0	5.0	-1047	4	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	185238	None	0	Human	Binding	pKi	=	7.0	7.0	57	4	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	185238	None	0	Human	Binding	pKi	=	7.0	7.0	57	4	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	186048	None	0	Human	Binding	pKi	=	7.0	7.0	93	4	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	186048	None	0	Human	Binding	pKi	=	7.0	7.0	93	4	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	2325	None	21	Human	Binding	pKi	=	6.0	6.0	-223	43	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	2325	None	21	Human	Binding	pKi	=	6.0	6.0	-223	43	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
	28864.0	2325	None	21	Human	Binding	pKi	=	6.0	6.0	-223	43	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	2325	None	21	Human	Binding	pKi	=	6.0	6.0	-223	43	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	2325	None	21	Human	Binding	pKi	=	6.0	6.0	-223	43	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	2325	None	21	Human	Binding	pKi	=	6.0	6.0	-223	43	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	205586	None	0	Human	Binding	pKi	=	5.0	5.0	-3235	3	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	205586	None	0	Human	Binding	pKi	=	5.0	5.0	-3235	3	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	205719	None	0	Human	Binding	pKi	=	5.0	5.0	-1584	3	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	205719	None	0	Human	Binding	pKi	=	5.0	5.0	-1584	3	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	137353	None	0	Human	Binding	pKi	=	5.0	5.0	-10	4	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	137353	None	0	Human	Binding	pKi	=	5.0	5.0	-10	4	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	140325	None	3	Human	Binding	pKi	=	5.0	5.0	-218	4	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	140325	None	3	Human	Binding	pKi	=	5.0	5.0	-218	4	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	398	None	47	Human	Binding	pKi	=	5.0	5.0	-6	31	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	398	None	47	Human	Binding	pKi	=	5.0	5.0	-6	31	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
	2157.0	398	None	47	Human	Binding	pKi	=	5.0	5.0	-6	31	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	398	None	47	Human	Binding	pKi	=	5.0	5.0	-6	31	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	398	None	47	Human	Binding	pKi	=	5.0	5.0	-6	31	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	398	None	47	Human	Binding	pKi	=	5.0	5.0	-6	31	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	186427	None	0	Human	Binding	pKi	=	7.0	7.0	275	4	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	186427	None	0	Human	Binding	pKi	=	7.0	7.0	275	4	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	193135	None	0	Human	Binding	pKi	=	6.0	6.0	-7	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193135	None	0	Human	Binding	pKi	=	6.0	6.0	-7	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193135	None	0	Human	Binding	pKi	=	6.0	6.0	-7	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193119	None	0	Human	Binding	pKi	=	7.0	7.0	-1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193119	None	0	Human	Binding	pKi	=	7.0	7.0	-1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193119	None	0	Human	Binding	pKi	=	7.0	7.0	-1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	163369	None	0	Human	Binding	pKi	=	5.0	5.0	-4265	3	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	163369	None	0	Human	Binding	pKi	=	5.0	5.0	-4265	3	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	205091	None	0	Human	Binding	pKi	=	5.0	5.0	-1202	3	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	205091	None	0	Human	Binding	pKi	=	5.0	5.0	-1202	3	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	205450	None	0	Human	Binding	pKi	=	5.0	5.0	-8709	3	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	205450	None	0	Human	Binding	pKi	=	5.0	5.0	-8709	3	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	163165	None	0	Human	Binding	pKi	=	6.0	6.0	-6	5	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	163165	None	0	Human	Binding	pKi	=	6.0	6.0	-6	5	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	1389	None	72	Human	Binding	pKi	=	6.0	6.0	-29	15	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
	124087.0	1389	None	72	Human	Binding	pKi	=	6.0	6.0	-29	15	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	1389	None	72	Human	Binding	pKi	=	6.0	6.0	-29	15	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	1389	None	72	Human	Binding	pKi	=	6.0	6.0	-29	15	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	1389	None	72	Human	Binding	pKi	=	6.0	6.0	-29	15	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	1389	None	72	Human	Binding	pKi	=	6.0	6.0	-29	15	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	193015	None	0	Human	Binding	pKi	=	7.0	7.0	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193015	None	0	Human	Binding	pKi	=	7.0	7.0	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193015	None	0	Human	Binding	pKi	=	7.0	7.0	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	102252	None	0	Human	Binding	pKi	=	5.0	5.0	-19054	3	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	102252	None	0	Human	Binding	pKi	=	5.0	5.0	-19054	3	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	163021	None	0	Human	Binding	pKi	=	6.0	6.0	-3	4	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	163021	None	0	Human	Binding	pKi	=	6.0	6.0	-3	4	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	217461	None	0	Human	Binding	pKi	=	7.0	7.0	-	1	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	186579	None	0	Human	Binding	pKi	=	6.0	6.0	1	6	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	186579	None	0	Human	Binding	pKi	=	6.0	6.0	1	6	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	205760	None	0	Human	Binding	pKi	=	5.0	5.0	-1174	3	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	205760	None	0	Human	Binding	pKi	=	5.0	5.0	-1174	3	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	176253	None	16	Human	Binding	pKi	=	6.0	6.0	-2	20	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	176253	None	16	Human	Binding	pKi	=	6.0	6.0	-2	20	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	176253	None	16	Human	Binding	pKi	=	6.0	6.0	-2	20	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	176253	None	16	Human	Binding	pKi	=	6.0	6.0	-2	20	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	185056	None	0	Human	Binding	pKi	=	6.9	6.9	-1	5	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	185056	None	0	Human	Binding	pKi	=	6.9	6.9	-1	5	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	3183	None	36	Human	Binding	pKi	=	5.9	5.9	-36	29	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	3183	None	36	Human	Binding	pKi	=	5.9	5.9	-36	29	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
	4927.0	3183	None	36	Human	Binding	pKi	=	5.9	5.9	-36	29	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	3183	None	36	Human	Binding	pKi	=	5.9	5.9	-36	29	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	3183	None	36	Human	Binding	pKi	=	5.9	5.9	-36	29	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	3183	None	36	Human	Binding	pKi	=	5.9	5.9	-36	29	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	1911	None	63	Human	Binding	pKi	=	5.9	5.9	-131	85	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	1911	None	63	Human	Binding	pKi	=	5.9	5.9	-131	85	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
	3559.0	1911	None	63	Human	Binding	pKi	=	5.9	5.9	-131	85	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	1911	None	63	Human	Binding	pKi	=	5.9	5.9	-131	85	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	1911	None	63	Human	Binding	pKi	=	5.9	5.9	-131	85	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	1911	None	63	Human	Binding	pKi	=	5.9	5.9	-131	85	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	184824	None	0	Human	Binding	pKi	=	5.9	5.9	38	4	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	184824	None	0	Human	Binding	pKi	=	5.9	5.9	38	4	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	181680	None	0	Human	Binding	pKi	=	5.9	5.9	-7	10	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	181680	None	0	Human	Binding	pKi	=	5.9	5.9	-7	10	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	92374	None	0	Human	Binding	pKi	=	5.9	5.9	2	8	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	92374	None	0	Human	Binding	pKi	=	5.9	5.9	2	8	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	205786	None	0	Human	Binding	pKi	=	4.9	4.9	-2884	3	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	205786	None	0	Human	Binding	pKi	=	4.9	4.9	-2884	3	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	109765	None	0	Human	Binding	pKi	=	4.9	4.9	-6918	4	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	109765	None	0	Human	Binding	pKi	=	4.9	4.9	-6918	4	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	597	None	17	Human	Binding	pKi	=	5.9	5.9	-74	20	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
	1201549.0	597	None	17	Human	Binding	pKi	=	5.9	5.9	-74	20	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	597	None	17	Human	Binding	pKi	=	5.9	5.9	-74	20	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	597	None	17	Human	Binding	pKi	=	5.9	5.9	-74	20	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	597	None	17	Human	Binding	pKi	=	5.9	5.9	-74	20	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	597	None	17	Human	Binding	pKi	=	5.9	5.9	-74	20	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	597	None	17	Human	Binding	pKi	=	5.9	5.9	-74	20	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	193149	None	0	Human	Binding	pKi	=	7.9	7.9	-851	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193149	None	0	Human	Binding	pKi	=	7.9	7.9	-851	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193149	None	0	Human	Binding	pKi	=	7.9	7.9	-851	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	4455	None	0	Human	Binding	pKi	=	5.9	5.9	-398	3	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	4455	None	0	Human	Binding	pKi	=	5.9	5.9	-398	3	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	205671	None	0	Human	Binding	pKi	=	4.9	4.9	-3981	3	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	205671	None	0	Human	Binding	pKi	=	4.9	4.9	-3981	3	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	205399	None	0	Human	Binding	pKi	=	4.9	4.9	-512	3	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	205399	None	0	Human	Binding	pKi	=	4.9	4.9	-512	3	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	1662	None	37	Human	Binding	pKi	=	5.9	5.9	-323	65	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	1662	None	37	Human	Binding	pKi	=	5.9	5.9	-323	65	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	1662	None	37	Human	Binding	pKi	=	5.9	5.9	-323	65	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
	3372.0	1662	None	37	Human	Binding	pKi	=	5.9	5.9	-323	65	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	1662	None	37	Human	Binding	pKi	=	5.9	5.9	-323	65	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	1662	None	37	Human	Binding	pKi	=	5.9	5.9	-323	65	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	78224	None	0	Human	Binding	pKi	=	5.9	5.9	-3090	16	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	78224	None	0	Human	Binding	pKi	=	5.9	5.9	-3090	16	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	101077	None	0	Human	Binding	pKi	=	4.9	4.9	-338	3	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	101077	None	0	Human	Binding	pKi	=	4.9	4.9	-338	3	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	205520	None	0	Human	Binding	pKi	=	4.9	4.9	-331	3	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	205520	None	0	Human	Binding	pKi	=	4.9	4.9	-331	3	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	164250	None	0	Human	Binding	pKi	=	4.9	4.9	-812	4	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	164250	None	0	Human	Binding	pKi	=	4.9	4.9	-812	4	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	205787	None	0	Human	Binding	pKi	=	4.9	4.9	-954	3	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	205787	None	0	Human	Binding	pKi	=	4.9	4.9	-954	3	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	185686	None	0	Human	Binding	pKi	=	6.9	6.9	64	4	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	185686	None	0	Human	Binding	pKi	=	6.9	6.9	64	4	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	205372	None	2	Human	Binding	pKi	=	4.9	4.9	-8912	3	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	205372	None	2	Human	Binding	pKi	=	4.9	4.9	-8912	3	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	205767	None	0	Human	Binding	pKi	=	4.9	4.9	-181	3	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	205767	None	0	Human	Binding	pKi	=	4.9	4.9	-181	3	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	106013	None	0	Human	Binding	pKi	=	4.9	4.9	-128	3	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	106013	None	0	Human	Binding	pKi	=	4.9	4.9	-128	3	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	104416	None	0	Human	Binding	pKi	=	4.9	4.9	-501	3	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	104416	None	0	Human	Binding	pKi	=	4.9	4.9	-501	3	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	205108	None	0	Human	Binding	pKi	=	4.9	4.9	-1513	3	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	205108	None	0	Human	Binding	pKi	=	4.9	4.9	-1513	3	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	4456	None	0	Human	Binding	pKi	=	4.9	4.9	-229	4	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	4456	None	0	Human	Binding	pKi	=	4.9	4.9	-229	4	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	5295	None	0	Human	Binding	pKi	=	4.9	4.9	-426	4	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	5295	None	0	Human	Binding	pKi	=	4.9	4.9	-426	4	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	178450	None	0	Human	Binding	pKi	=	7.9	7.9	-	1	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	178450	None	0	Human	Binding	pKi	=	7.9	7.9	-	1	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	178450	None	0	Human	Binding	pKi	=	7.9	7.9	-	1	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	178417	None	0	Human	Binding	pKi	=	7.9	7.9	-	1	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	178417	None	0	Human	Binding	pKi	=	7.9	7.9	-	1	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	178417	None	0	Human	Binding	pKi	=	7.9	7.9	-	1	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	178432	None	0	Human	Binding	pKi	=	5.9	5.9	-	1	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	178432	None	0	Human	Binding	pKi	=	5.9	5.9	-	1	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	178432	None	0	Human	Binding	pKi	=	5.9	5.9	-	1	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	204105	None	0	Human	Binding	pKi	=	4.9	4.9	-912	3	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	204105	None	0	Human	Binding	pKi	=	4.9	4.9	-912	3	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	94207	None	39	Human	Binding	pKi	=	4.9	4.9	-20892	3	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	94207	None	39	Human	Binding	pKi	=	4.9	4.9	-20892	3	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	3159	None	58	Human	Binding	pKi	=	4.9	4.9	-281	40	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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
	119570.0	3159	None	58	Human	Binding	pKi	=	4.9	4.9	-281	40	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	3159	None	58	Human	Binding	pKi	=	4.9	4.9	-281	40	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	3159	None	58	Human	Binding	pKi	=	4.9	4.9	-281	40	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	3159	None	58	Human	Binding	pKi	=	4.9	4.9	-281	40	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	3159	None	58	Human	Binding	pKi	=	4.9	4.9	-281	40	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	56360	None	12	Human	Binding	pKi	=	4.9	4.9	-5	6	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	56360	None	12	Human	Binding	pKi	=	4.9	4.9	-5	6	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	216454	None	39	Human	Binding	pKi	=	6.9	6.9	-1	22	GPCRScan assay: inhibition of H2GPCRScan assay: inhibition of H2	ChEMBL		None	None	None		CNCc1ccccc1-c1csc([C@@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1	10.6019/CHEMBL4507273
	CHEMBL4535474	216454	None	39	Human	Binding	pKi	=	6.9	6.9	-1	22	GPCRScan assay: inhibition of H2GPCRScan assay: inhibition of H2	ChEMBL		None	None	None		CNCc1ccccc1-c1csc([C@@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1	10.6019/CHEMBL4507273
	CHEMBL4535474	216454	None	39	Human	Binding	pKi	=	6.9	6.9	-1	22	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	10.6019/CHEMBL5212743
	1231	937	None	69	Human	Binding	pKi	=	6.9	6.9	-4	8	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	937	None	69	Human	Binding	pKi	=	6.9	6.9	-4	8	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
	2756.0	937	None	69	Human	Binding	pKi	=	6.9	6.9	-4	8	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	937	None	69	Human	Binding	pKi	=	6.9	6.9	-4	8	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	937	None	69	Human	Binding	pKi	=	6.9	6.9	-4	8	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	937	None	69	Human	Binding	pKi	=	6.9	6.9	-4	8	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	191760	None	0	Human	Binding	pKi	=	5.9	5.9	-67	15	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	191760	None	0	Human	Binding	pKi	=	5.9	5.9	-67	15	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
	158797	3771	None	19	Human	Binding	pKi	=	5.9	5.9	-33	14	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	303	7	1	2	4.6	COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C	10.6019/CHEMBL5442175
	718	3771	None	19	Human	Binding	pKi	=	5.9	5.9	-33	14	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	303	7	1	2	4.6	COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C	10.6019/CHEMBL5442175
	CHEMBL292376	3771	None	19	Human	Binding	pKi	=	5.9	5.9	-33	14	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	303	7	1	2	4.6	COc1cccc(c1)[C@H](NCCCc1ccccc1Cl)C	10.6019/CHEMBL5442175
	44304560	102818	None	0	Human	Binding	pKi	=	4.9	4.9	-10715	3	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	102818	None	0	Human	Binding	pKi	=	4.9	4.9	-10715	3	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	205359	None	0	Human	Binding	pKi	=	4.9	4.9	-229	3	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	205359	None	0	Human	Binding	pKi	=	4.9	4.9	-229	3	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	89759	None	0	Human	Binding	pKi	=	4.9	4.9	-1479	6	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	89759	None	0	Human	Binding	pKi	=	4.9	4.9	-1479	6	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
	CHEMBL4748908	216520	None	0	Human	Binding	pKi	=	6.8	6.8	-1	12	GPCRScan assay: inhibition of H2GPCRScan assay: inhibition of H2	ChEMBL		None	None	None		CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1	10.6019/CHEMBL4800732
	164610824	185216	None	0	Human	Binding	pKi	=	5.8	5.8	14	4	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	185216	None	0	Human	Binding	pKi	=	5.8	5.8	14	4	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	102186	None	0	Human	Binding	pKi	=	4.8	4.8	-537	3	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	102186	None	0	Human	Binding	pKi	=	4.8	4.8	-537	3	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	3331	None	72	Human	Binding	pKi	=	5.8	5.8	-281	67	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	3331	None	72	Human	Binding	pKi	=	5.8	5.8	-281	67	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
	5073.0	3331	None	72	Human	Binding	pKi	=	5.8	5.8	-281	67	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	3331	None	72	Human	Binding	pKi	=	5.8	5.8	-281	67	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	3331	None	72	Human	Binding	pKi	=	5.8	5.8	-281	67	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	3331	None	72	Human	Binding	pKi	=	5.8	5.8	-281	67	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	186189	None	0	Human	Binding	pKi	=	6.8	6.8	17	4	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	186189	None	0	Human	Binding	pKi	=	6.8	6.8	17	4	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	205356	None	0	Human	Binding	pKi	=	4.8	4.8	-912	3	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	205356	None	0	Human	Binding	pKi	=	4.8	4.8	-912	3	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	205732	None	0	Human	Binding	pKi	=	4.8	4.8	-1995	3	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	205732	None	0	Human	Binding	pKi	=	4.8	4.8	-1995	3	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	205259	None	0	Human	Binding	pKi	=	4.8	4.8	-275	3	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	205259	None	0	Human	Binding	pKi	=	4.8	4.8	-275	3	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
	CHEMBL4748908	216520	None	0	Human	Binding	pKi	=	6.8	6.8	-1	12	GPCRScan assay: inhibition of H2GPCRScan assay: inhibition of H2	ChEMBL		None	None	None		CN1CCN(c2ccnc(NCCc3ccccc3)n2)CC1	10.6019/CHEMBL4800732
	73347825	92592	None	0	Human	Binding	pKi	=	5.8	5.8	-1	3	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	92592	None	0	Human	Binding	pKi	=	5.8	5.8	-1	3	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	18873	None	78	Human	Binding	pKi	=	5.8	5.8	-1	3	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	18873	None	78	Human	Binding	pKi	=	5.8	5.8	-1	3	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	193035	None	0	Human	Binding	pKi	=	7.8	7.8	-5	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193035	None	0	Human	Binding	pKi	=	7.8	7.8	-5	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193035	None	0	Human	Binding	pKi	=	7.8	7.8	-5	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	177908	None	13	Human	Binding	pKi	=	7.8	7.8	-	1	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	177908	None	13	Human	Binding	pKi	=	7.8	7.8	-	1	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	78716	None	0	Human	Binding	pKi	=	4.8	4.8	-3715	4	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	78716	None	0	Human	Binding	pKi	=	4.8	4.8	-3715	4	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	205420	None	0	Human	Binding	pKi	=	4.8	4.8	-52	3	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	205420	None	0	Human	Binding	pKi	=	4.8	4.8	-52	3	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	193154	None	0	Human	Binding	pKi	=	6.8	6.8	3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193154	None	0	Human	Binding	pKi	=	6.8	6.8	3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193154	None	0	Human	Binding	pKi	=	6.8	6.8	3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	205631	None	0	Human	Binding	pKi	=	5.8	5.8	-117	3	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	205631	None	0	Human	Binding	pKi	=	5.8	5.8	-117	3	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	4918	None	0	Human	Binding	pKi	=	5.8	5.8	-575	3	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	4918	None	0	Human	Binding	pKi	=	5.8	5.8	-575	3	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	207971	None	50	Human	Binding	pKi	=	5.8	5.8	-19	34	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	207971	None	50	Human	Binding	pKi	=	5.8	5.8	-19	34	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	207971	None	50	Human	Binding	pKi	=	5.8	5.8	-19	34	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	185722	None	0	Human	Binding	pKi	=	6.8	6.8	93	2	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	185722	None	0	Human	Binding	pKi	=	6.8	6.8	93	2	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	206653	None	0	Human	Binding	pKi	=	5.8	5.8	-79	3	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	206653	None	0	Human	Binding	pKi	=	5.8	5.8	-79	3	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	206932	None	0	Human	Binding	pKi	=	5.8	5.8	-199	4	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	206932	None	0	Human	Binding	pKi	=	5.8	5.8	-199	4	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	206932	None	0	Human	Binding	pKi	=	5.8	5.8	-199	4	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	206932	None	0	Human	Binding	pKi	=	5.8	5.8	-199	4	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	1414	None	26	Human	Binding	pKi	=	5.8	5.8	-53	15	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
	3042.0	1414	None	26	Human	Binding	pKi	=	5.8	5.8	-53	15	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	1414	None	26	Human	Binding	pKi	=	5.8	5.8	-53	15	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	1414	None	26	Human	Binding	pKi	=	5.8	5.8	-53	15	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	1414	None	26	Human	Binding	pKi	=	5.8	5.8	-53	15	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	1414	None	26	Human	Binding	pKi	=	5.8	5.8	-53	15	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	4964	None	0	Human	Binding	pKi	=	5.8	5.8	-1000	3	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	4964	None	0	Human	Binding	pKi	=	5.8	5.8	-1000	3	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	78714	None	0	Human	Binding	pKi	=	5.8	5.8	-398	3	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	78714	None	0	Human	Binding	pKi	=	5.8	5.8	-398	3	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
	CHEMBL4576555	216491	None	5	Human	Binding	pKi	=	5.8	5.8	-1	20	GPCRScan assay: inhibition of H2GPCRScan assay: inhibition of H2	ChEMBL		None	None	None		CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1	10.6019/CHEMBL4507307
	2247	505	None	55	Human	Binding	pKi	=	5.8	5.8	-56	41	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	505	None	55	Human	Binding	pKi	=	5.8	5.8	-56	41	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	505	None	55	Human	Binding	pKi	=	5.8	5.8	-56	41	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	505	None	55	Human	Binding	pKi	=	5.8	5.8	-56	41	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	505	None	55	Human	Binding	pKi	=	5.8	5.8	-56	41	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	107447	None	0	Human	Binding	pKi	=	5.8	5.8	-14	3	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	107447	None	0	Human	Binding	pKi	=	5.8	5.8	-14	3	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	100663	None	0	Human	Binding	pKi	=	4.8	4.8	-97	3	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	100663	None	0	Human	Binding	pKi	=	4.8	4.8	-97	3	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	186573	None	0	Human	Binding	pKi	=	6.8	6.8	144	3	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	186573	None	0	Human	Binding	pKi	=	6.8	6.8	144	3	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	4926	None	0	Human	Binding	pKi	=	4.8	4.8	-2041	4	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	4926	None	0	Human	Binding	pKi	=	4.8	4.8	-2041	4	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	178378	None	0	Human	Binding	pKi	=	7.8	7.8	-	1	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	178378	None	0	Human	Binding	pKi	=	7.8	7.8	-	1	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	178378	None	0	Human	Binding	pKi	=	7.8	7.8	-	1	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	178411	None	0	Human	Binding	pKi	=	7.8	7.8	-	1	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	178411	None	0	Human	Binding	pKi	=	7.8	7.8	-	1	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	178411	None	0	Human	Binding	pKi	=	7.8	7.8	-	1	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	185204	None	0	Human	Binding	pKi	=	7.8	7.8	-2	6	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	185204	None	0	Human	Binding	pKi	=	7.8	7.8	-2	6	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	937	None	69	Human	Binding	pKi	=	6.8	6.8	-4	8	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	937	None	69	Human	Binding	pKi	=	6.8	6.8	-4	8	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
	2756.0	937	None	69	Human	Binding	pKi	=	6.8	6.8	-4	8	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	937	None	69	Human	Binding	pKi	=	6.8	6.8	-4	8	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	937	None	69	Human	Binding	pKi	=	6.8	6.8	-4	8	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	937	None	69	Human	Binding	pKi	=	6.8	6.8	-4	8	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	198033	None	2	Human	Binding	pKi	=	5.8	5.8	-2344	13	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	198033	None	2	Human	Binding	pKi	=	5.8	5.8	-2344	13	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	198033	None	2	Human	Binding	pKi	=	5.8	5.8	-2344	13	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
	CHEMBL4576555	216491	None	5	Human	Binding	pKi	=	5.8	5.8	-1	20	GPCRScan assay: inhibition of H2GPCRScan assay: inhibition of H2	ChEMBL		None	None	None		CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1	10.6019/CHEMBL4507307
	10064805	102431	None	0	Human	Binding	pKi	=	5.8	5.8	-95	4	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	102431	None	0	Human	Binding	pKi	=	5.8	5.8	-95	4	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	92595	None	0	Human	Binding	pKi	=	5.8	5.8	-2	8	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	92595	None	0	Human	Binding	pKi	=	5.8	5.8	-2	8	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	102540	None	0	Human	Binding	pKi	=	4.8	4.8	-691	3	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	102540	None	0	Human	Binding	pKi	=	4.8	4.8	-691	3	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	189888	None	0	Human	Binding	pKi	=	5.8	5.8	-13	17	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	189888	None	0	Human	Binding	pKi	=	5.8	5.8	-13	17	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	162497	None	0	Human	Binding	pKi	=	5.8	5.8	-6	16	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	162497	None	0	Human	Binding	pKi	=	5.8	5.8	-6	16	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	91868	None	6	Human	Binding	pKi	=	5.8	5.8	-17782	17	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	91868	None	6	Human	Binding	pKi	=	5.8	5.8	-17782	17	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
	72901200	119841	None	26	Human	Binding	pKi	=	5.8	5.8	-1288	33	GPCRScan assay: inhibition of H2GPCRScan assay: inhibition of H2	ChEMBL	322	7	2	4	3.8	Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1	10.6019/CHEMBL4507309
	CHEMBL3480577	119841	None	26	Human	Binding	pKi	=	5.8	5.8	-1288	33	GPCRScan assay: inhibition of H2GPCRScan assay: inhibition of H2	ChEMBL	322	7	2	4	3.8	Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1	10.6019/CHEMBL4507309
	44304385	205636	None	0	Human	Binding	pKi	=	4.8	4.8	-3548	3	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	205636	None	0	Human	Binding	pKi	=	4.8	4.8	-3548	3	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	205861	None	0	Human	Binding	pKi	=	4.8	4.8	-3019	3	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	205861	None	0	Human	Binding	pKi	=	4.8	4.8	-3019	3	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	205222	None	0	Human	Binding	pKi	=	4.8	4.8	-407	3	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	205222	None	0	Human	Binding	pKi	=	4.8	4.8	-407	3	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	83829	None	0	Human	Binding	pKi	=	5.8	5.8	1	3	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	83829	None	0	Human	Binding	pKi	=	5.8	5.8	1	3	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	3823	None	29	Human	Binding	pKi	=	7.8	7.8	-2	5	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	3823	None	29	Human	Binding	pKi	=	7.8	7.8	-2	5	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	3823	None	29	Human	Binding	pKi	=	7.8	7.8	-2	5	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	3823	None	29	Human	Binding	pKi	=	7.8	7.8	-2	5	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	4008	None	55	Human	Binding	pKi	=	6.8	6.8	-5	13	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
	71768094	4008	None	55	Human	Binding	pKi	=	6.8	6.8	-5	13	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
	71768094.0	4008	None	55	Human	Binding	pKi	=	6.8	6.8	-5	13	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	4008	None	55	Human	Binding	pKi	=	6.8	6.8	-5	13	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	4008	None	55	Human	Binding	pKi	=	6.8	6.8	-5	13	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
	9966051.0	4008	None	55	Human	Binding	pKi	=	6.8	6.8	-5	13	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	4008	None	55	Human	Binding	pKi	=	6.8	6.8	-5	13	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	4008	None	55	Human	Binding	pKi	=	6.8	6.8	-5	13	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	4646	None	0	Human	Binding	pKi	=	5.8	5.8	-660	3	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	4646	None	0	Human	Binding	pKi	=	5.8	5.8	-660	3	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	218015	None	0	Human	Binding	pKi	=	6.7	6.7	-	1	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	218015	None	0	Human	Binding	pKi	=	6.7	6.7	-	1	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	178377	None	0	Human	Binding	pKi	=	5.7	5.7	-1819	4	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	178377	None	0	Human	Binding	pKi	=	5.7	5.7	-1819	4	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	178377	None	0	Human	Binding	pKi	=	5.7	5.7	-1819	4	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	192990	None	0	Human	Binding	pKi	=	5.7	5.7	-9	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192990	None	0	Human	Binding	pKi	=	5.7	5.7	-9	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192990	None	0	Human	Binding	pKi	=	5.7	5.7	-9	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	56283	None	21	Human	Binding	pKi	=	5.7	5.7	-12589	20	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
	3158.0	56283	None	21	Human	Binding	pKi	=	5.7	5.7	-12589	20	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	56283	None	21	Human	Binding	pKi	=	5.7	5.7	-12589	20	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
	DB01142	56283	None	21	Human	Binding	pKi	=	5.7	5.7	-12589	20	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	205651	None	0	Human	Binding	pKi	=	5.7	5.7	-91	3	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	205651	None	0	Human	Binding	pKi	=	5.7	5.7	-91	3	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	205428	None	0	Human	Binding	pKi	=	4.7	4.7	-354	3	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	205428	None	0	Human	Binding	pKi	=	4.7	4.7	-354	3	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	205634	None	0	Human	Binding	pKi	=	4.7	4.7	-1174	3	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	205634	None	0	Human	Binding	pKi	=	4.7	4.7	-1174	3	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	4640	None	0	Human	Binding	pKi	=	4.7	4.7	-2630	4	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	4640	None	0	Human	Binding	pKi	=	4.7	4.7	-2630	4	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	92598	None	0	Human	Binding	pKi	=	5.7	5.7	-1	3	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	92598	None	0	Human	Binding	pKi	=	5.7	5.7	-1	3	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	178348	None	0	Human	Binding	pKi	=	7.7	7.7	-	1	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	178348	None	0	Human	Binding	pKi	=	7.7	7.7	-	1	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	178348	None	0	Human	Binding	pKi	=	7.7	7.7	-	1	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	193127	None	0	Human	Binding	pKi	=	7.7	7.7	-6	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193127	None	0	Human	Binding	pKi	=	7.7	7.7	-6	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193127	None	0	Human	Binding	pKi	=	7.7	7.7	-6	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193115	None	0	Human	Binding	pKi	=	6.7	6.7	3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193115	None	0	Human	Binding	pKi	=	6.7	6.7	3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193115	None	0	Human	Binding	pKi	=	6.7	6.7	3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	107598	None	0	Human	Binding	pKi	=	4.7	4.7	-977	4	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	107598	None	0	Human	Binding	pKi	=	4.7	4.7	-977	4	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	168511	None	37	Human	Binding	pKi	=	4.7	4.7	-724	3	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	168511	None	37	Human	Binding	pKi	=	4.7	4.7	-724	3	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	205352	None	0	Human	Binding	pKi	=	4.7	4.7	-363	3	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	205352	None	0	Human	Binding	pKi	=	4.7	4.7	-363	3	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	119841	None	26	Human	Binding	pKi	=	5.7	5.7	-1288	33	GPCRScan assay: inhibition of H2GPCRScan assay: inhibition of H2	ChEMBL	322	7	2	4	3.8	Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1	10.6019/CHEMBL4507309
	CHEMBL3480577	119841	None	26	Human	Binding	pKi	=	5.7	5.7	-1288	33	GPCRScan assay: inhibition of H2GPCRScan assay: inhibition of H2	ChEMBL	322	7	2	4	3.8	Cc1ccc2nc(CNCCCOc3ccccc3)cc(O)c2c1	10.6019/CHEMBL4507309
	72901200	119841	None	26	Human	Binding	pKi	=	5.7	5.7	-1288	33	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	10.6019/CHEMBL5212743
	CHEMBL3480577	119841	None	26	Human	Binding	pKi	=	5.7	5.7	-1288	33	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	10.6019/CHEMBL5212743
	5291	209896	None	64	Human	Binding	pKi	=	5.7	5.7	-1	2	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	209896	None	64	Human	Binding	pKi	=	5.7	5.7	-1	2	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	100669	None	0	Human	Binding	pKi	=	4.7	4.7	-660	3	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	100669	None	0	Human	Binding	pKi	=	4.7	4.7	-660	3	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	202726	None	0	Human	Binding	pKi	=	4.7	4.7	-4365	3	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	202726	None	0	Human	Binding	pKi	=	4.7	4.7	-4365	3	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	1301	None	39	Human	Binding	pKi	=	6.7	6.7	-43	49	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	1301	None	39	Human	Binding	pKi	=	6.7	6.7	-43	49	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
	2913.0	1301	None	39	Human	Binding	pKi	=	6.7	6.7	-43	49	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	1301	None	39	Human	Binding	pKi	=	6.7	6.7	-43	49	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	1301	None	39	Human	Binding	pKi	=	6.7	6.7	-43	49	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	1301	None	39	Human	Binding	pKi	=	6.7	6.7	-43	49	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	171207	None	0	Human	Binding	pKi	=	5.7	5.7	-316	6	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	171207	None	0	Human	Binding	pKi	=	5.7	5.7	-316	6	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	186254	None	0	Human	Binding	pKi	=	5.7	5.7	17	2	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	186254	None	0	Human	Binding	pKi	=	5.7	5.7	17	2	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	209921	None	0	Human	Binding	pKi	=	4.7	4.7	-31	3	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	209921	None	0	Human	Binding	pKi	=	4.7	4.7	-31	3	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	205267	None	0	Human	Binding	pKi	=	4.7	4.7	-1905	3	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	205267	None	0	Human	Binding	pKi	=	4.7	4.7	-1905	3	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	169490	None	0	Human	Binding	pKi	=	4.7	4.7	-1995	3	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	169490	None	0	Human	Binding	pKi	=	4.7	4.7	-1995	3	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
	14490466	194009	None	0	Human	Binding	pKi	=	8.7	8.7	-	1	Antagonist activity at histamine H2 receptor (unknown origin) assessed as inhibition constantAntagonist activity at histamine H2 receptor (unknown origin) assessed as inhibition constant	ChEMBL	415	13	2	8	4.1	CN(C)Cc1ccc(CSCCNc2nonc2NCCCc2ccccc2)o1	10.1021/acs.jmedchem.0c01901
	CHEMBL5276441	194009	None	0	Human	Binding	pKi	=	8.7	8.7	-	1	Antagonist activity at histamine H2 receptor (unknown origin) assessed as inhibition constantAntagonist activity at histamine H2 receptor (unknown origin) assessed as inhibition constant	ChEMBL	415	13	2	8	4.1	CN(C)Cc1ccc(CSCCNc2nonc2NCCCc2ccccc2)o1	10.1021/acs.jmedchem.0c01901
	164626153	186484	None	0	Human	Binding	pKi	=	8.7	8.7	4	6	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	186484	None	0	Human	Binding	pKi	=	8.7	8.7	4	6	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
	2398	954	None	43	Human	Binding	pKi	=	5.7	5.7	-13	28	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
	2801	954	None	43	Human	Binding	pKi	=	5.7	5.7	-13	28	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
	2801.0	954	None	43	Human	Binding	pKi	=	5.7	5.7	-13	28	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
	701	954	None	43	Human	Binding	pKi	=	5.7	5.7	-13	28	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
	CHEMBL415	954	None	43	Human	Binding	pKi	=	5.7	5.7	-13	28	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
	DB01242	954	None	43	Human	Binding	pKi	=	5.7	5.7	-13	28	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	314	4	0	2	4.5	CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C	nan
	156015243	178343	None	0	Human	Binding	pKi	=	5.7	5.7	-	1	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	178343	None	0	Human	Binding	pKi	=	5.7	5.7	-	1	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	178343	None	0	Human	Binding	pKi	=	5.7	5.7	-	1	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	102402	None	0	Human	Binding	pKi	=	4.7	4.7	-125	3	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	102402	None	0	Human	Binding	pKi	=	4.7	4.7	-125	3	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	203419	None	0	Human	Binding	pKi	=	4.7	4.7	-154	3	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	203419	None	0	Human	Binding	pKi	=	4.7	4.7	-154	3	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	205519	None	0	Human	Binding	pKi	=	4.7	4.7	-1659	3	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	205519	None	0	Human	Binding	pKi	=	4.7	4.7	-1659	3	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	205421	None	0	Human	Binding	pKi	=	4.7	4.7	-97	3	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	205421	None	0	Human	Binding	pKi	=	4.7	4.7	-97	3	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	216439	None	12	Human	Binding	pKi	=	7.7	7.7	3	26	GPCRScan assay: inhibition of H2GPCRScan assay: inhibition of H2	ChEMBL		None	None	None		CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1	10.6019/CHEMBL4507273
	CHEMBL4520788	216439	None	12	Human	Binding	pKi	=	7.7	7.7	3	26	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	10.6019/CHEMBL5212743
	156021166	178442	None	0	Human	Binding	pKi	=	7.7	7.7	-	1	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	178442	None	0	Human	Binding	pKi	=	7.7	7.7	-	1	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	178442	None	0	Human	Binding	pKi	=	7.7	7.7	-	1	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	217996	None	0	Human	Binding	pKi	=	7.7	7.7	-	1	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	91869	None	12	Human	Binding	pKi	=	5.7	5.7	-14125	44	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	91869	None	12	Human	Binding	pKi	=	5.7	5.7	-14125	44	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	166262	None	0	Human	Binding	pKi	=	5.7	5.7	-5248	13	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	166262	None	0	Human	Binding	pKi	=	5.7	5.7	-5248	13	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	193150	None	0	Human	Binding	pKi	=	6.7	6.7	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193150	None	0	Human	Binding	pKi	=	6.7	6.7	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193150	None	0	Human	Binding	pKi	=	6.7	6.7	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	172703	None	0	Human	Binding	pKi	=	5.7	5.7	-575	3	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	172703	None	0	Human	Binding	pKi	=	5.7	5.7	-575	3	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	56870	None	0	Human	Binding	pKi	=	5.7	5.7	3	2	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	56870	None	0	Human	Binding	pKi	=	5.7	5.7	3	2	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	56870	None	0	Human	Binding	pKi	=	5.7	5.7	3	2	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	56870	None	0	Human	Binding	pKi	=	5.7	5.7	3	2	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
	197033	201608	None	42	Human	Binding	pKi	=	6.7	6.7	-19	18	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	319	3	0	3	3.9	Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1	10.6019/CHEMBL5442175
	CHEMBL589390	201608	None	42	Human	Binding	pKi	=	6.7	6.7	-19	18	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	319	3	0	3	3.9	Cc1ccc2c(c1)c1c(n2CCc2ccc(C)nc2)CCN(C)C1	10.6019/CHEMBL5442175
	3823	50235	None	31	Human	Binding	pKi	=	4.7	4.7	-66	11	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	50235	None	31	Human	Binding	pKi	=	4.7	4.7	-66	11	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	50235	None	31	Human	Binding	pKi	=	4.7	4.7	-66	11	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	193009	None	0	Human	Binding	pKi	=	5.7	5.7	-53	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193009	None	0	Human	Binding	pKi	=	5.7	5.7	-53	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193009	None	0	Human	Binding	pKi	=	5.7	5.7	-53	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	102850	None	0	Human	Binding	pKi	=	4.7	4.7	-562	3	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	102850	None	0	Human	Binding	pKi	=	4.7	4.7	-562	3	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	192957	None	0	Human	Binding	pKi	=	7.6	7.6	-18	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192957	None	0	Human	Binding	pKi	=	7.6	7.6	-18	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192957	None	0	Human	Binding	pKi	=	7.6	7.6	-18	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	4633	None	0	Human	Binding	pKi	=	5.7	5.7	-199	3	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	4633	None	0	Human	Binding	pKi	=	5.7	5.7	-199	3	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	4997	None	0	Human	Binding	pKi	=	4.7	4.7	-144	3	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	4997	None	0	Human	Binding	pKi	=	4.7	4.7	-144	3	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	96835	None	0	Human	Binding	pKi	=	4.7	4.7	-407	3	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	96835	None	0	Human	Binding	pKi	=	4.7	4.7	-407	3	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	100598	None	0	Human	Binding	pKi	=	4.7	4.7	-3548	3	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	100598	None	0	Human	Binding	pKi	=	4.7	4.7	-3548	3	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	102748	None	0	Human	Binding	pKi	=	4.7	4.7	-6165	3	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	102748	None	0	Human	Binding	pKi	=	4.7	4.7	-6165	3	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	217957	None	0	Human	Binding	pKi	=	6.6	6.6	-	1	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	184822	None	0	Human	Binding	pKi	=	6.6	6.6	75	4	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	184822	None	0	Human	Binding	pKi	=	6.6	6.6	75	4	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	205626	None	0	Human	Binding	pKi	=	4.6	4.6	-2089	3	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	205626	None	0	Human	Binding	pKi	=	4.6	4.6	-2089	3	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	205691	None	0	Human	Binding	pKi	=	4.6	4.6	-3548	3	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	205691	None	0	Human	Binding	pKi	=	4.6	4.6	-3548	3	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	5105	None	0	Human	Binding	pKi	=	4.6	4.6	-194	4	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	5105	None	0	Human	Binding	pKi	=	4.6	4.6	-194	4	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	204485	None	0	Human	Binding	pKi	=	4.6	4.6	-9549	3	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	204485	None	0	Human	Binding	pKi	=	4.6	4.6	-9549	3	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
	1971	2866	None	32	Human	Binding	pKi	=	5.6	5.6	-16	29	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
	2404	2866	None	32	Human	Binding	pKi	=	5.6	5.6	-16	29	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
	4543	2866	None	32	Human	Binding	pKi	=	5.6	5.6	-16	29	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
	4543.0	2866	None	32	Human	Binding	pKi	=	5.6	5.6	-16	29	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
	CHEMBL445	2866	None	32	Human	Binding	pKi	=	5.6	5.6	-16	29	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
	DB00540	2866	None	32	Human	Binding	pKi	=	5.6	5.6	-16	29	DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine)	ChEMBL	263	3	1	1	3.8	CNCCC=C1c2ccccc2CCc2c1cccc2	nan
	44334214	4617	None	0	Human	Binding	pKi	=	5.6	5.6	-380	3	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	4617	None	0	Human	Binding	pKi	=	5.6	5.6	-380	3	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	192888	None	0	Human	Binding	pKi	=	6.6	6.6	3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192888	None	0	Human	Binding	pKi	=	6.6	6.6	3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192888	None	0	Human	Binding	pKi	=	6.6	6.6	3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193129	None	0	Human	Binding	pKi	=	6.6	6.6	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193129	None	0	Human	Binding	pKi	=	6.6	6.6	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193129	None	0	Human	Binding	pKi	=	6.6	6.6	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	204135	None	0	Human	Binding	pKi	=	4.6	4.6	-1096	3	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	204135	None	0	Human	Binding	pKi	=	4.6	4.6	-1096	3	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	5052	None	0	Human	Binding	pKi	=	4.6	4.6	-63	3	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	5052	None	0	Human	Binding	pKi	=	4.6	4.6	-63	3	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	5091	None	0	Human	Binding	pKi	=	4.6	4.6	-11220	4	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	5091	None	0	Human	Binding	pKi	=	4.6	4.6	-11220	4	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	108605	None	0	Human	Binding	pKi	=	4.6	4.6	-26	3	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	108605	None	0	Human	Binding	pKi	=	4.6	4.6	-26	3	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	189810	None	0	Human	Binding	pKi	=	5.6	5.6	-40	15	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	189810	None	0	Human	Binding	pKi	=	5.6	5.6	-40	15	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	193004	None	0	Human	Binding	pKi	=	6.6	6.6	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193004	None	0	Human	Binding	pKi	=	6.6	6.6	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193004	None	0	Human	Binding	pKi	=	6.6	6.6	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	101050	None	0	Human	Binding	pKi	=	4.6	4.6	-426	3	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	101050	None	0	Human	Binding	pKi	=	4.6	4.6	-426	3	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	102193	None	0	Human	Binding	pKi	=	4.6	4.6	-891	3	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	102193	None	0	Human	Binding	pKi	=	4.6	4.6	-891	3	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	171788	None	0	Human	Binding	pKi	=	5.6	5.6	-93	27	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	171788	None	0	Human	Binding	pKi	=	5.6	5.6	-93	27	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	218045	None	0	Human	Binding	pKi	=	6.6	6.6	-	1	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	218045	None	0	Human	Binding	pKi	=	6.6	6.6	-	1	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	170166	None	0	Human	Binding	pKi	=	4.6	4.6	-3981	3	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	170166	None	0	Human	Binding	pKi	=	4.6	4.6	-3981	3	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	1424	None	16	Human	Binding	pKi	=	4.6	4.6	-123	7	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	1424	None	16	Human	Binding	pKi	=	4.6	4.6	-123	7	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	1424	None	16	Human	Binding	pKi	=	4.6	4.6	-123	7	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	1424	None	16	Human	Binding	pKi	=	4.6	4.6	-123	7	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	167262	None	0	Human	Binding	pKi	=	6.6	6.6	-10	17	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	167262	None	0	Human	Binding	pKi	=	6.6	6.6	-10	17	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	206466	None	47	Human	Binding	pKi	=	5.6	5.6	-20	11	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	206466	None	47	Human	Binding	pKi	=	5.6	5.6	-20	11	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	206466	None	47	Human	Binding	pKi	=	5.6	5.6	-20	11	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	919	None	48	Human	Binding	pKi	=	5.6	5.6	-85	72	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
	2726.0	919	None	48	Human	Binding	pKi	=	5.6	5.6	-85	72	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	919	None	48	Human	Binding	pKi	=	5.6	5.6	-85	72	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	919	None	48	Human	Binding	pKi	=	5.6	5.6	-85	72	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	919	None	48	Human	Binding	pKi	=	5.6	5.6	-85	72	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	919	None	48	Human	Binding	pKi	=	5.6	5.6	-85	72	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
	13394327	193882	None	0	Human	Binding	pKi	=	7.6	7.6	-	1	Antagonist activity at histamine H2 receptor (unknown origin) assessed as inhibition constantAntagonist activity at histamine H2 receptor (unknown origin) assessed as inhibition constant	ChEMBL	297	8	2	8	1.7	CN(C)Cc1ccc(CSCCNc2nonc2N)o1	10.1021/acs.jmedchem.0c01901
	CHEMBL5273718	193882	None	0	Human	Binding	pKi	=	7.6	7.6	-	1	Antagonist activity at histamine H2 receptor (unknown origin) assessed as inhibition constantAntagonist activity at histamine H2 receptor (unknown origin) assessed as inhibition constant	ChEMBL	297	8	2	8	1.7	CN(C)Cc1ccc(CSCCNc2nonc2N)o1	10.1021/acs.jmedchem.0c01901
	168273745	192917	None	0	Human	Binding	pKi	=	7.6	7.6	-13	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192917	None	0	Human	Binding	pKi	=	7.6	7.6	-13	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192917	None	0	Human	Binding	pKi	=	7.6	7.6	-13	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	173314	None	0	Human	Binding	pKi	=	5.6	5.6	-234	7	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	173314	None	0	Human	Binding	pKi	=	5.6	5.6	-234	7	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
	156419	938	None	48	Human	Binding	pKi	=	5.6	5.6	-66	15	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	357	6	1	1	6.1	C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F	10.6019/CHEMBL5442175
	156419.0	938	None	48	Human	Binding	pKi	=	5.6	5.6	-66	15	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	357	6	1	1	6.1	C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F	10.6019/CHEMBL5442175
	3308	938	None	48	Human	Binding	pKi	=	5.6	5.6	-66	15	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	357	6	1	1	6.1	C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F	10.6019/CHEMBL5442175
	647	938	None	48	Human	Binding	pKi	=	5.6	5.6	-66	15	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	357	6	1	1	6.1	C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F	10.6019/CHEMBL5442175
	CHEMBL1201284	938	None	48	Human	Binding	pKi	=	5.6	5.6	-66	15	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	357	6	1	1	6.1	C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F	10.6019/CHEMBL5442175
	DB01012	938	None	48	Human	Binding	pKi	=	5.6	5.6	-66	15	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	357	6	1	1	6.1	C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F	10.6019/CHEMBL5442175
	1204	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	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	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	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	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	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	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	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
	774.0	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	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	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	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	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	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	218031	None	0	Human	Binding	pKi	=	6.6	6.6	-	1	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	218031	None	0	Human	Binding	pKi	=	6.6	6.6	-	1	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	218043	None	0	Human	Binding	pKi	=	6.6	6.6	-	1	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	218043	None	0	Human	Binding	pKi	=	6.6	6.6	-	1	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	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	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	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	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	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	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	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	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
	774.0	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	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	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	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	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	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	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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
	774.0	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	1932	None	74	Human	Binding	pKi	=	6.6	6.6	-173	24	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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
	8868	3547	None	23	Human	Binding	pKi	=	5.6	5.6	-8912	7	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	397	4	1	2	5.9	Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1	10.6019/CHEMBL5442175
	9887077	3547	None	23	Human	Binding	pKi	=	5.6	5.6	-8912	7	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	397	4	1	2	5.9	Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1	10.6019/CHEMBL5442175
	CHEMBL513136	3547	None	23	Human	Binding	pKi	=	5.6	5.6	-8912	7	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	397	4	1	2	5.9	Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1	10.6019/CHEMBL5442175
	156015793	178364	None	0	Human	Binding	pKi	=	6.6	6.6	-	1	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	178364	None	0	Human	Binding	pKi	=	6.6	6.6	-	1	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	178364	None	0	Human	Binding	pKi	=	6.6	6.6	-	1	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	205409	None	0	Human	Binding	pKi	=	5.6	5.6	-338	3	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	205409	None	0	Human	Binding	pKi	=	5.6	5.6	-338	3	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
	CHEMBL5086970	217548	None	0	Human	Binding	pKi	=	5.6	5.6	1	2	GPCRScan assay: inhibition of H2GPCRScan assay: inhibition of H2	ChEMBL		None	None	None		COc1ccc(CC[C@@H](OC(=O)[C@H]2CCCCN2C(=O)[C@@H](c2cc(OC)c(OC)c(OC)c2)C2CCCCC2)c2cccc(OCCN3CCOCC3)c2)cc1OC	10.6019/CHEMBL5058648
	44304516	165451	None	0	Human	Binding	pKi	=	4.6	4.6	-630	3	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	165451	None	0	Human	Binding	pKi	=	4.6	4.6	-630	3	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	206817	None	38	Human	Binding	pKi	=	4.6	4.6	-	1	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	206817	None	38	Human	Binding	pKi	=	4.6	4.6	-	1	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	206817	None	38	Human	Binding	pKi	=	4.6	4.6	-	1	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	168122	None	0	Human	Binding	pKi	=	4.6	4.6	-1000	3	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	168122	None	0	Human	Binding	pKi	=	4.6	4.6	-1000	3	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	203944	None	0	Human	Binding	pKi	=	4.6	4.6	-616	3	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	203944	None	0	Human	Binding	pKi	=	4.6	4.6	-616	3	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	57087	None	0	Human	Binding	pKi	=	6.6	6.6	-7	16	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	57087	None	0	Human	Binding	pKi	=	6.6	6.6	-7	16	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	185049	None	0	Human	Binding	pKi	=	7.5	7.5	-2	6	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	185049	None	0	Human	Binding	pKi	=	7.5	7.5	-2	6	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	185768	None	0	Human	Binding	pKi	=	7.5	7.5	446	4	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	185768	None	0	Human	Binding	pKi	=	7.5	7.5	446	4	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	3182	None	26	Human	Binding	pKi	=	5.6	5.6	-53	28	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	3182	None	26	Human	Binding	pKi	=	5.6	5.6	-53	28	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	3182	None	26	Human	Binding	pKi	=	5.6	5.6	-53	28	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	3182	None	26	Human	Binding	pKi	=	5.6	5.6	-53	28	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	3182	None	26	Human	Binding	pKi	=	5.6	5.6	-53	28	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	89762	None	0	Human	Binding	pKi	=	5.6	5.6	-346	6	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	89762	None	0	Human	Binding	pKi	=	5.6	5.6	-346	6	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
	11498	3019	None	34	Human	Binding	pKi	=	5.6	5.6	-173	13	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	392	3	1	5	4.1	CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC	10.6019/CHEMBL5442175
	4995951	3019	None	34	Human	Binding	pKi	=	5.6	5.6	-173	13	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	392	3	1	5	4.1	CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC	10.6019/CHEMBL5442175
	CHEMBL59898	3019	None	34	Human	Binding	pKi	=	5.6	5.6	-173	13	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	392	3	1	5	4.1	CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC	10.6019/CHEMBL5442175
	132060743	162330	None	0	Human	Binding	pKi	=	6.5	6.5	-1	13	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	162330	None	0	Human	Binding	pKi	=	6.5	6.5	-1	13	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	102913	None	65	Human	Binding	pKi	=	5.5	5.5	-24	25	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
	3191.0	102913	None	65	Human	Binding	pKi	=	5.5	5.5	-24	25	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	102913	None	65	Human	Binding	pKi	=	5.5	5.5	-24	25	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
	DB11742	102913	None	65	Human	Binding	pKi	=	5.5	5.5	-24	25	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	108606	None	0	Human	Binding	pKi	=	4.5	4.5	-1023	4	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	108606	None	0	Human	Binding	pKi	=	4.5	4.5	-1023	4	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	4865	None	0	Human	Binding	pKi	=	6.5	6.5	-75	3	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	4865	None	0	Human	Binding	pKi	=	6.5	6.5	-75	3	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	109273	None	0	Human	Binding	pKi	=	6.5	6.5	-57	3	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	109273	None	0	Human	Binding	pKi	=	6.5	6.5	-57	3	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	1932	None	74	Human	Binding	pKi	=	6.5	6.5	-173	24	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	1932	None	74	Human	Binding	pKi	=	6.5	6.5	-173	24	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	1932	None	74	Human	Binding	pKi	=	6.5	6.5	-173	24	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	1932	None	74	Human	Binding	pKi	=	6.5	6.5	-173	24	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
	774.0	1932	None	74	Human	Binding	pKi	=	6.5	6.5	-173	24	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	1932	None	74	Human	Binding	pKi	=	6.5	6.5	-173	24	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	1932	None	74	Human	Binding	pKi	=	6.5	6.5	-173	24	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	205310	None	0	Human	Binding	pKi	=	4.5	4.5	-6606	3	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	205310	None	0	Human	Binding	pKi	=	4.5	4.5	-6606	3	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
	CHEMBL5086970	217548	None	0	Human	Binding	pKi	=	5.5	5.5	1	2	GPCRScan assay: inhibition of H2GPCRScan assay: inhibition of H2	ChEMBL		None	None	None		COc1ccc(CC[C@@H](OC(=O)[C@H]2CCCCN2C(=O)[C@@H](c2cc(OC)c(OC)c(OC)c2)C2CCCCC2)c2cccc(OCCN3CCOCC3)c2)cc1OC	10.6019/CHEMBL5058648
	44634573	2748	None	1	Human	Binding	pKi	=	5.5	5.5	-28	12	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	465	6	0	2	5.0	Cc1n(C/C=C/c2ccccc2)c2[n+](c1P(=S)(c1ccccc1)c1ccccc1)cccc2	10.6019/CHEMBL5442175
	9168	2748	None	1	Human	Binding	pKi	=	5.5	5.5	-28	12	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	465	6	0	2	5.0	Cc1n(C/C=C/c2ccccc2)c2[n+](c1P(=S)(c1ccccc1)c1ccccc1)cccc2	10.6019/CHEMBL5442175
	CHEMBL1474387	2748	None	1	Human	Binding	pKi	=	5.5	5.5	-28	12	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	465	6	0	2	5.0	Cc1n(C/C=C/c2ccccc2)c2[n+](c1P(=S)(c1ccccc1)c1ccccc1)cccc2	10.6019/CHEMBL5442175
	CHEMBL1622930	2748	None	1	Human	Binding	pKi	=	5.5	5.5	-28	12	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	465	6	0	2	5.0	Cc1n(C/C=C/c2ccccc2)c2[n+](c1P(=S)(c1ccccc1)c1ccccc1)cccc2	10.6019/CHEMBL5442175
	168294767	193128	None	0	Human	Binding	pKi	=	8.5	8.5	-117	20	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193128	None	0	Human	Binding	pKi	=	8.5	8.5	-117	20	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193128	None	0	Human	Binding	pKi	=	8.5	8.5	-117	20	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	218026	None	0	Human	Binding	pKi	=	7.5	7.5	-	1	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	218026	None	0	Human	Binding	pKi	=	7.5	7.5	-	1	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	186535	None	0	Human	Binding	pKi	=	7.5	7.5	95	4	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	186535	None	0	Human	Binding	pKi	=	7.5	7.5	95	4	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	186038	None	0	Human	Binding	pKi	=	7.5	7.5	165	4	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	186038	None	0	Human	Binding	pKi	=	7.5	7.5	165	4	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	76809	None	6	Human	Binding	pKi	=	6.5	6.5	-223	17	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	76809	None	6	Human	Binding	pKi	=	6.5	6.5	-223	17	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	76809	None	6	Human	Binding	pKi	=	6.5	6.5	-223	17	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	178439	None	0	Human	Binding	pKi	=	6.5	6.5	-	1	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	178439	None	0	Human	Binding	pKi	=	6.5	6.5	-	1	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	178439	None	0	Human	Binding	pKi	=	6.5	6.5	-	1	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	192955	None	0	Human	Binding	pKi	=	6.5	6.5	-20	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192955	None	0	Human	Binding	pKi	=	6.5	6.5	-20	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192955	None	0	Human	Binding	pKi	=	6.5	6.5	-20	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192960	None	0	Human	Binding	pKi	=	6.5	6.5	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192960	None	0	Human	Binding	pKi	=	6.5	6.5	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192960	None	0	Human	Binding	pKi	=	6.5	6.5	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	2341	None	28	Human	Binding	pKi	=	5.5	5.5	-128	18	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	2341	None	28	Human	Binding	pKi	=	5.5	5.5	-128	18	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
	3955.0	2341	None	28	Human	Binding	pKi	=	5.5	5.5	-128	18	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	2341	None	28	Human	Binding	pKi	=	5.5	5.5	-128	18	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	2341	None	28	Human	Binding	pKi	=	5.5	5.5	-128	18	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	2341	None	28	Human	Binding	pKi	=	5.5	5.5	-128	18	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	92600	None	0	Human	Binding	pKi	=	5.5	5.5	-3	7	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	92600	None	0	Human	Binding	pKi	=	5.5	5.5	-3	7	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	193144	None	0	Human	Binding	pKi	=	6.5	6.5	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193144	None	0	Human	Binding	pKi	=	6.5	6.5	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193144	None	0	Human	Binding	pKi	=	6.5	6.5	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	184542	None	0	Human	Binding	pKi	=	7.5	7.5	-1	6	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	184542	None	0	Human	Binding	pKi	=	7.5	7.5	-1	6	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	184690	None	0	Human	Binding	pKi	=	7.5	7.5	323	4	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	184690	None	0	Human	Binding	pKi	=	7.5	7.5	323	4	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	107892	None	0	Human	Binding	pKi	=	4.5	4.5	-36	3	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	107892	None	0	Human	Binding	pKi	=	4.5	4.5	-36	3	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	193033	None	0	Human	Binding	pKi	=	6.5	6.5	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193033	None	0	Human	Binding	pKi	=	6.5	6.5	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193033	None	0	Human	Binding	pKi	=	6.5	6.5	2	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	56456	None	0	Human	Binding	pKi	=	5.5	5.5	-29512	8	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	56456	None	0	Human	Binding	pKi	=	5.5	5.5	-29512	8	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	102949	None	0	Human	Binding	pKi	=	5.5	5.5	-100	3	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	102949	None	0	Human	Binding	pKi	=	5.5	5.5	-100	3	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	185366	None	0	Human	Binding	pKi	=	5.5	5.5	7	2	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	185366	None	0	Human	Binding	pKi	=	5.5	5.5	7	2	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	89760	None	0	Human	Binding	pKi	=	5.5	5.5	-223	6	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	89760	None	0	Human	Binding	pKi	=	5.5	5.5	-223	6	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	209218	None	0	Human	Binding	pKi	=	4.5	4.5	-31	3	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	209218	None	0	Human	Binding	pKi	=	4.5	4.5	-31	3	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	101073	None	0	Human	Binding	pKi	=	4.5	4.5	-10000	3	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	101073	None	0	Human	Binding	pKi	=	4.5	4.5	-10000	3	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	102262	None	0	Human	Binding	pKi	=	4.5	4.5	-14791	3	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	102262	None	0	Human	Binding	pKi	=	4.5	4.5	-14791	3	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	102345	None	0	Human	Binding	pKi	=	4.5	4.5	-1862	3	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	102345	None	0	Human	Binding	pKi	=	4.5	4.5	-1862	3	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	187587	None	0	Human	Binding	pKi	=	4.5	4.5	-5888	5	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	187587	None	0	Human	Binding	pKi	=	4.5	4.5	-5888	5	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	155239	None	0	Human	Binding	pKi	=	5.5	5.5	-44	12	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	155239	None	0	Human	Binding	pKi	=	5.5	5.5	-44	12	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	84109	None	0	Human	Binding	pKi	=	5.5	5.5	-2089	7	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	84109	None	0	Human	Binding	pKi	=	5.5	5.5	-2089	7	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	206017	None	0	Human	Binding	pKi	=	5.5	5.5	-275	4	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	206017	None	0	Human	Binding	pKi	=	5.5	5.5	-275	4	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	178400	None	0	Human	Binding	pKi	=	6.5	6.5	-	1	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	178400	None	0	Human	Binding	pKi	=	6.5	6.5	-	1	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	178400	None	0	Human	Binding	pKi	=	6.5	6.5	-	1	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	217836	None	0	Human	Binding	pKi	=	7.5	7.5	-	1	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	192918	None	0	Human	Binding	pKi	=	7.5	7.5	-6	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192918	None	0	Human	Binding	pKi	=	7.5	7.5	-6	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192918	None	0	Human	Binding	pKi	=	7.5	7.5	-6	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	4631	None	0	Human	Binding	pKi	=	6.5	6.5	-72	3	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	4631	None	0	Human	Binding	pKi	=	6.5	6.5	-72	3	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
	70682037	75908	None	21	Human	Binding	pKi	=	5.5	5.5	-537	9	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	495	5	0	8	3.6	Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1	10.6019/CHEMBL5442175
	CHEMBL2048820	75908	None	21	Human	Binding	pKi	=	5.5	5.5	-537	9	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	495	5	0	8	3.6	Cc1cn2cc(CC(=O)N3CCC4(CC3)CN(Cc3ccc(-n5nccn5)cc3Cl)C4)nc2s1	10.6019/CHEMBL5442175
	168273549	192912	None	0	Human	Binding	pKi	=	6.5	6.5	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192912	None	0	Human	Binding	pKi	=	6.5	6.5	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192912	None	0	Human	Binding	pKi	=	6.5	6.5	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	5299	None	0	Human	Binding	pKi	=	4.5	4.5	-144	3	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	5299	None	0	Human	Binding	pKi	=	4.5	4.5	-144	3	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	102865	None	0	Human	Binding	pKi	=	4.5	4.5	-1096	3	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	102865	None	0	Human	Binding	pKi	=	4.5	4.5	-1096	3	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	185090	None	0	Human	Binding	pKi	=	6.5	6.5	162	4	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	185090	None	0	Human	Binding	pKi	=	6.5	6.5	162	4	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	138435	None	0	Human	Binding	pKi	=	5.5	5.5	-120	15	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	138435	None	0	Human	Binding	pKi	=	5.5	5.5	-120	15	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	138435	None	0	Human	Binding	pKi	=	5.5	5.5	-120	15	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	138435	None	0	Human	Binding	pKi	=	5.5	5.5	-120	15	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	138435	None	0	Human	Binding	pKi	=	5.5	5.5	-120	15	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	138435	None	0	Human	Binding	pKi	=	5.5	5.5	-120	15	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	4560	None	0	Human	Binding	pKi	=	4.5	4.5	-263	4	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	4560	None	0	Human	Binding	pKi	=	4.5	4.5	-263	4	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	192875	None	0	Human	Binding	pKi	=	6.5	6.5	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192875	None	0	Human	Binding	pKi	=	6.5	6.5	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192875	None	0	Human	Binding	pKi	=	6.5	6.5	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	205446	None	0	Human	Binding	pKi	=	5.5	5.5	-30	3	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	205446	None	0	Human	Binding	pKi	=	5.5	5.5	-30	3	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	205340	None	0	Human	Binding	pKi	=	4.5	4.5	-4897	3	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	205340	None	0	Human	Binding	pKi	=	4.5	4.5	-4897	3	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	205375	None	0	Human	Binding	pKi	=	4.5	4.5	-3388	3	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	205375	None	0	Human	Binding	pKi	=	4.5	4.5	-3388	3	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	92591	None	0	Human	Binding	pKi	=	5.5	5.5	1	3	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	92591	None	0	Human	Binding	pKi	=	5.5	5.5	1	3	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	207323	None	37	Human	Binding	pKi	=	5.5	5.5	-3	13	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	207323	None	37	Human	Binding	pKi	=	5.5	5.5	-3	13	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	207323	None	37	Human	Binding	pKi	=	5.5	5.5	-3	13	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	207323	None	37	Human	Binding	pKi	=	5.5	5.5	-3	13	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	185380	None	0	Human	Binding	pKi	=	7.5	7.5	223	4	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	185380	None	0	Human	Binding	pKi	=	7.5	7.5	223	4	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	4537	None	0	Human	Binding	pKi	=	5.5	5.5	-93	3	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	4537	None	0	Human	Binding	pKi	=	5.5	5.5	-93	3	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	178345	None	0	Human	Binding	pKi	=	5.5	5.5	-1548	4	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	178345	None	0	Human	Binding	pKi	=	5.5	5.5	-1548	4	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	178345	None	0	Human	Binding	pKi	=	5.5	5.5	-1548	4	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	958	None	57	Human	Binding	pKi	=	5.5	5.5	-64	91	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
	135398737.0	958	None	57	Human	Binding	pKi	=	5.5	5.5	-64	91	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	958	None	57	Human	Binding	pKi	=	5.5	5.5	-64	91	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	958	None	57	Human	Binding	pKi	=	5.5	5.5	-64	91	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	958	None	57	Human	Binding	pKi	=	5.5	5.5	-64	91	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	958	None	57	Human	Binding	pKi	=	5.5	5.5	-64	91	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	83835	None	0	Human	Binding	pKi	=	5.5	5.5	-3	12	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	83835	None	0	Human	Binding	pKi	=	5.5	5.5	-3	12	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	83835	None	0	Human	Binding	pKi	=	5.5	5.5	-3	12	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	83835	None	0	Human	Binding	pKi	=	5.5	5.5	-3	12	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	171947	None	0	Human	Binding	pKi	=	5.4	5.4	-15	3	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	171947	None	0	Human	Binding	pKi	=	5.4	5.4	-15	3	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	949	None	27	Human	Binding	pKi	=	6.4	6.4	-177	21	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
	26987.0	949	None	27	Human	Binding	pKi	=	6.4	6.4	-177	21	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	949	None	27	Human	Binding	pKi	=	6.4	6.4	-177	21	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	949	None	27	Human	Binding	pKi	=	6.4	6.4	-177	21	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	949	None	27	Human	Binding	pKi	=	6.4	6.4	-177	21	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	949	None	27	Human	Binding	pKi	=	6.4	6.4	-177	21	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	169924	None	0	Human	Binding	pKi	=	5.4	5.4	-177	3	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	169924	None	0	Human	Binding	pKi	=	5.4	5.4	-177	3	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	164770	None	0	Human	Binding	pKi	=	6.4	6.4	-12	13	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	164770	None	0	Human	Binding	pKi	=	6.4	6.4	-12	13	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	184650	None	0	Human	Binding	pKi	=	7.4	7.4	158	4	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	184650	None	0	Human	Binding	pKi	=	7.4	7.4	158	4	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	205571	None	0	Human	Binding	pKi	=	5.4	5.4	-12	3	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	205571	None	0	Human	Binding	pKi	=	5.4	5.4	-12	3	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	205761	None	0	Human	Binding	pKi	=	5.4	5.4	-371	3	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	205761	None	0	Human	Binding	pKi	=	5.4	5.4	-371	3	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	205653	None	0	Human	Binding	pKi	=	4.4	4.4	-4073	3	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	205653	None	0	Human	Binding	pKi	=	4.4	4.4	-4073	3	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	205983	None	0	Human	Binding	pKi	=	5.4	5.4	-1513	4	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	205983	None	0	Human	Binding	pKi	=	5.4	5.4	-1513	4	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
	CHEMBL4558518	216481	None	0	Human	Binding	pKi	=	5.4	5.4	-177	14	GPCRScan assay: inhibition of H2GPCRScan assay: inhibition of H2	ChEMBL		None	None	None		CC(C)(C)OC(=O)N1CCCC1CNC1CCC(c2cc(F)ccc2F)(S(=O)(=O)c2ccc(Cl)cc2)CC1	10.6019/CHEMBL4507288
	CHEMBL4558518	216481	None	0	Human	Binding	pKi	=	5.4	5.4	-177	14	Selectivity interaction (GPCR panel (PDSP screen)) EUB0000741a HRH2Selectivity interaction (GPCR panel (PDSP screen)) EUB0000741a HRH2	ChEMBL		None	None	None		CC(C)(C)OC(=O)N1CCCC1CNC1CCC(c2cc(F)ccc2F)(S(=O)(=O)c2ccc(Cl)cc2)CC1	10.6019/CHEMBL5212743
	44334782	5427	None	0	Human	Binding	pKi	=	6.4	6.4	-91	3	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	5427	None	0	Human	Binding	pKi	=	6.4	6.4	-91	3	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	192944	None	0	Human	Binding	pKi	=	6.4	6.4	-1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192944	None	0	Human	Binding	pKi	=	6.4	6.4	-1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192944	None	0	Human	Binding	pKi	=	6.4	6.4	-1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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
	CHEMBL4558518	216481	None	0	Human	Binding	pKi	=	5.4	5.4	-177	14	GPCRScan assay: inhibition of H2GPCRScan assay: inhibition of H2	ChEMBL		None	None	None		CC(C)(C)OC(=O)N1CCCC1CNC1CCC(c2cc(F)ccc2F)(S(=O)(=O)c2ccc(Cl)cc2)CC1	10.6019/CHEMBL4507288
	44335571	5274	None	0	Human	Binding	pKi	=	4.4	4.4	-1513	4	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	5274	None	0	Human	Binding	pKi	=	4.4	4.4	-1513	4	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	205325	None	0	Human	Binding	pKi	=	4.4	4.4	-478	3	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	205325	None	0	Human	Binding	pKi	=	4.4	4.4	-478	3	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	193002	None	0	Human	Binding	pKi	=	6.4	6.4	-22	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193002	None	0	Human	Binding	pKi	=	6.4	6.4	-22	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193002	None	0	Human	Binding	pKi	=	6.4	6.4	-22	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193019	None	0	Human	Binding	pKi	=	6.4	6.4	-22	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193019	None	0	Human	Binding	pKi	=	6.4	6.4	-22	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193019	None	0	Human	Binding	pKi	=	6.4	6.4	-22	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	92593	None	0	Human	Binding	pKi	=	5.4	5.4	-4	7	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	92593	None	0	Human	Binding	pKi	=	5.4	5.4	-4	7	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	184560	None	0	Human	Binding	pKi	=	7.4	7.4	1	6	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	184560	None	0	Human	Binding	pKi	=	7.4	7.4	1	6	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	82440	None	34	Human	Binding	pKi	=	6.4	6.4	-27	23	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	82440	None	34	Human	Binding	pKi	=	6.4	6.4	-27	23	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	5123	None	0	Human	Binding	pKi	=	5.4	5.4	-144	3	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	5123	None	0	Human	Binding	pKi	=	5.4	5.4	-144	3	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	15502	None	19	Human	Binding	pKi	=	5.4	5.4	-25	7	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	15502	None	19	Human	Binding	pKi	=	5.4	5.4	-25	7	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	206960	None	0	Human	Binding	pKi	=	5.4	5.4	-125	3	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	206960	None	0	Human	Binding	pKi	=	5.4	5.4	-125	3	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	15502	None	19	Human	Binding	pKi	=	5.4	5.4	-25	7	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	15502	None	19	Human	Binding	pKi	=	5.4	5.4	-25	7	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	186175	None	0	Human	Binding	pKi	=	5.4	5.4	7	2	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	186175	None	0	Human	Binding	pKi	=	5.4	5.4	7	2	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	1932	None	74	Human	Binding	pKi	=	4.4	4.4	-173	24	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	1932	None	74	Human	Binding	pKi	=	4.4	4.4	-173	24	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	1932	None	74	Human	Binding	pKi	=	4.4	4.4	-173	24	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	1932	None	74	Human	Binding	pKi	=	4.4	4.4	-173	24	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
	774.0	1932	None	74	Human	Binding	pKi	=	4.4	4.4	-173	24	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	1932	None	74	Human	Binding	pKi	=	4.4	4.4	-173	24	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	1932	None	74	Human	Binding	pKi	=	4.4	4.4	-173	24	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	205386	None	0	Human	Binding	pKi	=	4.4	4.4	-7943	3	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	205386	None	0	Human	Binding	pKi	=	4.4	4.4	-7943	3	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	162882	None	0	Human	Binding	pKi	=	4.4	4.4	-1348	3	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	162882	None	0	Human	Binding	pKi	=	4.4	4.4	-1348	3	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	185483	None	0	Human	Binding	pKi	=	8.4	8.4	-85	20	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	185483	None	0	Human	Binding	pKi	=	8.4	8.4	-85	20	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	7974	None	0	Human	Binding	pKi	=	8.4	8.4	-6	2	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	7974	None	0	Human	Binding	pKi	=	8.4	8.4	-6	2	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	192910	None	0	Human	Binding	pKi	=	8.3	8.3	12	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192910	None	0	Human	Binding	pKi	=	8.3	8.3	12	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192910	None	0	Human	Binding	pKi	=	8.3	8.3	12	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	83827	None	0	Human	Binding	pKi	=	6.4	6.4	-12	10	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	83827	None	0	Human	Binding	pKi	=	6.4	6.4	-12	10	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	110101	None	0	Human	Binding	pKi	=	5.4	5.4	-79	3	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	110101	None	0	Human	Binding	pKi	=	5.4	5.4	-79	3	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	4761	None	0	Human	Binding	pKi	=	4.4	4.4	-128	3	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	4761	None	0	Human	Binding	pKi	=	4.4	4.4	-128	3	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	166803	None	0	Human	Binding	pKi	=	6.4	6.4	-3	11	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	166803	None	0	Human	Binding	pKi	=	6.4	6.4	-3	11	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	2182	None	36	Human	Binding	pKi	=	5.4	5.4	-151	24	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	2182	None	36	Human	Binding	pKi	=	5.4	5.4	-151	24	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
	3827.0	2182	None	36	Human	Binding	pKi	=	5.4	5.4	-151	24	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	2182	None	36	Human	Binding	pKi	=	5.4	5.4	-151	24	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	2182	None	36	Human	Binding	pKi	=	5.4	5.4	-151	24	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	2182	None	36	Human	Binding	pKi	=	5.4	5.4	-151	24	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	217773	None	0	Human	Binding	pKi	=	6.4	6.4	-	1	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	5778	None	7	Human	Binding	pKi	=	5.4	5.4	-70	4	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	5778	None	7	Human	Binding	pKi	=	5.4	5.4	-70	4	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	205290	None	0	Human	Binding	pKi	=	4.4	4.4	-21379	3	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	205290	None	0	Human	Binding	pKi	=	4.4	4.4	-21379	3	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	1621	None	68	Human	Binding	pKi	=	7.4	7.4	-1	2	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	1621	None	68	Human	Binding	pKi	=	7.4	7.4	-1	2	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	1621	None	68	Human	Binding	pKi	=	7.4	7.4	-1	2	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	1621	None	68	Human	Binding	pKi	=	7.4	7.4	-1	2	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	1621	None	68	Human	Binding	pKi	=	7.4	7.4	-1	2	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	1621	None	68	Human	Binding	pKi	=	7.4	7.4	-1	2	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	1621	None	68	Human	Binding	pKi	=	7.4	7.4	-1	2	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	205373	None	0	Human	Binding	pKi	=	4.4	4.4	-2041	3	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	205373	None	0	Human	Binding	pKi	=	4.4	4.4	-2041	3	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	84110	None	0	Human	Binding	pKi	=	5.4	5.4	-2187	7	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	84110	None	0	Human	Binding	pKi	=	5.4	5.4	-2187	7	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	90779	None	28	Human	Binding	pKi	=	5.4	5.4	-109	18	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	90779	None	28	Human	Binding	pKi	=	5.4	5.4	-109	18	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	184489	None	0	Human	Binding	pKi	=	6.4	6.4	75	4	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	184489	None	0	Human	Binding	pKi	=	6.4	6.4	75	4	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	90779	None	28	Human	Binding	pKi	=	5.4	5.4	-109	18	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	90779	None	28	Human	Binding	pKi	=	5.4	5.4	-109	18	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	169319	None	0	Human	Binding	pKi	=	4.4	4.4	-630	3	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	169319	None	0	Human	Binding	pKi	=	4.4	4.4	-630	3	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	186514	None	0	Human	Binding	pKi	=	7.4	7.4	144	4	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	186514	None	0	Human	Binding	pKi	=	7.4	7.4	144	4	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	56871	None	0	Human	Binding	pKi	=	5.4	5.4	-6	10	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	56871	None	0	Human	Binding	pKi	=	5.4	5.4	-6	10	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	56871	None	0	Human	Binding	pKi	=	5.4	5.4	-6	10	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	56871	None	0	Human	Binding	pKi	=	5.4	5.4	-6	10	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	56872	None	0	Human	Binding	pKi	=	5.4	5.4	-2	3	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	56872	None	0	Human	Binding	pKi	=	5.4	5.4	-2	3	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	56872	None	0	Human	Binding	pKi	=	5.4	5.4	-2	3	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	56872	None	0	Human	Binding	pKi	=	5.4	5.4	-2	3	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	202955	None	0	Human	Binding	pKi	=	5.4	5.4	-309	3	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	202955	None	0	Human	Binding	pKi	=	5.4	5.4	-309	3	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	186441	None	0	Human	Binding	pKi	=	5.4	5.4	3	2	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	186441	None	0	Human	Binding	pKi	=	5.4	5.4	3	2	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	192974	None	0	Human	Binding	pKi	=	5.4	5.4	-52	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192974	None	0	Human	Binding	pKi	=	5.4	5.4	-52	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192974	None	0	Human	Binding	pKi	=	5.4	5.4	-52	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193123	None	0	Human	Binding	pKi	=	6.3	6.3	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193123	None	0	Human	Binding	pKi	=	6.3	6.3	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193123	None	0	Human	Binding	pKi	=	6.3	6.3	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	100839	None	0	Human	Binding	pKi	=	4.3	4.3	-5370	3	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	100839	None	0	Human	Binding	pKi	=	4.3	4.3	-5370	3	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	185674	None	0	Human	Binding	pKi	=	7.3	7.3	95	4	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	185674	None	0	Human	Binding	pKi	=	7.3	7.3	95	4	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	84114	None	0	Human	Binding	pKi	=	6.3	6.3	-75	7	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	84114	None	0	Human	Binding	pKi	=	6.3	6.3	-75	7	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	107323	None	0	Human	Binding	pKi	=	4.3	4.3	-77	3	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	107323	None	0	Human	Binding	pKi	=	4.3	4.3	-77	3	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	205234	None	0	Human	Binding	pKi	=	4.3	4.3	-2570	3	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	205234	None	0	Human	Binding	pKi	=	4.3	4.3	-2570	3	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	204042	None	0	Human	Binding	pKi	=	4.3	4.3	-2041	3	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	204042	None	0	Human	Binding	pKi	=	4.3	4.3	-2041	3	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	101001	None	0	Human	Binding	pKi	=	4.3	4.3	-645	3	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	101001	None	0	Human	Binding	pKi	=	4.3	4.3	-645	3	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	937	None	69	Human	Binding	pKi	=	6.3	6.3	-4	8	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	937	None	69	Human	Binding	pKi	=	6.3	6.3	-4	8	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
	2756.0	937	None	69	Human	Binding	pKi	=	6.3	6.3	-4	8	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	937	None	69	Human	Binding	pKi	=	6.3	6.3	-4	8	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	937	None	69	Human	Binding	pKi	=	6.3	6.3	-4	8	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	937	None	69	Human	Binding	pKi	=	6.3	6.3	-4	8	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	124602	None	0	Human	Binding	pKi	=	5.3	5.3	3	2	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	124602	None	0	Human	Binding	pKi	=	5.3	5.3	3	2	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	193140	None	0	Human	Binding	pKi	=	8.3	8.3	-147	20	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193140	None	0	Human	Binding	pKi	=	8.3	8.3	-147	20	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193140	None	0	Human	Binding	pKi	=	8.3	8.3	-147	20	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193082	None	0	Human	Binding	pKi	=	8.3	8.3	-537	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193082	None	0	Human	Binding	pKi	=	8.3	8.3	-537	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193082	None	0	Human	Binding	pKi	=	8.3	8.3	-537	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192914	None	0	Human	Binding	pKi	=	8.3	8.3	-6	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192914	None	0	Human	Binding	pKi	=	8.3	8.3	-6	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192914	None	0	Human	Binding	pKi	=	8.3	8.3	-6	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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
	3036780	107587	None	16	Human	Binding	pKi	=	8.2	8.2	-21	53	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
	3036780.0	107587	None	16	Human	Binding	pKi	=	8.2	8.2	-21	53	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	107587	None	16	Human	Binding	pKi	=	8.2	8.2	-21	53	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	107587	None	16	Human	Binding	pKi	=	8.2	8.2	-21	53	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
	9903970.0	107587	None	16	Human	Binding	pKi	=	8.2	8.2	-21	53	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	107587	None	16	Human	Binding	pKi	=	8.2	8.2	-21	53	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	107587	None	16	Human	Binding	pKi	=	8.2	8.2	-21	53	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
	CHEMBL504548	107587	None	16	Human	Binding	pKi	=	8.2	8.2	-21	53	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
	DB06216	107587	None	16	Human	Binding	pKi	=	8.2	8.2	-21	53	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
	3036780	107587	None	16	Human	Binding	pKi	=	8.2	8.2	-21	53	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
	3036780.0	107587	None	16	Human	Binding	pKi	=	8.2	8.2	-21	53	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	107587	None	16	Human	Binding	pKi	=	8.2	8.2	-21	53	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	107587	None	16	Human	Binding	pKi	=	8.2	8.2	-21	53	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
	9903970.0	107587	None	16	Human	Binding	pKi	=	8.2	8.2	-21	53	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	107587	None	16	Human	Binding	pKi	=	8.2	8.2	-21	53	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	107587	None	16	Human	Binding	pKi	=	8.2	8.2	-21	53	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
	CHEMBL504548	107587	None	16	Human	Binding	pKi	=	8.2	8.2	-21	53	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
	DB06216	107587	None	16	Human	Binding	pKi	=	8.2	8.2	-21	53	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	4963	None	0	Human	Binding	pKi	=	6.3	6.3	-144	3	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	4963	None	0	Human	Binding	pKi	=	6.3	6.3	-144	3	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	1932	None	74	Human	Binding	pKi	=	5.3	5.3	-173	24	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	1932	None	74	Human	Binding	pKi	=	5.3	5.3	-173	24	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	1932	None	74	Human	Binding	pKi	=	5.3	5.3	-173	24	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	1932	None	74	Human	Binding	pKi	=	5.3	5.3	-173	24	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
	774.0	1932	None	74	Human	Binding	pKi	=	5.3	5.3	-173	24	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	1932	None	74	Human	Binding	pKi	=	5.3	5.3	-173	24	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	1932	None	74	Human	Binding	pKi	=	5.3	5.3	-173	24	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	109739	None	0	Human	Binding	pKi	=	5.3	5.3	-25	3	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	109739	None	0	Human	Binding	pKi	=	5.3	5.3	-25	3	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	107892	None	0	Human	Binding	pKi	=	4.3	4.3	-36	3	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	107892	None	0	Human	Binding	pKi	=	4.3	4.3	-36	3	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	2019	None	19	Human	Binding	pKi	=	6.3	6.3	-7	7	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	2019	None	19	Human	Binding	pKi	=	6.3	6.3	-7	7	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	2019	None	19	Human	Binding	pKi	=	6.3	6.3	-7	7	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	103675	None	0	Human	Binding	pKi	=	5.3	5.3	-251	3	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	103675	None	0	Human	Binding	pKi	=	5.3	5.3	-251	3	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	102779	None	1	Human	Binding	pKi	=	4.3	4.3	-5754	3	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	102779	None	1	Human	Binding	pKi	=	4.3	4.3	-5754	3	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	205591	None	0	Human	Binding	pKi	=	4.3	4.3	-416	3	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	205591	None	0	Human	Binding	pKi	=	4.3	4.3	-416	3	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	1932	None	74	Human	Binding	pKi	=	4.3	4.3	-173	24	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	1932	None	74	Human	Binding	pKi	=	4.3	4.3	-173	24	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	1932	None	74	Human	Binding	pKi	=	4.3	4.3	-173	24	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	1932	None	74	Human	Binding	pKi	=	4.3	4.3	-173	24	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
	774.0	1932	None	74	Human	Binding	pKi	=	4.3	4.3	-173	24	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	1932	None	74	Human	Binding	pKi	=	4.3	4.3	-173	24	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	1932	None	74	Human	Binding	pKi	=	4.3	4.3	-173	24	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	162734	None	0	Human	Binding	pKi	=	6.3	6.3	-8	10	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	162734	None	0	Human	Binding	pKi	=	6.3	6.3	-8	10	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	4781	None	63	Human	Binding	pKi	=	5.3	5.3	-33	34	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	4781	None	63	Human	Binding	pKi	=	5.3	5.3	-33	34	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	185968	None	0	Human	Binding	pKi	=	7.3	7.3	-2	6	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	185968	None	0	Human	Binding	pKi	=	7.3	7.3	-2	6	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	186671	None	0	Human	Binding	pKi	=	6.3	6.3	1	6	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	186671	None	0	Human	Binding	pKi	=	6.3	6.3	1	6	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	83551	None	0	Human	Binding	pKi	=	5.3	5.3	-1	3	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	83551	None	0	Human	Binding	pKi	=	5.3	5.3	-1	3	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	174270	None	0	Human	Binding	pKi	=	6.3	6.3	-40	4	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	174270	None	0	Human	Binding	pKi	=	6.3	6.3	-40	4	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	185822	None	0	Human	Binding	pKi	=	5.3	5.3	-	1	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	185822	None	0	Human	Binding	pKi	=	5.3	5.3	-	1	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	167073	None	0	Human	Binding	pKi	=	6.3	6.3	-1	12	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	167073	None	0	Human	Binding	pKi	=	6.3	6.3	-1	12	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	193077	None	0	Human	Binding	pKi	=	7.3	7.3	-1737	20	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193077	None	0	Human	Binding	pKi	=	7.3	7.3	-1737	20	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193077	None	0	Human	Binding	pKi	=	7.3	7.3	-1737	20	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	84113	None	0	Human	Binding	pKi	=	6.3	6.3	-660	7	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	84113	None	0	Human	Binding	pKi	=	6.3	6.3	-660	7	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	205685	None	0	Human	Binding	pKi	=	4.3	4.3	-1778	3	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	205685	None	0	Human	Binding	pKi	=	4.3	4.3	-1778	3	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	184005	None	0	Human	Binding	pKi	=	6.3	6.3	-269	20	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	184005	None	0	Human	Binding	pKi	=	6.3	6.3	-269	20	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	937	None	69	Human	Binding	pKi	=	5.3	5.3	-4	8	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	937	None	69	Human	Binding	pKi	=	5.3	5.3	-4	8	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
	2756.0	937	None	69	Human	Binding	pKi	=	5.3	5.3	-4	8	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	937	None	69	Human	Binding	pKi	=	5.3	5.3	-4	8	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	937	None	69	Human	Binding	pKi	=	5.3	5.3	-4	8	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	937	None	69	Human	Binding	pKi	=	5.3	5.3	-4	8	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	174922	None	0	Human	Binding	pKi	=	6.3	6.3	1	3	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	174922	None	0	Human	Binding	pKi	=	6.3	6.3	1	3	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	57086	None	0	Human	Binding	pKi	=	6.3	6.3	-2	17	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	57086	None	0	Human	Binding	pKi	=	6.3	6.3	-2	17	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	179517	None	0	Human	Binding	pKi	=	5.3	5.3	-50	3	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	179517	None	0	Human	Binding	pKi	=	5.3	5.3	-50	3	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	192871	None	0	Human	Binding	pKi	=	6.3	6.3	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192871	None	0	Human	Binding	pKi	=	6.3	6.3	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192871	None	0	Human	Binding	pKi	=	6.3	6.3	1	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	84112	None	0	Human	Binding	pKi	=	5.3	5.3	-1445	7	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	84112	None	0	Human	Binding	pKi	=	5.3	5.3	-1445	7	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	176771	None	0	Human	Binding	pKi	=	6.3	6.3	-	1	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	176771	None	0	Human	Binding	pKi	=	6.3	6.3	-	1	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	176771	None	0	Human	Binding	pKi	=	6.3	6.3	-	1	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	218024	None	0	Human	Binding	pKi	=	6.3	6.3	-	1	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	218024	None	0	Human	Binding	pKi	=	6.3	6.3	-	1	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	5069	None	0	Human	Binding	pKi	=	5.3	5.3	-29	3	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	5069	None	0	Human	Binding	pKi	=	5.3	5.3	-29	3	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	192935	None	0	Human	Binding	pKi	=	5.3	5.3	-87	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192935	None	0	Human	Binding	pKi	=	5.3	5.3	-87	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192935	None	0	Human	Binding	pKi	=	5.3	5.3	-87	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	205224	None	0	Human	Binding	pKi	=	4.3	4.3	-10471	3	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	205224	None	0	Human	Binding	pKi	=	4.3	4.3	-10471	3	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	163551	None	0	Human	Binding	pKi	=	4.2	4.2	-20	3	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	163551	None	0	Human	Binding	pKi	=	4.2	4.2	-20	3	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	203066	None	0	Human	Binding	pKi	=	4.2	4.2	-4786	3	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	203066	None	0	Human	Binding	pKi	=	4.2	4.2	-4786	3	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
	3929516	107426	None	4	Human	Binding	pKi	=	6.2	6.2	-100	17	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	343	4	0	2	4.7	CN1C2CCC1CC(OC(c1ccc(F)cc1)c1ccc(F)cc1)C2	10.6019/CHEMBL5442175
	CHEMBL317757	107426	None	4	Human	Binding	pKi	=	6.2	6.2	-100	17	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	343	4	0	2	4.7	CN1C2CCC1CC(OC(c1ccc(F)cc1)c1ccc(F)cc1)C2	10.6019/CHEMBL5442175
	CHEMBL543113	107426	None	4	Human	Binding	pKi	=	6.2	6.2	-100	17	PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HRH2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.	ChEMBL	343	4	0	2	4.7	CN1C2CCC1CC(OC(c1ccc(F)cc1)c1ccc(F)cc1)C2	10.6019/CHEMBL5442175
	137645406	157994	None	0	Human	Binding	pKi	=	6.2	6.2	-75	13	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	157994	None	0	Human	Binding	pKi	=	6.2	6.2	-75	13	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	193157	None	0	Human	Binding	pKi	=	8.2	8.2	-3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193157	None	0	Human	Binding	pKi	=	8.2	8.2	-3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193157	None	0	Human	Binding	pKi	=	8.2	8.2	-3	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192894	None	0	Human	Binding	pKi	=	8.2	8.2	-2	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192894	None	0	Human	Binding	pKi	=	8.2	8.2	-2	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	192894	None	0	Human	Binding	pKi	=	8.2	8.2	-2	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	184531	None	0	Human	Binding	pKi	=	7.2	7.2	-1	6	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	184531	None	0	Human	Binding	pKi	=	7.2	7.2	-1	6	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	185239	None	0	Human	Binding	pKi	=	6.2	6.2	38	4	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	185239	None	0	Human	Binding	pKi	=	6.2	6.2	38	4	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	163367	None	0	Human	Binding	pKi	=	4.2	4.2	-2951	3	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	163367	None	0	Human	Binding	pKi	=	4.2	4.2	-2951	3	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	100656	None	0	Human	Binding	pKi	=	4.2	4.2	-15135	3	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	100656	None	0	Human	Binding	pKi	=	4.2	4.2	-15135	3	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	167895	None	0	Human	Binding	pKi	=	5.2	5.2	-154	3	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	167895	None	0	Human	Binding	pKi	=	5.2	5.2	-154	3	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	84111	None	0	Human	Binding	pKi	=	5.2	5.2	-1348	7	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	84111	None	0	Human	Binding	pKi	=	5.2	5.2	-1348	7	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	79549	None	0	Human	Binding	pKi	=	5.2	5.2	-104	3	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	79549	None	0	Human	Binding	pKi	=	5.2	5.2	-104	3	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	4447	None	0	Human	Binding	pKi	=	5.2	5.2	-112	3	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	4447	None	0	Human	Binding	pKi	=	5.2	5.2	-112	3	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	92585	None	0	Human	Binding	pKi	=	5.2	5.2	-32	13	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	92585	None	0	Human	Binding	pKi	=	5.2	5.2	-32	13	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	217845	None	0	Human	Binding	pKi	=	7.2	7.2	-	1	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	185558	None	0	Human	Binding	pKi	=	7.2	7.2	407	4	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	185558	None	0	Human	Binding	pKi	=	7.2	7.2	407	4	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	185828	None	0	Human	Binding	pKi	=	7.2	7.2	-1	6	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	185828	None	0	Human	Binding	pKi	=	7.2	7.2	-1	6	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	186125	None	0	Human	Binding	pKi	=	7.2	7.2	177	4	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	186125	None	0	Human	Binding	pKi	=	7.2	7.2	177	4	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	404	None	24	Human	Binding	pKi	=	5.2	5.2	-1	3	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	404	None	24	Human	Binding	pKi	=	5.2	5.2	-1	3	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	404	None	24	Human	Binding	pKi	=	5.2	5.2	-1	3	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	174061	None	0	Human	Binding	pKi	=	5.2	5.2	1	2	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	174061	None	0	Human	Binding	pKi	=	5.2	5.2	1	2	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	193106	None	0	Human	Binding	pKi	=	7.2	7.2	-11	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193106	None	0	Human	Binding	pKi	=	7.2	7.2	-11	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193106	None	0	Human	Binding	pKi	=	7.2	7.2	-11	6	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	183695	None	0	Human	Binding	pKi	=	5.2	5.2	-323	3	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	183695	None	0	Human	Binding	pKi	=	5.2	5.2	-323	3	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	218019	None	0	Human	Binding	pKi	=	7.2	7.2	-	1	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	218019	None	0	Human	Binding	pKi	=	7.2	7.2	-	1	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	209380	None	58	Human	Binding	pKi	=	5.2	5.2	-36	34	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	209380	None	58	Human	Binding	pKi	=	5.2	5.2	-36	34	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	209380	None	58	Human	Binding	pKi	=	5.2	5.2	-36	34	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	172011	None	0	Human	Binding	pKi	=	5.2	5.2	-144	24	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	172011	None	0	Human	Binding	pKi	=	5.2	5.2	-144	24	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	178677	None	4	Human	Binding	pKi	=	6.2	6.2	-338	22	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	178677	None	4	Human	Binding	pKi	=	6.2	6.2	-338	22	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	193088	None	0	Human	Binding	pKi	=	6.2	6.2	-5	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193088	None	0	Human	Binding	pKi	=	6.2	6.2	-5	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	193088	None	0	Human	Binding	pKi	=	6.2	6.2	-5	4	Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysisDisplacement of [3H]UR-DE257 from human histamine 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	100726	None	0	Human	Binding	pKi	=	5.2	5.2	-933	3	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	100726	None	0	Human	Binding	pKi	=	5.2	5.2	-933	3	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	95448	None	0	Human	Binding	pKi	=	4.2	4.2	-9332	4	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	95448	None	0	Human	Binding	pKi	=	4.2	4.2	-9332	4	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	209205	None	27	Human	Binding	pKi	=	5.2	5.2	-7	17	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
	4601.0	209205	None	27	Human	Binding	pKi	=	5.2	5.2	-7	17	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	209205	None	27	Human	Binding	pKi	=	5.2	5.2	-7	17	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	209205	None	27	Human	Binding	pKi	=	5.2	5.2	-7	17	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
	DB01173	209205	None	27	Human	Binding	pKi	=	5.2	5.2	-7	17	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	182316	None	0	Human	Binding	pKi	=	5.2	5.2	-50	3	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	182316	None	0	Human	Binding	pKi	=	5.2	5.2	-50	3	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	185194	None	0	Human	Binding	pKi	=	7.2	7.2	-1	6	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	185194	None	0	Human	Binding	pKi	=	7.2	7.2	-1	6	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	186262	None	0	Human	Binding	pKi	=	6.2	6.2	1	5	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	186262	None	0	Human	Binding	pKi	=	6.2	6.2	1	5	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	137372	None	0	Human	Binding	pKi	=	5.2	5.2	-4	4	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	137372	None	0	Human	Binding	pKi	=	5.2	5.2	-4	4	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	205083	None	0	Human	Binding	pKi	=	4.2	4.2	-9549	3	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	205083	None	0	Human	Binding	pKi	=	4.2	4.2	-9549	3	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	4986	None	0	Human	Binding	pKi	=	4.2	4.2	-79	3	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	4986	None	0	Human	Binding	pKi	=	4.2	4.2	-79	3	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	937	None	69	Human	Binding	pKi	=	7.2	7.2	-4	8	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	937	None	69	Human	Binding	pKi	=	7.2	7.2	-4	8	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
	2756.0	937	None	69	Human	Binding	pKi	=	7.2	7.2	-4	8	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	937	None	69	Human	Binding	pKi	=	7.2	7.2	-4	8	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	937	None	69	Human	Binding	pKi	=	7.2	7.2	-4	8	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	937	None	69	Human	Binding	pKi	=	7.2	7.2	-4	8	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	937	None	69	Human	Binding	pKi	=	7.2	7.2	-4	8	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	937	None	69	Human	Binding	pKi	=	7.2	7.2	-4	8	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
	2756.0	937	None	69	Human	Binding	pKi	=	7.2	7.2	-4	8	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	937	None	69	Human	Binding	pKi	=	7.2	7.2	-4	8	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	937	None	69	Human	Binding	pKi	=	7.2	7.2	-4	8	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	937	None	69	Human	Binding	pKi	=	7.2	7.2	-4	8	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	185304	None	0	Human	Binding	pKi	=	7.2	7.2	1	6	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	185304	None	0	Human	Binding	pKi	=	7.2	7.2	1	6	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	109141	None	0	Human	Binding	pKi	=	6.2	6.2	-229	3	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	109141	None	0	Human	Binding	pKi	=	6.2	6.2	-229	3	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	203669	None	0	Human	Binding	pKi	=	5.2	5.2	-426	3	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	203669	None	0	Human	Binding	pKi	=	5.2	5.2	-426	3	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	196	None	15	Human	Binding	pKi	=	4.2	4.2	-35481	5	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	196	None	15	Human	Binding	pKi	=	4.2	4.2	-35481	5	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	196	None	15	Human	Binding	pKi	=	4.2	4.2	-35481	5	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	163584	None	0	Human	Binding	pKi	=	6.2	6.2	-64	3	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	163584	None	0	Human	Binding	pKi	=	6.2	6.2	-64	3	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	109735	None	0	Human	Binding	pKi	=	5.2	5.2	-707	3	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	109735	None	0	Human	Binding	pKi	=	5.2	5.2	-707	3	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	401	None	38	Human	Binding	pKi	=	6.1	6.1	-1412	39	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	401	None	38	Human	Binding	pKi	=	6.1	6.1	-1412	39	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	401	None	38	Human	Binding	pKi	=	6.1	6.1	-1412	39	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
	2160.0	401	None	38	Human	Binding	pKi	=	6.1	6.1	-1412	39	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	401	None	38	Human	Binding	pKi	=	6.1	6.1	-1412	39	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	401	None	38	Human	Binding	pKi	=	6.1	6.1	-1412	39	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	185009	None	0	Human	Binding	pKi	=	7.1	7.1	1	6	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	185009	None	0	Human	Binding	pKi	=	7.1	7.1	1	6	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	205592	None	0	Human	Binding	pKi	=	4.1	4.1	-2511	3	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	205592	None	0	Human	Binding	pKi	=	4.1	4.1	-2511	3	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	140389	None	0	Human	Binding	pKi	=	5.1	5.1	-33	4	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	140389	None	0	Human	Binding	pKi	=	5.1	5.1	-33	4	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	83834	None	0	Human	Binding	pKi	=	5.1	5.1	-11	8	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	83834	None	0	Human	Binding	pKi	=	5.1	5.1	-11	8	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	5016	None	0	Human	Binding	pKi	=	6.1	6.1	-138	3	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	5016	None	0	Human	Binding	pKi	=	6.1	6.1	-138	3	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	140332	None	0	Human	Binding	pKi	=	5.1	5.1	-25	4	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	140332	None	0	Human	Binding	pKi	=	5.1	5.1	-25	4	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	5051	None	0	Human	Binding	pKi	=	5.1	5.1	-1202	4	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	5051	None	0	Human	Binding	pKi	=	5.1	5.1	-1202	4	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	83828	None	0	Human	Binding	pKi	=	6.1	6.1	1	9	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	83828	None	0	Human	Binding	pKi	=	6.1	6.1	1	9	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	182152	None	0	Human	Binding	pKi	=	5.1	5.1	-123	3	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	182152	None	0	Human	Binding	pKi	=	5.1	5.1	-123	3	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
	147326216	196748	None	0	Human	Binding	pKi	=	6.1	6.1	-7	15	Binding affinity to histamine H2 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H2 receptor (unknown origin) assessed as inhibition constant	ChEMBL	424	10	2	6	4.3	CCN(CC)CCCC(C)Nc1cnc(C(=O)Nc2cc(F)cc3cccnc23)cn1	10.1021/acs.jmedchem.2c01769
	CHEMBL5431371	196748	None	0	Human	Binding	pKi	=	6.1	6.1	-7	15	Binding affinity to histamine H2 receptor (unknown origin) assessed as inhibition constantBinding affinity to histamine H2 receptor (unknown origin) assessed as inhibition constant	ChEMBL	424	10	2	6	4.3	CCN(CC)CCCC(C)Nc1cnc(C(=O)Nc2cc(F)cc3cccnc23)cn1	10.1021/acs.jmedchem.2c01769
	44435200	149763	None	0	Human	Binding	pKi	=	5.1	5.1	-4	4	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	149763	None	0	Human	Binding	pKi	=	5.1	5.1	-4	4	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	5169	None	0	Human	Binding	pKi	=	5.1	5.1	-46	3	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	5169	None	0	Human	Binding	pKi	=	5.1	5.1	-46	3	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	205657	None	0	Human	Binding	pKi	=	5.1	5.1	-562	3	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	205657	None	0	Human	Binding	pKi	=	5.1	5.1	-562	3	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	178338	None	0	Human	Binding	pKi	=	7.1	7.1	-	1	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	178338	None	0	Human	Binding	pKi	=	7.1	7.1	-	1	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	178338	None	0	Human	Binding	pKi	=	7.1	7.1	-	1	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

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Main reference

Ligand source activities (1 row/activity)